1096:. In Elaris EM-I, the percentage of women who had a clinical response with respect to dysmenorrhea was 46.4% in the lower-dose elagolix group and 75.8% in the higher-dose elagolix group, as compared with 19.6% in the placebo group; in Elaris EM-II, the corresponding percentages were 43.4% and 72.4%, as compared with 22.7% (P < 0.001 for all comparisons). In Elaris EM-I, the percentage of women who had a clinical response with respect to non-menstrual pelvic pain was 50.4% in the lower-dose elagolix group and 54.5% in the higher-dose elagolix group, as compared with 36.5% in the placebo group (P < 0.001 for all comparisons); in Elaris EM-II, the corresponding percentages were 49.8% and 57.8%, as compared with 36.5% (P = 0.003 and P < 0.001, respectively). The reductions in symptoms of endometriosis with elagolix resulted in an improved
2370:
1971:, a strong inducer of CYP3A4 and other CYP450 enzymes, increased peak levels of and total exposure to a single 150 mg dose of elagolix as well. A single dose of rifampin increased peak levels of elagolix by 4.4-fold and total exposure by 5.6-fold, whereas continuous rifampin therapy increased peak levels of elagolix by 2-fold and total exposure by 1.7-fold. The use of elagolix at 200 mg twice per day concomitantly with rifampin is not recommended, whereas the concomitant use of elagolix at 150 mg once per day with rifampin should be limited to 6 months. No significant changes in exposure to elagolix were observed with concomitant administration of
701:
678:
1270:. Severe hepatic impairment is associated with 7-fold increased exposure to elagolix, which may increase the risk of bone loss. In women with moderate hepatic impairment, which is associated with 3-fold increased exposure to elagolix, the medication at 200 mg twice per day should not be used, while 150 mg once per day should be used for no more than 6 months. OATP1B1 inhibitors are likely to greatly increase exposure to elagolix similarly to moderate to severe hepatic impairment.
4714:
2268:
can be dose-dependently adjusted as needed, for instance with higher-dose twice-daily administration to achieve greater hormonal suppression. Because of its short duration in the body, the effects of elagolix are rapidly reversible upon discontinuation. In addition, due to its partial and incomplete suppression of estradiol levels, the side effects of elagolix, such as hot flashes and decreased BMD, are lower than with first-generation GnRH modulators.
49:
2318:
premenopausal women. Suppression of gonadotropin and sex hormone levels with elagolix occurs rapidly, within hours, and upon discontinuation of elagolix, gonadotropin and sex hormone levels remain suppressed for at least 12 hours, but show recovery within 24 to 48 hours. As a consequence of its suppression of gonadotropin and sex hormone levels, elagolix inhibits
2387:
2293:
2281:
40:
6696:
1835:. Amenorrhea, the cessation of menstruation, was observed in 4 to 17% of women with 150 mg once per day and in 7 to 57% of women with 200 mg twice per day, compared to less than 1% of women given placebo. The decreased menstrual bleeding caused by elagolix may impede the ability to recognize
4735:
Tucci FC, Zhu YF, Struthers RS, Guo Z, Gross TD, Rowbottom MW, Acevedo O, Gao Y, Saunders J, Xie Q, Reinhart GJ, Liu XJ, Ling N, Bonneville AK, Chen T, Bozigian H, Chen C (February 2005). "3--1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and
2267:
of elagolix in the body, the activation of the GnRHR by GnRH is not fully blocked throughout the day with once-daily administration of elagolix. As a result, gonadotropin and sex hormone levels are only partially suppressed when elagolix is taken once per day. In addition, the degree of suppression
1820:. This is why the duration of use of elagolix should be limited. In women with risk factors for bone loss and osteoporosis, such as a history of low-trauma fracture, assessment of BMD may be considered. Elagolix should not be used in premenopausal women with known osteoporosis. Supplementation with
1803:
BMD was decreased by 0.3 to 1.3% with 150 mg once per day and by 2.5 to 3.1% with 200 mg twice per day. The decrease in BMD during elagolix therapy may not be fully reversible with discontinuation, as only partial recovery was observed 12 months after discontinuation of therapy. The
2312:
levels) with 200 mg twice daily. In a 21-day study in premenopausal women, the effects of elagolix on FSH levels were found to be maximal at a dosage of 300 mg twice per day or above, whereas its effects on LH and estradiol levels were maximal at a dosage of 200 mg twice per day or
2806:. The medication was approved by the FDA for the treatment of endometriosis-associated pain in the United States on 23 July 2018. It was the first new medication to be approved by the FDA for the treatment of endometriosis in more than a decade. Elagolix was the first member of a new class of
2317:
levels (<2 ng/mL) across the 21-day study period at dosages of elagolix of 100 mg twice per day and above. A dosage of elagolix of 400 mg twice per day appears to produce no greater suppression in gonadotropin or estradiol levels than a dosage of 300 mg twice per day in
1919:
and should be treated on a symptomatic basis as needed. Elagolix has been assessed in clinical studies at a dose as high as a single administration of 1,200 mg, which resulted in concentrations of the medication that were 17 times higher than with the typical high clinical dosage of
2097:
therapy is known to be effective in the treatment of endometriosis similarly to GnRH antagonists. On the basis of limited clinical research, combined birth control pills have also been found to be effective in the treatment of endometriosis, but are likely not as effective as GnRH modulator
1875:
occurred in a few women (0.2–0.4%), with one suicide observed. People taking elagolix with new or existing depressive symptoms should be promptly evaluated to determine whether the benefits of treatment outweigh the risks. In those with new or existing depressive symptoms, referral to a
1894:
of at least 3-fold the upper limit, in clinical trials. This was observed in one woman (0.2%) with 150 mg once per day and in five women (1.1%) with 200 mg twice per day, compared to one woman (0.1%) given placebo. Medical attention should be sought if signs or symptoms of
1903:, are noticed. The lowest effective dosage of elagolix may be used to minimize the risk of liver problems, and in those who develop elevated liver enzymes during elagolix therapy, prompt evaluation should be done to determine whether the benefits of treatment outweigh the risks.
5027:
Surrey E, Taylor HS, Giudice L, Lessey BA, Abrao MS, Archer DF, Diamond MP, Johnson NP, Watts NB, Gallagher JC, Simon JA, Carr BR, Dmowski WP, Leyland N, Singh SS, Rechberger T, Agarwal SK, Duan WR, Schwefel B, Thomas JW, Peloso PM, Ng J, Soliman AM, Chwalisz K (July 2018).
4015:
Surrey E, Taylor HS, Giudice L, Lessey BA, Abrao MS, Archer DF, Diamond MP, Johnson NP, Watts NB, Gallagher JC, Simon JA, Carr BR, Dmowski WP, Leyland N, Singh SS, Rechberger T, Agarwal SK, Duan WR, Schwefel B, Thomas JW, Peloso PM, Ng J, Soliman AM, Chwalisz K (July 2018).
2797:
for endometriosis in
November 2016. Two phase III clinical trials, the Elaris Endometriosis I and II (EM-I and EM-II) studies, were conducted. The studies included almost 1,700 women, about 950 of whom were treated with elagolix. In September 2017, AbbVie filed a
1280:
component, is expected to decrease the effectiveness of elagolix in the treatment of endometriosis, and hence is not recommended. Other forms of birth control, such as non-hormonal birth control, can be used instead. Elagolix is not contraindicated in women who are
1114:, elagolix should be taken at approximately the same time each day. In the case of twice-daily administration, elagolix should be taken at approximate 12-hour intervals, for instance once in the morning and once at night. It can be taken with or without
3953:
Taylor HS, Giudice LC, Lessey BA, Abrao MS, Kotarski J, Archer DF, Diamond MP, Surrey E, Johnson NP, Watts NB, Gallagher JC, Simon JA, Carr BR, Dmowski WP, Leyland N, Rowan JP, Duan WR, Ng J, Schwefel B, Thomas JW, Jain RI, Chwalisz K (July 2017).
4517:
Diamond MP, Carr B, Dmowski WP, Koltun W, O'Brien C, Jiang P, Burke J, Jimenez R, Garner E, Chwalisz K (2014). "Elagolix treatment for endometriosis-associated pain: results from a phase 2, randomized, double-blind, placebo-controlled study".
4712:, Zhiqiang Guo, Yongsheng Chen, Dongpei Wu, Chen Chen, Warren Wade, Wesley J. Dwight, Charles Q. Huang, Fabio C. Tucci, "Gonadotropin-releasing hormone receptor antagonists and methods relating thereto", published 2006-06-06
5253:
3760:
R-(+)-4-{2-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor".
3759:
Chen C, Wu D, Guo Z, Xie Q, Reinhart GJ, Madan A, Wen J, Chen T, Huang CQ, Chen M, Chen Y, Tucci FC, Rowbottom M, Pontillo J, Zhu YF, Wade W, Saunders J, Bozigian H, Struthers RS (December 2008). "Discovery of sodium
1920:
200 mg twice per day. No adverse effects were mentioned. Chronic overdosage of elagolix may result in greater suppression of estradiol levels and a consequent increased risk of bone loss with long-term therapy.
776:
2018:
characterized by reduced OATP1B1 transporter function. The concomitant use of elagolix with medications that inhibit OATP1B1 may increase elagolix levels, and the use of elagolix with strong OATP1B1 inhibitors like
1164:. The 150 mg tablets are light pink, oblong, and film-coated with "EL 150" debossed on one side, while the 200 mg tablets are light orange, oblong, and film-coated with "EL 200" debossed on one side. The
818:
InChI=1S/C32H30F5N3O5/c1-19-28(21-11-6-14-26(45-2)29(21)34)30(43)40(18-25(20-9-4-3-5-10-20)38-16-8-15-27(41)42)31(44)39(19)17-22-23(32(35,36)37)12-7-13-24(22)33/h3-7,9-14,25,38H,8,15-18H2,1-2H3,(H,41,42)/t25-/m0/s1
1858:
The incidence of depression and mood changes in clinical trials with elagolix was increased in premenopausal women taking elagolix relative to placebo. Mood- and depression-type side effects such as altered mood,
6293:
4775:
3655:
Clemenza S, Sorbi F, Noci I, Capezzuoli T, Turrini I, Carriero C, Buffi N, Fambrini M, Petraglia F (February 2018). "From pathogenesis to clinical practice: Emerging medical treatments for endometriosis".
1002:
as it is not structurally related to GnRH. Elagolix was the first second-generation and orally active GnRH modulator to be introduced for medical use. The introduction of elagolix in the United States and
4952:
Alessandro P, Luigi N, Felice S, Maria PA, Benedetto MG, Stefano A (April 2017). "Research development of a new GnRH antagonist (Elagolix) for the treatment of endometriosis: a review of the literature".
1107:, and the lowest effective dosage should be used. Elagolix can be used for up to 24 months at the 150 mg once per day dosage and for up to 6 months at the 200 mg twice per day dosage.
5246:
2510:
of elagolix is typically about 4 to 6 hours. A study found that its half-life was 2.4 to 6.3 hours with a single dose and was 2.2 to 10.8 hours with continuous administration. The oral
2304:
In clinical trials, elagolix produced dose-dependent decreases in gonadotropin, estradiol, and progesterone levels in women. Median levels of estradiol were partially suppressed to 42 pg/mL (
1086:) in women with endometriosis. The medication is used at a lower dosage of 150 mg once per day or at a higher dosage of 200 mg twice per day, depending on the severity of symptoms.
5239:
4256:
2830:
in
January 2019. In addition to endometriosis, elagolix is under development for the treatment of uterine fibroids and menorrhagia. It is in phase III clinical trials for these indications.
4915:
Melis GB, Neri M, Corda V, Malune ME, Piras B, Pirarba S, Guerriero S, Orrù M, D'Alterio MN, Angioni S, Paoletti AM (May 2016). "Overview of elagolix for the treatment of endometriosis".
2581:, but is increased by approximately 3-fold in women with moderate hepatic impairment and by approximately 7-fold in women with severe hepatic impairment. There were no differences in the
6286:
3926:
2546:
levels of elagolix have been found to be increased by 78% relative to in people with normal OATP1B1 function (SLCO1B1 521T/T genotype). The frequency of this reduced function OATP1B1
2445:
study found that levels of elagolix in women after a single dose of 1,200 mg were 17 times higher than in women taking 200 mg twice daily. Taking elagolix with a high-
1266:, and should discontinue the medication if they become or wish to become pregnant. Elagolix should not be used in women with osteoporosis because it may increase the risk of further
1792:. Elagolix was discontinued due to side effects by 5 to 10% of women in clinical trials, with the most common reasons being hot flashes or night sweats, nausea, and decreased BMD.
2790:). In June 2010, Neurocrine Biosciences and Abbott announced a global agreement to develop and commercialize elagolix for the treatment of endometriosis. The medication completed
2612:. Inhibitors of OATP1B1 may increase circulating levels of elagolix, and elagolix is considered to be contraindicated in combination with strong OATP1B1 inhibitors. Elagolix is a
249:
2963:, for the treatment of menorrhagia associated with uterine fibroids in premenopausal women has been published. The medication was also under investigation for the treatment of
2433:
of elagolix at 150 mg once per day is 0.98 and at 200 mg twice per day is 0.89, indicating that it is not accumulated in the body with continuous administration. At
2369:
4854:
6279:
6242:
3277:
2326:, the ovulation rate with elagolix was 50% at 150 mg once daily and 32% at 200 mg twice daily. Because ovulation is triggered by a surge in estradiol levels at
4152:
5690:
4209:
Tan O, Carr BR, Beshay VE, Bukulmez O (January 2013). "The extrapituitary effects of GnRH antagonists and their potential clinical implications: a narrated review".
6550:
4771:
2620:, but the effect of inhibitors and inducers of P-glycoprotein on the pharmacokinetics of elagolix is unknown. Elagolix itself is an inhibitor of P-glycoprotein.
143:
3468:"Suppression of gonadotropins and estradiol in premenopausal women by oral administration of the nonpeptide gonadotropin-releasing hormone antagonist elagolix"
4851:"Endometriosis treatment: elagolix could help the painful uterus disorder: Women with endometriosis experience terrible pain. There's finally a new treatment"
4563:"Elagolix, an oral GnRH antagonist, versus subcutaneous depot medroxyprogesterone acetate for the treatment of endometriosis: effects on bone mineral density"
1121:
Elagolix is approved only for the treatment of endometriosis. Other approved and off-label uses of GnRH antagonists in general are the same as those of GnRHR
790:
2256:. By suppressing estrogen production and levels, elagolix decreases the growth of the endometrium and decreases endometriosis symptoms such as pelvic pain.
1089:
The effectiveness of elagolix in the treatment of symptoms of endometriosis was demonstrated in the 6-month Elaris
Endometriosis I and II (EM-I and EM-II)
6260:
5860:
5335:
3356:
3318:
955:. Elagolix is a short-acting GnRH antagonist, and can be used to achieve either partial or more substantial suppression of sex hormone levels. Reduced
5810:
5311:
841:
5716:
4252:
2297:
Levels of LH, FSH, estradiol, and progesterone after the first dose on day 1 and after the last dose on day 21 with elagolix in premenopausal women
6322:
6302:
5724:
2629:
2127:
915:
1867:
occurred in 3 to 6% of women with 150 mg per day and in 5 to 6% of women with 200 mg twice per day, compared to 2 to 3% in women given
5975:
5734:
1240:
5176:
Barra F, Scala C, Ferrero S (April 2019). "Elagolix sodium for the treatment of women with moderate to severe endometriosis-associated pain".
4736:
orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization".
6599:
6209:
4623:
4489:
4378:
4294:
3922:
6271:
6255:
6250:
5683:
4384:
4688:
4495:
4300:
6041:
5945:
4629:
6756:
6716:
2585:
of elagolix between individuals of different racial and ethnic groups. Similarly, the pharmacokinetics of elagolix were unaffected by
1967:
has been found to increase peak levels of and total exposure to a single 150 mg dose of elagolix by about 2-fold. Paradoxically,
2851:
1473:
810:
108:
2437:, peak levels of elagolix at 150 mg once per day are 574 ng/mL and at 200 mg twice per day are 774 ng/mL while
970:
Elagolix was first described in 2008 and was approved for medical use in July 2018. It has been described as a "second-generation"
4850:
4100:
Hembree WC, Cohen-Kettenis P, Delemarre-van de Waal HA, Gooren LJ, Meyer WJ, Spack NP, Tangpricha V, Montori VM (September 2009).
2514:
of elagolix is 123 L/hour at 150 mg once per day and 144 L/hour at 200 mg twice per day. The major pathway of
4827:
4660:
4184:
3269:
2441:
of elagolix at 150 mg once per day are 1,292 ng•hour/mL and at 200 mg twice per day are 1,725 ng•hour/mL. A
1880:, as appropriate, may be warranted. Immediate medical attention should be sought for those with suicidal ideation and behavior.
5676:
5613:
2469:
2434:
2077:
contain an estrogen, and because elagolix treats endometriosis by decreasing estrogen levels in the endometrium, these form of
1122:
403:
279:
175:
4141:
3804:
6371:
6015:
5699:
5296:
5284:
5262:
3735:
2421:
elagolix showed a low oral bioavailability of 5.8% in rats and 11% in monkeys. Following administration, elagolix is rapidly
2141:
2082:
929:
4882:"Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain"
3544:"Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain"
1301:
child. The use of elagolix in women who are breastfeeding should be considered carefully, weighing both benefits and risks.
4772:"Abbott and Neurocrine Announce Global Agreement to Develop and Commercialize Elagolix for the Treatment of Endometriosis"
2422:
6686:
4719:
2211:
production of testosterone and estradiol, decreasing the circulating levels of these hormones similarly. Unlike previous
2034:
of CYP3A, and may decrease levels of medications that are substrates of CYP3A4. In addition, elagolix is an inhibitor of
6623:
6574:
6158:
5897:
5892:
5439:
3834:
2968:
2410:
2172:
1173:
1016:
865:
533:
3985:
3840:
6766:
6226:
6166:
5481:
5395:
2921:
2791:
2551:
2500:
2453:
2438:
2070:
1142:
1090:
657:
2081:
are likely and expected to decrease the effectiveness of elagolix in the treatment of this condition. The effect of
194:
2860:
2515:
1877:
1776:(0.2%), though it is unknown if these were due to elagolix. Other serious adverse effects of elagolix may include
6751:
6741:
6057:
4801:
2414:
1103:
The duration of use of elagolix in the treatment of endometriosis should be limited due to a progressive risk of
1020:
1828:
during treatment with elagolix has not been studied, but may be beneficial for helping to maintain bone health.
6726:
5884:
5668:
2613:
2511:
1976:
1933:
1891:
482:
4437:"Dose-Dependent Suppression of Gonadotropins and Ovarian Hormones by Elagolix in Healthy Premenopausal Women"
2391:
Levels of elagolix over 12- or 24-hour dosing intervals on days 1 and 21 with elagolix in premenopausal women
6569:
6214:
3349:
3308:
2430:
2402:
2149:
223:
696:
6426:
6120:
2956:
2948:
2779:
2776:
2465:
2457:
2452:
has been found to decrease its peak levels by 36% and its area-under-the-curve levels by 24%. In terms of
2123:
2116:
2078:
2074:
1884:
1852:
1789:
1768:. Rare but serious adverse effects that were observed during elagolix therapy in clinical trials included
1579:
1273:
618:
333:
6653:
6638:
2390:
2296:
2284:
6736:
6541:
6311:
6150:
6112:
2952:
2461:
2342:
2285:
Levels of LH, FSH, estradiol, and progesterone over a 21-day period with elagolix in premenopausal women
1812:. The consequences of the effects of elagolix on BMD are unknown, but may be an increase in the risk of
1277:
1177:
473:
2207:, and thereby decreases the circulating levels of these hormones. In men, GnRH modulators suppress the
5231:
2665:
of GnRH. Other small-molecule and non-peptide orally active GnRH antagonists besides elagolix include
6618:
6162:
5578:
5447:
2799:
1758:
1663:
1067:. Around 10% of women may be affected by endometriosis. Elagolix significantly decreases symptoms of
907:
360:
673:
6761:
6579:
6154:
6078:
5998:
5902:
5507:
2819:
2787:
2426:
2399:
2231:
2168:
2120:
1805:
1730:
1682:
1247:
1197:
1158:
983:
911:
879:
869:
420:
230:
1851:
and thereby decreases the likelihood of pregnancy, but has not been shown to be a fully effective
1843:
in early pregnancy, and so should be discontinued if pregnancy occurs. If pregnancy is suspected,
6411:
6314:
6132:
6082:
5386:
5201:
5015:
4978:
4940:
4543:
4234:
4082:
3681:
2909:
2578:
2519:
2507:
2264:
2260:
2176:
1832:
1236:
1185:
1138:
1111:
1083:
205:
6494:
6421:
5547:
5537:
5030:"Long-Term Outcomes of Elagolix in Women With Endometriosis: Results From Two Extension Studies"
4990:
Perricos A, Wenzl R (September 2017). "Efficacy of elagolix in the treatment of endometriosis".
4018:"Long-Term Outcomes of Elagolix in Women With Endometriosis: Results From Two Extension Studies"
6669:
6504:
6499:
6484:
6464:
6449:
4366:
872:
once or twice per day. It can be taken for up to 6 to 24 months, depending on the dosage.
639:
598:
6474:
6396:
6346:
6341:
6170:
5193:
5164:
5129:
5086:
5051:
5007:
4970:
4932:
4903:
4753:
4682:
4619:
4592:
4535:
4485:
4477:
4458:
4374:
4344:
4290:
4282:
4226:
4123:
4102:"Endocrine treatment of transsexual persons: an Endocrine Society clinical practice guideline"
4074:
4057:
Huirne JA, Lambalk CB (November 2001). "Gonadotropin-releasing-hormone-receptor antagonists".
4039:
3977:
3896:
3777:
3673:
3614:
3565:
3497:
3427:
2716:
2662:
2642:
2484:
2308:
levels) with 150 mg once daily and were fully or near-fully suppressed to 12 pg/mL (
2227:
2131:
1844:
1726:
1722:
1595:
1441:
1262:
in early pregnancy. Women should avoid pregnancy while taking elagolix, for instance by using
1209:
1189:
1161:
919:
899:
629:
305:
293:
125:
6479:
4611:
3466:
Struthers RS, Nicholls AJ, Grundy J, Chen T, Jimenez R, Yen SS, Bozigian HP (February 2009).
2330:, estrogen exposure during elagolix therapy might be greater around this time in some women.
522:
6746:
6633:
6628:
6351:
6128:
6061:
6053:
6031:
5745:
5185:
5154:
5119:
5111:
5076:
5041:
4999:
4962:
4924:
4893:
4745:
4582:
4574:
4527:
4448:
4334:
4218:
4113:
4066:
4029:
3967:
3886:
3878:
3769:
3665:
3604:
3596:
3555:
3487:
3479:
3417:
3407:
2740:
2688:
2597:
2582:
2574:
2358:
2354:
2305:
2043:
1948:
1929:
1916:
1655:
1224:
1193:
1052:
713:
437:
429:
315:
66:
2775:
Elagolix was first described in the literature in 2005. It was originally developed by the
550:
542:
6731:
6721:
6700:
6124:
5935:
4723:
3739:
2964:
2928:
2590:
2418:
2406:
2323:
2157:
2145:
2138:
1937:
1489:
1134:
1097:
1072:
991:
861:
853:
700:
677:
343:
323:
242:
4561:
Carr B, Dmowski WP, O'Brien C, Jiang P, Burke J, Jimenez R, Garner E, Chwalisz K (2014).
2472:
is 1,674 L at 150 mg once per day and 881 L at 200 mg twice per day.
1963:
of elagolix and increase or decrease its circulating levels. The strong CYP3A4 inhibitor
868:
in men as well, but development for these conditions was discontinued. Elagolix is taken
5220:
2373:
Levels of elagolix following a single oral dose of different doses of elagolix in women.
2085:
on the effectiveness of elagolix in endometriosis is unknown. However, progestogens are
2038:, and may increase levels of medications that are substrates of P-glycoprotein, such as
2014:
transporter. Levels of elagolix have been found to be increased by 78% in people with a
1839:
in a timely manner. Based on its mechanism of action, elagolix may increase the risk of
6648:
6220:
6136:
6102:
6090:
5912:
5623:
5427:
5417:
5124:
5099:
4587:
4562:
3891:
3866:
3609:
3584:
3492:
3467:
3422:
3395:
2924:
2815:
2807:
2794:
2635:
2617:
2605:
2346:
2334:
2224:
2086:
2059:
2055:
2035:
2031:
1952:
1738:
1635:
1213:
1205:
1093:
979:
971:
153:
48:
4823:
4657:"ChemIDplus - 834153-87-6 - HEAUOKZIVMZVQL-VWLOTQADSA-N - Elagolix [USAN:INN]"
4253:"Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers"
4070:
2681:, although none of these compounds have been introduced for medical use at this time.
6710:
6584:
5527:
5407:
5205:
4656:
4177:
3313:
2803:
2704:
2646:
2309:
2253:
2216:
2099:
1817:
1809:
1765:
1298:
1282:
1263:
1130:
1036:
999:
849:
689:
462:
167:
5019:
4982:
4944:
4238:
4086:
2971:(enlarged prostate) in men, but development for these indications was discontinued.
2593:. Peak and area-under-the-curve levels of elagolix have been shown to be altered by
6008:
5971:
5965:
5961:
5953:
5875:
5708:
5608:
5588:
5346:
5275:
5266:
4547:
3956:"Treatment of Endometriosis-Associated Pain with Elagolix, an Oral GnRH Antagonist"
3685:
2936:
2847:
2601:
2543:
2535:
2212:
2204:
2200:
2180:
2165:
2135:
2047:
1972:
1964:
1896:
1813:
1800:
1796:
1777:
1769:
1762:
1754:
1750:
1706:
1651:
1639:
1559:
1538:
1267:
1232:
1104:
1068:
1040:
987:
952:
948:
936:
923:
262:
257:
5189:
5003:
4928:
3800:
3732:
3669:
2802:(NDA) for elagolix for the treatment of pain associated with endometriosis in the
5046:
5029:
4034:
4017:
3394:
Tukun FL, Olberg DE, Riss PJ, Haraldsen I, Kaass A, Klaveness J (December 2017).
2333:
In addition to its activity as a GnRH antagonist, elagolix is a weak to moderate
1729:
changes. Less common side effects of elagolix (incidence ≥3% and <5%) include
6416:
6391:
6376:
6191:
6142:
6098:
6094:
6086:
6071:
6065:
6002:
5992:
5800:
5785:
5765:
5643:
5603:
5593:
5583:
5569:
5542:
5493:
5472:
5453:
5412:
5367:
2944:
2932:
2811:
2650:
2639:
2586:
2314:
2245:
2241:
2220:
2184:
2102:
during elagolix therapy and for one week following discontinuation of elagolix.
2024:
2020:
2004:
1888:
1872:
1864:
1840:
1785:
1781:
1742:
1690:
1678:
1643:
1345:
1290:
1259:
1255:
1251:
1146:
1126:
1079:
1075:
1064:
1060:
1044:
975:
960:
940:
887:
875:
857:
161:
5081:
5064:
3955:
2007:(a strong inhibitor of CYP2C19 and a moderate inhibitor of CYP2C9 and CYP3A4).
6643:
6589:
6516:
6454:
6366:
6361:
6186:
6116:
5907:
5851:
5826:
5760:
5755:
5648:
5638:
5633:
5628:
5618:
5532:
5463:
5443:
5372:
5362:
5357:
5316:
5115:
4966:
4709:
3882:
3600:
3412:
2892:
Elagolix is available in the United States and Canada. A similar medication,
2696:
2666:
2654:
2476:
2442:
2350:
2063:
1992:
1960:
1860:
1799:
women with long-term therapy. After 6 months of treatment with elagolix,
1718:
1702:
1521:
1409:
1361:
895:
752:
513:
237:
4578:
4531:
4222:
411:
4-methyl]-4-methyl-2,6-dioxopyrimidin-1-yl]-1-phenylethyl]amino]butanoic acid
6531:
6526:
6469:
6459:
6406:
6401:
6386:
6381:
6356:
6146:
6106:
5988:
5984:
5957:
5856:
5836:
5831:
5795:
5790:
5780:
5775:
5770:
5750:
5653:
5598:
5559:
5331:
5326:
5306:
5301:
5159:
5142:
3825:
2960:
2893:
2823:
2744:
2678:
2674:
2559:
2555:
2327:
2319:
2196:
2161:
2094:
2051:
1848:
1836:
1825:
1773:
1746:
1686:
1647:
1505:
1341:
1294:
1286:
1228:
1165:
1008:
944:
883:
798:
COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C(NCCCC(=O)O)c3ccccc3)c2=O)c1F
377:
147:
17:
5197:
5168:
5141:
Vercellini P, Viganò P, Barbara G, Buggio L, Somigliana E (February 2019).
5133:
5090:
5055:
5011:
4974:
4936:
4907:
4757:
4596:
4539:
4462:
4348:
4230:
4127:
4078:
4043:
3981:
3900:
3781:
3677:
3618:
3569:
3501:
3431:
3972:
6521:
6489:
6439:
6049:
5821:
5554:
5516:
5458:
4453:
4436:
4118:
4101:
3483:
2940:
2670:
2609:
2547:
2539:
2237:
2208:
2015:
1968:
1915:
of elagolix, the person should be monitored for any signs or symptoms of
1912:
1900:
1734:
1710:
1694:
1631:
1457:
1377:
1181:
1169:
964:
956:
891:
493:
189:
31:
2156:) of elagolix for the GnRHR is 54 pM. By blocking the GnRHR in the
502:
6551:
6444:
6181:
2658:
2523:
2249:
2039:
2011:
1984:
1980:
1868:
1821:
1714:
1709:). The next most frequent side effects of elagolix (incidence ≥5%) are
1611:
1425:
1244:
1056:
995:
926:
903:
448:
4898:
4881:
4797:
4749:
4339:
4322:
3773:
3560:
3543:
1011:(brand name Relumina), the next second-generation GnRH antagonist, in
860:
in women. The medication was under investigation for the treatment of
4148:
2783:
2692:
2685:
2594:
2527:
2496:
2492:
2090:
2027:, which may markedly increase elagolix exposure, is contraindicated.
2000:
1996:
1956:
1941:
1698:
1393:
1048:
1004:
609:
4824:"The FDA Approved the First New Endometriosis Treatment In a Decade"
39:
2191:. In women, elagolix dose-dependently suppresses the production of
1310:
Side effects of elagolix in clinical trials (mostly ≥5% incidence)
578:
570:
2827:
2700:
2567:
2563:
2488:
2480:
2368:
2338:
2192:
2188:
2098:
monotherapy. It is advised that women use non-hormonal methods of
1988:
1944:
1157:
Elagolix is available in the form of
Orilissa 150 and 200 mg
1012:
933:
932:(GnRH). By blocking the GnRHR, it dose-dependently suppresses the
775:
766:
645:
589:
387:
382:
352:
348:
2782:, and was later developed together by Neurocrine Biosciences and
2518:
of elagolix is hepatic metabolism. Elagolix is taken up from the
2904:
Prior to its introduction, elagolix was estimated to cost about
2531:
2449:
1685:. The most common side effects of elagolix (incidence ≥10%) are
1201:
1115:
1032:
845:
561:
6323:
6303:
6275:
5672:
5235:
844:(GnRH antagonist) medication which is used in the treatment of
299:
184:
5976:
2446:
2042:. Elagolix has been found to increase exposure to digoxin and
6600:
3865:
Bulletti C, Coccia ME, Battistoni S, Borini A (August 2010).
852:
in women. It is also under development for the treatment of
662:
5143:"Elagolix for endometriosis: all that glitters is not gold"
2263:
of typically about 4 to 6 hours. Because of the short
87:
78:
72:
4142:"Orilissa Product Monograph Including Patient Information"
2868:. It is also known by its former developmental code names
2630:
Gonadotropin-releasing hormone receptor § Antagonists
1831:
Elagolix decreases the amount, intensity, and duration of
1757:. Other common side effects of elagolix include decreased
2852:
1795:
Elagolix dose- and duration-dependently decreases BMD in
1276:
is not contraindicated with elagolix, but because of the
93:
84:
3795:
3793:
3791:
2691:
of elagolix. It is a white to off white to light yellow
1031:
Elagolix is used in the treatment of moderate to severe
998:
and first-generation GnRH modulators, elagolix is not a
288:
6556:
Tooltip
Luteinizing hormone/choriogonadotropin receptor
4287:
Principles and
Practice of Endocrinology and Metabolism
2711:)-2-methyl}-4-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2
1863:, depressed mood, depression, depressive symptoms, and
6661:
6243:
6042:
6016:
6009:
5946:
5717:
5700:
3264:
3262:
3260:
3258:
3256:
3254:
3252:
3250:
3248:
3246:
3244:
3242:
3240:
3238:
3236:
3234:
3232:
3230:
3228:
3226:
3224:
3222:
3220:
3218:
3216:
3214:
3212:
3210:
3208:
3206:
3204:
3202:
3200:
3198:
3196:
3194:
3192:
3190:
3188:
3186:
3184:
6684:
4373:. Lippincott Williams & Wilkins. pp. 1411–.
3350:"Orilissa (elagolix) Health Canada Product Monograph"
3182:
3180:
3178:
3176:
3174:
3172:
3170:
3168:
3166:
3164:
3162:
3160:
3158:
3156:
3154:
3152:
3150:
3148:
3146:
3144:
3142:
3140:
3138:
3136:
3134:
3132:
3130:
3128:
3126:
3124:
3122:
3120:
3118:
3116:
3114:
3112:
3110:
3108:
3106:
3104:
3102:
3100:
3098:
3096:
3094:
3092:
3090:
3088:
3086:
3084:
3082:
3080:
3078:
3076:
3074:
3072:
3070:
3068:
3066:
3064:
3062:
3060:
3058:
3056:
3054:
3052:
3050:
3048:
3046:
3044:
3042:
3040:
3038:
3036:
3034:
3032:
3030:
3028:
3026:
3024:
3022:
3020:
3018:
3016:
3014:
3012:
3010:
3008:
3006:
3004:
910:, among others. Elagolix is a GnRH antagonist, or an
109:
99:
96:
69:
4360:
4358:
4289:. Lippincott Williams & Wilkins. pp. 975–.
3396:"Recent Development of Non-Peptide GnRH Antagonists"
3002:
3000:
2998:
2996:
2994:
2992:
2990:
2988:
2986:
2984:
2884:
Elagolix is marketed under the brand name
Orilissa.
2046:, whereas it has been found to decrease exposure to
90:
75:
6598:
6549:
6540:
6321:
6040:Sex steroid agonists (via negative feedback on the
6030:
5934:
5925:
5883:
5874:
5809:
5733:
5715:
5568:
5515:
5506:
5480:
5426:
5394:
5385:
5345:
5283:
5274:
4684:
2379:
2273:
2259:Elagolix is a short-acting GnRH antagonist, with a
764:
751:
712:
707:
688:
656:
628:
608:
588:
560:
532:
512:
492:
481:
472:
447:
419:
394:
376:
359:
342:
332:
322:
314:
278:
273:
248:
236:
222:
204:
174:
160:
142:
134:
124:
81:
60:
55:
5944:Sex steroid antagonists (via disinhibition of the
4435:Ng J, Chwalisz K, Carter DC, Klein CE (May 2017).
2861:
2501:
1855:and should not be relied on to prevent pregnancy.
1327:
3923:"FDA approves drug to control endometriosis pain"
3537:
3535:
3533:
3531:
3344:
3342:
3340:
3338:
3336:
2405:, in contrast to other GnRH modulators. The oral
2357:of other medications, and this may contribute to
2313:above. Levels of progesterone were maintained at
1847:can be performed. Elagolix decreases the rate of
1630:Side effects reported in ≥3% but <5% included
1319:
1043:women. Endometriosis is a condition in which the
328:Low (5.8% in rats, 11% in monkeys; no human data)
4430:
4428:
4426:
4424:
4422:
3529:
3527:
3525:
3523:
3521:
3519:
3517:
3515:
3513:
3511:
3303:
3301:
3299:
3297:
3295:
461:
6328:Tooltip Gonadotropin-releasing hormone receptor
6308:Tooltip Gonadotropin-releasing hormone receptor
4610:McCartney CR, Marshall JC (13 September 2013).
4420:
4418:
4416:
4414:
4412:
4410:
4408:
4406:
4404:
4402:
4010:
4008:
4006:
4004:
4002:
3948:
3946:
3944:
3860:
3858:
3754:
3752:
3750:
3748:
3650:
3648:
3461:
2947:study of elagolix in combination with add-back
2822:to be marketed. A second member of this group,
1051:, grows outside of the uterus into surrounding
967:of elagolix in the treatment of endometriosis.
436:
428:
6179:Others (mixed or unknown mechanism of action):
5981:Tooltip Selective estrogen receptor modulators
3727:
3725:
3723:
3721:
3719:
3717:
3715:
3646:
3644:
3642:
3640:
3638:
3636:
3634:
3632:
3630:
3628:
3459:
3457:
3455:
3453:
3451:
3449:
3447:
3445:
3443:
3441:
3389:
3387:
3385:
3383:
3381:
3379:
3377:
2810:described as "second-generation" due to their
2715:)-yl]-1-phenylethyl}amino)butanoate. It has a
2409:of elagolix in humans is not described in the
1804:cause of the decrease in BMD with elagolix is
1285:, but it is unknown whether the medication is
6605:Tooltip Follicle-stimulating hormone receptor
6287:
5684:
5247:
4651:
4649:
4647:
4276:
4274:
3713:
3711:
3709:
3707:
3705:
3703:
3701:
3699:
3697:
3695:
2767:and a molecular weight of 631.60 g/mol.
2747:form of elagolix has a molecular formula of C
2526:carrier. In people with two reduced function
2215:and antagonists, referred to collectively as
8:
2538:OATP1B1 (SLCO1B1 521T>C; SLCO1B1 521 C/C
1664:
1560:
1539:
193:
30:
4484:. Elsevier Health Sciences. pp. 752–.
4476:Matsumoto AM, Bremmer WJ (1 January 2016).
2429:occurring after 0.5 to 1.5 hours. The
1808:, and is analogous to that associated with
6644:Menotropin (human menopausal gonadotropin)
6590:Menotropin (human menopausal gonadotropin)
6546:
6294:
6280:
6272:
5931:
5880:
5730:
5691:
5677:
5669:
5512:
5391:
5280:
5254:
5240:
5232:
4618:. Elsevier Health Sciences. pp. 19–.
4616:Yen and Jaffe's Reproductive Endocrinology
3916:
3914:
3912:
3910:
3801:"Relugolix - Myovant/Takeda - AdisInsight"
1308:
699:
676:
521:
5158:
5123:
5080:
5045:
4897:
4614:. In Strauss III JF, Barbieri RL (eds.).
4586:
4452:
4365:Lemke TL, Williams DA (24 January 2012).
4338:
4117:
4033:
3971:
3890:
3608:
3559:
3491:
3421:
3411:
2857:Tooltip International Nonproprietary Name
2826:(brand name Relumina), was introduced in
2684:Elagolix is used as elagolix sodium, the
842:gonadotropin-releasing hormone antagonist
549:
541:
4371:Foye's Principles of Medicinal Chemistry
3270:"Orilissa- elagolix tablet, film coated"
2573:Exposure to elagolix is not affected by
6691:
2980:
2349:. As a result, elagolix may affect the
2160:, elagolix suppresses the GnRH-induced
2128:gonadotropin-releasing hormone receptor
2010:Elagolix is a substrate of the hepatic
1625:
916:gonadotropin-releasing hormone receptor
815:
795:
672:
501:
408:
166:
6021:Tooltip gonadotropin-releasing hormone
5705:Tooltip Gonadotropin-releasing hormone
4798:"Orilissa (elagolix) Medication Guide"
3843:from the original on 17 September 2020
3280:from the original on 24 September 2020
2920:As of November 2018, elagolix in
2376:
2270:
1932:with other medications. Elagolix is a
1681:of elagolix are in general similar to
1241:organic anion-transporting polypeptide
1149:adolescents and adults, among others.
690:
29:
4687:, U.S. National Library of Medicine,
4387:from the original on 21 December 2016
4183:. Contemporary OB/GYN. pp. 2–6.
3362:from the original on 16 February 2019
638:
617:
597:
152:
7:
6246:and gonadotropin receptor modulators
5227:. U.S. National Library of Medicine.
4323:"Progestin therapy in endometriosis"
4190:from the original on 19 October 2021
4158:from the original on 19 October 2021
2908:per month. It is not available as a
1258:. Elagolix may increase the risk of
644:
261:
3658:Best Pract Res Clin Obstet Gynaecol
2707:of elagolix sodium is sodium 4-({(1
2322:in women. Over the course of three
1928:Elagolix has a number of potential
1883:Elagolix dose-dependently produced
1772:(0.3%), abdominal pain (0.2%), and
1129:, and include uterine fibroids and
1125:therapy with GnRH agonists such as
577:
569:
452:
4880:Ezzati M, Carr BR (January 2015).
4482:Williams Textbook of Endocrinology
3929:from the original on 25 April 2022
3542:Ezzati M, Carr BR (January 2015).
2935:(abnormally heavy bleeding during
2866:Tooltip United States Adopted Name
2550:is generally less than 5% in most
1239:, and concomitant use with strong
25:
6261:Progestogens and antiprogestogens
5861:+estradiol/norethisterone acetate
5336:+estradiol/norethisterone acetate
5100:"Elagolix: First Global Approval"
4857:from the original on 26 July 2018
4830:from the original on 31 July 2018
4691:from the original on 26 July 2018
4663:from the original on 26 July 2018
4632:from the original on 10 June 2022
4498:from the original on 27 July 2020
3585:"Elagolix: First Global Approval"
1474:Upper respiratory tract infection
6694:
5065:"Use of Elagolix in Gynaecology"
4778:from the original on 2 July 2018
4259:from the original on 10 May 2016
3321:from the original on 1 June 2022
2491:and minor pathways including by
2385:
2291:
2279:
1293:or if it has adverse effects on
1110:Because of its relatively short
939:and hence circulating levels of
736:
730:
724:
65:
47:
38:
5263:Hypothalamic-pituitary hormones
4804:from the original on 2018-08-16
4774:. FierceBiotech. 16 June 2010.
4612:"Endocrinology of Reproduction"
4321:Gezer A, Oral E (August 2015).
4303:from the original on 2022-06-10
3988:from the original on 2020-06-12
3867:"Endometriosis and infertility"
3826:New Drug Therapy Approvals 2018
3807:from the original on 2018-09-20
2030:Elagolix is a weak to moderate
1212:in the 150 mg tablets and
823:Key:HEAUOKZIVMZVQL-VWLOTQADSA-N
5285:Gonadotropin-releasing hormone
4917:Expert Opin Drug Metab Toxicol
3309:"Orilissa Product information"
2522:into the liver by the hepatic
2142:gonadotropin-releasing hormone
2083:progestogen-only birth control
1873:Suicidal ideation and behavior
930:gonadotropin-releasing hormone
742:
718:
1:
5190:10.1358/dot.2019.55.4.2930713
5004:10.1080/14656566.2017.1359258
4929:10.1517/17425255.2016.1171316
4071:10.1016/S0140-6736(01)06797-6
3670:10.1016/j.bpobgyn.2018.01.021
2240:like estradiol stimulate the
1216:in the 200 mg tablets).
1071:(menstrual pelvic pain), non-
6624:Follicle-stimulating hormone
6575:Human chorionic gonadotropin
6159:hydroxyprogesterone caproate
5898:Human chorionic gonadotropin
5893:Follicle-stimulating hormone
5440:Insulin-like growth factor 1
5047:10.1097/AOG.0000000000002675
4035:10.1097/AOG.0000000000002675
3835:Food and Drug Administration
2969:benign prostatic hyperplasia
2411:Food and Drug Administration
2179:, and thereby decreases the
2173:follicle-stimulating hormone
2071:combined birth control pills
1669:Tooltip alanine transaminase
1174:sodium carbonate monohydrate
1017:Food and Drug Administration
836:, sold under the brand name
6256:Estrogens and antiestrogens
6251:Androgens and antiandrogens
6167:medroxyprogesterone acetate
5482:Thyroid-stimulating hormone
5396:Adrenocorticotropic hormone
4822:Ducharme J (25 July 2018).
2460:of elagolix is 80% and its
2439:area-under-the-curve levels
2417:for the medication, but in
1019:(FDA) considers it to be a
6783:
5098:Lamb YN (September 2018).
5082:10.1016/j.jogc.2018.01.004
4441:J. Clin. Endocrinol. Metab
4106:J. Clin. Endocrinol. Metab
3583:Lamb YN (September 2018).
3472:J. Clin. Endocrinol. Metab
2743:of 653.58 g/mol. The
2627:
1887:, including elevations of
1878:mental health professional
1047:, the inner lining of the
1015:in January 2019. The U.S.
708:Chemical and physical data
372:Continuous: 2.2–10.8 hours
6757:Trifluoromethyl compounds
6717:Drugs developed by AbbVie
6204:
5116:10.1007/s40265-018-0977-4
4967:10.1007/s00404-017-4328-6
4849:Belluz J (26 July 2018).
4255:. FDA. 14 November 2017.
4178:"Orilissa AbbVie Leaflet"
3883:10.1007/s10815-010-9436-1
3601:10.1007/s40265-018-0977-4
3413:10.3390/molecules22122188
2896:, is available in Japan.
2695:. The compound is freely
2645:. This is in contrast to
2504:-glucuronosyltransferases
2398:Elagolix is taken by the
2384:
2290:
2278:
2144:(GnRH). As such, it is a
1995:(a moderate inhibitor of
1761:(BMD) and changes in the
1671:>3 times upper limit.
1626:
1021:first-in-class medication
806:
786:
399:
46:
37:
6392:Leuprorelin (leuprolide)
5786:Leuprorelin (leuprolide)
4992:Expert Opin Pharmacother
4579:10.1177/1933719114549848
4532:10.1177/1933719113497292
4223:10.1177/1933719112459244
3871:J. Assist. Reprod. Genet
3839:(Report). January 2019.
2931:(uterine leiomyoma) and
2248:, and thereby aggravate
1892:alanine aminotransferase
1133:in premenopausal women,
1007:was followed by that of
963:are responsible for the
880:menopausal-like symptoms
858:heavy menstrual bleeding
370:Single dose: 2.4–6.3 hrs
6570:Choriogonadotropin alfa
5225:Drug Information Portal
5063:Taylor HS (July 2018).
3921:Cone A (25 July 2018).
2431:drug accumulation ratio
2403:route of administration
1168:in the tablets include
6427:Zoptarelin doxorubicin
4478:"Testicular Disorders"
2957:norethisterone acetate
2780:Neurocrine Biosciences
2777:pharmaceutical company
2466:volume of distribution
2458:plasma protein binding
2374:
2124:competitive antagonist
2079:hormonal birth control
2075:combined birth control
1885:elevated liver enzymes
1790:elevated liver enzymes
1580:Elevated liver enzymes
1274:Combined birth control
6505:Teverelix (antarelix)
6312:gonadotropin receptor
6151:chlormadinone acetate
5160:10.1093/humrep/dey368
5069:J Obstet Gynaecol Can
4955:Arch. Gynecol. Obstet
4710:US patent 7056927
4480:. In Melmed S (ed.).
3973:10.1056/NEJMoa1700089
2927:for the treatment of
2462:blood-to-plasma ratio
2372:
1178:pregelatinized starch
6619:Corifollitropin alfa
6485:Ornirelix (ornitide)
6163:gestonorone caproate
5999:Aromatase inhibitors
5448:Mecasermin rinfabate
4454:10.1210/jc.2016-3845
4119:10.1210/jc.2009-0345
3484:10.1210/jc.2008-1695
2850:of the drug and its
2800:New Drug Application
2558:groups. Elagolix is
1759:bone mineral density
1227:of elagolix include
1166:inactive ingredients
878:of elagolix include
6654:Varfollitropin alfa
6639:Follitropin epsilon
6580:Luteinizing hormone
6155:cyproterone acetate
6083:prolactin releasers
5903:Luteinizing hormone
5508:Posterior pituitary
4151:. 29 October 2021.
2834:Society and culture
2788:Abbott Laboratories
2427:peak concentrations
2195:hormones including
2169:luteinizing hormone
2115:Elagolix acts as a
2073:and other forms of
1911:In the event of an
1806:estrogen deficiency
1731:decreased sex drive
1683:menopausal symptoms
1442:Depressive symptoms
1410:Mood changes/swings
1311:
1198:polyethylene glycol
34:
6767:Uracil derivatives
6231:Never to phase III
6133:diethylstilbestrol
5387:Anterior pituitary
4722:2020-11-27 at the
4281:Becker KL (2001).
4065:(9295): 1793–803.
3738:2016-12-20 at the
3355:. 4 October 2018.
2910:generic medication
2579:hepatic impairment
2508:terminal half-life
2375:
2261:terminal half-life
2230:that can be taken
2177:anterior pituitary
1833:menstrual bleeding
1309:
1237:hepatic impairment
1186:magnesium stearate
1139:precocious puberty
1084:sexual intercourse
576:Sodium salt:
548:Sodium salt:
435:Sodium salt:
368:Typical: 4–6 hours
138:NBI-56418, ABT-620
6682:
6681:
6678:
6677:
6475:Iturelix (antide)
6269:
6268:
6200:
6199:
6171:megestrol acetate
6062:nandrolone esters
6054:anabolic steroids
6032:Antigonadotropins
5921:
5920:
5870:
5869:
5666:
5665:
5662:
5661:
5502:
5501:
5381:
5380:
5110:(14): 1501–1508.
4998:(13): 1391–1397.
4899:10.2217/whe.14.68
4750:10.1021/jm049218c
4625:978-1-4557-2758-2
4491:978-0-323-29738-7
4380:978-1-60913-345-0
4340:10.2217/whe.15.42
4296:978-0-7817-1750-2
3774:10.1021/jm8006454
3595:(14): 1501–1508.
3561:10.2217/whe.14.68
3317:. 25 April 2012.
2717:molecular formula
2483:, with the major
2396:
2395:
2359:drug interactions
2302:
2301:
2132:biological target
1930:drug interactions
1917:adverse reactions
1845:pregnancy testing
1675:
1674:
1596:Suicidal ideation
1225:Contraindications
1220:Contraindications
1210:carmine high tint
1204:, and a distinct
1190:polyvinyl alcohol
1141:in children, and
920:biological target
866:enlarged prostate
831:
830:
777:Interactive image
658:CompTox Dashboard
303:
291:
187:
130:Orilissa, Oriahnn
27:Chemical compound
16:(Redirected from
6774:
6752:Pyrimidinediones
6742:GnRH antagonists
6699:
6698:
6697:
6690:
6663:
6634:Follitropin beta
6629:Follitropin alfa
6606:
6602:
6557:
6553:
6547:
6352:Azagly-nafarelin
6329:
6325:
6309:
6305:
6296:
6289:
6282:
6273:
6245:
6129:ethinylestradiol
6125:estradiol esters
6044:
6022:
6018:
6011:
5982:
5978:
5948:
5936:Progonadotropins
5932:
5881:
5746:Azagly-nafarelin
5731:
5719:
5706:
5702:
5693:
5686:
5679:
5670:
5513:
5392:
5281:
5256:
5249:
5242:
5233:
5228:
5209:
5172:
5162:
5137:
5127:
5094:
5084:
5059:
5049:
5023:
4986:
4948:
4911:
4901:
4867:
4866:
4864:
4862:
4846:
4840:
4839:
4837:
4835:
4819:
4813:
4812:
4810:
4809:
4794:
4788:
4787:
4785:
4783:
4768:
4762:
4761:
4732:
4726:
4718:
4717:
4713:
4706:
4700:
4699:
4698:
4696:
4679:
4673:
4672:
4670:
4668:
4653:
4642:
4641:
4639:
4637:
4607:
4601:
4600:
4590:
4558:
4552:
4551:
4514:
4508:
4507:
4505:
4503:
4473:
4467:
4466:
4456:
4447:(5): 1683–1691.
4432:
4397:
4396:
4394:
4392:
4362:
4353:
4352:
4342:
4318:
4312:
4311:
4309:
4308:
4278:
4269:
4268:
4266:
4264:
4249:
4243:
4242:
4206:
4200:
4199:
4197:
4195:
4189:
4182:
4174:
4168:
4167:
4165:
4163:
4157:
4146:
4138:
4132:
4131:
4121:
4097:
4091:
4090:
4054:
4048:
4047:
4037:
4012:
3997:
3996:
3994:
3993:
3975:
3950:
3939:
3938:
3936:
3934:
3918:
3905:
3904:
3894:
3862:
3853:
3852:
3850:
3848:
3830:
3822:
3816:
3815:
3813:
3812:
3797:
3786:
3785:
3756:
3743:
3729:
3690:
3689:
3652:
3623:
3622:
3612:
3580:
3574:
3573:
3563:
3539:
3506:
3505:
3495:
3463:
3436:
3435:
3425:
3415:
3391:
3372:
3371:
3369:
3367:
3361:
3354:
3346:
3331:
3330:
3328:
3326:
3305:
3290:
3289:
3287:
3285:
3266:
2929:uterine fibroids
2907:
2867:
2863:
2858:
2854:
2741:molecular weight
2583:pharmacokinetics
2575:renal impairment
2562:less than 3% in
2503:
2389:
2388:
2377:
2365:Pharmacokinetics
2324:menstrual cycles
2306:follicular phase
2295:
2294:
2283:
2282:
2271:
2219:, elagolix is a
2111:Pharmacodynamics
2093:, and high-dose
2044:ethinylestradiol
1670:
1666:
1662:= Asymptomatic;
1656:decreased libido
1562:
1541:
1329:
1321:
1312:
1194:titanium dioxide
1035:associated with
992:GnRH antagonists
906:, and decreased
854:uterine fibroids
848:associated with
779:
759:
744:
738:
732:
726:
720:
703:
692:
681:
680:
666:
664:
648:
642:
621:
601:
581:
573:
553:
545:
525:
505:
485:
465:
455:
454:
440:
432:
364:
301:
298:
290:
287:
265:
197:
186:
183:
170:
156:
116:
112:
106:
105:
102:
101:
98:
95:
92:
89:
86:
83:
80:
77:
74:
71:
51:
42:
35:
33:
21:
6782:
6781:
6777:
6776:
6775:
6773:
6772:
6771:
6727:CYP3A4 inducers
6707:
6706:
6705:
6695:
6693:
6685:
6683:
6674:
6604:
6594:
6555:
6536:
6327:
6317:
6307:
6300:
6270:
6265:
6236:
6221:Clinical trials
6196:
6075:
6026:
6020:
5980:
5927:
5917:
5866:
5805:
5722:
5711:
5704:
5697:
5667:
5658:
5611:
5564:
5550:
5498:
5476:
5422:
5377:
5341:
5309:
5270:
5265:and analogues (
5260:
5219:
5216:
5175:
5140:
5097:
5062:
5026:
4989:
4951:
4914:
4879:
4876:
4874:Further reading
4871:
4870:
4860:
4858:
4848:
4847:
4843:
4833:
4831:
4821:
4820:
4816:
4807:
4805:
4796:
4795:
4791:
4781:
4779:
4770:
4769:
4765:
4734:
4733:
4729:
4724:Wayback Machine
4715:
4708:
4707:
4703:
4694:
4692:
4681:
4680:
4676:
4666:
4664:
4655:
4654:
4645:
4635:
4633:
4626:
4609:
4608:
4604:
4573:(11): 1341–51.
4560:
4559:
4555:
4516:
4515:
4511:
4501:
4499:
4492:
4475:
4474:
4470:
4434:
4433:
4400:
4390:
4388:
4381:
4367:"Womens Health"
4364:
4363:
4356:
4320:
4319:
4315:
4306:
4304:
4297:
4283:"Endometriosis"
4280:
4279:
4272:
4262:
4260:
4251:
4250:
4246:
4208:
4207:
4203:
4193:
4191:
4187:
4180:
4176:
4175:
4171:
4161:
4159:
4155:
4144:
4140:
4139:
4135:
4099:
4098:
4094:
4056:
4055:
4051:
4014:
4013:
4000:
3991:
3989:
3960:N. Engl. J. Med
3952:
3951:
3942:
3932:
3930:
3920:
3919:
3908:
3864:
3863:
3856:
3846:
3844:
3828:
3824:
3823:
3819:
3810:
3808:
3799:
3798:
3789:
3768:(23): 7478–85.
3758:
3757:
3746:
3740:Wayback Machine
3730:
3693:
3654:
3653:
3626:
3582:
3581:
3577:
3541:
3540:
3509:
3465:
3464:
3439:
3393:
3392:
3375:
3365:
3363:
3359:
3352:
3348:
3347:
3334:
3324:
3322:
3307:
3306:
3293:
3283:
3281:
3268:
3267:
2982:
2977:
2965:prostate cancer
2939:) in women. An
2925:clinical trials
2918:
2905:
2902:
2890:
2882:
2865:
2856:
2841:
2836:
2808:GnRH modulators
2795:clinical trials
2773:
2766:
2762:
2758:
2754:
2750:
2738:
2734:
2730:
2726:
2722:
2632:
2626:
2591:body mass index
2419:animal research
2407:bioavailability
2386:
2367:
2361:with elagolix.
2292:
2280:
2274:External images
2175:(FSH) from the
2158:pituitary gland
2155:
2146:GnRH antagonist
2139:peptide hormone
2113:
2108:
1938:cytochrome P450
1926:
1909:
1668:
1490:Nasopharyngitis
1335:
1330:
1322:
1307:
1295:milk production
1222:
1155:
1153:Available forms
1143:hormone therapy
1135:prostate cancer
1123:desensitization
1098:quality of life
1094:clinical trials
1029:
982:nature and its
862:prostate cancer
827:
824:
819:
814:
813:
802:
799:
794:
793:
782:
757:
747:
741:
735:
729:
723:
684:
660:
652:
624:
604:
584:
556:
528:
508:
488:
468:
451:
443:
415:
412:
407:
406:
386:
371:
369:
362:
334:Protein binding
324:Bioavailability
316:Pharmacokinetic
310:
269:
243:GnRH antagonist
225:
218:
215:Contraindicated
207:
200:
114:
110:
107:
68:
64:
28:
23:
22:
15:
12:
11:
5:
6780:
6778:
6770:
6769:
6764:
6759:
6754:
6749:
6744:
6739:
6734:
6729:
6724:
6719:
6709:
6708:
6704:
6703:
6680:
6679:
6676:
6675:
6673:
6672:
6657:
6656:
6651:
6649:Urofollitropin
6646:
6641:
6636:
6631:
6626:
6621:
6609:
6607:
6596:
6595:
6593:
6592:
6587:
6582:
6577:
6572:
6560:
6558:
6544:
6538:
6537:
6535:
6534:
6529:
6524:
6519:
6514:
6502:
6497:
6492:
6487:
6482:
6477:
6472:
6467:
6462:
6457:
6452:
6447:
6442:
6430:
6429:
6424:
6419:
6414:
6409:
6404:
6399:
6394:
6389:
6384:
6379:
6374:
6369:
6364:
6359:
6354:
6349:
6344:
6332:
6330:
6319:
6318:
6301:
6299:
6298:
6291:
6284:
6276:
6267:
6266:
6264:
6263:
6258:
6253:
6248:
6240:
6235:
6234:
6233:
6232:
6229:
6218:
6212:
6206:
6205:
6202:
6201:
6198:
6197:
6195:
6194:
6189:
6184:
6175:
6174:
6140:
6137:paroxypropione
6110:
6103:chlorpromazine
6091:metoclopramide
6073:
6069:
6036:
6034:
6028:
6027:
6025:
6024:
6006:
5996:
5969:
5940:
5938:
5929:
5923:
5922:
5919:
5918:
5916:
5915:
5913:Urofollitropin
5910:
5905:
5900:
5895:
5889:
5887:
5878:
5872:
5871:
5868:
5867:
5865:
5864:
5854:
5849:
5840:
5839:
5834:
5829:
5824:
5815:
5813:
5807:
5806:
5804:
5803:
5798:
5793:
5788:
5783:
5778:
5773:
5768:
5763:
5758:
5753:
5748:
5739:
5737:
5728:
5713:
5712:
5698:
5696:
5695:
5688:
5681:
5673:
5664:
5663:
5660:
5659:
5657:
5656:
5651:
5646:
5641:
5636:
5631:
5626:
5624:Demeclocycline
5621:
5606:
5601:
5596:
5591:
5586:
5574:
5572:
5566:
5565:
5563:
5562:
5557:
5545:
5540:
5535:
5530:
5521:
5519:
5510:
5504:
5503:
5500:
5499:
5497:
5496:
5487:
5485:
5478:
5477:
5467:
5466:
5461:
5456:
5451:
5433:
5431:
5428:Growth hormone
5424:
5423:
5421:
5420:
5418:Tetracosactide
5415:
5410:
5401:
5399:
5389:
5383:
5382:
5379:
5378:
5376:
5375:
5370:
5365:
5360:
5351:
5349:
5343:
5342:
5340:
5339:
5329:
5324:
5319:
5304:
5299:
5290:
5288:
5278:
5272:
5271:
5261:
5259:
5258:
5251:
5244:
5236:
5230:
5229:
5215:
5214:External links
5212:
5211:
5210:
5184:(4): 237–246.
5173:
5153:(2): 193–199.
5138:
5095:
5075:(7): 931–934.
5060:
5040:(1): 147–160.
5034:Obstet Gynecol
5024:
4987:
4961:(4): 827–832.
4949:
4912:
4886:Women's Health
4875:
4872:
4869:
4868:
4841:
4814:
4789:
4763:
4744:(4): 1169–78.
4727:
4701:
4674:
4659:. ChemIDplus.
4643:
4624:
4602:
4553:
4509:
4490:
4468:
4398:
4379:
4354:
4327:Women's Health
4313:
4295:
4270:
4244:
4201:
4169:
4133:
4112:(9): 3132–54.
4092:
4049:
4028:(1): 147–160.
4022:Obstet Gynecol
3998:
3940:
3906:
3854:
3817:
3787:
3744:
3691:
3624:
3575:
3548:Women's Health
3507:
3437:
3373:
3332:
3291:
3276:. 5 May 2020.
2979:
2978:
2976:
2973:
2917:
2914:
2901:
2898:
2889:
2886:
2881:
2878:
2840:
2837:
2835:
2832:
2816:small-molecule
2772:
2769:
2764:
2760:
2756:
2752:
2748:
2736:
2732:
2728:
2724:
2720:
2647:GnRH analogues
2636:small-molecule
2634:Elagolix is a
2625:
2622:
2618:P-glycoprotein
2394:
2393:
2382:
2381:
2380:External image
2366:
2363:
2347:P-glycoprotein
2310:postmenopausal
2300:
2299:
2288:
2287:
2276:
2275:
2225:small-molecule
2217:GnRH analogues
2153:
2112:
2109:
2107:
2104:
2087:antiestrogenic
2060:norelgestromin
2056:norethisterone
2036:P-glycoprotein
1959:may alter the
1925:
1922:
1908:
1905:
1739:abdominal pain
1721:(joint pain),
1705:(cessation of
1673:
1672:
1636:abdominal pain
1624:
1623:
1620:
1617:
1614:
1608:
1607:
1604:
1601:
1598:
1592:
1591:
1588:
1585:
1582:
1576:
1575:
1572:
1569:
1566:
1555:
1554:
1551:
1548:
1545:
1534:
1533:
1530:
1527:
1524:
1518:
1517:
1514:
1511:
1508:
1502:
1501:
1498:
1495:
1492:
1486:
1485:
1482:
1479:
1476:
1470:
1469:
1466:
1463:
1460:
1454:
1453:
1450:
1447:
1444:
1438:
1437:
1434:
1431:
1428:
1422:
1421:
1418:
1415:
1412:
1406:
1405:
1402:
1399:
1396:
1390:
1389:
1386:
1383:
1380:
1374:
1373:
1370:
1367:
1364:
1358:
1357:
1354:
1351:
1348:
1338:
1337:
1332:
1324:
1316:
1306:
1303:
1221:
1218:
1214:iron oxide red
1206:color additive
1154:
1151:
1028:
1025:
980:small-molecule
972:GnRH modulator
959:levels in the
829:
828:
826:
825:
822:
820:
817:
809:
808:
807:
804:
803:
801:
800:
797:
789:
788:
787:
784:
783:
781:
780:
772:
770:
762:
761:
755:
749:
748:
745:
739:
733:
727:
721:
716:
710:
709:
705:
704:
694:
686:
685:
683:
682:
674:DTXSID40232348
669:
667:
654:
653:
651:
650:
634:
632:
626:
625:
623:
622:
614:
612:
606:
605:
603:
602:
594:
592:
586:
585:
583:
582:
574:
566:
564:
558:
557:
555:
554:
546:
538:
536:
530:
529:
527:
526:
518:
516:
510:
509:
507:
506:
498:
496:
490:
489:
487:
486:
478:
476:
470:
469:
467:
466:
458:
456:
445:
444:
442:
441:
433:
425:
423:
417:
416:
414:
413:
410:
402:
401:
400:
397:
396:
392:
391:
380:
374:
373:
366:
357:
356:
346:
340:
339:
336:
330:
329:
326:
320:
319:
312:
311:
309:
308:
296:
284:
282:
276:
275:
271:
270:
268:
267:
254:
252:
246:
245:
240:
234:
233:
228:
226:administration
220:
219:
217:
216:
212:
210:
202:
201:
199:
198:
180:
178:
172:
171:
164:
158:
157:
150:
140:
139:
136:
132:
131:
128:
122:
121:
62:
58:
57:
53:
52:
44:
43:
26:
24:
14:
13:
10:
9:
6:
4:
3:
2:
6779:
6768:
6765:
6763:
6760:
6758:
6755:
6753:
6750:
6748:
6745:
6743:
6740:
6738:
6735:
6733:
6730:
6728:
6725:
6723:
6720:
6718:
6715:
6714:
6712:
6702:
6692:
6688:
6671:
6668:
6667:Non-peptides:
6665:
6659:
6658:
6655:
6652:
6650:
6647:
6645:
6642:
6640:
6637:
6635:
6632:
6630:
6627:
6625:
6622:
6620:
6617:
6614:
6611:
6610:
6608:
6603:
6597:
6591:
6588:
6586:
6585:Lutropin alfa
6583:
6581:
6578:
6576:
6573:
6571:
6568:
6565:
6562:
6561:
6559:
6554:
6548:
6545:
6543:
6539:
6533:
6530:
6528:
6525:
6523:
6520:
6518:
6515:
6513:
6510:
6509:Non-peptides:
6506:
6503:
6501:
6498:
6496:
6493:
6491:
6488:
6486:
6483:
6481:
6478:
6476:
6473:
6471:
6468:
6466:
6463:
6461:
6458:
6456:
6453:
6451:
6448:
6446:
6443:
6441:
6438:
6435:
6432:
6431:
6428:
6425:
6423:
6420:
6418:
6415:
6413:
6410:
6408:
6405:
6403:
6400:
6398:
6395:
6393:
6390:
6388:
6385:
6383:
6380:
6378:
6375:
6373:
6370:
6368:
6365:
6363:
6360:
6358:
6355:
6353:
6350:
6348:
6345:
6343:
6340:
6337:
6334:
6333:
6331:
6326:
6320:
6316:
6313:
6306:
6297:
6292:
6290:
6285:
6283:
6278:
6277:
6274:
6262:
6259:
6257:
6254:
6252:
6249:
6247:
6241:
6238:
6237:
6230:
6228:
6225:
6224:
6222:
6219:
6216:
6213:
6211:
6208:
6207:
6203:
6193:
6190:
6188:
6185:
6183:
6180:
6177:
6176:
6172:
6168:
6164:
6160:
6156:
6152:
6148:
6144:
6141:
6138:
6134:
6130:
6126:
6122:
6118:
6114:
6111:
6108:
6104:
6100:
6096:
6092:
6088:
6084:
6080:
6077:
6070:
6067:
6063:
6059:
6055:
6051:
6048:
6046:
6038:
6037:
6035:
6033:
6029:
6019:
6013:
6007:
6004:
6000:
5997:
5994:
5990:
5986:
5979:
5973:
5972:Antiestrogens
5970:
5967:
5963:
5959:
5955:
5954:Antiandrogens
5952:
5950:
5942:
5941:
5939:
5937:
5933:
5930:
5924:
5914:
5911:
5909:
5906:
5904:
5901:
5899:
5896:
5894:
5891:
5890:
5888:
5886:
5882:
5879:
5877:
5876:Gonadotropins
5873:
5862:
5858:
5855:
5853:
5850:
5848:
5845:
5842:
5841:
5838:
5835:
5833:
5830:
5828:
5825:
5823:
5820:
5817:
5816:
5814:
5812:
5808:
5802:
5799:
5797:
5794:
5792:
5789:
5787:
5784:
5782:
5779:
5777:
5774:
5772:
5769:
5767:
5764:
5762:
5759:
5757:
5754:
5752:
5749:
5747:
5744:
5741:
5740:
5738:
5736:
5732:
5729:
5726:
5721:
5714:
5710:
5709:gonadotropins
5703:
5694:
5689:
5687:
5682:
5680:
5675:
5674:
5671:
5655:
5652:
5650:
5647:
5645:
5642:
5640:
5637:
5635:
5632:
5630:
5627:
5625:
5622:
5620:
5616:
5615:
5610:
5607:
5605:
5602:
5600:
5597:
5595:
5592:
5590:
5587:
5585:
5582:
5580:
5576:
5575:
5573:
5571:
5567:
5561:
5558:
5556:
5553:
5549:
5546:
5544:
5541:
5539:
5536:
5534:
5531:
5529:
5528:Argiprestocin
5526:
5523:
5522:
5520:
5518:
5514:
5511:
5509:
5505:
5495:
5492:
5489:
5488:
5486:
5483:
5479:
5475:
5474:
5471:
5465:
5462:
5460:
5457:
5455:
5452:
5449:
5445:
5441:
5438:
5435:
5434:
5432:
5429:
5425:
5419:
5416:
5414:
5411:
5409:
5408:Corticotropin
5406:
5403:
5402:
5400:
5397:
5393:
5390:
5388:
5384:
5374:
5371:
5369:
5366:
5364:
5361:
5359:
5356:
5353:
5352:
5350:
5348:
5344:
5337:
5333:
5330:
5328:
5325:
5323:
5320:
5318:
5315:
5313:
5308:
5305:
5303:
5300:
5298:
5295:
5292:
5291:
5289:
5286:
5282:
5279:
5277:
5273:
5268:
5264:
5257:
5252:
5250:
5245:
5243:
5238:
5237:
5234:
5226:
5222:
5218:
5217:
5213:
5207:
5203:
5199:
5195:
5191:
5187:
5183:
5179:
5174:
5170:
5166:
5161:
5156:
5152:
5148:
5144:
5139:
5135:
5131:
5126:
5121:
5117:
5113:
5109:
5105:
5101:
5096:
5092:
5088:
5083:
5078:
5074:
5070:
5066:
5061:
5057:
5053:
5048:
5043:
5039:
5035:
5031:
5025:
5021:
5017:
5013:
5009:
5005:
5001:
4997:
4993:
4988:
4984:
4980:
4976:
4972:
4968:
4964:
4960:
4956:
4950:
4946:
4942:
4938:
4934:
4930:
4926:
4922:
4918:
4913:
4909:
4905:
4900:
4895:
4891:
4887:
4883:
4878:
4877:
4873:
4856:
4852:
4845:
4842:
4829:
4825:
4818:
4815:
4803:
4799:
4793:
4790:
4777:
4773:
4767:
4764:
4759:
4755:
4751:
4747:
4743:
4739:
4731:
4728:
4725:
4721:
4711:
4705:
4702:
4690:
4686:
4685:
4678:
4675:
4662:
4658:
4652:
4650:
4648:
4644:
4631:
4627:
4621:
4617:
4613:
4606:
4603:
4598:
4594:
4589:
4584:
4580:
4576:
4572:
4568:
4564:
4557:
4554:
4549:
4545:
4541:
4537:
4533:
4529:
4526:(3): 363–71.
4525:
4521:
4513:
4510:
4497:
4493:
4487:
4483:
4479:
4472:
4469:
4464:
4460:
4455:
4450:
4446:
4442:
4438:
4431:
4429:
4427:
4425:
4423:
4421:
4419:
4417:
4415:
4413:
4411:
4409:
4407:
4405:
4403:
4399:
4386:
4382:
4376:
4372:
4368:
4361:
4359:
4355:
4350:
4346:
4341:
4336:
4333:(5): 643–52.
4332:
4328:
4324:
4317:
4314:
4302:
4298:
4292:
4288:
4284:
4277:
4275:
4271:
4258:
4254:
4248:
4245:
4240:
4236:
4232:
4228:
4224:
4220:
4216:
4212:
4205:
4202:
4186:
4179:
4173:
4170:
4154:
4150:
4143:
4137:
4134:
4129:
4125:
4120:
4115:
4111:
4107:
4103:
4096:
4093:
4088:
4084:
4080:
4076:
4072:
4068:
4064:
4060:
4053:
4050:
4045:
4041:
4036:
4031:
4027:
4023:
4019:
4011:
4009:
4007:
4005:
4003:
3999:
3987:
3983:
3979:
3974:
3969:
3965:
3961:
3957:
3949:
3947:
3945:
3941:
3928:
3924:
3917:
3915:
3913:
3911:
3907:
3902:
3898:
3893:
3888:
3884:
3880:
3876:
3872:
3868:
3861:
3859:
3855:
3842:
3838:
3836:
3827:
3821:
3818:
3806:
3802:
3796:
3794:
3792:
3788:
3783:
3779:
3775:
3771:
3767:
3763:
3755:
3753:
3751:
3749:
3745:
3741:
3737:
3734:
3731:AdisInsight:
3728:
3726:
3724:
3722:
3720:
3718:
3716:
3714:
3712:
3710:
3708:
3706:
3704:
3702:
3700:
3698:
3696:
3692:
3687:
3683:
3679:
3675:
3671:
3667:
3663:
3659:
3651:
3649:
3647:
3645:
3643:
3641:
3639:
3637:
3635:
3633:
3631:
3629:
3625:
3620:
3616:
3611:
3606:
3602:
3598:
3594:
3590:
3586:
3579:
3576:
3571:
3567:
3562:
3557:
3553:
3549:
3545:
3538:
3536:
3534:
3532:
3530:
3528:
3526:
3524:
3522:
3520:
3518:
3516:
3514:
3512:
3508:
3503:
3499:
3494:
3489:
3485:
3481:
3478:(2): 545–51.
3477:
3473:
3469:
3462:
3460:
3458:
3456:
3454:
3452:
3450:
3448:
3446:
3444:
3442:
3438:
3433:
3429:
3424:
3419:
3414:
3409:
3405:
3401:
3397:
3390:
3388:
3386:
3384:
3382:
3380:
3378:
3374:
3358:
3351:
3345:
3343:
3341:
3339:
3337:
3333:
3320:
3316:
3315:
3314:Health Canada
3310:
3304:
3302:
3300:
3298:
3296:
3292:
3279:
3275:
3271:
3265:
3263:
3261:
3259:
3257:
3255:
3253:
3251:
3249:
3247:
3245:
3243:
3241:
3239:
3237:
3235:
3233:
3231:
3229:
3227:
3225:
3223:
3221:
3219:
3217:
3215:
3213:
3211:
3209:
3207:
3205:
3203:
3201:
3199:
3197:
3195:
3193:
3191:
3189:
3187:
3185:
3183:
3181:
3179:
3177:
3175:
3173:
3171:
3169:
3167:
3165:
3163:
3161:
3159:
3157:
3155:
3153:
3151:
3149:
3147:
3145:
3143:
3141:
3139:
3137:
3135:
3133:
3131:
3129:
3127:
3125:
3123:
3121:
3119:
3117:
3115:
3113:
3111:
3109:
3107:
3105:
3103:
3101:
3099:
3097:
3095:
3093:
3091:
3089:
3087:
3085:
3083:
3081:
3079:
3077:
3075:
3073:
3071:
3069:
3067:
3065:
3063:
3061:
3059:
3057:
3055:
3053:
3051:
3049:
3047:
3045:
3043:
3041:
3039:
3037:
3035:
3033:
3031:
3029:
3027:
3025:
3023:
3021:
3019:
3017:
3015:
3013:
3011:
3009:
3007:
3005:
3003:
3001:
2999:
2997:
2995:
2993:
2991:
2989:
2987:
2985:
2981:
2974:
2972:
2970:
2966:
2962:
2958:
2954:
2950:
2946:
2942:
2938:
2934:
2930:
2926:
2923:
2915:
2913:
2911:
2899:
2897:
2895:
2887:
2885:
2879:
2877:
2875:
2871:
2864:
2855:
2849:
2845:
2839:Generic names
2838:
2833:
2831:
2829:
2825:
2821:
2820:oral activity
2817:
2813:
2809:
2805:
2804:United States
2801:
2796:
2793:
2789:
2785:
2781:
2778:
2770:
2768:
2746:
2742:
2718:
2714:
2710:
2706:
2705:chemical name
2702:
2698:
2694:
2690:
2687:
2682:
2680:
2676:
2672:
2668:
2664:
2660:
2656:
2652:
2648:
2644:
2641:
2637:
2631:
2623:
2621:
2619:
2615:
2611:
2607:
2603:
2599:
2596:
2592:
2588:
2584:
2580:
2576:
2571:
2569:
2565:
2561:
2557:
2553:
2549:
2545:
2541:
2537:
2533:
2529:
2525:
2521:
2517:
2513:
2509:
2505:
2498:
2494:
2490:
2486:
2482:
2478:
2473:
2471:
2467:
2463:
2459:
2455:
2451:
2448:
2444:
2440:
2436:
2432:
2428:
2424:
2420:
2416:
2412:
2408:
2404:
2401:
2392:
2383:
2378:
2371:
2364:
2362:
2360:
2356:
2352:
2348:
2344:
2340:
2336:
2331:
2329:
2325:
2321:
2316:
2311:
2307:
2298:
2289:
2286:
2277:
2272:
2269:
2266:
2262:
2257:
2255:
2254:endometriosis
2251:
2247:
2243:
2239:
2235:
2233:
2229:
2226:
2222:
2218:
2214:
2213:GnRH agonists
2210:
2206:
2202:
2198:
2194:
2190:
2186:
2182:
2178:
2174:
2170:
2167:
2166:gonadotropins
2163:
2159:
2151:
2147:
2143:
2140:
2137:
2133:
2130:(GnRHR), the
2129:
2125:
2122:
2118:
2110:
2105:
2103:
2101:
2100:birth control
2096:
2092:
2088:
2084:
2080:
2076:
2072:
2067:
2065:
2061:
2057:
2053:
2049:
2045:
2041:
2037:
2033:
2028:
2026:
2022:
2017:
2013:
2008:
2006:
2002:
1998:
1994:
1990:
1986:
1982:
1978:
1974:
1970:
1966:
1962:
1958:
1954:
1950:
1946:
1943:
1939:
1935:
1931:
1923:
1921:
1918:
1914:
1906:
1904:
1902:
1898:
1893:
1890:
1886:
1881:
1879:
1874:
1870:
1866:
1862:
1856:
1854:
1853:contraceptive
1850:
1846:
1842:
1838:
1834:
1829:
1827:
1823:
1819:
1815:
1811:
1810:postmenopause
1807:
1802:
1798:
1797:premenopausal
1793:
1791:
1787:
1783:
1779:
1775:
1771:
1767:
1764:
1760:
1756:
1752:
1748:
1744:
1740:
1736:
1732:
1728:
1724:
1720:
1716:
1712:
1708:
1704:
1700:
1696:
1692:
1688:
1684:
1680:
1667:
1661:
1657:
1653:
1649:
1645:
1641:
1637:
1633:
1629:
1621:
1618:
1615:
1613:
1610:
1609:
1605:
1602:
1599:
1597:
1594:
1593:
1589:
1586:
1583:
1581:
1578:
1577:
1573:
1570:
1567:
1564:
1557:
1556:
1552:
1549:
1546:
1543:
1536:
1535:
1531:
1528:
1525:
1523:
1520:
1519:
1515:
1512:
1509:
1507:
1504:
1503:
1499:
1496:
1493:
1491:
1488:
1487:
1483:
1480:
1477:
1475:
1472:
1471:
1467:
1464:
1461:
1459:
1456:
1455:
1451:
1448:
1445:
1443:
1440:
1439:
1435:
1432:
1429:
1427:
1424:
1423:
1419:
1416:
1413:
1411:
1408:
1407:
1403:
1400:
1397:
1395:
1392:
1391:
1387:
1384:
1381:
1379:
1376:
1375:
1371:
1368:
1365:
1363:
1360:
1359:
1355:
1352:
1349:
1347:
1343:
1340:
1339:
1333:
1325:
1317:
1314:
1313:
1304:
1302:
1300:
1296:
1292:
1288:
1284:
1283:breastfeeding
1279:
1275:
1271:
1269:
1265:
1264:birth control
1261:
1257:
1253:
1249:
1246:
1242:
1238:
1234:
1230:
1226:
1219:
1217:
1215:
1211:
1207:
1203:
1199:
1195:
1191:
1187:
1183:
1179:
1175:
1171:
1167:
1163:
1160:
1152:
1150:
1148:
1144:
1140:
1136:
1132:
1131:breast cancer
1128:
1124:
1119:
1117:
1113:
1108:
1106:
1101:
1099:
1095:
1092:
1087:
1085:
1082:(pain during
1081:
1077:
1074:
1070:
1066:
1062:
1058:
1054:
1050:
1046:
1042:
1041:premenopausal
1038:
1037:endometriosis
1034:
1026:
1024:
1022:
1018:
1014:
1010:
1006:
1001:
1000:GnRH analogue
997:
993:
989:
988:GnRH agonists
985:
984:oral activity
981:
977:
973:
968:
966:
962:
958:
954:
950:
946:
942:
938:
935:
931:
928:
925:
921:
918:(GnRHR), the
917:
913:
909:
905:
901:
897:
893:
889:
885:
881:
877:
873:
871:
867:
863:
859:
855:
851:
850:endometriosis
847:
843:
839:
835:
821:
816:
812:
805:
796:
792:
785:
778:
774:
773:
771:
768:
763:
756:
754:
750:
717:
715:
711:
706:
702:
698:
695:
693:
691:ECHA InfoCard
687:
679:
675:
671:
670:
668:
659:
655:
647:
646:RCSB PDB
641:
636:
635:
633:
631:
627:
620:
619:ChEMBL1208155
616:
615:
613:
611:
607:
600:
596:
595:
593:
591:
587:
580:
575:
572:
568:
567:
565:
563:
559:
552:
547:
544:
540:
539:
537:
535:
531:
524:
520:
519:
517:
515:
511:
504:
500:
499:
497:
495:
491:
484:
480:
479:
477:
475:
471:
464:
460:
459:
457:
450:
446:
439:
434:
431:
427:
426:
424:
422:
418:
409:
405:
398:
393:
389:
384:
381:
379:
375:
367:
365:
358:
354:
350:
347:
345:
341:
337:
335:
331:
327:
325:
321:
317:
313:
307:
297:
295:
286:
285:
283:
281:
277:
272:
264:
259:
256:
255:
253:
251:
247:
244:
241:
239:
235:
232:
229:
227:
221:
214:
213:
211:
209:
203:
196:
191:
182:
181:
179:
177:
173:
169:
165:
163:
159:
155:
151:
149:
145:
141:
137:
133:
129:
127:
123:
119:
118:
104:
63:
61:Pronunciation
59:
56:Clinical data
54:
50:
45:
41:
36:
19:
6737:Fluoroarenes
6666:
6660:
6615:
6612:
6566:
6563:
6542:Gonadotropin
6511:
6508:
6436:
6434:Antagonists:
6433:
6338:
6335:
6178:
6143:Progestogens
6058:testosterone
6039:
5966:enzalutamide
5962:bicalutamide
5943:
5885:Preparations
5846:
5844:Non-peptide:
5843:
5818:
5742:
5612:
5609:Terlipressin
5589:Desmopressin
5577:
5552:Antagonists:
5551:
5524:
5490:
5470:Antagonists:
5469:
5468:
5436:
5404:
5354:
5347:Somatostatin
5321:
5310:
5293:
5276:Hypothalamus
5224:
5181:
5177:
5150:
5146:
5107:
5103:
5072:
5068:
5037:
5033:
4995:
4991:
4958:
4954:
4923:(5): 581–8.
4920:
4916:
4892:(1): 19–28.
4889:
4885:
4859:. Retrieved
4844:
4832:. Retrieved
4817:
4806:. Retrieved
4792:
4780:. Retrieved
4766:
4741:
4738:J. Med. Chem
4737:
4730:
4704:
4693:, retrieved
4683:
4677:
4665:. Retrieved
4634:. Retrieved
4615:
4605:
4570:
4566:
4556:
4523:
4519:
4512:
4500:. Retrieved
4481:
4471:
4444:
4440:
4389:. Retrieved
4370:
4330:
4326:
4316:
4305:. Retrieved
4286:
4261:. Retrieved
4247:
4217:(1): 16–25.
4214:
4210:
4204:
4192:. Retrieved
4172:
4160:. Retrieved
4136:
4109:
4105:
4095:
4062:
4058:
4052:
4025:
4021:
3990:. Retrieved
3966:(1): 28–40.
3963:
3959:
3931:. Retrieved
3877:(8): 441–7.
3874:
3870:
3847:16 September
3845:. Retrieved
3832:
3820:
3809:. Retrieved
3765:
3762:J. Med. Chem
3761:
3661:
3657:
3592:
3588:
3578:
3554:(1): 19–28.
3551:
3547:
3475:
3471:
3406:(12): 2188.
3403:
3399:
3364:. Retrieved
3323:. Retrieved
3312:
3282:. Retrieved
3273:
2937:menstruation
2919:
2903:
2891:
2888:Availability
2883:
2873:
2869:
2848:generic name
2843:
2842:
2786:(previously
2774:
2712:
2708:
2683:
2657:, which are
2633:
2602:ketoconazole
2572:
2475:Elagolix is
2474:
2470:steady state
2464:is 0.6. The
2454:distribution
2435:steady state
2397:
2332:
2303:
2258:
2236:
2205:testosterone
2201:progesterone
2185:sex hormones
2136:hypothalamic
2114:
2106:Pharmacology
2068:
2048:rosuvastatin
2029:
2009:
1973:rosuvastatin
1965:ketoconazole
1927:
1924:Interactions
1910:
1897:liver injury
1882:
1857:
1830:
1801:lumbar spine
1794:
1770:appendicitis
1755:irritability
1751:constipation
1707:menstruation
1691:night sweats
1679:side effects
1676:
1659:
1652:irritability
1640:constipation
1627:
1565:(12 months)
1346:night sweats
1326:200 mg
1318:150 mg
1315:Side effect
1305:Side effects
1272:
1233:osteoporosis
1223:
1156:
1120:
1109:
1102:
1088:
1069:dysmenorrhea
1030:
1027:Medical uses
994:, which are
969:
953:testosterone
949:progesterone
941:sex hormones
924:hypothalamic
908:bone density
888:night sweats
876:Side effects
874:
837:
833:
832:
599:CHEBI:177453
361:Elimination
280:Legal status
274:Legal status
176:License data
18:C32H30F5N3O5
6417:Triptorelin
6412:Salmon GnRH
6377:Gonadorelin
6217:from market
6192:Metallibure
6099:haloperidol
6095:risperidone
6087:domperidone
6079:antagonists
6066:oxandrolone
6003:anastrozole
5993:enclomifene
5811:Antagonists
5801:Triptorelin
5766:Gonadorelin
5644:Relcovaptan
5614:Antagonists
5604:Ornipressin
5594:Felypressin
5584:Argipressin
5570:Vasopressin
5543:Demoxytocin
5494:Thyrotropin
5473:Pegvisomant
5454:Somapacitan
5413:Cosyntropin
5368:Pasireotide
5312:Antagonists
5297:Gonadorelin
5178:Drugs Today
5147:Hum. Reprod
3366:15 February
2933:menorrhagia
2880:Brand names
2818:nature and
2812:non-peptide
2651:leuprorelin
2640:non-peptide
2604:and CYP3A4
2587:body weight
2566:and 90% in
2520:circulation
2516:elimination
2477:metabolized
2315:anovulatory
2246:endometrium
2221:non-peptide
2025:gemfibrozil
2021:ciclosporin
2005:fluconazole
1865:tearfulness
1861:mood swings
1841:miscarriage
1786:suicidality
1782:miscarriage
1763:blood lipid
1743:weight gain
1687:hot flashes
1644:weight gain
1544:(6 months)
1342:Hot flashes
1291:breast milk
1260:miscarriage
1256:gemfibrozil
1252:ciclosporin
1147:transgender
1127:leuprorelin
1080:dyspareunia
1076:pelvic pain
1065:infertility
1061:pelvic pain
1055:and causes
1045:endometrium
976:non-peptide
974:due to its
961:endometrium
884:hot flashes
760: g·mol
697:100.259.758
438:832720-36-2
430:834153-87-6
395:Identifiers
162:MedlinePlus
135:Other names
126:Trade names
6762:Triketones
6711:Categories
6517:Linzagolix
6495:Prazarelix
6455:Cetrorelix
6422:Zoptarelin
6367:Fertirelin
6362:Deslorelin
6315:modulators
6187:Gestrinone
6147:progestins
6117:bifluranol
6085:) (incl.,
5928:(indirect)
5908:Menotropin
5852:Linzagolix
5827:Cetrorelix
5761:Fertirelin
5756:Deslorelin
5720:modulators
5649:Satavaptan
5639:Nelivaptan
5634:Mozavaptan
5629:Lixivaptan
5619:Conivaptan
5548:Nacartocin
5538:Cargutocin
5533:Carbetocin
5464:Somatrogon
5444:Mecasermin
5373:Vapreotide
5363:Octreotide
5358:Lanreotide
5317:Cetrorelix
5221:"Elagolix"
4808:2018-08-16
4567:Reprod Sci
4520:Reprod Sci
4391:24 October
4307:2018-07-26
4211:Reprod Sci
3992:2018-11-07
3811:2019-02-16
3664:: 92–101.
2975:References
2667:linzagolix
2655:cetrorelix
2628:See also:
2598:inhibitors
2443:toxicology
2351:metabolism
2209:testicular
2181:production
2064:norgestrel
1993:sertraline
1961:metabolism
1949:inhibitors
1899:, such as
1723:depression
1719:arthralgia
1703:amenorrhea
1660:Footnotes:
1616:0.2 (n=1)
1603:0.2 (n=1)
1600:0.2 (n=1)
1590:0.1 (n=1)
1587:1.1 (n=5)
1584:0.2 (n=1)
1522:Arthralgia
1362:Amenorrhea
1248:inhibitors
990:and older
937:production
912:antagonist
896:amenorrhea
765:3D model (
753:Molar mass
630:PDB ligand
551:5948VUI423
543:5B2546MB5Z
514:ChemSpider
474:IUPHAR/BPS
421:CAS Number
404:IUPAC name
344:Metabolism
238:Drug class
6670:ADX-61623
6616:Peptides:
6613:Agonists:
6567:Peptides:
6564:Agonists:
6532:Sufugolix
6527:Relugolix
6500:Ramorelix
6470:Ganirelix
6465:Detirelix
6460:Degarelix
6450:Azaline B
6437:Peptides:
6407:Peforelin
6402:Nafarelin
6387:Histrelin
6382:Goserelin
6357:Buserelin
6339:Peptides:
6336:Agonists:
6227:Phase III
6215:Withdrawn
6121:estradiol
6113:Estrogens
6107:sulpiride
6050:Androgens
5989:clomifene
5985:tamoxifen
5958:flutamide
5857:Relugolix
5837:Ganirelix
5832:Degarelix
5796:Peforelin
5791:Nafarelin
5781:Lecirelin
5776:Histrelin
5771:Goserelin
5751:Buserelin
5725:analogues
5654:Tolvaptan
5599:Lypressin
5560:Barusiban
5525:Agonists:
5491:Agonists:
5442:(IGF-1) (
5437:Agonists:
5405:Agonists:
5355:Agonists:
5332:Relugolix
5327:Ganirelix
5307:Histrelin
5302:Nafarelin
5294:Agonists:
5206:143434963
3400:Molecules
2961:progestin
2949:estradiol
2922:phase III
2900:Economics
2894:relugolix
2870:NBI-56418
2824:relugolix
2792:phase III
2745:free acid
2739:Na and a
2679:sufugolix
2675:relugolix
2663:analogues
2624:Chemistry
2614:substrate
2512:clearance
2487:being by
2355:transport
2343:inhibitor
2328:mid-cycle
2320:ovulation
2238:Estrogens
2197:estradiol
2171:(LH) and
2162:secretion
2121:selective
2095:progestin
2052:midazolam
1977:substrate
1940:(CYP450)
1934:substrate
1849:ovulation
1837:pregnancy
1826:vitamin D
1818:fractures
1814:bone loss
1778:bone loss
1774:back pain
1747:dizziness
1695:headaches
1648:dizziness
1506:Sinusitis
1378:Headaches
1369:7; 13–57
1299:breastfed
1268:bone loss
1235:, severe
1229:pregnancy
1105:bone loss
1091:phase III
1073:menstrual
1009:relugolix
986:. Unlike
945:estradiol
902:changes,
378:Excretion
363:half-life
224:Routes of
206:Pregnancy
154:Monograph
148:Drugs.com
6701:Medicine
6522:Opigolix
6512:Elagolix
6490:Ozarelix
6440:Abarelix
6397:Lutrelin
6347:Avorelin
6342:Alarelin
6239:See also
6149:, e.g.,
6115:(incl.,
6076:receptor
6012:agonists
5847:Elagolix
5822:Abarelix
5819:Peptide:
5743:Peptide:
5735:Agonists
5579:Agonists
5555:Atosiban
5517:Oxytocin
5459:Somatrem
5322:Elagolix
5198:31050692
5169:30551159
5134:30194661
5091:29921430
5056:29889764
5020:32467159
5012:28737050
4983:26422467
4975:28255765
4945:28684228
4937:27021205
4908:25581052
4855:Archived
4828:Archived
4826:. Time.
4802:Archived
4776:Archived
4758:15715483
4720:Archived
4689:archived
4661:Archived
4630:Archived
4597:25249568
4540:23885105
4496:Archived
4463:28323948
4385:Archived
4349:26389558
4301:Archived
4257:Archived
4239:21376889
4231:23012318
4185:Archived
4153:Archived
4128:19509099
4087:34316585
4079:11734258
4044:29889764
3986:Archived
3982:28525302
3927:Archived
3901:20574791
3841:Archived
3805:Archived
3782:19006286
3736:Archived
3733:Elagolix
3678:29559388
3619:30194661
3570:25581052
3502:19033369
3432:29232843
3357:Archived
3319:Archived
3278:Archived
3274:DailyMed
2953:estrogen
2941:efficacy
2916:Research
2844:Elagolix
2671:opigolix
2659:peptides
2649:such as
2643:compound
2610:rifampin
2606:inducers
2577:or mild
2560:excreted
2548:genotype
2540:genotype
2423:absorbed
2265:duration
2250:symptoms
2228:compound
2150:affinity
2069:Because
2016:genotype
1969:rifampin
1953:inducers
1913:overdose
1907:Overdose
1901:jaundice
1735:diarrhea
1711:insomnia
1632:diarrhea
1563:decrease
1547:<1–2
1542:decrease
1458:Insomnia
1366:4; 6–17
1287:excreted
1278:estrogen
1250:such as
1231:, known
1182:povidone
1170:mannitol
1137:in men,
1112:duration
1059:such as
1057:symptoms
996:peptides
965:efficacy
957:estrogen
943:such as
892:insomnia
882:such as
870:by mouth
838:Orilissa
834:Elagolix
494:DrugBank
463:11250647
385:: <3%
250:ATC code
231:By mouth
208:category
195:Elagolix
190:DailyMed
32:Elagolix
6747:Lactams
6480:LXT-101
6445:Acyline
6182:Danazol
6145:(incl.
6056:(e.g.,
6014:(e.g.,
6001:(e.g.,
5983:(e.g.,
5956:(e.g.,
5723:(incl.
5125:6244606
4861:31 July
4853:. Vox.
4834:31 July
4782:31 July
4695:31 July
4667:31 July
4636:26 July
4588:4212335
4548:9607500
4502:26 July
4263:31 July
3933:31 July
3925:. UPI.
3892:2941592
3686:3952054
3610:6244606
3493:2646513
3423:6149776
2906:US$ 850
2874:ABT-620
2846:is the
2771:History
2697:soluble
2536:encodes
2530:of the
2528:alleles
2524:OATP1B1
2485:pathway
2479:in the
2425:, with
2353:and/or
2341:and an
2335:inducer
2244:of the
2193:ovarian
2187:by the
2164:of the
2134:of the
2126:of the
2089:in the
2040:digoxin
2032:inducer
2012:OATP1B1
1985:OATP1B3
1981:OATP1B1
1936:of the
1869:placebo
1824:and/or
1822:calcium
1766:profile
1715:anxiety
1612:Suicide
1558:>8%
1537:>8%
1426:Anxiety
1334:Placebo
1297:or the
1243:(OATP)
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