911:
1119:
participants in the trial had advanced prostate cancer. Participants were randomly assigned to receive either one relugolix tablet daily (on the first day they received three tables) or an active control (leuprolide acetate) which was given as an injection under the skin every three months. The participants and healthcare providers were aware of which treatment was being given. The treatment lasted for 48 weeks. The efficacy of relugolix was assessed by the percentage of participants who achieved and maintained low testosterone level equal to castration.
592:
40:
31:
3868:
1896:
1964:
1555:
Miwa K, Hitaka T, Imada T, Sasaki S, Yoshimatsu M, Kusaka M, et al. (July 2011). "Discovery of 1-{4--3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothienopyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing
1596:
Nakata D, Masaki T, Tanaka A, Yoshimatsu M, Akinaga Y, Asada M, et al. (January 2014). "Suppression of the hypothalamic-pituitary-gonadal axis by TAK-385 (relugolix), a novel, investigational, orally active, small molecule gonadotropin-releasing hormone (GnRH) antagonist: studies in human GnRH
944:
levels (<20 pg/mL) within 24 hours in premenopausal women. In the control group of women, estradiol levels fluctuated between 50 and 250 pg/mL. Estradiol levels have been found to return to normal concentrations within 4 weeks of discontinuation of relugolix in premenopausal
1205:
adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product
Orgovyx, intended for the treatment of prostate cancer. The applicant for this medicinal product is Myovant Sciences Ireland Limited. Relugolix was approved for medical use in the European
1118:
The FDA approved relugolix based on evidence from a clinical trial (NCT03085095) of 930 participants 48 to 97 years old with advanced prostate cancer. The trial was conducted at 155 sites in the United States, Canada, and countries in South
America, Europe and the Asia Pacific region. All
1111:(developmental code name TAK-013), which was developed by the same researchers. Relugolix was approved for the treatment of uterine fibroids in Japan in January 2019. It was the second orally active GnRH antagonist to be introduced for medical use, following
2425:
3465:
1004:
are reached within 7 days with 40 mg/day relugolix administration. There is an approximate 2-fold accumulation of relugolix by 2 weeks of continuous administration. Food diminishes the oral
1780:
2418:
674:
716:
InChI=1S/C29H27F2N7O5S/c1-36(2)14-19-24-26(39)38(22-12-13-23(42-3)34-33-22)29(41)37(15-18-20(30)6-5-7-21(18)31)27(24)44-25(19)16-8-10-17(11-9-16)32-28(40)35-43-4/h5-13H,14-15H2,1-4H3,(H2,32,35,40)
289:
1365:
2411:
2225:
Elancheran R, Maruthanila VL, Ramanathan M, Kabilan S, Devi R, Kunnumakara A, Kotoky J (2015). "Recent discoveries and developments of androgen receptor based therapy for prostate cancer".
2310:
Elsharoud A, Ali M, Al-Hendy A (2019). "Relugolix. GnRH (LHRH) receptor antagonist, Treatment of uterine fibroids, Treatment of endometriosis-related pain, Treatment of prostate cancer".
1894:, Cho N, Imada T, Hitaka T, Miwa K, Kusaka M, Suzuki N, "Thienopyrimidine compounds and use thereof", issued 27 November 2007, assigned to Takeda Pharmaceutical Co Ltd.
3458:
1169:
Relugolix is sold under the brand name
Orgovyx for the treatment of prostate cancer and under the brand name Relumina for the treatment of uterine fibroids. Relugolix compounded with
225:
830:
Relugolix was approved for use for the treatment of uterine fibroids in Japan in
January 2019, and for the treatment of prostate cancer in the United States in December 2020.
3451:
3414:
2862:
910:
3722:
1510:
1198:
137:
1844:"Suppression of gonadotropins and estradiol in premenopausal women by oral administration of the nonpeptide gonadotropin-releasing hormone antagonist elagolix"
688:
3432:
3032:
2507:
2982:
2483:
743:
2888:
2049:
1799:
Streuli I, de
Ziegler D, Borghese B, Santulli P, Batteux F, Chapron C (March 2012). "New treatment strategies and emerging drugs in endometriosis".
3494:
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2896:
926:
789:
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2070:
Text was copied from this source which is copyright
European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
1483:
Text was copied from this source which is copyright
European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
3771:
3381:
930:
3443:
3427:
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1115:(brand name Orilissa) in July 2018. Relugolix was approved for the treatment of prostate cancer in the United States on 18 December 2020.
3213:
3117:
1140:
708:
102:
965:
levels (<20 ng/dL) in men. It additionally suppresses luteinizing hormone and follicle-stimulating hormone levels in men.
3888:
2020:
1436:
2848:
2785:
389:
274:
169:
3543:
3187:
2871:
2468:
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2434:
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suppression in the treatment of endometriosis and uterine fibroids. This is intended to reduce the incidence and severity of
2347:
Barra F, Seca M, Della Corte L, Giampaolino P, Ferrero S (August 2019). "Relugolix for the treatment of uterine fibroids".
2147:
Goenka L, George M, Sen M (June 2017). "A peek into the drug development scenario of endometriosis - A systematic review".
1296:
Barra F, Seca M, Della Corte L, Giampaolino P, Ferrero S (August 2019). "Relugolix for the treatment of uterine fibroids".
1021:
3858:
914:
Estradiol levels with 40 mg relugolix once per day in premenopausal women relative to untreated premenopausal women.
3795:
3746:
3330:
3069:
3064:
2611:
1947:
954:
511:
1693:"Medical Castration Using the Investigational Oral GnRH Antagonist TAK-385 (Relugolix): Phase 1 Study in Healthy Males"
1521:
3398:
3338:
2653:
2567:
1044:
1025:
571:
1941:
188:
1781:"Myovant Provides Corporate Updates and Reports Financial Results for Third Fiscal Quarter Ended December 31, 2018"
1149:
3903:
3229:
1469:
1202:
874:
3056:
2840:
1013:
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for "A Study to
Evaluate the Safety and Efficacy of Relugolix in Men With Advanced Prostate Cancer (HERO)" at
1043:
of relugolix is 36 to 65 hours across a dosage range of 20 to 180 mg/day. There is moderate to high
460:
3741:
3386:
1207:
765:
199:
3598:
3292:
2080:
1158:
1029:
957:
in premenopausal women. Relugolix at a dosage of 40 mg or more once per day has been found to reduce
560:
340:
3825:
3810:
2057:
3898:
3713:
3483:
3322:
3284:
1393:
1040:
451:
2403:
3918:
3913:
3790:
3334:
2750:
2619:
350:
587:
3923:
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3326:
3250:
3170:
3074:
2679:
1096:
1001:
997:
985:
973:
950:
922:
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855:
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406:
206:
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2250:
2207:
1824:
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2719:
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A dosage of relugolix of 40 mg once per day has been found to suppress estradiol levels to
3841:
3676:
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3656:
3636:
3621:
838:
Relugolix is approved in the United States, Canada and the United
Kingdom for the treatment of
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Struthers RS, Nicholls AJ, Grundy J, Chen T, Jimenez R, Yen SS, Bozigian HP (February 2009).
500:
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3300:
3233:
3225:
3203:
2917:
2356:
2319:
2282:
2234:
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2021:"Myfembree- relugolix, estradiol hemihydrate, and norethindrone acetate tablet, film coated"
1863:
1855:
1808:
1712:
1704:
1658:
1648:
1606:
1565:
1464:
1305:
1032:
of relugolix is approximately 68 to 71% over a concentration range of 0.05 to 5 μg/mL.
968:
Lower doses of relugolix (<40 mg/day) are under investigation for achieving partial
608:
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332:
57:
520:
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1006:
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751:
747:
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218:
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39:
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3308:
3274:
3262:
3084:
2795:
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2589:
2182:
Dellis A, Papatsoris A (October 2017). "Therapeutic outcomes of the LHRH antagonists".
1868:
1843:
1717:
1692:
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1636:
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Union in April 2022, and in the United
Kingdom in July 2022 (although not available in
1075:
1017:
805:
793:
258:
3882:
3756:
2699:
2579:
2376:
1984:
1968:
1398:
1370:
1366:"Notice: Multiple additions to the Prescription Drug List (PDL) [2023-12-22]"
1325:
1219:
1174:
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890:
773:
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1--5--3-(6-methoxypyridazin-3-yl)-2,4-dioxothienopyrimidin-6-yl]phenyl]-3-methoxyurea
161:
2339:
2302:
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2211:
1828:
3180:
3143:
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3133:
3125:
3047:
2880:
2780:
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2518:
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1910:
1136:
1090:
981:
958:
946:
894:
781:
249:
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2195:
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1635:
Tukun FL, Olberg DE, Riss PJ, Haraldsen I, Kaass A, Klaveness J (December 2017).
1610:
147:
3588:
3563:
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3363:
3314:
3270:
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3258:
3243:
3237:
3174:
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2714:
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2644:
2625:
2584:
2539:
1071:
969:
882:
870:
816:
801:
761:
155:
2286:
1166:. It is also known by its former developmental code names RVT-601 and TAK-385.
3815:
3761:
3688:
3626:
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3288:
3079:
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2704:
2635:
2615:
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2534:
2529:
2488:
1891:
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occurs with relugolix (21.7% decrease by week 12, 24.4% decrease by week 24).
824:
650:
491:
213:
2331:
2246:
696:
CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nn2)c(=O)n3Cc2c(F)cccc2F)cc1
3703:
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22:
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746:(GnRH receptor antagonist) medication which is used in the treatment of
480:
3723:
3616:
3353:
2238:
426:
1569:
30:
1036:
1000:
of relugolix of 29 ng/mL (47 nmol/L) after 1.5 hours.
551:
2002:
540:
1062:(4%). Only about 6% of a dose of relugolix is excreted unchanged.
1059:
1055:
996:
A single 40-mg oral dose of relugolix has been found to result in
909:
673:
664:
373:
368:
1967:
This article incorporates text from this source, which is in the
1340:"Therapeutic Goods (Poisons Standard—June 2024) Instrument 2024"
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531:
319:
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3475:
3447:
2844:
2407:
2044:
2042:
307:
178:
3148:
3772:
2273:
Markham A (April 2019). "Relugolix: First Global Approval".
576:
1218:
Relugolix is under development for use in the treatment of
283:
81:
66:
2184:
Expert Review of Pharmacoeconomics & Outcomes Research
2127:"Relugolix for treating hormone-sensitive prostate cancer"
1189:
Relugolix is available in the United States and in Japan.
72:
2106:"ORGOVYX FILM-COATED TABLETS RELUGOLIX - PLGB 00142/1272"
1141:
854:
Relugolix is available in the form of 40 and 120 mg
87:
78:
945:
women. The medication additionally suppresses levels of
296:
3728:
Tooltip Luteinizing hormone/choriogonadotropin receptor
1691:
MacLean DB, Shi H, Faessel HM, Saad F (December 2015).
3833:
3415:
3214:
3188:
3181:
3118:
2889:
2872:
3856:
1107:
Relugolix was first described in 2004. It superseded
103:
93:
90:
60:
1848:
The Journal of Clinical Endocrinology and Metabolism
1697:
The Journal of Clinical Endocrinology and Metabolism
1637:"Recent Development of Non-Peptide GnRH Antagonists"
84:
69:
63:
3770:
3721:
3712:
3493:
3212:Sex steroid agonists (via negative feedback on the
3202:
3106:
3097:
3055:
3046:
2981:
2905:
2887:
2740:
2687:
2678:
2652:
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2517:
2455:
2446:
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1421:
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1417:
662:
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607:
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331:
273:
268:
224:
212:
198:
168:
154:
136:
128:
118:
75:
51:
46:
3116:Sex steroid antagonists (via disinhibition of the
1150:
1775:
1773:
1771:
1769:
1767:
439:
3500:Tooltip Gonadotropin-releasing hormone receptor
3480:Tooltip Gonadotropin-releasing hormone receptor
1936:
1934:
1932:
1930:
1928:
1926:
1924:
1794:
1792:
1790:
1686:
1684:
1682:
1630:
1628:
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1275:
1273:
1271:
1269:
1267:
1265:
1263:
1261:
1259:
1257:
1255:
414:
3351:Others (mixed or unknown mechanism of action):
3153:Tooltip Selective estrogen receptor modulators
1748:
1746:
1744:
1742:
1740:
1738:
1736:
1591:
1589:
1587:
1550:
1548:
1546:
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1542:
1505:
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1501:
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1489:
1459:
1457:
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1247:
1245:
1243:
1241:
1239:
1237:
1235:
1199:Committee for Medicinal Products for Human Use
1159:
3777:Tooltip Follicle-stimulating hormone receptor
3459:
2856:
2419:
1979:
1977:
1394:"Summary Basis of Decision (SBD) for Orgovyx"
893:(9.4–15.2% vs. 0% for placebo). In addition,
8:
187:
21:
1520:(in Japanese). January 2019. Archived from
3816:Menotropin (human menopausal gonadotropin)
3762:Menotropin (human menopausal gonadotropin)
3718:
3466:
3452:
3444:
3103:
3052:
2902:
2863:
2849:
2841:
2684:
2563:
2452:
2426:
2412:
2404:
2009:. Kyoto Encyclopedia of Genes and Genomes.
1911:"Elagolix - Abbvie/Neurocrine Biosciences"
1020:, which may have a limiting effect on its
873:of relugolix for uterine fibroids include
590:
499:
1867:
1716:
1662:
1652:
1146:Tooltip International Nonproprietary Name
842:in men and in Japan for the treatment of
744:gonadotropin-releasing hormone antagonist
519:
1437:"Orgovyx- relugolix tablet, film coated"
784:. Relugolix is a GnRH antagonist, or an
3863:
1231:
1181:for the treatment of uterine fibroids.
927:gonadotropin-releasing hormone receptor
790:gonadotropin-releasing hormone receptor
713:
693:
586:
479:
394:
160:
3193:Tooltip gonadotropin-releasing hormone
2877:Tooltip Gonadotropin-releasing hormone
800:(brand name Orilissa), relugolix is a
20:
931:half-maximal inhibitory concentration
559:
146:
7:
3418:and gonadotropin receptor modulators
2085:Union Register of medicinal products
1991:. U.S. National Library of Medicine.
1081:, and is structurally distinct from
248:
237:
1047:in systemic exposure to relugolix.
885:(12.1–49.3% vs. 9.4% for placebo),
877:(24.6–48.6% vs. 6.3% for placebo),
539:
430:
2056:. 24 February 2022. Archived from
1511:"Relumina (relugolix) Information"
1155:Tooltip United States Adopted Name
14:
3433:Progestogens and antiprogestogens
3033:+estradiol/norethisterone acetate
2508:+estradiol/norethisterone acetate
2149:Biomedicine & Pharmacotherapy
1917:. Springer Nature Switzerland AG.
1760:. Springer Nature Switzerland AG.
1035:Relugolix is not a substrate for
881:(42.8–45.5% vs. 0% for placebo),
3866:
1962:
1801:Expert Opinion on Emerging Drugs
1599:European Journal of Pharmacology
631:
625:
619:
56:
38:
29:
2435:Hypothalamic-pituitary hormones
1344:Federal Register of Legislation
1058:(83%) and to a small degree in
721:Key:AOMXMOCNKJTRQP-UHFFFAOYSA-N
2457:Gonadotropin-releasing hormone
2050:"Orgovyx: Pending EC decision"
1942:"Drug Trial Snapshot: Orgovyx"
1558:Journal of Medicinal Chemistry
1164:Tooltip Japanese Accepted Name
982:decreased bone mineral density
895:decreased bone mineral density
846:(uterine leiomyoma) in women.
782:decreased bone mineral density
643:
637:
613:
1:
3909:Hormonal antineoplastic drugs
2361:10.1358/dot.2019.55.8.3020179
2324:10.1358/dof.2019.44.2.2927590
2196:10.1080/14737167.2017.1375855
2081:"Orgovyx Product information"
1310:10.1358/dot.2019.55.8.3020179
1177:is sold under the brand name
827:range in both women and men.
734:, sold under the brand names
3796:Follicle-stimulating hormone
3747:Human chorionic gonadotropin
3331:hydroxyprogesterone caproate
3070:Human chorionic gonadotropin
3065:Follicle-stimulating hormone
2612:Insulin-like growth factor 1
2161:10.1016/j.biopha.2017.03.092
1948:Food and Drug Administration
1813:10.1517/14728214.2012.668885
1754:"Relugolix - Myovant/Takeda"
1611:10.1016/j.ejphar.2013.12.001
1210:England until August 2024).
955:follicle-stimulating hormone
3428:Estrogens and antiestrogens
3423:Androgens and antiandrogens
3339:medroxyprogesterone acetate
2654:Thyroid-stimulating hormone
2568:Adrenocorticotropic hormone
1045:interindividual variability
1009:of relugolix by about 50%.
3945:
2287:10.1007/s40265-019-01105-0
603:Chemical and physical data
3376:
2054:European Medicines Agency
1654:10.3390/molecules22122188
1597:receptor knock-in mice".
1470:European Medicines Agency
1203:European Medicines Agency
875:abnormal uterine bleeding
704:
684:
385:
37:
28:
3564:Leuprorelin (leuprolide)
2958:Leuprorelin (leuprolide)
883:heavy menstrual bleeding
3889:Dimethylamino compounds
3742:Choriogonadotropin alfa
766:menstrual abnormalities
3599:Zoptarelin doxorubicin
2391:Clinical trial number
1197:In February 2022, the
1030:plasma protein binding
984:that are secondary to
915:
754:in women. It is taken
3677:Teverelix (antarelix)
3484:gonadotropin receptor
3323:chlormadinone acetate
1041:elimination half-life
913:
764:of relugolix include
132:RGX; RVT-601; TAK-385
3791:Corifollitropin alfa
3657:Ornirelix (ornitide)
3335:gestonorone caproate
3171:Aromatase inhibitors
2620:Mecasermin rinfabate
1860:10.1210/jc.2008-1695
1709:10.1210/jc.2015-2770
1139:of the drug and its
961:levels to sustained
792:. Unlike most other
253:) (combination with
3826:Varfollitropin alfa
3811:Follitropin epsilon
3752:Luteinizing hormone
3327:cyproterone acetate
3255:prolactin releasers
3075:Luteinizing hormone
2680:Posterior pituitary
2312:Drugs of the Future
2060:on 27 February 2022
1556:hormone receptor".
1527:on 16 February 2019
1518:ASKA Pharmaceutical
1123:Society and culture
1002:Steady-state levels
986:estrogen deficiency
974:menopausal symptoms
951:luteinizing hormone
937:) of 0.12 nM.
796:, but similarly to
742:among others, is a
358:36 to 65 hours
292:(Prescription only)
25:
3403:Never to phase III
3305:diethylstilbestrol
2559:Anterior pituitary
2399:ClinicalTrials.gov
2239:10.1039/C4MD00416G
2007:KEGG DRUG Database
1952:. 18 December 2020
1473:. 22 February 2022
1402:. 16 February 2024
1374:. 22 December 2023
916:
891:excessive sweating
889:(12.3–15.2%), and
774:excessive sweating
3854:
3853:
3850:
3849:
3647:Iturelix (antide)
3441:
3440:
3372:
3371:
3343:megestrol acetate
3234:nandrolone esters
3226:anabolic steroids
3204:Antigonadotropins
3093:
3092:
3042:
3041:
2838:
2837:
2834:
2833:
2674:
2673:
2553:
2552:
2227:Med. Chem. Commun
2027:. 18 January 2024
1703:(12): 4579–4587.
1570:10.1021/jm200216q
1564:(14): 4998–5012.
1171:ethinyl estradiol
729:
728:
675:Interactive image
572:CompTox Dashboard
323:
311:
299:
287:
181:
124:Orgovyx, Relumina
16:Chemical compound
3936:
3904:GnRH antagonists
3871:
3870:
3869:
3862:
3835:
3806:Follitropin beta
3801:Follitropin alfa
3778:
3774:
3729:
3725:
3719:
3524:Azagly-nafarelin
3501:
3497:
3481:
3477:
3468:
3461:
3454:
3445:
3417:
3301:ethinylestradiol
3297:estradiol esters
3216:
3194:
3190:
3183:
3154:
3150:
3120:
3108:Progonadotropins
3104:
3053:
2918:Azagly-nafarelin
2903:
2891:
2878:
2874:
2865:
2858:
2851:
2842:
2685:
2564:
2453:
2428:
2421:
2414:
2405:
2380:
2343:
2306:
2259:
2258:
2222:
2216:
2215:
2179:
2173:
2172:
2144:
2138:
2137:
2135:
2133:
2123:
2117:
2116:
2114:
2112:
2102:
2096:
2095:
2093:
2091:
2077:
2071:
2069:
2067:
2065:
2046:
2037:
2036:
2034:
2032:
2017:
2011:
2010:
1999:
1993:
1992:
1981:
1972:
1966:
1965:
1961:
1959:
1957:
1938:
1919:
1918:
1907:
1901:
1900:
1899:
1895:
1888:
1882:
1881:
1871:
1839:
1833:
1832:
1796:
1785:
1784:
1783:(Press release).
1777:
1762:
1761:
1750:
1731:
1730:
1720:
1688:
1677:
1676:
1666:
1656:
1632:
1623:
1622:
1593:
1582:
1581:
1552:
1537:
1536:
1534:
1532:
1526:
1515:
1507:
1484:
1482:
1480:
1478:
1461:
1452:
1451:
1449:
1447:
1433:
1412:
1411:
1409:
1407:
1390:
1384:
1383:
1381:
1379:
1362:
1356:
1355:
1353:
1351:
1336:
1330:
1329:
1293:
1165:
1161:
1156:
1152:
1147:
1143:
992:Pharmacokinetics
929:(GnRHR), with a
906:Pharmacodynamics
844:uterine fibroids
815:. It suppresses
752:uterine fibroids
677:
657:
645:
639:
633:
627:
621:
615:
595:
594:
580:
578:
563:
543:
523:
503:
483:
463:
443:
433:
432:
418:
354:
321:
318:
309:
306:
298:
295:
285:
282:
252:
241:
191:
180:
177:
164:
150:
110:
106:
100:
99:
96:
95:
92:
89:
86:
83:
80:
77:
74:
71:
68:
65:
62:
42:
33:
26:
24:
3944:
3943:
3939:
3938:
3937:
3935:
3934:
3933:
3879:
3878:
3877:
3867:
3865:
3857:
3855:
3846:
3776:
3766:
3727:
3708:
3499:
3489:
3479:
3472:
3442:
3437:
3408:
3393:Clinical trials
3368:
3247:
3198:
3192:
3152:
3099:
3089:
3038:
2977:
2894:
2883:
2876:
2869:
2839:
2830:
2783:
2736:
2722:
2670:
2648:
2594:
2549:
2513:
2481:
2442:
2437:and analogues (
2432:
2388:
2383:
2346:
2309:
2272:
2268:
2266:Further reading
2263:
2262:
2224:
2223:
2219:
2181:
2180:
2176:
2146:
2145:
2141:
2131:
2129:
2125:
2124:
2120:
2110:
2108:
2104:
2103:
2099:
2089:
2087:
2079:
2078:
2074:
2063:
2061:
2048:
2047:
2040:
2030:
2028:
2019:
2018:
2014:
2001:
2000:
1996:
1983:
1982:
1975:
1963:
1955:
1953:
1940:
1939:
1922:
1909:
1908:
1904:
1897:
1890:
1889:
1885:
1841:
1840:
1836:
1798:
1797:
1788:
1779:
1778:
1765:
1752:
1751:
1734:
1690:
1689:
1680:
1634:
1633:
1626:
1595:
1594:
1585:
1554:
1553:
1540:
1530:
1528:
1524:
1513:
1509:
1508:
1487:
1476:
1474:
1463:
1462:
1455:
1445:
1443:
1435:
1434:
1415:
1405:
1403:
1392:
1391:
1387:
1377:
1375:
1364:
1363:
1359:
1349:
1347:
1338:
1337:
1333:
1295:
1294:
1233:
1228:
1216:
1195:
1187:
1163:
1154:
1145:
1130:
1125:
1105:
1070:Relugolix is a
1068:
1012:Relugolix is a
1007:bioavailability
994:
936:
918:Relugolix is a
908:
903:
867:
852:
850:Available forms
840:prostate cancer
836:
794:GnRH modulators
748:prostate cancer
725:
722:
717:
712:
711:
700:
697:
692:
691:
680:
655:
642:
636:
630:
624:
618:
598:
574:
566:
546:
526:
506:
486:
466:
446:
429:
421:
401:
398:
393:
392:
372:
352:
341:Protein binding
333:Pharmacokinetic
327:
264:
243:
219:GnRH antagonist
201:
194:
108:
104:
101:
59:
55:
17:
12:
11:
5:
3942:
3940:
3932:
3931:
3926:
3921:
3916:
3911:
3906:
3901:
3896:
3891:
3881:
3880:
3876:
3875:
3852:
3851:
3848:
3847:
3845:
3844:
3829:
3828:
3823:
3821:Urofollitropin
3818:
3813:
3808:
3803:
3798:
3793:
3781:
3779:
3768:
3767:
3765:
3764:
3759:
3754:
3749:
3744:
3732:
3730:
3716:
3710:
3709:
3707:
3706:
3701:
3696:
3691:
3686:
3674:
3669:
3664:
3659:
3654:
3649:
3644:
3639:
3634:
3629:
3624:
3619:
3614:
3602:
3601:
3596:
3591:
3586:
3581:
3576:
3571:
3566:
3561:
3556:
3551:
3546:
3541:
3536:
3531:
3526:
3521:
3516:
3504:
3502:
3491:
3490:
3473:
3471:
3470:
3463:
3456:
3448:
3439:
3438:
3436:
3435:
3430:
3425:
3420:
3412:
3407:
3406:
3405:
3404:
3401:
3390:
3384:
3378:
3377:
3374:
3373:
3370:
3369:
3367:
3366:
3361:
3356:
3347:
3346:
3312:
3309:paroxypropione
3282:
3275:chlorpromazine
3263:metoclopramide
3245:
3241:
3208:
3206:
3200:
3199:
3197:
3196:
3178:
3168:
3141:
3112:
3110:
3101:
3095:
3094:
3091:
3090:
3088:
3087:
3085:Urofollitropin
3082:
3077:
3072:
3067:
3061:
3059:
3050:
3044:
3043:
3040:
3039:
3037:
3036:
3026:
3021:
3012:
3011:
3006:
3001:
2996:
2987:
2985:
2979:
2978:
2976:
2975:
2970:
2965:
2960:
2955:
2950:
2945:
2940:
2935:
2930:
2925:
2920:
2911:
2909:
2900:
2885:
2884:
2870:
2868:
2867:
2860:
2853:
2845:
2836:
2835:
2832:
2831:
2829:
2828:
2823:
2818:
2813:
2808:
2803:
2798:
2796:Demeclocycline
2793:
2778:
2773:
2768:
2763:
2758:
2746:
2744:
2738:
2737:
2735:
2734:
2729:
2717:
2712:
2707:
2702:
2693:
2691:
2682:
2676:
2675:
2672:
2671:
2669:
2668:
2659:
2657:
2650:
2649:
2639:
2638:
2633:
2628:
2623:
2605:
2603:
2600:Growth hormone
2596:
2595:
2593:
2592:
2590:Tetracosactide
2587:
2582:
2573:
2571:
2561:
2555:
2554:
2551:
2550:
2548:
2547:
2542:
2537:
2532:
2523:
2521:
2515:
2514:
2512:
2511:
2501:
2496:
2491:
2476:
2471:
2462:
2460:
2450:
2444:
2443:
2433:
2431:
2430:
2423:
2416:
2408:
2402:
2401:
2387:
2386:External links
2384:
2382:
2381:
2355:(8): 503–512.
2349:Drugs of Today
2344:
2307:
2281:(6): 675–679.
2269:
2267:
2264:
2261:
2260:
2233:(5): 746–768.
2217:
2190:(5): 481–488.
2174:
2139:
2118:
2097:
2072:
2038:
2012:
1994:
1973:
1920:
1902:
1883:
1854:(2): 545–551.
1834:
1786:
1763:
1732:
1678:
1624:
1583:
1538:
1485:
1465:"Orgovyx EPAR"
1453:
1413:
1385:
1357:
1331:
1304:(8): 503–512.
1298:Drugs of Today
1230:
1229:
1227:
1224:
1215:
1212:
1201:(CHMP) of the
1194:
1191:
1186:
1183:
1129:
1126:
1124:
1121:
1104:
1101:
1083:GnRH analogues
1076:small-molecule
1067:
1064:
1018:P-glycoprotein
993:
990:
942:postmenopausal
934:
907:
904:
902:
899:
866:
863:
851:
848:
835:
832:
821:postmenopausal
819:levels to the
806:small-molecule
727:
726:
724:
723:
720:
718:
715:
707:
706:
705:
702:
701:
699:
698:
695:
687:
686:
685:
682:
681:
679:
678:
670:
668:
660:
659:
653:
647:
646:
640:
634:
628:
622:
616:
611:
605:
604:
600:
599:
597:
596:
588:DTXSID40224167
583:
581:
568:
567:
565:
564:
556:
554:
548:
547:
545:
544:
536:
534:
528:
527:
525:
524:
516:
514:
508:
507:
505:
504:
496:
494:
488:
487:
485:
484:
476:
474:
468:
467:
465:
464:
456:
454:
448:
447:
445:
444:
436:
434:
423:
422:
420:
419:
411:
409:
403:
402:
400:
399:
396:
388:
387:
386:
383:
382:
378:
377:
366:
360:
359:
356:
347:
346:
343:
337:
336:
329:
328:
326:
325:
316:
304:
293:
279:
277:
271:
270:
266:
265:
263:
262:
259:norethisterone
230:
228:
222:
221:
216:
210:
209:
204:
202:administration
196:
195:
193:
192:
174:
172:
166:
165:
158:
152:
151:
144:
134:
133:
130:
126:
125:
122:
116:
115:
53:
49:
48:
44:
43:
35:
34:
15:
13:
10:
9:
6:
4:
3:
2:
3941:
3930:
3927:
3925:
3922:
3920:
3917:
3915:
3912:
3910:
3907:
3905:
3902:
3900:
3897:
3895:
3892:
3890:
3887:
3886:
3884:
3874:
3864:
3860:
3843:
3840:
3839:Non-peptides:
3837:
3831:
3830:
3827:
3824:
3822:
3819:
3817:
3814:
3812:
3809:
3807:
3804:
3802:
3799:
3797:
3794:
3792:
3789:
3786:
3783:
3782:
3780:
3775:
3769:
3763:
3760:
3758:
3757:Lutropin alfa
3755:
3753:
3750:
3748:
3745:
3743:
3740:
3737:
3734:
3733:
3731:
3726:
3720:
3717:
3715:
3711:
3705:
3702:
3700:
3697:
3695:
3692:
3690:
3687:
3685:
3682:
3681:Non-peptides:
3678:
3675:
3673:
3670:
3668:
3665:
3663:
3660:
3658:
3655:
3653:
3650:
3648:
3645:
3643:
3640:
3638:
3635:
3633:
3630:
3628:
3625:
3623:
3620:
3618:
3615:
3613:
3610:
3607:
3604:
3603:
3600:
3597:
3595:
3592:
3590:
3587:
3585:
3582:
3580:
3577:
3575:
3572:
3570:
3567:
3565:
3562:
3560:
3557:
3555:
3552:
3550:
3547:
3545:
3542:
3540:
3537:
3535:
3532:
3530:
3527:
3525:
3522:
3520:
3517:
3515:
3512:
3509:
3506:
3505:
3503:
3498:
3492:
3488:
3485:
3478:
3469:
3464:
3462:
3457:
3455:
3450:
3449:
3446:
3434:
3431:
3429:
3426:
3424:
3421:
3419:
3413:
3410:
3409:
3402:
3400:
3397:
3396:
3394:
3391:
3388:
3385:
3383:
3380:
3379:
3375:
3365:
3362:
3360:
3357:
3355:
3352:
3349:
3348:
3344:
3340:
3336:
3332:
3328:
3324:
3320:
3316:
3313:
3310:
3306:
3302:
3298:
3294:
3290:
3286:
3283:
3280:
3276:
3272:
3268:
3264:
3260:
3256:
3252:
3249:
3242:
3239:
3235:
3231:
3227:
3223:
3220:
3218:
3210:
3209:
3207:
3205:
3201:
3191:
3185:
3179:
3176:
3172:
3169:
3166:
3162:
3158:
3151:
3145:
3144:Antiestrogens
3142:
3139:
3135:
3131:
3127:
3126:Antiandrogens
3124:
3122:
3114:
3113:
3111:
3109:
3105:
3102:
3096:
3086:
3083:
3081:
3078:
3076:
3073:
3071:
3068:
3066:
3063:
3062:
3060:
3058:
3054:
3051:
3049:
3048:Gonadotropins
3045:
3034:
3030:
3027:
3025:
3022:
3020:
3017:
3014:
3013:
3010:
3007:
3005:
3002:
3000:
2997:
2995:
2992:
2989:
2988:
2986:
2984:
2980:
2974:
2971:
2969:
2966:
2964:
2961:
2959:
2956:
2954:
2951:
2949:
2946:
2944:
2941:
2939:
2936:
2934:
2931:
2929:
2926:
2924:
2921:
2919:
2916:
2913:
2912:
2910:
2908:
2904:
2901:
2898:
2893:
2886:
2882:
2881:gonadotropins
2875:
2866:
2861:
2859:
2854:
2852:
2847:
2846:
2843:
2827:
2824:
2822:
2819:
2817:
2814:
2812:
2809:
2807:
2804:
2802:
2799:
2797:
2794:
2792:
2788:
2787:
2782:
2779:
2777:
2774:
2772:
2769:
2767:
2764:
2762:
2759:
2757:
2754:
2752:
2748:
2747:
2745:
2743:
2739:
2733:
2730:
2728:
2725:
2721:
2718:
2716:
2713:
2711:
2708:
2706:
2703:
2701:
2700:Argiprestocin
2698:
2695:
2694:
2692:
2690:
2686:
2683:
2681:
2677:
2667:
2664:
2661:
2660:
2658:
2655:
2651:
2647:
2646:
2643:
2637:
2634:
2632:
2629:
2627:
2624:
2621:
2617:
2613:
2610:
2607:
2606:
2604:
2601:
2597:
2591:
2588:
2586:
2583:
2581:
2580:Corticotropin
2578:
2575:
2574:
2572:
2569:
2565:
2562:
2560:
2556:
2546:
2543:
2541:
2538:
2536:
2533:
2531:
2528:
2525:
2524:
2522:
2520:
2516:
2509:
2505:
2502:
2500:
2497:
2495:
2492:
2490:
2487:
2485:
2480:
2477:
2475:
2472:
2470:
2467:
2464:
2463:
2461:
2458:
2454:
2451:
2449:
2445:
2440:
2436:
2429:
2424:
2422:
2417:
2415:
2410:
2409:
2406:
2400:
2396:
2395:
2390:
2389:
2385:
2378:
2374:
2370:
2366:
2362:
2358:
2354:
2350:
2345:
2341:
2337:
2333:
2329:
2325:
2321:
2317:
2313:
2308:
2304:
2300:
2296:
2292:
2288:
2284:
2280:
2276:
2271:
2270:
2265:
2256:
2252:
2248:
2244:
2240:
2236:
2232:
2228:
2221:
2218:
2213:
2209:
2205:
2201:
2197:
2193:
2189:
2185:
2178:
2175:
2170:
2166:
2162:
2158:
2154:
2150:
2143:
2140:
2128:
2122:
2119:
2107:
2101:
2098:
2086:
2082:
2076:
2073:
2059:
2055:
2051:
2045:
2043:
2039:
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1399:Health Canada
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1373:
1372:
1371:Health Canada
1367:
1361:
1358:
1346:. 30 May 2024
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1220:endometriosis
1213:
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1192:
1190:
1184:
1182:
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1175:norethindrone
1172:
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1120:
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1092:
1088:
1084:
1080:
1077:
1073:
1065:
1063:
1061:
1057:
1053:
1050:Relugolix is
1048:
1046:
1042:
1038:
1033:
1031:
1027:
1023:
1019:
1015:
1010:
1008:
1003:
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857:
849:
847:
845:
841:
833:
831:
828:
826:
822:
818:
814:
813:orally active
810:
807:
803:
799:
795:
791:
787:
783:
779:
775:
771:
767:
763:
759:
757:
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733:
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652:
648:
612:
610:
606:
601:
593:
589:
585:
584:
582:
573:
569:
562:
561:ChEMBL1800159
558:
557:
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549:
542:
538:
537:
535:
533:
529:
522:
518:
517:
515:
513:
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384:
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348:
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324: Rx-only
317:
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305:
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294:
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281:
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272:
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256:
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112:
98:
54:
52:Pronunciation
50:
47:Clinical data
45:
41:
36:
32:
27:
19:
3899:Fluoroarenes
3838:
3832:
3787:
3784:
3738:
3735:
3714:Gonadotropin
3698:
3680:
3608:
3606:Antagonists:
3605:
3510:
3507:
3350:
3315:Progestogens
3230:testosterone
3211:
3138:enzalutamide
3134:bicalutamide
3115:
3057:Preparations
3028:
3016:Non-peptide:
3015:
2990:
2914:
2784:
2781:Terlipressin
2761:Desmopressin
2749:
2724:Antagonists:
2723:
2696:
2662:
2642:Antagonists:
2641:
2640:
2608:
2576:
2526:
2519:Somatostatin
2503:
2482:
2465:
2448:Hypothalamus
2392:
2352:
2348:
2315:
2311:
2278:
2274:
2230:
2226:
2220:
2187:
2183:
2177:
2152:
2148:
2142:
2132:20 September
2130:. Retrieved
2121:
2111:20 September
2109:. Retrieved
2100:
2088:. Retrieved
2084:
2075:
2062:. Retrieved
2058:the original
2053:
2029:. Retrieved
2024:
2015:
2006:
1997:
1988:
1954:. Retrieved
1945:
1914:
1905:
1886:
1851:
1847:
1837:
1804:
1800:
1757:
1700:
1696:
1647:(12): 2188.
1644:
1640:
1602:
1598:
1561:
1557:
1529:. Retrieved
1522:the original
1517:
1475:. Retrieved
1468:
1444:. Retrieved
1440:
1404:. Retrieved
1397:
1388:
1376:. Retrieved
1369:
1360:
1348:. Retrieved
1343:
1334:
1301:
1297:
1217:
1196:
1193:Legal status
1188:
1185:Availability
1168:
1137:generic name
1132:
1131:
1117:
1106:
1086:
1069:
1049:
1034:
1026:distribution
1011:
995:
967:
959:testosterone
947:progesterone
939:
917:
901:Pharmacology
871:side effects
868:
865:Side effects
853:
837:
834:Medical uses
829:
762:Side effects
760:
739:
735:
731:
730:
351:Elimination
275:Legal status
269:Legal status
170:License data
18:
3919:Pyrimidines
3914:Pyridazines
3589:Triptorelin
3584:Salmon GnRH
3549:Gonadorelin
3389:from market
3364:Metallibure
3271:haloperidol
3267:risperidone
3259:domperidone
3251:antagonists
3238:oxandrolone
3175:anastrozole
3165:enclomifene
2983:Antagonists
2973:Triptorelin
2938:Gonadorelin
2816:Relcovaptan
2786:Antagonists
2776:Ornipressin
2766:Felypressin
2756:Argipressin
2742:Vasopressin
2715:Demoxytocin
2666:Thyrotropin
2645:Pegvisomant
2626:Somapacitan
2585:Cosyntropin
2540:Pasireotide
2484:Antagonists
2469:Gonadorelin
2394:NCT03085095
2155:: 575–585.
2064:27 February
2031:24 February
2003:"Relugolix"
1985:"Relugolix"
1915:AdisInsight
1758:AdisInsight
1605:: 167–174.
1531:16 February
1406:24 February
1085:. It is an
1072:non-peptide
998:peak levels
978:hot flushes
970:sex hormone
879:hot flashes
817:sex hormone
802:non-peptide
770:hot flashes
750:in men and
658: g·mol
416:737789-87-6
381:Identifiers
156:MedlinePlus
129:Other names
120:Trade names
3924:Triketones
3883:Categories
3689:Linzagolix
3667:Prazarelix
3627:Cetrorelix
3594:Zoptarelin
3539:Fertirelin
3534:Deslorelin
3487:modulators
3359:Gestrinone
3319:progestins
3289:bifluranol
3257:) (incl.,
3100:(indirect)
3080:Menotropin
3024:Linzagolix
2999:Cetrorelix
2933:Fertirelin
2928:Deslorelin
2892:modulators
2821:Satavaptan
2811:Nelivaptan
2806:Mozavaptan
2801:Lixivaptan
2791:Conivaptan
2720:Nacartocin
2710:Cargutocin
2705:Carbetocin
2636:Somatrogon
2616:Mecasermin
2545:Vapreotide
2535:Octreotide
2530:Lanreotide
2489:Cetrorelix
2318:(2): 131.
1989:ChemIDplus
1892:US 7300935
1807:: 83–104.
1226:References
1097:derivative
1054:mainly in
1022:absorption
923:antagonist
786:antagonist
663:3D model (
651:Molar mass
521:P76B05O5V6
492:ChemSpider
452:IUPHAR/BPS
407:CAS Number
390:IUPAC name
214:Drug class
3842:ADX-61623
3788:Peptides:
3785:Agonists:
3739:Peptides:
3736:Agonists:
3704:Sufugolix
3699:Relugolix
3672:Ramorelix
3642:Ganirelix
3637:Detirelix
3632:Degarelix
3622:Azaline B
3609:Peptides:
3579:Peforelin
3574:Nafarelin
3559:Histrelin
3554:Goserelin
3529:Buserelin
3511:Peptides:
3508:Agonists:
3399:Phase III
3387:Withdrawn
3293:estradiol
3285:Estrogens
3279:sulpiride
3222:Androgens
3161:clomifene
3157:tamoxifen
3130:flutamide
3029:Relugolix
3009:Ganirelix
3004:Degarelix
2968:Peforelin
2963:Nafarelin
2953:Lecirelin
2948:Histrelin
2943:Goserelin
2923:Buserelin
2897:analogues
2826:Tolvaptan
2771:Lypressin
2732:Barusiban
2697:Agonists:
2663:Agonists:
2614:(IGF-1) (
2609:Agonists:
2577:Agonists:
2527:Agonists:
2504:Relugolix
2499:Ganirelix
2479:Histrelin
2474:Nafarelin
2466:Agonists:
2377:201654739
2332:0377-8282
2247:2040-2503
1956:6 January
1641:Molecules
1378:3 January
1326:201654739
1179:Myfembree
1133:Relugolix
1109:sufugolix
1066:Chemistry
1014:substrate
920:selective
869:The main
732:Relugolix
364:Excretion
353:half-life
255:estradiol
200:Routes of
189:Relugolix
148:Monograph
142:Drugs.com
23:Relugolix
3873:Medicine
3694:Opigolix
3684:Elagolix
3662:Ozarelix
3612:Abarelix
3569:Lutrelin
3519:Avorelin
3514:Alarelin
3411:See also
3321:, e.g.,
3287:(incl.,
3248:receptor
3184:agonists
3019:Elagolix
2994:Abarelix
2991:Peptide:
2915:Peptide:
2907:Agonists
2751:Agonists
2727:Atosiban
2689:Oxytocin
2631:Somatrem
2494:Elagolix
2369:31461087
2340:87369995
2303:89616869
2295:30937733
2255:72654573
2212:38014222
2204:28870102
2169:28407578
2025:DailyMed
1878:19033369
1829:27472695
1821:22439891
1727:26502357
1673:29232843
1619:24333551
1578:21657270
1441:DailyMed
1318:31461087
1214:Research
1113:elagolix
1079:compound
1052:excreted
976:such as
963:castrate
887:headache
825:castrate
809:compound
798:elagolix
778:headache
756:by mouth
740:Relumina
472:DrugBank
441:10348973
226:ATC code
207:By mouth
184:DailyMed
3652:LXT-101
3617:Acyline
3354:Danazol
3317:(incl.
3228:(e.g.,
3186:(e.g.,
3173:(e.g.,
3155:(e.g.,
3128:(e.g.,
2895:(incl.
2090:3 March
1869:2646513
1718:4667159
1664:6149776
1477:3 March
1350:10 June
1135:is the
1103:History
925:of the
859:tablets
811:and is
788:of the
736:Orgovyx
609:Formula
501:8524431
481:DB11853
427:PubChem
300::
247: (
245:H01CC54
242:)
236: (
234:L02BX04
186::
162:a621006
3894:Ethers
3859:Portal
3724:LH/hCG
3382:WHO-EM
3098:Others
2570:(ACTH)
2459:(GnRH)
2375:
2367:
2338:
2330:
2301:
2293:
2253:
2245:
2210:
2202:
2167:
1898:
1876:
1866:
1827:
1819:
1725:
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1671:
1661:
1617:
1576:
1446:25 May
1324:
1316:
1157:, and
1091:phenyl
1039:. The
1037:CYP3A4
1028:. The
953:, and
780:, and
689:SMILES
656:623.64
552:ChEMBL
541:D10888
345:68–71%
314:℞-only
312:
302:℞-only
288:
182:
114:
3929:Ureas
3149:SERMs
2656:(TSH)
2373:S2CID
2336:S2CID
2299:S2CID
2275:Drugs
2251:S2CID
2208:S2CID
1950:(FDA)
1946:U.S.
1825:S2CID
1525:(PDF)
1514:(PDF)
1322:S2CID
1128:Names
1060:urine
1056:feces
709:InChI
665:JSmol
374:Urine
371:: 82%
369:Feces
111:-liks
107:-luu-
3834:NAMs
3544:GnRH
3496:GnRH
3482:and
3476:GnRH
3416:GnRH
3217:axis
3189:GnRH
3182:GnRH
3121:axis
2890:GnRH
2879:and
2873:GnRH
2602:(GH)
2365:PMID
2328:ISSN
2291:PMID
2243:ISSN
2200:PMID
2165:PMID
2134:2024
2113:2024
2092:2023
2066:2022
2033:2024
1958:2021
1874:PMID
1817:PMID
1723:PMID
1669:PMID
1615:PMID
1574:PMID
1533:2019
1479:2023
1448:2021
1408:2024
1380:2024
1352:2024
1314:PMID
1173:and
1151:USAN
1094:urea
1024:and
1016:for
980:and
856:oral
738:and
532:KEGG
512:UNII
461:5586
376:: 4%
335:data
257:and
138:AHFS
3773:FSH
3215:HPG
3119:HPG
2439:H01
2357:doi
2320:doi
2283:doi
2235:doi
2192:doi
2157:doi
1864:PMC
1856:doi
1809:doi
1713:PMC
1705:doi
1701:100
1659:PMC
1649:doi
1607:doi
1603:723
1566:doi
1306:doi
1208:NHS
1160:JAN
1142:INN
933:(IC
823:or
577:EPA
431:CID
250:WHO
239:WHO
109:GOH
3885::
3679:;
3395::
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3337:,
3333:,
3329:,
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