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Saquinavir

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Roche requested and received approval of Invirase via the FDA's "Accelerated Approval" program—a process designed to speed drugs to market for the treatment of serious diseases—a decision that was controversial, as AIDS activists disagreed over the benefits of thorough testing versus early access to
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by a few months. This new class of antiretrovirals played a critical role in the development of highly active antiretroviral therapy (HAART), which helped significantly lower the risk of death from AIDS-related causes, as seen by a reduction of the annual U.S. HIV-associated death rate, from over
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InChI=1S/C38H50N6O5/c1-38(2,3)43-37(49)32-20-26-14-7-8-15-27(26)22-44(32)23-33(45)30(19-24-11-5-4-6-12-24)41-36(48)31(21-34(39)46)42-35(47)29-18-17-25-13-9-10-16-28(25)40-29/h4-6,9-13,16-18,26-27,30-33,45H,7-8,14-15,19-23H2,1-3H3,(H2,39,46)(H,41,48)(H,42,47)(H,43,49)/t26-,27+,30-,31-,32-,33+/m0/s1
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are enzymes that cleave protein molecules into smaller fragments. HIV protease is vital for both viral replication within the cell and release of mature viral particles from an infected cell. Saquinavir binds to the active site of the viral protease and prevents cleavage of viral polyproteins,
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isozyme. Normally, this enzyme metabolizes saquinavir to an inactive form, but with the ritonavir inhibiting this enzyme, the saquinavir blood plasma levels increased considerably. Additionally, ritonavir also inhibits multidrug transporters, although to a much lower extent.
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Saquinavir, in the Invirase formulation, has a low and variable oral bioavailability, when given alone. The Fortovase formulation at the standard dosage delivers approximately eightfold more active drug than Invirase, also at the standard dosage.
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ascribes this to "highly active antiretroviral therapy", without mention of either of these drugs, see the preceding citation. A further citation is needed to make this accurate connection between this drop and the introduction of the protease
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New HIV infections and deaths, before and after the FDA approval of "highly active antiretroviral therapy", of which saquinavir, ritonavir and indinavir were key as the first three protease inhibitors.
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In the clinic, it was found that the oral bioavailability of saquinavir in both formulations significantly increases when patients also receive the PI
121: 2208: 2266: 2186: 939:. Roche announced in May 2005 that, given reduced demand, Fortovase would cease being marketed early in 2006, in favor of Invirase boosted with 2271: 2712: 2219: 1620: 70: 2241: 2225: 679: 2594: 2589: 1144: 2236: 1265: 2246: 1462: 1561: 1217:"Effect of omeprazole on the pharmacokinetics of saquinavir-500 mg formulation with ritonavir in healthy male and female volunteers" 2513: 1317: 2157: 1058: 842:
The mechanism behind this welcome observation was not directly known, but later it was determined that ritonavir inhibits the
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Common side effects include nausea, vomiting, diarrhea, and feeling tired. More serious side effects include problems with
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The most frequent adverse events with saquinavir in either formulation are mild gastrointestinal symptoms, including
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new drugs. It was approved again on November 7, 1997, as Fortovase, a soft gel capsule reformulated for improved
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As a result of the new therapies, HIV deaths in the United States fell dramatically within two years.
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Winston A, Back D, Fletcher C, Robinson L, Unsworth J, Tolowinska I, et al. (June 2006).
1159: 1128: 918:. Saquinavir was the sixth antiretroviral and the first protease inhibitor approved by the US 2722: 2702: 2488: 2301: 2181: 2051: 1650: 403: 452: 367: 2371: 2197: 2046: 1804: 1486: 472: 302: 1628: 1587: 1469: 886: 8: 2737: 2306: 2165: 2037: 1955: 1754: 1633: 1569: 1297: 1059:"Invirase- saquinavir mesylate capsule INVIRASE- saquinavir mesylate tablet, film coated" 804: 754: 358: 271: 1233: 1216: 591: 1543: 1246: 961: 853:
Unlike other protease inhibitors, the absorption of saquinavir seems to be improved by
149: 823:, loose stools and abdominal discomfort. Invirase is better tolerated than Fortovase. 2448: 2111: 1535: 1309: 1271: 1238: 1165: 1134: 915: 543: 247: 94: 1547: 1250: 2473: 1527: 1228: 608: 392: 257: 202: 2647: 1101: 1013: 80: 2674: 2549: 2508: 1668: 1531: 985: 936: 875: 765: 289: 265: 1295: 2686: 2623: 1629: 1406: 773: 687:
O=C(N)C(NC(=O)c1nc2c(cc1)cccc2)C(=O)N(Cc3ccccc3)(O)CN5(C(=O)NC(C)(C)C)C4CCCC4C5
2696: 2389: 2139: 1974: 1860: 992: 39: 2443: 2433: 2014: 2004: 1822: 1779: 1774: 1769: 1731: 1711: 1641: 1539: 1513:"Microemulsions for oral administration and their therapeutic applications" 1313: 1242: 1193: 781: 523: 197: 22: 1562:"Roche to discontinue the sale and distribution of Fortovase (saquinavir)" 2569: 2544: 2483: 2468: 2463: 2127: 2094: 2009: 1989: 1784: 1764: 1743: 1690: 1658: 1404: 769: 88: 432: 2574: 2554: 2539: 2534: 2498: 2493: 2407: 2352: 2322: 2134: 2122: 2117: 2089: 2029: 2019: 1994: 1979: 1969: 1918: 1913: 1901: 1875: 1855: 1817: 1727: 1715: 1707: 1407:"Drugs! Drugs! Drugs! An Overview of the Approved Anti-HIV Medications" 943:, owing to the ability of the latter co-formulated drug to inhibit the 854: 795:
Saquinavir is used together with other medications to treat or prevent
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Centers for Disease Control and Prevention (CDC) (3 June 2011).
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preventing maturation of the virus. Saquinavir inhibits both
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Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
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Elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil
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used together with other medications to treat or prevent
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Darunavir/cobicistat/emtricitabine/tenofovir alafenamide
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Saquinavir was patented in 1988 and first sold in 1995.
1433:"Drug Approval Package: Fortovase/Saquinavir NDA 20828" 914:
Saquinavir was developed by the pharmaceutical company
894:"Protease inhibitors give wings to combination therapy" 2658: 1104:. The American Society of Health-System Pharmacists. 931:50,000 to about 18,000 over a period of two years. 411: 1006: 2694: 2209:Dolutegravir/emtricitabine/tenofovir alafenamide 391: 2267:Emtricitabine/rilpivirine/tenofovir alafenamide 2187:Bictegravir/emtricitabine/tenofovir alafenamide 1405:AIDS Community Research Initiative of America. 1366:"Antiretroviral Drug Discovery and Development" 1157: 1130:Handbook of Assay Development in Drug Discovery 366: 2272:Emtricitabine/rilpivirine/tenofovir disoproxil 1758:(Integrase strand transfer inhibitors (INSTI)) 1263: 1039:Roche Products Pty Limited (6 November 2018). 991:a soft-gel capsule formulation of saquinavir ( 2220:Dolutegravir/lamivudine/tenofovir alafenamide 1614: 1051: 1047:– via MedAdvisor International Pty Ltd. 2242:Efavirenz/emtricitabine/tenofovir disoproxil 2226:Dolutegravir/lamivudine/tenofovir disoproxil 1510: 1302:Morbidity and Mortality Weekly Report (MMWR) 531: 137: 1298:"HIV Surveillance—United States, 1981-2008" 1291: 1289: 1287: 2237:Doravirine/lamivudine/tenofovir disoproxil 1621: 1607: 1096: 1094: 1092: 1090: 1088: 1086: 1084: 1082: 1080: 1032: 590: 451: 2247:Efavirenz/lamivudine/tenofovir disoproxil 1232: 471: 2514:Zinc finger protein transcription factor 1284: 1264:Dolin R, Masur H, Saag MS, eds. (1999). 885: 1341:"F.D.A. Backs A New Drug To Fight AIDS" 1077: 586: 431: 93: 2695: 1392:Morbidity and Mortality Weekly Report, 1270:. Churchill Livingstone. p. 129. 1164:. John Wiley & Sons. p. 509. 1151: 1120: 976:a hard-gel capsule formulation of the 950: 945:enzyme that metabolizes the AIDS drugs 860: 111: 1602: 1338: 1126: 1108:from the original on 8 September 2015 972:Two formulations have been marketed: 960:As of 2015, it is not available as a 891: 827:Bioavailability and drug interactions 552: 511: 241: 128: 79: 2713:Drugs developed by Hoffmann-La Roche 1594:. U.S. National Library of Medicine. 1413:from the original on 9 November 2013 1320:from the original on 9 November 2013 757:to increase its effect. It is taken 558: 201: 2262:Emtricitabine/tenofovir alafenamide 1234:10.1097/01.aids.0000233573.41597.8a 1147:from the original on 31 March 2016. 1133:. Hoboken: CRC Press. p. 117. 491: 382: 13: 2277:Emtricitabine/tenofovir disoproxil 1511:Gibaud S, Attivi D (August 2012). 14: 2749: 1580: 1041:"Invirase® (Saquinavir mesilate)" 1014:"Saquinavir Use During Pregnancy" 228: 160: 2680: 2668: 2650:. Formerly or rarely used agent. 2287:Lamivudine/nevirapine/zidovudine 2171:Abacavir/dolutegravir/lamivudine 780:class and works by blocking the 625: 619: 38: 29: 2454:Epigallocatechin gallate (EGCG) 2297:Lamivudine/tenofovir disoproxil 2282:Lamivudine/nevirapine/stavudine 1554: 1520:Expert Opinion on Drug Delivery 1504: 1487:"Generic Invirase Availability" 1479: 1463:"Withdrawal of Fortovase (PDF)" 1455: 1425: 1398: 1384: 1358: 1332: 1192:. 22 March 2019. Archived from 1158:Fischer J, Ganellin CR (2006). 967: 810: 790: 712:Key:QWAXKHKRTORLEM-UGJKXSETSA-N 2177:Abacavir/lamivudine/zidovudine 1257: 1208: 1178: 1045:Australian Product Information 631: 613: 1: 1568:. 18 May 2005. Archived from 1161:Analogue-based Drug Discovery 999: 2718:Drugs developed by Genentech 1532:10.1517/17425247.2012.694865 1439:Food and Drug Administration 1339:Hilts PJ (8 December 1995). 955: 920:Food and Drug Administration 892:Cully M (28 November 2018). 799:. Typically it is used with 749:. Typically it is used with 737:, sold under the brand name 7: 2052:Tenofovir alafenamide (TAF) 984:to increase the saquinavir 10: 2754: 2047:Tenofovir disoproxil (TDF) 881: 603:Chemical and physical data 320:feces (81%) and urine (3%) 2607: 2522: 2416: 2398: 2380: 2362: 2343: 2336: 2315: 2156: 2103: 2077: 2068:Discovery and development 2060: 1943: 1931: 1894: 1848: 1839:Discovery and development 1831: 1803: 1753: 1675:Discovery and development 1667: 1649: 743:antiretroviral medication 720: 695: 675: 653: 640: 607: 602: 570: 542: 522: 502: 482: 462: 442: 422: 402: 377: 357: 329: 324: 314: 301: 288: 278: 264: 256: 218: 213: 188: 174: 148: 101: 87: 69: 61: 51: 46: 37: 28: 2364:Transcription inhibitors 2316:Pharmacokinetic boosters 2232:Dolutegravir/rilpivirine 2193:Cabotegravir/rilpivirine 1833:Protease Inhibitors (PI) 807:to increase its effect. 2728:HIV protease inhibitors 2648:initial regimen options 2214:Dolutegravir/lamivudine 1691:Enfuvirtide (ENF, T-20) 1669:Entry/fusion inhibitors 1592:Drug Information Portal 270:~4% (without ritonavir 2733:Decahydroisoquinolines 2489:Portmanteau inhibitors 2382:Translation inhibitors 2292:Lamivudine/raltegravir 2062:Non-nucleoside (NNRTI) 2020:Islatravir (EFdA, ISL) 911: 2504:Synergistic enhancers 2302:Lamivudine/zidovudine 2182:Atazanavir/cobicistat 2158:Combined formulations 1995:Zidovudine (AZT, ZDV) 1933:Reverse-transcriptase 1805:Maturation inhibitors 889: 878:and HIV-2 proteases. 2345:Uncoating inhibitors 2198:Darunavir/cobicistat 2038:Nucleotide analogues 1956:Nucleoside analogues 1755:Integrase inhibitors 1634:antiretroviral drugs 1572:on 22 February 2015. 741:among others, is an 2337:Experimental agents 2307:Lopinavir/ritonavir 2166:Abacavir/lamivudine 2140:Elsulfavirine (ESV) 1975:Emtricitabine (FTC) 1861:Fosamprenavir (FPV) 951:Society and culture 861:Mechanism of action 805:lopinavir/ritonavir 755:lopinavir/ritonavir 237:(Prescription only) 57:Invirase, Fortovase 25: 2634:Never to phase III 1780:Elvitegravir (EVG) 1775:Dolutegravir (DTG) 1770:Cabotegravir (CAB) 1443:. 24 December 1999 1372:. 26 November 2018 1065:. 26 December 2019 962:generic medication 912: 867:protease inhibitor 778:protease inhibitor 21: 2708:CYP3A4 inhibitors 2656: 2655: 2603: 2602: 2449:Diarylpyrimidines 2152: 2151: 2148: 2147: 2128:Rilpivirine (RPV) 2112:diarylpyrimidines 2095:Delavirdine (DLV) 1990:Zalcitabine (ddC) 1947:nucleotide (NRTI) 1927: 1926: 1785:Raltegravir (RAL) 1765:Bictegravir (BIC) 1744:Fostemsavir (FTR) 1659:Lenacapavir (LEN) 1651:Capsid inhibitors 1227:(10): 1401–1406. 1127:Minor LK (2006). 900:. Open Publishing 774:high blood lipids 732: 731: 666:Interactive image 572:CompTox Dashboard 294:Liver, mainly by 245: 232: 164: 131: 114: 16:Chemical compound 2745: 2685: 2684: 2673: 2672: 2671: 2664: 2474:Hydroxycarbamide 2341: 2340: 2135:Doravirine (DOR) 2123:Etravirine (ETR) 2118:Dapivirine (DPV) 2090:Nevirapine (NVP) 2075: 2074: 1980:Lamivudine (3TC) 1970:Didanosine (ddI) 1941: 1940: 1914:Tipranavir (TPV) 1902:Atazanavir (ATV) 1886:Saquinavir (SQV) 1876:Nelfinavir (NFV) 1856:Amprenavir (APV) 1846: 1845: 1728:Ibalizumab (IBA) 1623: 1616: 1609: 1600: 1599: 1595: 1574: 1573: 1566:News-Medical.Net 1558: 1552: 1551: 1517: 1508: 1502: 1501: 1499: 1497: 1483: 1477: 1476: 1474: 1468:. Archived from 1467: 1459: 1453: 1452: 1450: 1448: 1429: 1423: 1422: 1420: 1418: 1402: 1396: 1390:The CDC, in its 1388: 1382: 1381: 1379: 1377: 1362: 1356: 1355: 1353: 1351: 1336: 1330: 1329: 1327: 1325: 1293: 1282: 1281: 1261: 1255: 1254: 1236: 1212: 1206: 1205: 1203: 1201: 1196:on 28 April 2020 1182: 1176: 1175: 1155: 1149: 1148: 1124: 1118: 1117: 1115: 1113: 1098: 1075: 1074: 1072: 1070: 1055: 1049: 1048: 1036: 1030: 1029: 1027: 1025: 1010: 909: 907: 905: 865:Saquinavir is a 728: 727: 668: 648: 633: 627: 621: 615: 595: 594: 580: 578: 562: 556: 535: 515: 495: 475: 455: 435: 415: 395: 385: 384: 370: 306: 243: 240: 230: 227: 205: 162: 159: 141: 130: 127: 124: 113: 110: 97: 83: 42: 33: 26: 24: 20: 2753: 2752: 2748: 2747: 2746: 2744: 2743: 2742: 2693: 2692: 2691: 2679: 2669: 2667: 2659: 2657: 2652: 2651: 2639: 2624:Clinical trials 2599: 2550:Dexelvucitabine 2518: 2509:Tre recombinase 2412: 2394: 2376: 2372:Tat antagonists 2358: 2332: 2311: 2144: 2099: 2085:Efavirenz (EFV) 2064: 2056: 1985:Stavudine (d4T) 1946: 1934: 1923: 1908:Darunavir (DRV) 1890: 1881:Ritonavir (RTV) 1871:Lopinavir (LPV) 1866:Indinavir (IDV) 1835: 1827: 1799: 1757: 1749: 1703:Maraviroc (MVC) 1671: 1663: 1645: 1630:Antiviral drugs 1627: 1586: 1583: 1578: 1577: 1560: 1559: 1555: 1515: 1509: 1505: 1495: 1493: 1485: 1484: 1480: 1475:on 14 May 2006. 1472: 1465: 1461: 1460: 1456: 1446: 1444: 1431: 1430: 1426: 1416: 1414: 1403: 1399: 1389: 1385: 1375: 1373: 1364: 1363: 1359: 1349: 1347: 1337: 1333: 1323: 1321: 1308:(21): 689–693. 1294: 1285: 1278: 1262: 1258: 1213: 1209: 1199: 1197: 1184: 1183: 1179: 1172: 1156: 1152: 1141: 1125: 1121: 1111: 1109: 1100: 1099: 1078: 1068: 1066: 1057: 1056: 1052: 1037: 1033: 1023: 1021: 1020:. 20 March 2018 1012: 1011: 1007: 1002: 986:bioavailability 970: 958: 953: 937:bioavailability 922:(FDA), leading 903: 901: 898:Nature Research 884: 863: 844:cytochrome P450 829: 813: 793: 766:QT prolongation 723: 721: 716: 713: 708: 703: 702: 691: 688: 683: 682: 671: 646: 636: 630: 624: 618: 598: 574: 566: 538: 518: 498: 478: 458: 438: 418: 398: 381: 373: 353: 350: 337: 336: 304: 280:Protein binding 266:Bioavailability 258:Pharmacokinetic 252: 209: 177: 170: 151: 144: 17: 12: 11: 5: 2751: 2741: 2740: 2735: 2730: 2725: 2720: 2715: 2710: 2705: 2690: 2689: 2677: 2654: 2653: 2638: 2637: 2636: 2635: 2632: 2621: 2615: 2609: 2608: 2605: 2604: 2601: 2600: 2598: 2597: 2592: 2587: 2582: 2577: 2572: 2567: 2562: 2557: 2552: 2547: 2542: 2537: 2532: 2526: 2524: 2520: 2519: 2517: 2516: 2511: 2506: 2501: 2496: 2491: 2486: 2481: 2476: 2471: 2466: 2461: 2456: 2451: 2446: 2441: 2436: 2431: 2426: 2420: 2418: 2414: 2413: 2411: 2410: 2404: 2402: 2396: 2395: 2393: 2392: 2386: 2384: 2378: 2377: 2375: 2374: 2368: 2366: 2360: 2359: 2357: 2356: 2349: 2347: 2338: 2334: 2333: 2331: 2330: 2325: 2323:Cobicistat (c) 2319: 2317: 2313: 2312: 2310: 2309: 2304: 2299: 2294: 2289: 2284: 2279: 2274: 2269: 2264: 2259: 2254: 2249: 2244: 2239: 2234: 2229: 2223: 2217: 2211: 2206: 2200: 2195: 2190: 2184: 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35: 34: 15: 9: 6: 4: 3: 2: 2750: 2739: 2736: 2734: 2731: 2729: 2726: 2724: 2721: 2719: 2716: 2714: 2711: 2709: 2706: 2704: 2701: 2700: 2698: 2688: 2683: 2678: 2676: 2666: 2665: 2662: 2649: 2646: 2643: 2633: 2631: 2628: 2627: 2625: 2622: 2619: 2616: 2614: 2611: 2610: 2606: 2596: 2593: 2591: 2588: 2586: 2583: 2581: 2578: 2576: 2573: 2571: 2568: 2566: 2563: 2561: 2558: 2556: 2553: 2551: 2548: 2546: 2543: 2541: 2538: 2536: 2533: 2531: 2528: 2527: 2525: 2523:Failed agents 2521: 2515: 2512: 2510: 2507: 2505: 2502: 2500: 2497: 2495: 2492: 2490: 2487: 2485: 2482: 2480: 2477: 2475: 2472: 2470: 2467: 2465: 2462: 2460: 2457: 2455: 2452: 2450: 2447: 2445: 2442: 2440: 2437: 2435: 2432: 2430: 2427: 2425: 2422: 2421: 2419: 2415: 2409: 2406: 2405: 2403: 2401: 2397: 2391: 2390:Trichosanthin 2388: 2387: 2385: 2383: 2379: 2373: 2370: 2369: 2367: 2365: 2361: 2354: 2351: 2350: 2348: 2346: 2342: 2339: 2335: 2329: 2328:Ritonavir (r) 2326: 2324: 2321: 2320: 2318: 2314: 2308: 2305: 2303: 2300: 2298: 2295: 2293: 2290: 2288: 2285: 2283: 2280: 2278: 2275: 2273: 2270: 2268: 2265: 2263: 2260: 2258: 2255: 2253: 2250: 2248: 2245: 2243: 2240: 2238: 2235: 2233: 2230: 2227: 2224: 2221: 2218: 2215: 2212: 2210: 2207: 2204: 2201: 2199: 2196: 2194: 2191: 2188: 2185: 2183: 2180: 2178: 2175: 2172: 2169: 2167: 2164: 2163: 2161: 2159: 2155: 2141: 2138: 2136: 2133: 2129: 2126: 2124: 2121: 2119: 2116: 2115: 2114: 2113: 2109: 2108: 2106: 2102: 2096: 2093: 2091: 2088: 2086: 2083: 2082: 2080: 2076: 2073: 2071: 2069: 2063: 2059: 2053: 2050: 2048: 2045: 2043: 2039: 2035: 2034: 2031: 2028: 2026: 2023: 2021: 2018: 2016: 2013: 2011: 2008: 2006: 2003: 2001: 1998: 1996: 1993: 1991: 1988: 1986: 1983: 1981: 1978: 1976: 1973: 1971: 1968: 1966: 1963: 1961: 1957: 1953: 1952: 1950: 1948: 1942: 1939: 1936: 1930: 1920: 1917: 1915: 1912: 1909: 1906: 1903: 1900: 1899: 1897: 1893: 1887: 1884: 1882: 1879: 1877: 1874: 1872: 1869: 1867: 1864: 1862: 1859: 1857: 1854: 1853: 1851: 1847: 1844: 1842: 1840: 1834: 1830: 1824: 1821: 1819: 1816: 1814: 1811: 1810: 1808: 1806: 1802: 1796: 1793: 1791: 1788: 1786: 1783: 1781: 1778: 1776: 1773: 1771: 1768: 1766: 1763: 1762: 1760: 1756: 1752: 1745: 1741: 1740: 1736: 1733: 1729: 1725: 1724: 1720: 1717: 1713: 1709: 1706: 1704: 1700: 1699: 1695: 1692: 1688: 1687: 1683: 1682: 1680: 1678: 1676: 1670: 1666: 1660: 1657: 1656: 1654: 1652: 1648: 1643: 1639: 1636:used against 1635: 1631: 1624: 1619: 1617: 1612: 1610: 1605: 1604: 1601: 1593: 1589: 1585: 1584: 1571: 1567: 1563: 1557: 1549: 1545: 1541: 1537: 1533: 1529: 1525: 1521: 1514: 1507: 1492: 1488: 1482: 1471: 1464: 1458: 1442: 1440: 1434: 1428: 1412: 1408: 1401: 1393: 1387: 1371: 1367: 1361: 1346: 1342: 1335: 1319: 1315: 1311: 1307: 1303: 1299: 1292: 1290: 1288: 1279: 1277:9780443075926 1273: 1269: 1268: 1260: 1252: 1248: 1244: 1240: 1235: 1230: 1226: 1222: 1218: 1211: 1195: 1191: 1187: 1181: 1173: 1171:9783527607495 1167: 1163: 1162: 1154: 1146: 1142: 1140:9781420015706 1136: 1132: 1131: 1123: 1107: 1103: 1097: 1095: 1093: 1091: 1089: 1087: 1085: 1083: 1081: 1064: 1060: 1054: 1046: 1042: 1035: 1019: 1015: 1009: 1005: 994: 993:microemulsion 990: 987: 983: 979: 975: 974: 973: 965: 963: 948: 946: 942: 938: 932: 929: 925: 921: 917: 899: 895: 888: 879: 877: 872: 868: 858: 856: 851: 848: 845: 840: 838: 833: 824: 822: 818: 808: 806: 802: 798: 788: 785: 783: 779: 775: 771: 767: 762: 760: 756: 752: 748: 744: 740: 736: 726: 719: 710: 705: 704: 701: 694: 685: 684: 681: 674: 667: 663: 662: 660: 657: 652: 645: 643: 639: 612: 610: 606: 601: 593: 589: 588:DTXSID6044012 585: 584: 582: 573: 569: 561: 560:RCSB PDB 555: 550: 549: 547: 545: 541: 534: 530: 529: 527: 525: 521: 514: 510: 509: 507: 505: 501: 494: 490: 489: 487: 485: 481: 474: 470: 469: 467: 465: 461: 454: 450: 449: 447: 445: 441: 434: 430: 429: 427: 425: 421: 414: 410: 409: 407: 405: 401: 394: 390: 389: 387: 380: 376: 369: 365: 364: 362: 360: 356: 348: 344: 339: 338: 335: 328: 323: 319: 317: 313: 309: 307: 300: 297: 293: 291: 287: 283: 281: 277: 273: 269: 267: 263: 259: 255: 249: 239: 236: 226: 225: 223: 221: 217: 212: 204: 199: 196: 195: 193: 191: 187: 184: 181: 179: 173: 167: 158: 157: 155: 153: 147: 140: 135: 126: 123: 118: 109: 108: 106: 104: 100: 96: 92: 90: 86: 82: 78: 76: 72: 68: 64: 60: 56: 54: 50: 47:Clinical data 45: 41: 36: 32: 27: 19: 2723:Hepatotoxins 2703:Carboxamides 2644: 2444:Cyanovirin-N 2434:Calanolide A 2110: 2104:2 generation 2078:1 generation 2065: 2036: 2015:Elvucitabine 2005:Apricitabine 1954: 1895:2 generation 1885: 1849:1 generation 1836: 1823:Fipravirimat 1737: 1732:Semzuvolimab 1721: 1712:Cenicriviroc 1696: 1684: 1672: 1591: 1588:"Saquinavir" 1570:the original 1565: 1556: 1523: 1519: 1506: 1494:. Retrieved 1490: 1481: 1470:the original 1457: 1445:. Retrieved 1436: 1427: 1415:. Retrieved 1409:. The Body. 1400: 1391: 1386: 1374:. Retrieved 1369: 1360: 1348:. Retrieved 1344: 1334: 1322:. Retrieved 1305: 1301: 1267:AIDS Therapy 1266: 1259: 1224: 1220: 1210: 1198:. Retrieved 1194:the original 1189: 1180: 1160: 1153: 1129: 1122: 1110:. Retrieved 1102:"Saquinavir" 1067:. Retrieved 1062: 1053: 1044: 1034: 1022:. Retrieved 1017: 1008: 971: 968:Formulations 959: 933: 913: 902:. Retrieved 897: 864: 852: 841: 834: 830: 814: 811:Side effects 794: 791:Medical uses 786: 782:HIV protease 763: 738: 734: 733: 722:   524:NIAID ChemDB 346: 342: 303:Elimination 220:Legal status 214:Legal status 103:License data 18: 2645:recommended 2620:from market 2570:Lersivirine 2545:Capravirine 2484:Miltefosine 2469:Griffithsin 2464:Fosdevirine 2010:Censavudine 1640:(primarily 1417:20 February 1395:inhibitors. 1186:"Fortovase" 1112:5 September 770:heart block 649: g·mol 368:127779-20-8 325:Identifiers 89:MedlinePlus 62:Other names 53:Trade names 2738:Quinolines 2697:Categories 2575:Lodenosine 2555:Droxinavir 2540:Brecanavir 2535:Atevirdine 2499:Seliciclib 2494:Scytovirin 2408:Elipovimab 2353:TRIM5alpha 2030:Stampidine 1935:inhibitors 1919:TMC-310911 1818:BMS-955176 1716:Leronlimab 1708:Vicriviroc 1447:28 January 1376:29 October 1350:28 October 1324:8 November 1200:28 January 1069:28 January 1024:28 January 1000:References 904:28 October 855:omeprazole 735:Saquinavir 654:3D model ( 642:Molar mass 544:PDB ligand 473:L3JE09KZ2F 444:ChemSpider 404:IUPHAR/BPS 359:CAS Number 334:IUPAC name 310:9–15 hours 290:Metabolism 139:Saquinavir 23:Saquinavir 2630:Phase III 2618:Withdrawn 2595:Telinavir 2590:Palinavir 2585:Mozenavir 2565:Emivirine 2560:Lasinavir 2530:Aplaviroc 2459:Foscarnet 2439:Ceragenin 2000:Amdoxovir 1813:Bevirimat 1790:BI 224436 1491:Drugs.com 1190:Drugs.com 1018:Drugs.com 982:ritonavir 956:Economics 941:ritonavir 928:indinavir 924:ritonavir 871:Proteases 837:ritonavir 817:diarrhoea 801:ritonavir 751:ritonavir 513:ChEMBL114 316:Excretion 305:half-life 176:Routes of 150:Pregnancy 81:Monograph 75:Drugs.com 2675:Medicine 2580:Loviride 1548:28468973 1540:22663249 1411:Archived 1318:Archived 1314:21637182 1251:44506039 1243:16791014 1145:Archived 1106:Archived 1063:DailyMed 978:mesylate 797:HIV/AIDS 759:by mouth 747:HIV/AIDS 739:Invirase 725:(verify) 424:DrugBank 272:boosting 190:ATC code 183:By mouth 165: B1 152:category 134:DailyMed 2687:Viruses 2661:Portals 2479:KP-1461 2025:Racivir 1795:MK-2048 882:History 647:670.855 609:Formula 433:DB01232 379:PubChem 206:) 200: ( 198:J05AE01 136::  119::  95:a696001 2613:WHO-EM 2429:BIT225 2424:Abzyme 2355:(gene) 2042:NtRTIs 1937:(RTIs) 1546:  1538:  1496:9 July 1312:  1274:  1249:  1241:  1168:  1137:  821:nausea 680:SMILES 533:000640 504:ChEMBL 493:D00429 453:390016 393:441243 296:CYP3A4 248:â„ž-only 246: 233: 132:  122:by INN 115:  2417:Other 2400:BNAbs 1960:NRTIs 1739:gp120 1544:S2CID 1516:(PDF) 1473:(PDF) 1466:(PDF) 1441:(FDA) 1437:U.S. 1247:S2CID 916:Roche 876:HIV-1 700:InChI 656:JSmol 551:ROC ( 2642:DHHS 1698:CCR5 1686:gp41 1536:PMID 1498:2020 1449:2020 1419:2013 1378:2020 1352:2020 1326:2013 1310:PMID 1272:ISBN 1239:PMID 1221:AIDS 1202:2020 1166:ISBN 1135:ISBN 1114:2015 1071:2020 1026:2020 926:and 906:2020 554:PDBe 484:KEGG 464:UNII 413:4813 260:data 71:AHFS 1723:CD4 1642:J05 1638:HIV 1528:doi 1370:NIH 1229:doi 847:3A4 803:or 753:or 577:EPA 383:CID 284:98% 203:WHO 117:EMA 65:SQV 2699:: 2626:: 1730:, 1714:, 1710:, 1632:: 1590:. 1564:. 1542:. 1534:. 1522:. 1518:. 1489:. 1435:. 1368:. 1343:. 1316:. 1306:60 1304:. 1300:. 1286:^ 1245:. 1237:. 1225:20 1223:. 1219:. 1188:. 1143:. 1079:^ 1061:. 1043:. 1016:. 964:. 947:. 896:. 869:. 857:. 819:, 784:. 772:, 768:, 761:. 623:50 617:38 557:, 345:)- 341:(2 242:US 235:S4 229:AU 161:AU 129:US 112:EU 2663:: 2640:° 2228:° 2222:° 2216:° 2205:° 2189:° 2173:° 2070:) 2066:( 2044:: 2040:/ 1962:: 1958:/ 1910:° 1904:° 1841:) 1837:( 1746:) 1742:( 1734:) 1726:( 1718:) 1701:( 1693:) 1689:( 1677:) 1673:( 1644:) 1622:e 1615:t 1608:v 1550:. 1530:: 1524:9 1500:. 1451:. 1421:. 1380:. 1354:. 1328:. 1280:. 1253:. 1231:: 1204:. 1174:. 1116:. 1073:. 1028:. 988:; 908:. 658:) 635:5 632:O 629:6 626:N 620:H 614:C 579:) 575:( 563:) 347:N 343:S 274:) 244:: 231:: 163:: 73:/

Index



Trade names
AHFS
Drugs.com
Monograph
MedlinePlus
a696001
License data
EMA
by INN
DailyMed
Saquinavir
Pregnancy
category

Routes of
administration

By mouth
ATC code
J05AE01
WHO
Legal status
S4
â„ž-only
Pharmacokinetic
Bioavailability
boosting
Protein binding
Metabolism
CYP3A4
Elimination half-life
Excretion

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