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Raltegravir

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622: 599: 42: 955: 51: 1596: 853: 3357: 3345: 1061:. This statistically significant difference in viral load reduction has caused some HIV researchers to begin questioning long held paradigms about HIV viral dynamics and decay. Research into raltegravir's ability to affect latent viral reservoirs and possibly aid in the eradication of HIV is currently ongoing. 875:
regimens for adults and children use these cocktails). Raltegravir is available in chewable form, but because the two tablet formulations are not interchangeable, the chewable pills are only approved for use in children two to 11. Older adolescents will use the adult formulation.
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Summa V, Petrocchi A, Bonelli F, Crescenzi B, Donghi M, Ferrara M, et al. (September 2008). "Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection".
1113: 868:(FDA) granted expanded approval for raltegravir for use in all patients. As with any HAART medication, raltegravir is unlikely to show durability if used as monotherapy, due to the highly mutagenic nature of HIV. 1040:
authorised the first generic raltegravir medicines for adult and paediatric patients with HIV who weigh at least 40kg. Authorisation was granted to Lupin Healthcare (UK) Limited and Zentiva Pharma UK Limited.
1372:"Rapid and durable antiretroviral effect of the HIV-1 Integrase inhibitor raltegravir as part of combination therapy in treatment-naive patients with HIV-1 infection: results of a 48-week controlled study" 912:
Raltegravir was generally well tolerated when used in combination with optimized background therapy regimens in treatment-experienced patients with HIV-1 infection in trials of up to 48 weeks' duration.
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and decay and further research in this area is ongoing. In clinical trials patients taking raltegravir achieved viral loads less than 50 copies per millitre sooner than those taking similarly potent
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In December 2011, it approval for use in children over the age of two, taken in pill form orally twice a day by prescription with two other antiretroviral medications to form the cocktail (most
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on July 24, 2008. The authors concluded that "raltegravir plus optimized background therapy provided better viral suppression than optimized background therapy alone for at least 48 weeks."
2483: 1594:, Gurjar MK, Sonawane SP, Maikap GS, Patil GD, Shinde SB, Patil PS Mehta SS, "Synthesis of raltegravir", published 2013-07-04, assigned to Emcure Pharmaceuticals Ltd 3407: 1955: 2922: 183: 2119: 1610: 1037: 1022: 2489: 2547: 2467: 2552: 2500: 1901: 81: 2522: 2506: 1614: 1317: 708: 736:
InChI=1S/C20H21FN6O5/c1-10-25-26-17(32-10)16(30)24-20(2,3)19-23-13(14(28)18(31)27(19)4)15(29)22-9-11-5-7-12(21)8-6-11/h5-8,28H,9H2,1-4H3,(H,22,29)(H,24,30)
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levels below detection at a more rapid rate. After 24 and 48 weeks of treatment, raltegravir did not result in increased serum levels of total
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In a study of the drug as part of combination therapy, raltegravir exhibited potent and durable antiretroviral activity similar to that of
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Croxtall JD, Keam SJ (May 2009). "Raltegravir: a review of its use in the management of HIV infection in treatment-experienced patients".
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for "Impact of MK-0518 (Raltegravir) Intensification on HIV-1 Viral Latency in Patients With Previous Complete Viral Suppression" at
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Stephenson J (April 2007). "Researchers buoyed by novel HIV drugs: will expand drug arsenal against resistant virus".
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In January 2013, a Phase II trial was initiated to evaluate the therapeutic benefit of raltegravir in treating
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Raltegravir was initially approved only for use in individuals whose infection has proven resistant to other
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N-(4-Fluorobenzyl)-5-hydroxy-1-methyl-2-(2-{amino}-2-propanyl)-6-oxo-1,6-dihydro-4-pyrimidinecarboxamide
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Markowitz M, Nguyen BY, Gotuzzo E, Mendo F, Ratanasuwan W, Kovacs C, et al. (October 2007).
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Steigbigel RT, Cooper DA, Kumar PN, Eron JE, Schechter M, Markowitz M, et al. (July 2008).
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In one method used for its manufacture, 2-amino-2-methylpropanenitrile is reacted with the
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Hunt JA (2010). "Raltegravir (Isentress): The First-in-Class HIV-1 Integrase Inhibitor".
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Raltegravir was approved for medical use in the United States in 2007. It is on the
50: 3237: 3136: 3019: 3009: 2724: 2714: 2295: 2285: 2103: 2060: 2055: 2050: 2012: 1992: 1922: 1405: 530: 196: 191: 1846: 1769: 1142:"Isentress 400 mg Film-coated Tablets - Summary of Product Characteristics (SmPC)" 1787: 1388: 1371: 3297: 3212: 3166: 3161: 3146: 3131: 3106: 2850: 2825: 2764: 2749: 2744: 2408: 2375: 2290: 2270: 2045: 2024: 1971: 1939: 1002: 998: 934: 893: 852: 99: 1497: 937:, a critical step in the HIV infection model. The drug is metabolized away via 774:, to prevent HIV infection following potential exposure. It is taken by mouth. 3227: 3222: 3217: 3176: 3171: 3126: 3086: 3065: 2855: 2835: 2820: 2815: 2779: 2774: 2688: 2633: 2603: 2415: 2403: 2398: 2370: 2310: 2300: 2275: 2260: 2250: 2199: 2194: 2182: 2166: 2156: 2136: 2098: 2008: 1996: 1988: 1524: 1025:
to receive approval in the United States in October 2007. It was developed by
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common to retroviruses that integrates the viral genetic material into human
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Raltegravir has been synthesized in several ways, which have been reviewed.
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World Health Organization model list of essential medicines: 21st list 2019
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so that methylation occurs on the nitrogen atom of the pyrimidone.
989:. The synthesis is completed by conversion of the remaining methyl 479: 471: 2019: 994: 990: 861: 851: 693: 684: 566: 490: 716:
Cc1nnc(o1)C(=O)NC(C)(C)C\3=N\C(C(=O)NCc2ccc(F)cc2)=C(\O)C(=O)N/3C
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ring of the drug is then created when the amidoxime reacts with
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Common side effects include trouble sleeping, feeling tired,
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Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
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Elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil
1828:"Drug against AIDS could be effective against herpesvirus" 2484:
Darunavir/cobicistat/emtricitabine/tenofovir alafenamide
1299:. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO. 222: 830:
World Health Organization's List of Essential Medicines
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of 5-methyl-1,3,4-oxadiazole-2-carboxylic acid using
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Vardanyan R, Hruby V (2016). "34: Antiviral Drugs".
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Medicines and Healthcare products Regulatory Agency
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Use of that reagent ensures the required 3182: 2962: 2948: 2940: 2621: 2518:Doravirine/lamivudine/tenofovir disoproxil 2355: 2221: 2126: 1902: 1888: 1880: 1498:"HIV Antiretroviral Agents in Development" 1255: 1253: 1251: 1249: 1247: 1245: 1243: 620: 597: 430: 2528:Efavirenz/lamivudine/tenofovir disoproxil 1803: 1666: 1656: 1611:"FDA approval of Isentress (raltegravir)" 1557: 1387: 1294: 450: 2795:Zinc finger protein transcription factor 1868:World patent covering the potassium salt 1639:Durrant JD, McCammon JA (October 2011). 1224:British national formulary : BNF 69 1114:"Product monograph brand safety updates" 1033:in the Journal of Medicinal Chemistry. 864:drugs. However, in July 2009, the U.S. 3340: 1218: 1216: 1105: 1064:Research results were published in the 815:HIV integrase strand transfer inhibitor 733: 713: 593: 410: 345: 104: 973:. The product is treated with aqueous 888:at 24 and 48 weeks but achieved HIV-1 611: 31: 3285:Merck Manual of Diagnosis and Therapy 1751:"Faster Viral Decay With Raltegravir" 1289:. Geneva: World Health Organization. 1049:Raltegravir significantly alters HIV 559: 518: 498: 90: 7: 1617:(FDA). June 25, 2009. Archived from 565: 195: 2543:Emtricitabine/tenofovir alafenamide 1792:The New England Journal of Medicine 478: 470: 381: 3383:Drugs developed by Merck & Co. 2558:Emtricitabine/tenofovir disoproxil 1559:10.1016/B978-0-12-411492-0.00034-1 789:. Severe side effects may include 770:. It may also be used, as part of 25: 1615:U.S. Food and Drug Administration 1318:U.S. Food and Drug Administration 1314:"Isentress Drug Approval Package" 1088:(MS). The drug is active against 3355: 3343: 2931:. Formerly or rarely used agent. 2568:Lamivudine/nevirapine/zidovudine 2452:Abacavir/dolutegravir/lamivudine 1468:10.2165/00003495-200969080-00007 953: 817:which blocks the functioning of 654: 651: 645: 49: 40: 2735:Epigallocatechin gallate (EGCG) 2578:Lamivudine/tenofovir disoproxil 2563:Lamivudine/nevirapine/stavudine 1067:New England Journal of Medicine 987:dimethyl acetylenedicarboxylate 741:Key:CZFFBEXEKNGXKS-UHFFFAOYSA-N 2458:Abacavir/lamivudine/zidovudine 1731:European Pharmaceutical Review 1693:Journal of Medicinal Chemistry 1550:Synthesis of Best-Seller Drugs 805:. It is unclear if use during 660: 639: 1: 1090:Human Endogenous Retroviruses 1845:Giovannoni G (24 May 2017). 1389:10.1097/QAI.0b013e318157131c 866:Food and Drug Administration 754:, sold under the brand name 3268:Merck Headquarters Building 2333:Tenofovir alafenamide (TAF) 1007:trimethylsulfoxonium iodide 813:is safe. Raltegravir is an 3424: 2328:Tenofovir disoproxil (TDF) 1021:Raltegravir was the first 993:of the intermediate to an 762:used, together with other 629:Chemical and physical data 2888: 2349:Discovery and development 2120:Discovery and development 1956:Discovery and development 1525:10.1002/9780470768594.ch1 1283:World Health Organization 1197:European Medicines Agency 772:post exposure prophylaxis 760:antiretroviral medication 724: 704: 336: 48: 39: 3403:4-Fluorophenyl compounds 2645:Transcription inhibitors 2597:Pharmacokinetic boosters 2513:Dolutegravir/rilpivirine 2474:Cabotegravir/rilpivirine 2114:Protease Inhibitors (PI) 1592:WO patent 2013098854 1433:10.1001/jama.297.14.1535 1320:(FDA). February 22, 2008 795:Stevens–Johnson syndrome 2929:initial regimen options 2495:Dolutegravir/lamivudine 1972:Enfuvirtide (ENF, T-20) 1950:Entry/fusion inhibitors 1261:"Raltegravir Potassium" 1036:In July 2024, the UK's 898:low-density lipoprotein 3051:Cubist Pharmaceuticals 2770:Portmanteau inhibitors 2663:Translation inhibitors 2573:Lamivudine/raltegravir 2343:Non-nucleoside (NNRTI) 2301:Islatravir (EFdA, ISL) 1767:Clinical trial number 1658:10.1186/1741-7007-9-71 1029:and reported by Summa 925:, raltegravir targets 857: 834:Lamivudine/raltegravir 3208:Ezetimibe/simvastatin 3102:Ezetimibe/simvastatin 3056:H. K. Mulford Company 2971:Merck & Co., Inc. 2785:Synergistic enhancers 2583:Lamivudine/zidovudine 2463:Atazanavir/cobicistat 2439:Combined formulations 2276:Zidovudine (AZT, ZDV) 2214:Reverse-transcriptase 2086:Maturation inhibitors 1805:10.1056/NEJMoa0708975 1517:Modern Drug Synthesis 1092:(HERVs) and possibly 1075:human cytomegalovirus 855: 844:, is also available. 3378:Integrase inhibitors 2626:Uncoating inhibitors 2479:Darunavir/cobicistat 2319:Nucleotide analogues 2237:Nucleoside analogues 2036:Integrase inhibitors 1915:antiretroviral drugs 1552:. pp. 719–720. 821:which is needed for 2978:Corporate directors 2618:Experimental agents 2588:Lopinavir/ritonavir 2447:Abacavir/lamivudine 2421:Elsulfavirine (ESV) 2256:Emtricitabine (FTC) 2142:Fosamprenavir (FPV) 1201:. 17 September 2018 1059:protease inhibitors 1023:integrase inhibitor 923:integrase inhibitor 917:Mechanism of action 242:(Prescription only) 36: 3233:Rocuronium bromide 3157:rVSV-ZEBOV vaccine 2915:Never to phase III 2061:Elvitegravir (EVG) 2056:Dolutegravir (DTG) 2051:Cabotegravir (CAB) 1873:2007-10-14 at the 1851:clinicaltrials.gov 1775:ClinicalTrials.gov 1755:www.thebodypro.com 1094:Epstein–Barr virus 1086:multiple sclerosis 967:N-methylmorpholine 858: 791:allergic reactions 3331: 3330: 3292:The Merck Manuals 3256: 3255: 2937: 2936: 2884: 2883: 2730:Diarylpyrimidines 2433: 2432: 2429: 2428: 2409:Rilpivirine (RPV) 2393:diarylpyrimidines 2376:Delavirdine (DLV) 2271:Zalcitabine (ddC) 2228:nucleotide (NRTI) 2208: 2207: 2066:Raltegravir (RAL) 2046:Bictegravir (BIC) 2025:Fostemsavir (FTR) 1940:Lenacapavir (LEN) 1932:Capsid inhibitors 1705:10.1021/jm800245z 1699:(18): 5843–5855. 1569:978-0-12-411492-0 1534:978-0-470-76859-4 1519:. pp. 1–15. 1427:(14): 1535–1536. 1233:978-0-85711-156-2 856:Isentress tablets 823:viral replication 749: 748: 695:Interactive image 579:CompTox Dashboard 262: 250: 237: 225: 158: 125: 27:Chemical compound 16:(Redirected from 3415: 3360: 3359: 3348: 3347: 3346: 3339: 3183: 3046:Acceleron Pharma 3005:Rochelle Lazarus 2995:William Harrison 2964: 2957: 2950: 2941: 2755:Hydroxycarbamide 2622: 2416:Doravirine (DOR) 2404:Etravirine (ETR) 2399:Dapivirine (DPV) 2371:Nevirapine (NVP) 2356: 2261:Lamivudine (3TC) 2251:Didanosine (ddI) 2222: 2195:Tipranavir (TPV) 2183:Atazanavir (ATV) 2167:Saquinavir (SQV) 2157:Nelfinavir (NFV) 2137:Amprenavir (APV) 2127: 2009:Ibalizumab (IBA) 1904: 1897: 1890: 1881: 1855: 1854: 1842: 1836: 1835: 1824: 1818: 1817: 1807: 1783: 1777: 1765: 1759: 1758: 1747: 1741: 1740: 1738: 1737: 1723: 1717: 1716: 1687: 1681: 1680: 1670: 1660: 1636: 1630: 1629: 1627: 1626: 1621:on July 10, 2009 1607: 1601: 1600: 1599: 1595: 1588: 1582: 1581: 1561: 1545: 1539: 1538: 1512: 1506: 1505: 1504:. 30 March 2006. 1494: 1488: 1487: 1462:(8): 1059–1075. 1451: 1445: 1444: 1416: 1410: 1409: 1391: 1367: 1361: 1360: 1353: 1347: 1346: 1335: 1329: 1328: 1326: 1325: 1310: 1301: 1300: 1298: 1279: 1273: 1272: 1270: 1268: 1257: 1238: 1237: 1220: 1211: 1210: 1208: 1206: 1192:"Isentress EPAR" 1188: 1182: 1181: 1179: 1177: 1163: 1157: 1156: 1154: 1152: 1138: 1132: 1131: 1129: 1127: 1110: 1011:chemoselectivity 957: 900:cholesterol, or 799:muscle breakdown 783:high blood sugar 697: 677: 662: 656: 653: 647: 641: 624: 613: 602: 601: 587: 585: 569: 563: 542: 522: 502: 482: 474: 454: 434: 414: 394: 384: 383: 369: 313: 260: 257: 248: 245: 235: 232: 224: 221: 199: 156: 153: 135: 124: 121: 108: 94: 53: 44: 37: 35: 21: 3423: 3422: 3418: 3417: 3416: 3414: 3413: 3412: 3368: 3367: 3366: 3354: 3344: 3342: 3334: 3332: 3327: 3272: 3252: 3193:Coppertone sign 3186:Schering-Plough 3181: 3070: 3061:Schering-Plough 3034: 2973: 2968: 2938: 2933: 2932: 2920: 2905:Clinical trials 2880: 2831:Dexelvucitabine 2799: 2790:Tre recombinase 2693: 2675: 2657: 2653:Tat antagonists 2639: 2613: 2592: 2425: 2380: 2366:Efavirenz (EFV) 2345: 2337: 2266:Stavudine (d4T) 2227: 2215: 2204: 2189:Darunavir (DRV) 2171: 2162:Ritonavir (RTV) 2152:Lopinavir (LPV) 2147:Indinavir (IDV) 2116: 2108: 2080: 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binding 280:Bioavailability 272:Pharmacokinetic 266: 203: 171: 164: 145: 138: 28: 23: 22: 15: 12: 11: 5: 3421: 3419: 3411: 3410: 3405: 3400: 3395: 3390: 3385: 3380: 3370: 3369: 3365: 3364: 3352: 3329: 3328: 3326: 3325: 3324: 3323: 3316: 3309: 3302: 3288: 3280: 3278: 3274: 3273: 3271: 3270: 3264: 3262: 3258: 3257: 3254: 3253: 3251: 3250: 3248:Urofollitropin 3245: 3240: 3235: 3230: 3225: 3220: 3215: 3210: 3205: 3200: 3195: 3189: 3187: 3180: 3179: 3174: 3169: 3164: 3159: 3154: 3149: 3144: 3139: 3134: 3129: 3124: 3119: 3114: 3109: 3104: 3099: 3094: 3089: 3084: 3078: 3076: 3072: 3071: 3069: 3068: 3063: 3058: 3053: 3048: 3042: 3040: 3036: 3035: 3033: 3032: 3027: 3022: 3017: 3012: 3007: 3002: 3000:William Kelley 2997: 2992: 2990:Johnnetta Cole 2987: 2981: 2979: 2975: 2974: 2969: 2967: 2966: 2959: 2952: 2944: 2935: 2934: 2919: 2918: 2917: 2916: 2913: 2902: 2896: 2890: 2889: 2886: 2885: 2882: 2881: 2879: 2878: 2873: 2868: 2863: 2858: 2853: 2848: 2843: 2838: 2833: 2828: 2823: 2818: 2813: 2807: 2805: 2801: 2800: 2798: 2797: 2792: 2787: 2782: 2777: 2772: 2767: 2762: 2757: 2752: 2747: 2742: 2737: 2732: 2727: 2722: 2717: 2712: 2707: 2701: 2699: 2695: 2694: 2692: 2691: 2685: 2683: 2677: 2676: 2674: 2673: 2667: 2665: 2659: 2658: 2656: 2655: 2649: 2647: 2641: 2640: 2638: 2637: 2630: 2628: 2619: 2615: 2614: 2612: 2611: 2606: 2604:Cobicistat (c) 2600: 2598: 2594: 2593: 2591: 2590: 2585: 2580: 2575: 2570: 2565: 2560: 2555: 2550: 2545: 2540: 2535: 2530: 2525: 2520: 2515: 2510: 2504: 2498: 2492: 2487: 2481: 2476: 2471: 2465: 2460: 2455: 2449: 2443: 2441: 2435: 2434: 2431: 2430: 2427: 2426: 2424: 2423: 2418: 2413: 2412: 2411: 2406: 2401: 2388: 2386: 2382: 2381: 2379: 2378: 2373: 2368: 2362: 2360: 2353: 2339: 2338: 2336: 2335: 2330: 2314: 2313: 2308: 2303: 2298: 2293: 2288: 2283: 2278: 2273: 2268: 2263: 2258: 2253: 2248: 2246:Abacavir (ABC) 2232: 2230: 2226:Nucleoside and 2219: 2210: 2209: 2206: 2205: 2203: 2202: 2197: 2192: 2186: 2179: 2177: 2173: 2172: 2170: 2169: 2164: 2159: 2154: 2149: 2144: 2139: 2133: 2131: 2124: 2110: 2109: 2107: 2106: 2101: 2096: 2090: 2088: 2082: 2081: 2079: 2078: 2073: 2068: 2063: 2058: 2053: 2048: 2042: 2040: 2032: 2031: 2029: 2028: 2016: 2000: 1986: 1975: 1962: 1960: 1946: 1945: 1943: 1942: 1936: 1934: 1928: 1927: 1909: 1907: 1906: 1899: 1892: 1884: 1878: 1877: 1863: 1862:External links 1860: 1857: 1856: 1837: 1819: 1798:(4): 339–354. 1778: 1760: 1742: 1718: 1682: 1631: 1602: 1583: 1568: 1540: 1533: 1507: 1489: 1446: 1411: 1382:(2): 125–133. 1362: 1348: 1330: 1302: 1274: 1239: 1232: 1212: 1183: 1158: 1133: 1104: 1103: 1101: 1098: 1051:viral dynamics 1046: 1043: 1018: 1015: 1001:, followed by 981:. The central 959: 958: 946: 943: 918: 915: 909: 906: 881: 878: 873:anti-HIV drugs 849: 846: 803:liver problems 747: 746: 744: 743: 740: 738: 735: 727: 726: 725: 722: 721: 719: 718: 715: 707: 706: 705: 702: 701: 699: 698: 690: 688: 680: 679: 673: 667: 666: 663: 657: 648: 642: 637: 631: 630: 626: 625: 615: 607: 606: 604: 603: 590: 588: 575: 574: 572: 571: 555: 553: 547: 546: 544: 543: 535: 533: 527: 526: 524: 523: 515: 513: 507: 506: 504: 503: 495: 493: 487: 486: 484: 483: 477:as salt:  475: 467: 465: 459: 458: 456: 455: 447: 445: 439: 438: 436: 435: 427: 425: 419: 418: 416: 415: 407: 405: 399: 398: 396: 395: 387: 385: 374: 373: 371: 370: 362: 360: 354: 353: 351: 350: 347: 339: 338: 337: 334: 333: 329: 328: 325: 319: 318: 315: 306: 305: 304:Liver (UGT1A1) 302: 296: 295: 292: 286: 285: 282: 276: 275: 268: 267: 265: 264: 255: 243: 230: 218: 216: 210: 209: 205: 204: 202: 201: 188: 186: 180: 179: 174: 172:administration 166: 165: 163: 162: 160: 150: 148: 140: 139: 137: 136: 118: 116: 110: 109: 102: 96: 95: 88: 78: 77: 74: 70: 69: 66: 60: 59: 55: 54: 46: 45: 26: 24: 14: 13: 10: 9: 6: 4: 3: 2: 3420: 3409: 3406: 3404: 3401: 3399: 3396: 3394: 3391: 3389: 3386: 3384: 3381: 3379: 3376: 3375: 3373: 3363: 3358: 3353: 3351: 3341: 3337: 3322: 3321: 3317: 3315: 3314: 3310: 3308: 3307: 3303: 3301: 3300: 3296: 3295: 3294: 3293: 3289: 3287: 3286: 3282: 3281: 3279: 3275: 3269: 3266: 3265: 3263: 3259: 3249: 3246: 3244: 3241: 3239: 3236: 3234: 3231: 3229: 3226: 3224: 3221: 3219: 3216: 3214: 3211: 3209: 3206: 3204: 3201: 3199: 3198:Desloratadine 3196: 3194: 3191: 3190: 3188: 3184: 3178: 3175: 3173: 3170: 3168: 3165: 3163: 3160: 3158: 3155: 3153: 3150: 3148: 3145: 3143: 3140: 3138: 3135: 3133: 3130: 3128: 3125: 3123: 3120: 3118: 3115: 3113: 3112:Fosaprepitant 3110: 3108: 3105: 3103: 3100: 3098: 3095: 3093: 3090: 3088: 3085: 3083: 3080: 3079: 3077: 3073: 3067: 3064: 3062: 3059: 3057: 3054: 3052: 3049: 3047: 3044: 3043: 3041: 3037: 3031: 3030:Peter Wendell 3028: 3026: 3025:Wendell Weeks 3023: 3021: 3018: 3016: 3013: 3011: 3008: 3006: 3003: 3001: 2998: 2996: 2993: 2991: 2988: 2986: 2985:Richard Clark 2983: 2982: 2980: 2976: 2972: 2965: 2960: 2958: 2953: 2951: 2946: 2945: 2942: 2930: 2927: 2924: 2914: 2912: 2909: 2908: 2906: 2903: 2900: 2897: 2895: 2892: 2891: 2887: 2877: 2874: 2872: 2869: 2867: 2864: 2862: 2859: 2857: 2854: 2852: 2849: 2847: 2844: 2842: 2839: 2837: 2834: 2832: 2829: 2827: 2824: 2822: 2819: 2817: 2814: 2812: 2809: 2808: 2806: 2804:Failed agents 2802: 2796: 2793: 2791: 2788: 2786: 2783: 2781: 2778: 2776: 2773: 2771: 2768: 2766: 2763: 2761: 2758: 2756: 2753: 2751: 2748: 2746: 2743: 2741: 2738: 2736: 2733: 2731: 2728: 2726: 2723: 2721: 2718: 2716: 2713: 2711: 2708: 2706: 2703: 2702: 2700: 2696: 2690: 2687: 2686: 2684: 2682: 2678: 2672: 2671:Trichosanthin 2669: 2668: 2666: 2664: 2660: 2654: 2651: 2650: 2648: 2646: 2642: 2635: 2632: 2631: 2629: 2627: 2623: 2620: 2616: 2610: 2609:Ritonavir (r) 2607: 2605: 2602: 2601: 2599: 2595: 2589: 2586: 2584: 2581: 2579: 2576: 2574: 2571: 2569: 2566: 2564: 2561: 2559: 2556: 2554: 2551: 2549: 2546: 2544: 2541: 2539: 2536: 2534: 2531: 2529: 2526: 2524: 2521: 2519: 2516: 2514: 2511: 2508: 2505: 2502: 2499: 2496: 2493: 2491: 2488: 2485: 2482: 2480: 2477: 2475: 2472: 2469: 2466: 2464: 2461: 2459: 2456: 2453: 2450: 2448: 2445: 2444: 2442: 2440: 2436: 2422: 2419: 2417: 2414: 2410: 2407: 2405: 2402: 2400: 2397: 2396: 2395: 2394: 2390: 2389: 2387: 2383: 2377: 2374: 2372: 2369: 2367: 2364: 2363: 2361: 2357: 2354: 2352: 2350: 2344: 2340: 2334: 2331: 2329: 2326: 2324: 2320: 2316: 2315: 2312: 2309: 2307: 2304: 2302: 2299: 2297: 2294: 2292: 2289: 2287: 2284: 2282: 2279: 2277: 2274: 2272: 2269: 2267: 2264: 2262: 2259: 2257: 2254: 2252: 2249: 2247: 2244: 2242: 2238: 2234: 2233: 2231: 2229: 2223: 2220: 2217: 2211: 2201: 2198: 2196: 2193: 2190: 2187: 2184: 2181: 2180: 2178: 2174: 2168: 2165: 2163: 2160: 2158: 2155: 2153: 2150: 2148: 2145: 2143: 2140: 2138: 2135: 2134: 2132: 2128: 2125: 2123: 2121: 2115: 2111: 2105: 2102: 2100: 2097: 2095: 2092: 2091: 2089: 2087: 2083: 2077: 2074: 2072: 2069: 2067: 2064: 2062: 2059: 2057: 2054: 2052: 2049: 2047: 2044: 2043: 2041: 2037: 2033: 2026: 2022: 2021: 2017: 2014: 2010: 2006: 2005: 2001: 1998: 1994: 1990: 1987: 1985: 1981: 1980: 1976: 1973: 1969: 1968: 1964: 1963: 1961: 1959: 1957: 1951: 1947: 1941: 1938: 1937: 1935: 1933: 1929: 1924: 1920: 1917:used against 1916: 1912: 1905: 1900: 1898: 1893: 1891: 1886: 1885: 1882: 1876: 1872: 1869: 1866: 1865: 1861: 1852: 1848: 1841: 1838: 1833: 1829: 1823: 1820: 1815: 1811: 1806: 1801: 1797: 1793: 1789: 1782: 1779: 1776: 1772: 1771: 1764: 1761: 1756: 1752: 1746: 1743: 1732: 1728: 1722: 1719: 1714: 1710: 1706: 1702: 1698: 1694: 1686: 1683: 1678: 1674: 1669: 1664: 1659: 1654: 1650: 1646: 1642: 1635: 1632: 1620: 1616: 1612: 1606: 1603: 1593: 1587: 1584: 1579: 1575: 1571: 1565: 1560: 1555: 1551: 1544: 1541: 1536: 1530: 1526: 1522: 1518: 1511: 1508: 1503: 1499: 1493: 1490: 1485: 1481: 1477: 1473: 1469: 1465: 1461: 1457: 1450: 1447: 1442: 1438: 1434: 1430: 1426: 1422: 1415: 1412: 1407: 1403: 1399: 1395: 1390: 1385: 1381: 1377: 1373: 1366: 1363: 1358: 1352: 1349: 1345:. 2009-07-10. 1344: 1340: 1334: 1331: 1319: 1315: 1309: 1307: 1303: 1297: 1292: 1288: 1284: 1278: 1275: 1262: 1256: 1254: 1252: 1250: 1248: 1246: 1244: 1240: 1235: 1229: 1225: 1219: 1217: 1213: 1200: 1198: 1193: 1187: 1184: 1172: 1168: 1162: 1159: 1147: 1143: 1137: 1134: 1122:. 7 July 2016 1121: 1120: 1119:Health Canada 1115: 1109: 1106: 1099: 1097: 1095: 1091: 1087: 1082: 1080: 1079:herpesviruses 1076: 1071: 1069: 1068: 1062: 1060: 1056: 1052: 1044: 1042: 1039: 1034: 1032: 1028: 1024: 1016: 1014: 1012: 1008: 1004: 1000: 997:with 4-fluoro 996: 992: 988: 984: 980: 976: 975:hydroxylamine 972: 968: 964: 963:acid chloride 956: 952: 951: 950: 944: 942: 940: 936: 932: 928: 924: 916: 914: 907: 905: 903: 902:triglycerides 899: 895: 891: 887: 879: 877: 874: 869: 867: 863: 854: 847: 845: 843: 839: 835: 831: 826: 824: 820: 819:HIV integrase 816: 812: 811:breastfeeding 808: 804: 800: 796: 792: 788: 784: 780: 775: 773: 769: 765: 761: 757: 753: 739: 734: 730: 723: 714: 710: 703: 696: 692: 691: 689: 686: 681: 674: 672: 668: 638: 636: 632: 627: 623: 619: 616: 614: 612:ECHA InfoCard 608: 600: 596: 595:DTXSID2048660 592: 591: 589: 580: 576: 568: 567:RCSB PDB 562: 557: 556: 554: 552: 548: 541: 537: 536: 534: 532: 528: 521: 517: 516: 514: 512: 508: 501: 497: 496: 494: 492: 488: 481: 476: 473: 469: 468: 466: 464: 460: 453: 449: 448: 446: 444: 440: 433: 429: 428: 426: 424: 420: 413: 409: 408: 406: 404: 400: 393: 389: 388: 386: 379: 375: 368: 364: 363: 361: 359: 355: 346: 342: 335: 330: 326: 324: 320: 316: 314: 307: 303: 301: 297: 293: 291: 287: 283: 281: 277: 273: 269: 263: Rx-only 256: 254: 244: 241: 231: 229: 220: 219: 217: 215: 211: 206: 198: 193: 190: 189: 187: 185: 181: 178: 175: 173: 167: 161: 152: 151: 149: 147: 141: 134: 129: 120: 119: 117: 115: 111: 107: 103: 101: 97: 93: 89: 87: 83: 79: 75: 71: 67: 65: 61: 58:Clinical data 56: 52: 47: 43: 38: 30: 19: 3393:Carboxamides 3319: 3312: 3305: 3298: 3290: 3283: 3277:Publications 3238:Temozolomide 3141: 3137:Omarigliptin 3039:Subsidiaries 3020:Samuel Thier 3015:Anne Tatlock 3010:Thomas Shenk 2925: 2725:Cyanovirin-N 2715:Calanolide A 2391: 2385:2 generation 2359:1 generation 2346: 2317: 2296:Elvucitabine 2286:Apricitabine 2235: 2176:2 generation 2130:1 generation 2117: 2104:Fipravirimat 2065: 2018: 2013:Semzuvolimab 2002: 1993:Cenicriviroc 1977: 1965: 1953: 1850: 1840: 1832:ScienceDaily 1831: 1822: 1795: 1791: 1781: 1768: 1763: 1754: 1745: 1734:. Retrieved 1730: 1721: 1696: 1692: 1685: 1648: 1644: 1634: 1623:. Retrieved 1619:the original 1605: 1586: 1549: 1543: 1516: 1510: 1501: 1492: 1459: 1455: 1449: 1424: 1420: 1414: 1379: 1375: 1365: 1351: 1342: 1333: 1322:. Retrieved 1296:10665/325771 1286: 1277: 1265:. Retrieved 1223: 1203:. Retrieved 1195: 1186: 1174:. Retrieved 1170: 1161: 1149:. Retrieved 1145: 1136: 1124:. Retrieved 1117: 1108: 1083: 1073:Research on 1072: 1065: 1063: 1048: 1035: 1030: 1020: 960: 948: 920: 911: 908:Side effects 883: 870: 859: 848:Medical uses 827: 776: 755: 751: 750: 531:NIAID ChemDB 520:ChEMBL254316 310:Elimination 214:Legal status 208:Legal status 114:License data 29: 3398:Pyrimidones 3388:Oxadiazoles 3213:Famciclovir 3167:Sitagliptin 3162:Simvastatin 3147:Rizatriptan 3142:Raltegravir 3132:Montelukast 3107:Finasteride 3082:Alendronate 2926:recommended 2901:from market 2851:Lersivirine 2826:Capravirine 2765:Miltefosine 2750:Griffithsin 2745:Fosdevirine 2291:Censavudine 1921:(primarily 1770:NCT00554398 1645:BMC Biology 1003:methylation 999:benzylamine 977:to form an 935:chromosomes 894:cholesterol 838:combination 766:, to treat 752:Raltegravir 678: g·mol 618:100.124.631 500:CHEBI:82960 367:518048-05-0 332:Identifiers 133:Raltegravir 100:MedlinePlus 73:Other names 64:Trade names 34:Raltegravir 3372:Categories 3320:Geriatrics 3313:Veterinary 3261:Facilities 3228:Mometasone 3223:Loratadine 3218:Infliximab 3177:Vorinostat 3172:Vericiguat 3127:Lovastatin 3087:Aprepitant 3066:Viralytics 2856:Lodenosine 2836:Droxinavir 2821:Brecanavir 2816:Atevirdine 2780:Seliciclib 2775:Scytovirin 2689:Elipovimab 2634:TRIM5alpha 2311:Stampidine 2216:inhibitors 2200:TMC-310911 2099:BMS-955176 1997:Leronlimab 1989:Vicriviroc 1736:2024-07-29 1625:2009-11-15 1324:2009-11-15 1267:8 December 1100:References 983:pyrimidone 842:lamivudine 793:including 764:medication 683:3D model ( 671:Molar mass 551:PDB ligand 452:22VKV8053U 423:ChemSpider 358:CAS Number 341:IUPAC name 300:Metabolism 3203:Ezetimibe 3152:Rofecoxib 3117:Indinavir 3097:Ezetimibe 3092:Ertapenem 2911:Phase III 2899:Withdrawn 2876:Telinavir 2871:Palinavir 2866:Mozenavir 2846:Emivirine 2841:Lasinavir 2811:Aplaviroc 2740:Foscarnet 2720:Ceragenin 2281:Amdoxovir 2094:Bevirimat 2071:BI 224436 1651:(1): 71. 1484:195685470 979:amidoxime 945:Chemistry 927:integrase 886:efavirenz 807:pregnancy 787:headaches 756:Isentress 323:Excretion 312:half-life 284:60% (FDA) 170:Routes of 144:Pregnancy 92:Monograph 86:Drugs.com 68:Isentress 18:Isentress 3350:Medicine 3243:Tibolone 3122:Losartan 3075:Products 2861:Loviride 1871:Archived 1814:18650512 1713:18763751 1677:22035460 1578:75449475 1476:19496631 1441:17426263 1398:17721395 1285:(2019). 1171:DailyMed 1045:Research 880:Efficacy 768:HIV/AIDS 758:, is an 432:16445111 403:DrugBank 392:54671008 184:ATC code 177:By mouth 159: B3 146:category 128:DailyMed 3362:Viruses 3336:Portals 2760:KP-1461 2306:Racivir 2076:MK-2048 1668:3203851 1406:6130143 1343:Reuters 1205:12 July 1176:11 July 1151:11 July 1126:1 April 1017:History 676:444.423 635:Formula 412:DB06817 378:PubChem 317:9 hours 226:: 200:) 194: ( 192:J05AJ01 130::  106:a608004 3306:Manual 2894:WHO-EM 2710:BIT225 2705:Abzyme 2636:(gene) 2323:NtRTIs 2218:(RTIs) 1812:  1711:  1675:  1665:  1598:  1576:  1566:  1531:  1482:  1474:  1439:  1404:  1396:  1230:  1031:et al. 1005:using 931:enzyme 921:As an 801:, and 785:, and 779:nausea 709:SMILES 540:471309 511:ChEMBL 480:D07133 472:D06676 253:â„ž-only 251: 238: 228:â„ž-only 126:  3299:Index 2698:Other 2681:BNAbs 2241:NRTIs 2020:gp120 1574:S2CID 1480:S2CID 1456:Drugs 1402:S2CID 1199:(EMA) 1146:(emc) 1027:Merck 995:amide 991:ester 929:, an 862:HAART 840:with 729:InChI 685:JSmol 558:RLT ( 491:ChEBI 2923:DHHS 1979:CCR5 1967:gp41 1810:PMID 1709:PMID 1673:PMID 1564:ISBN 1529:ISBN 1472:PMID 1437:PMID 1421:JAMA 1394:PMID 1269:2017 1228:ISBN 1207:2021 1178:2021 1153:2021 1128:2024 971:base 836:, a 561:PDBe 463:KEGG 443:UNII 274:data 82:AHFS 2004:CD4 1923:J05 1919:HIV 1800:doi 1796:359 1701:doi 1663:PMC 1653:doi 1554:doi 1521:doi 1464:doi 1429:doi 1425:297 1384:doi 1291:hdl 1057:or 969:as 890:RNA 809:or 584:EPA 382:CID 294:83% 240:POM 197:WHO 76:RAL 3374:: 2907:: 2011:, 1995:, 1991:, 1913:: 1849:. 1830:. 1808:. 1794:. 1790:. 1753:. 1729:. 1707:. 1697:51 1695:. 1671:. 1661:. 1647:. 1643:. 1613:. 1572:. 1562:. 1527:. 1500:. 1478:. 1470:. 1460:69 1458:. 1435:. 1423:. 1400:. 1392:. 1380:46 1378:. 1374:. 1341:. 1316:. 1305:^ 1242:^ 1215:^ 1194:. 1169:. 1144:. 1116:. 1081:. 941:. 904:. 896:, 832:. 825:. 797:, 781:, 649:21 643:20 564:, 259:EU 247:US 234:UK 223:CA 155:AU 123:US 3338:: 2963:e 2956:t 2949:v 2921:° 2509:° 2503:° 2497:° 2486:° 2470:° 2454:° 2351:) 2347:( 2325:: 2321:/ 2243:: 2239:/ 2191:° 2185:° 2122:) 2118:( 2027:) 2023:( 2015:) 2007:( 1999:) 1982:( 1974:) 1970:( 1958:) 1954:( 1925:) 1903:e 1896:t 1889:v 1853:. 1834:. 1816:. 1802:: 1739:. 1715:. 1703:: 1679:. 1655:: 1649:9 1628:. 1580:. 1556:: 1537:. 1523:: 1486:. 1466:: 1443:. 1431:: 1408:. 1386:: 1359:. 1327:. 1293:: 1271:. 1236:. 1209:. 1180:. 1155:. 1130:. 687:) 664:5 661:O 658:6 655:N 652:F 646:H 640:C 586:) 582:( 570:) 261:: 249:: 236:: 157:: 84:/ 20:)

Index

Isentress
2

Trade names
AHFS
Drugs.com
Monograph
MedlinePlus
a608004
License data
DailyMed
Raltegravir
Pregnancy
category

Routes of
administration

By mouth
ATC code
J05AJ01
WHO
Legal status
â„ž-only
POM
â„ž-only
Pharmacokinetic
Bioavailability
Protein binding
Metabolism
Elimination half-life
Excretion
IUPAC name
CAS Number

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