Knowledge

Saquinavir

Source đź“ť

898: 603: 51: 42: 2693: 2681: 945:
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
941:
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
718:
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
884:
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,
676: 860:
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.
842:
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.
1405:
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
2078: 901:
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.
2052: 850:. For patients, this has the major benefit that they can take less saquinavir, while maintaining sufficient saquinavir blood plasma levels to efficiently suppress the replication of HIV. 1970: 245: 904: 2072: 2262: 2267: 2213: 1685: 2652: 200: 1849: 846:
In the clinic, it was found that the oral bioavailability of saquinavir in both formulations significantly increases when patients also receive the PI
132: 2219: 2277: 2197: 950:. Roche announced in May 2005 that, given reduced demand, Fortovase would cease being marketed early in 2006, in favor of Invirase boosted with 2282: 2723: 2230: 1631: 81: 2252: 2236: 690: 2605: 2600: 1155: 2247: 1276: 2257: 1473: 1572: 1228:"Effect of omeprazole on the pharmacokinetics of saquinavir-500 mg formulation with ritonavir in healthy male and female volunteers" 2524: 1328: 2168: 1069: 853:
The mechanism behind this welcome observation was not directly known, but later it was determined that ritonavir inhibits the
2728: 2623: 2514: 1116: 775:
Common side effects include nausea, vomiting, diarrhea, and feeling tired. More serious side effects include problems with
1421: 2272: 1609: 1523: 2287: 1196: 826:
The most frequent adverse events with saquinavir in either formulation are mild gastrointestinal symptoms, including
735: 149: 1843: 1624: 1286: 1180: 1149: 877: 788: 710: 2738: 2640: 2297: 2181: 2743: 2307: 2292: 1955: 1943: 1443: 946:
new drugs. It was approved again on November 7, 1997, as Fortovase, a soft gel capsule reformulated for improved
344: 230: 113: 1376: 1351: 2187: 423: 1617: 1449: 930: 474: 2392: 582: 1006:, orally-administered formulation), with trade name Fortovase, which was discontinued worldwide in 2006. 2718: 2671: 523: 1051: 921:
As a result of the new therapies, HIV deaths in the United States fell dramatically within two years.
753: 127: 2464: 2374: 2355: 2242: 2203: 598: 17: 543: 2628: 2224: 854: 186: 63: 2302: 564: 290: 2410: 1226:
Winston A, Back D, Fletcher C, Robinson L, Unsworth J, Tolowinska I, et al. (June 2006).
1170: 1139: 929:. Saquinavir was the sixth antiretroviral and the first protease inhibitor approved by the US 2733: 2713: 2499: 2312: 2192: 2062: 1661: 414: 463: 378: 2382: 2208: 2057: 1815: 1497: 483: 313: 1639: 1598: 1480: 897: 8: 2748: 2317: 2176: 2048: 1966: 1765: 1644: 1580: 1308: 1070:"Invirase- saquinavir mesylate capsule INVIRASE- saquinavir mesylate tablet, film coated" 815: 765: 369: 282: 1244: 1227: 602: 1554: 1257: 972: 864:
Unlike other protease inhibitors, the absorption of saquinavir seems to be improved by
160: 834:, loose stools and abdominal discomfort. Invirase is better tolerated than Fortovase. 2459: 2122: 1546: 1320: 1282: 1249: 1176: 1145: 926: 554: 258: 105: 1558: 1261: 2484: 1538: 1239: 619: 403: 268: 213: 2658: 1112: 1024: 91: 2685: 2560: 2519: 1679: 1542: 996: 947: 886: 776: 300: 276: 1306: 2697: 2634: 1640: 1417: 784: 698:
O=C(N)C(NC(=O)c1nc2c(cc1)cccc2)C(=O)N(Cc3ccccc3)(O)CN5(C(=O)NC(C)(C)C)C4CCCC4C5
2707: 2400: 2150: 1985: 1871: 1003: 50: 2454: 2444: 2025: 2015: 1833: 1790: 1785: 1780: 1742: 1722: 1652: 1550: 1524:"Microemulsions for oral administration and their therapeutic applications" 1324: 1253: 1204: 792: 534: 208: 33: 1573:"Roche to discontinue the sale and distribution of Fortovase (saquinavir)" 2580: 2555: 2494: 2479: 2474: 2138: 2105: 2020: 2000: 1795: 1775: 1754: 1701: 1669: 1415: 780: 99: 443: 2585: 2565: 2550: 2545: 2509: 2504: 2418: 2363: 2333: 2145: 2133: 2128: 2100: 2040: 2030: 2005: 1990: 1980: 1929: 1924: 1912: 1886: 1866: 1828: 1738: 1726: 1718: 1418:"Drugs! Drugs! Drugs! An Overview of the Approved Anti-HIV Medications" 954:, owing to the ability of the latter co-formulated drug to inhibit the 865: 806:
Saquinavir is used together with other medications to treat or prevent
787:, and liver problems. It appears to be safe in pregnancy. It is in the 652: 454: 360:--3-hydroxy-1-phenylbutan-2-yl]-2-(quinolin-2-ylformamido)butanediamide 41: 2595: 2575: 2570: 2540: 2469: 2449: 2338: 2095: 2010: 1995: 1918: 1891: 1881: 1876: 1823: 1800: 1713: 992: 951: 938: 934: 847: 827: 811: 761: 389: 326: 85: 2590: 1975: 988: 881: 807: 769: 757: 503: 434: 193: 144: 675: 570: 2489: 2035: 1805: 1307:
Centers for Disease Control and Prevention (CDC) (3 June 2011).
2439: 2434: 955: 857: 831: 514: 306: 131: 1749: 885:
preventing maturation of the virus. Saquinavir inhibits both
666: 2692: 991:, with trade name Invirase, which requires combination with 587: 2263:
Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
1708: 1696: 1225: 494: 2268:
Elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil
1049: 1733: 1648: 756:
used together with other medications to treat or prevent
2214:
Darunavir/cobicistat/emtricitabine/tenofovir alafenamide
837: 798:
Saquinavir was patented in 1988 and first sold in 1995.
1444:"Drug Approval Package: Fortovase/Saquinavir NDA 20828" 925:
Saquinavir was developed by the pharmaceutical company
905:"Protease inhibitors give wings to combination therapy" 2669: 1115:. The American Society of Health-System Pharmacists. 942:50,000 to about 18,000 over a period of two years. 422: 1017: 2705: 2220:Dolutegravir/emtricitabine/tenofovir alafenamide 402: 2278:Emtricitabine/rilpivirine/tenofovir alafenamide 2198:Bictegravir/emtricitabine/tenofovir alafenamide 1416:AIDS Community Research Initiative of America. 1377:"Antiretroviral Drug Discovery and Development" 1168: 1141:Handbook of Assay Development in Drug Discovery 377: 2283:Emtricitabine/rilpivirine/tenofovir disoproxil 1769:(Integrase strand transfer inhibitors (INSTI)) 1274: 1050:Roche Products Pty Limited (6 November 2018). 1002:a soft-gel capsule formulation of saquinavir ( 2231:Dolutegravir/lamivudine/tenofovir alafenamide 1625: 1062: 1058:– via MedAdvisor International Pty Ltd. 2253:Efavirenz/emtricitabine/tenofovir disoproxil 2237:Dolutegravir/lamivudine/tenofovir disoproxil 1521: 1313:Morbidity and Mortality Weekly Report (MMWR) 542: 148: 1309:"HIV Surveillance—United States, 1981-2008" 1302: 1300: 1298: 2248:Doravirine/lamivudine/tenofovir disoproxil 1632: 1618: 1107: 1105: 1103: 1101: 1099: 1097: 1095: 1093: 1091: 1043: 601: 462: 2258:Efavirenz/lamivudine/tenofovir disoproxil 1243: 482: 2525:Zinc finger protein transcription factor 1295: 1275:Dolin R, Masur H, Saag MS, eds. (1999). 896: 1352:"F.D.A. Backs A New Drug To Fight AIDS" 1088: 597: 442: 104: 14: 2706: 1403:Morbidity and Mortality Weekly Report, 1281:. Churchill Livingstone. p. 129. 1175:. John Wiley & Sons. p. 509. 1162: 1131: 987:a hard-gel capsule formulation of the 961: 956:enzyme that metabolizes the AIDS drugs 871: 122: 1613: 1349: 1137: 1119:from the original on 8 September 2015 983:Two formulations have been marketed: 971:As of 2015, it is not available as a 902: 838:Bioavailability and drug interactions 563: 522: 252: 139: 90: 2724:Drugs developed by Hoffmann-La Roche 1605:. U.S. National Library of Medicine. 1424:from the original on 9 November 2013 1331:from the original on 9 November 2013 768:to increase its effect. It is taken 569: 212: 2273:Emtricitabine/tenofovir alafenamide 1245:10.1097/01.aids.0000233573.41597.8a 1158:from the original on 31 March 2016. 1144:. Hoboken: CRC Press. p. 117. 502: 393: 24: 2288:Emtricitabine/tenofovir disoproxil 1522:Gibaud S, Attivi D (August 2012). 25: 2760: 1591: 1052:"Invirase® (Saquinavir mesilate)" 1025:"Saquinavir Use During Pregnancy" 239: 171: 2691: 2679: 2661:. Formerly or rarely used agent. 2298:Lamivudine/nevirapine/zidovudine 2182:Abacavir/dolutegravir/lamivudine 791:class and works by blocking the 636: 630: 49: 40: 2465:Epigallocatechin gallate (EGCG) 2308:Lamivudine/tenofovir disoproxil 2293:Lamivudine/nevirapine/stavudine 1565: 1531:Expert Opinion on Drug Delivery 1515: 1498:"Generic Invirase Availability" 1490: 1474:"Withdrawal of Fortovase (PDF)" 1466: 1436: 1409: 1395: 1369: 1343: 1203:. 22 March 2019. Archived from 1169:Fischer J, Ganellin CR (2006). 978: 821: 801: 723:Key:QWAXKHKRTORLEM-UGJKXSETSA-N 2188:Abacavir/lamivudine/zidovudine 1268: 1219: 1189: 1056:Australian Product Information 642: 624: 13: 1: 1579:. 18 May 2005. Archived from 1172:Analogue-based Drug Discovery 1010: 2729:Drugs developed by Genentech 1543:10.1517/17425247.2012.694865 1450:Food and Drug Administration 1350:Hilts PJ (8 December 1995). 966: 931:Food and Drug Administration 903:Cully M (28 November 2018). 810:. Typically it is used with 760:. Typically it is used with 748:, sold under the brand name 7: 2063:Tenofovir alafenamide (TAF) 995:to increase the saquinavir 10: 2765: 2058:Tenofovir disoproxil (TDF) 892: 614:Chemical and physical data 331:feces (81%) and urine (3%) 2618: 2533: 2427: 2409: 2391: 2373: 2354: 2347: 2326: 2167: 2114: 2088: 2079:Discovery and development 2071: 1954: 1942: 1905: 1859: 1850:Discovery and development 1842: 1814: 1764: 1686:Discovery and development 1678: 1660: 754:antiretroviral medication 731: 706: 686: 664: 651: 618: 613: 581: 553: 533: 513: 493: 473: 453: 433: 413: 388: 368: 340: 335: 325: 312: 299: 289: 275: 267: 229: 224: 199: 185: 159: 112: 98: 80: 72: 62: 57: 48: 39: 2375:Transcription inhibitors 2327:Pharmacokinetic boosters 2243:Dolutegravir/rilpivirine 2204:Cabotegravir/rilpivirine 1844:Protease Inhibitors (PI) 818:to increase its effect. 2739:HIV protease inhibitors 2659:initial regimen options 2225:Dolutegravir/lamivudine 1702:Enfuvirtide (ENF, T-20) 1680:Entry/fusion inhibitors 1603:Drug Information Portal 281:~4% (without ritonavir 2744:Decahydroisoquinolines 2500:Portmanteau inhibitors 2393:Translation inhibitors 2303:Lamivudine/raltegravir 2073:Non-nucleoside (NNRTI) 2031:Islatravir (EFdA, ISL) 922: 2515:Synergistic enhancers 2313:Lamivudine/zidovudine 2193:Atazanavir/cobicistat 2169:Combined formulations 2006:Zidovudine (AZT, ZDV) 1944:Reverse-transcriptase 1816:Maturation inhibitors 900: 889:and HIV-2 proteases. 2356:Uncoating inhibitors 2209:Darunavir/cobicistat 2049:Nucleotide analogues 1967:Nucleoside analogues 1766:Integrase inhibitors 1645:antiretroviral drugs 1583:on 22 February 2015. 752:among others, is an 2348:Experimental agents 2318:Lopinavir/ritonavir 2177:Abacavir/lamivudine 2151:Elsulfavirine (ESV) 1986:Emtricitabine (FTC) 1872:Fosamprenavir (FPV) 962:Society and culture 872:Mechanism of action 816:lopinavir/ritonavir 766:lopinavir/ritonavir 248:(Prescription only) 68:Invirase, Fortovase 36: 2645:Never to phase III 1791:Elvitegravir (EVG) 1786:Dolutegravir (DTG) 1781:Cabotegravir (CAB) 1454:. 24 December 1999 1383:. 26 November 2018 1076:. 26 December 2019 973:generic medication 923: 878:protease inhibitor 789:protease inhibitor 32: 2719:CYP3A4 inhibitors 2667: 2666: 2614: 2613: 2460:Diarylpyrimidines 2163: 2162: 2159: 2158: 2139:Rilpivirine (RPV) 2123:diarylpyrimidines 2106:Delavirdine (DLV) 2001:Zalcitabine (ddC) 1958:nucleotide (NRTI) 1938: 1937: 1796:Raltegravir (RAL) 1776:Bictegravir (BIC) 1755:Fostemsavir (FTR) 1670:Lenacapavir (LEN) 1662:Capsid inhibitors 1238:(10): 1401–1406. 1138:Minor LK (2006). 911:. Open Publishing 785:high blood lipids 743: 742: 677:Interactive image 583:CompTox Dashboard 305:Liver, mainly by 256: 243: 175: 142: 125: 27:Chemical compound 16:(Redirected from 2756: 2696: 2695: 2684: 2683: 2682: 2675: 2485:Hydroxycarbamide 2352: 2351: 2146:Doravirine (DOR) 2134:Etravirine (ETR) 2129:Dapivirine (DPV) 2101:Nevirapine (NVP) 2086: 2085: 1991:Lamivudine (3TC) 1981:Didanosine (ddI) 1952: 1951: 1925:Tipranavir (TPV) 1913:Atazanavir (ATV) 1897:Saquinavir (SQV) 1887:Nelfinavir (NFV) 1867:Amprenavir (APV) 1857: 1856: 1739:Ibalizumab (IBA) 1634: 1627: 1620: 1611: 1610: 1606: 1585: 1584: 1577:News-Medical.Net 1569: 1563: 1562: 1528: 1519: 1513: 1512: 1510: 1508: 1494: 1488: 1487: 1485: 1479:. Archived from 1478: 1470: 1464: 1463: 1461: 1459: 1440: 1434: 1433: 1431: 1429: 1413: 1407: 1401:The CDC, in its 1399: 1393: 1392: 1390: 1388: 1373: 1367: 1366: 1364: 1362: 1347: 1341: 1340: 1338: 1336: 1304: 1293: 1292: 1272: 1266: 1265: 1247: 1223: 1217: 1216: 1214: 1212: 1207:on 28 April 2020 1193: 1187: 1186: 1166: 1160: 1159: 1135: 1129: 1128: 1126: 1124: 1109: 1086: 1085: 1083: 1081: 1066: 1060: 1059: 1047: 1041: 1040: 1038: 1036: 1021: 920: 918: 916: 876:Saquinavir is a 739: 738: 679: 659: 644: 638: 632: 626: 606: 605: 591: 589: 573: 567: 546: 526: 506: 486: 466: 446: 426: 406: 396: 395: 381: 317: 254: 251: 241: 238: 216: 173: 170: 152: 141: 138: 135: 124: 121: 108: 94: 53: 44: 37: 35: 31: 21: 2764: 2763: 2759: 2758: 2757: 2755: 2754: 2753: 2704: 2703: 2702: 2690: 2680: 2678: 2670: 2668: 2663: 2662: 2650: 2635:Clinical trials 2610: 2561:Dexelvucitabine 2529: 2520:Tre recombinase 2423: 2405: 2387: 2383:Tat antagonists 2369: 2343: 2322: 2155: 2110: 2096:Efavirenz (EFV) 2075: 2067: 1996:Stavudine (d4T) 1957: 1945: 1934: 1919:Darunavir (DRV) 1901: 1892:Ritonavir (RTV) 1882:Lopinavir (LPV) 1877:Indinavir (IDV) 1846: 1838: 1810: 1768: 1760: 1714:Maraviroc (MVC) 1682: 1674: 1656: 1641:Antiviral drugs 1638: 1597: 1594: 1589: 1588: 1571: 1570: 1566: 1526: 1520: 1516: 1506: 1504: 1496: 1495: 1491: 1486:on 14 May 2006. 1483: 1476: 1472: 1471: 1467: 1457: 1455: 1442: 1441: 1437: 1427: 1425: 1414: 1410: 1400: 1396: 1386: 1384: 1375: 1374: 1370: 1360: 1358: 1348: 1344: 1334: 1332: 1319:(21): 689–693. 1305: 1296: 1289: 1273: 1269: 1224: 1220: 1210: 1208: 1195: 1194: 1190: 1183: 1167: 1163: 1152: 1136: 1132: 1122: 1120: 1111: 1110: 1089: 1079: 1077: 1068: 1067: 1063: 1048: 1044: 1034: 1032: 1031:. 20 March 2018 1023: 1022: 1018: 1013: 997:bioavailability 981: 969: 964: 948:bioavailability 933:(FDA), leading 914: 912: 909:Nature Research 895: 874: 855:cytochrome P450 840: 824: 804: 777:QT prolongation 734: 732: 727: 724: 719: 714: 713: 702: 699: 694: 693: 682: 657: 647: 641: 635: 629: 609: 585: 577: 549: 529: 509: 489: 469: 449: 429: 409: 392: 384: 364: 361: 348: 347: 315: 291:Protein binding 277:Bioavailability 269:Pharmacokinetic 263: 220: 188: 181: 162: 155: 28: 23: 22: 15: 12: 11: 5: 2762: 2752: 2751: 2746: 2741: 2736: 2731: 2726: 2721: 2716: 2701: 2700: 2688: 2665: 2664: 2649: 2648: 2647: 2646: 2643: 2632: 2626: 2620: 2619: 2616: 2615: 2612: 2611: 2609: 2608: 2603: 2598: 2593: 2588: 2583: 2578: 2573: 2568: 2563: 2558: 2553: 2548: 2543: 2537: 2535: 2531: 2530: 2528: 2527: 2522: 2517: 2512: 2507: 2502: 2497: 2492: 2487: 2482: 2477: 2472: 2467: 2462: 2457: 2452: 2447: 2442: 2437: 2431: 2429: 2425: 2424: 2422: 2421: 2415: 2413: 2407: 2406: 2404: 2403: 2397: 2395: 2389: 2388: 2386: 2385: 2379: 2377: 2371: 2370: 2368: 2367: 2360: 2358: 2349: 2345: 2344: 2342: 2341: 2336: 2334:Cobicistat (c) 2330: 2328: 2324: 2323: 2321: 2320: 2315: 2310: 2305: 2300: 2295: 2290: 2285: 2280: 2275: 2270: 2265: 2260: 2255: 2250: 2245: 2240: 2234: 2228: 2222: 2217: 2211: 2206: 2201: 2195: 2190: 2185: 2179: 2173: 2171: 2165: 2164: 2161: 2160: 2157: 2156: 2154: 2153: 2148: 2143: 2142: 2141: 2136: 2131: 2118: 2116: 2112: 2111: 2109: 2108: 2103: 2098: 2092: 2090: 2083: 2069: 2068: 2066: 2065: 2060: 2044: 2043: 2038: 2033: 2028: 2023: 2018: 2013: 2008: 2003: 1998: 1993: 1988: 1983: 1978: 1976:Abacavir (ABC) 1962: 1960: 1956:Nucleoside and 1949: 1940: 1939: 1936: 1935: 1933: 1932: 1927: 1922: 1916: 1909: 1907: 1903: 1902: 1900: 1899: 1894: 1889: 1884: 1879: 1874: 1869: 1863: 1861: 1854: 1840: 1839: 1837: 1836: 1831: 1826: 1820: 1818: 1812: 1811: 1809: 1808: 1803: 1798: 1793: 1788: 1783: 1778: 1772: 1770: 1762: 1761: 1759: 1758: 1746: 1730: 1716: 1705: 1692: 1690: 1676: 1675: 1673: 1672: 1666: 1664: 1658: 1657: 1637: 1636: 1629: 1622: 1614: 1608: 1607: 1593: 1592:External links 1590: 1587: 1586: 1564: 1537:(8): 937–951. 1514: 1489: 1465: 1435: 1408: 1394: 1368: 1356:New York Times 1342: 1294: 1287: 1267: 1218: 1188: 1181: 1161: 1150: 1130: 1087: 1061: 1042: 1015: 1014: 1012: 1009: 1008: 1007: 1000: 980: 977: 968: 965: 963: 960: 894: 891: 873: 870: 839: 836: 823: 820: 803: 800: 741: 740: 729: 728: 726: 725: 722: 720: 717: 709: 708: 707: 704: 703: 701: 700: 697: 689: 688: 687: 684: 683: 681: 680: 672: 670: 662: 661: 655: 649: 648: 645: 639: 633: 627: 622: 616: 615: 611: 610: 608: 607: 594: 592: 579: 578: 576: 575: 559: 557: 551: 550: 548: 547: 539: 537: 531: 530: 528: 527: 519: 517: 511: 510: 508: 507: 499: 497: 491: 490: 488: 487: 479: 477: 471: 470: 468: 467: 459: 457: 451: 450: 448: 447: 439: 437: 431: 430: 428: 427: 419: 417: 411: 410: 408: 407: 399: 397: 386: 385: 383: 382: 374: 372: 366: 365: 363: 362: 351: 343: 342: 341: 338: 337: 333: 332: 329: 323: 322: 319: 310: 309: 303: 297: 296: 293: 287: 286: 279: 273: 272: 265: 264: 262: 261: 249: 235: 233: 227: 226: 222: 221: 219: 218: 205: 203: 197: 196: 191: 189:administration 183: 182: 180: 179: 177: 167: 165: 157: 156: 154: 153: 136: 118: 116: 110: 109: 102: 96: 95: 88: 78: 77: 74: 70: 69: 66: 60: 59: 55: 54: 46: 45: 26: 9: 6: 4: 3: 2: 2761: 2750: 2747: 2745: 2742: 2740: 2737: 2735: 2732: 2730: 2727: 2725: 2722: 2720: 2717: 2715: 2712: 2711: 2709: 2699: 2694: 2689: 2687: 2677: 2676: 2673: 2660: 2657: 2654: 2644: 2642: 2639: 2638: 2636: 2633: 2630: 2627: 2625: 2622: 2621: 2617: 2607: 2604: 2602: 2599: 2597: 2594: 2592: 2589: 2587: 2584: 2582: 2579: 2577: 2574: 2572: 2569: 2567: 2564: 2562: 2559: 2557: 2554: 2552: 2549: 2547: 2544: 2542: 2539: 2538: 2536: 2534:Failed agents 2532: 2526: 2523: 2521: 2518: 2516: 2513: 2511: 2508: 2506: 2503: 2501: 2498: 2496: 2493: 2491: 2488: 2486: 2483: 2481: 2478: 2476: 2473: 2471: 2468: 2466: 2463: 2461: 2458: 2456: 2453: 2451: 2448: 2446: 2443: 2441: 2438: 2436: 2433: 2432: 2430: 2426: 2420: 2417: 2416: 2414: 2412: 2408: 2402: 2401:Trichosanthin 2399: 2398: 2396: 2394: 2390: 2384: 2381: 2380: 2378: 2376: 2372: 2365: 2362: 2361: 2359: 2357: 2353: 2350: 2346: 2340: 2339:Ritonavir (r) 2337: 2335: 2332: 2331: 2329: 2325: 2319: 2316: 2314: 2311: 2309: 2306: 2304: 2301: 2299: 2296: 2294: 2291: 2289: 2286: 2284: 2281: 2279: 2276: 2274: 2271: 2269: 2266: 2264: 2261: 2259: 2256: 2254: 2251: 2249: 2246: 2244: 2241: 2238: 2235: 2232: 2229: 2226: 2223: 2221: 2218: 2215: 2212: 2210: 2207: 2205: 2202: 2199: 2196: 2194: 2191: 2189: 2186: 2183: 2180: 2178: 2175: 2174: 2172: 2170: 2166: 2152: 2149: 2147: 2144: 2140: 2137: 2135: 2132: 2130: 2127: 2126: 2125: 2124: 2120: 2119: 2117: 2113: 2107: 2104: 2102: 2099: 2097: 2094: 2093: 2091: 2087: 2084: 2082: 2080: 2074: 2070: 2064: 2061: 2059: 2056: 2054: 2050: 2046: 2045: 2042: 2039: 2037: 2034: 2032: 2029: 2027: 2024: 2022: 2019: 2017: 2014: 2012: 2009: 2007: 2004: 2002: 1999: 1997: 1994: 1992: 1989: 1987: 1984: 1982: 1979: 1977: 1974: 1972: 1968: 1964: 1963: 1961: 1959: 1953: 1950: 1947: 1941: 1931: 1928: 1926: 1923: 1920: 1917: 1914: 1911: 1910: 1908: 1904: 1898: 1895: 1893: 1890: 1888: 1885: 1883: 1880: 1878: 1875: 1873: 1870: 1868: 1865: 1864: 1862: 1858: 1855: 1853: 1851: 1845: 1841: 1835: 1832: 1830: 1827: 1825: 1822: 1821: 1819: 1817: 1813: 1807: 1804: 1802: 1799: 1797: 1794: 1792: 1789: 1787: 1784: 1782: 1779: 1777: 1774: 1773: 1771: 1767: 1763: 1756: 1752: 1751: 1747: 1744: 1740: 1736: 1735: 1731: 1728: 1724: 1720: 1717: 1715: 1711: 1710: 1706: 1703: 1699: 1698: 1694: 1693: 1691: 1689: 1687: 1681: 1677: 1671: 1668: 1667: 1665: 1663: 1659: 1654: 1650: 1647:used against 1646: 1642: 1635: 1630: 1628: 1623: 1621: 1616: 1615: 1612: 1604: 1600: 1596: 1595: 1582: 1578: 1574: 1568: 1560: 1556: 1552: 1548: 1544: 1540: 1536: 1532: 1525: 1518: 1503: 1499: 1493: 1482: 1475: 1469: 1453: 1451: 1445: 1439: 1423: 1419: 1412: 1404: 1398: 1382: 1378: 1372: 1357: 1353: 1346: 1330: 1326: 1322: 1318: 1314: 1310: 1303: 1301: 1299: 1290: 1288:9780443075926 1284: 1280: 1279: 1271: 1263: 1259: 1255: 1251: 1246: 1241: 1237: 1233: 1229: 1222: 1206: 1202: 1198: 1192: 1184: 1182:9783527607495 1178: 1174: 1173: 1165: 1157: 1153: 1151:9781420015706 1147: 1143: 1142: 1134: 1118: 1114: 1108: 1106: 1104: 1102: 1100: 1098: 1096: 1094: 1092: 1075: 1071: 1065: 1057: 1053: 1046: 1030: 1026: 1020: 1016: 1005: 1004:microemulsion 1001: 998: 994: 990: 986: 985: 984: 976: 974: 959: 957: 953: 949: 943: 940: 936: 932: 928: 910: 906: 899: 890: 888: 883: 879: 869: 867: 862: 859: 856: 851: 849: 844: 835: 833: 829: 819: 817: 813: 809: 799: 796: 794: 790: 786: 782: 778: 773: 771: 767: 763: 759: 755: 751: 747: 737: 730: 721: 716: 715: 712: 705: 696: 695: 692: 685: 678: 674: 673: 671: 668: 663: 656: 654: 650: 623: 621: 617: 612: 604: 600: 599:DTXSID6044012 596: 595: 593: 584: 580: 572: 571:RCSB PDB 566: 561: 560: 558: 556: 552: 545: 541: 540: 538: 536: 532: 525: 521: 520: 518: 516: 512: 505: 501: 500: 498: 496: 492: 485: 481: 480: 478: 476: 472: 465: 461: 460: 458: 456: 452: 445: 441: 440: 438: 436: 432: 425: 421: 420: 418: 416: 412: 405: 401: 400: 398: 391: 387: 380: 376: 375: 373: 371: 367: 359: 355: 350: 349: 346: 339: 334: 330: 328: 324: 320: 318: 311: 308: 304: 302: 298: 294: 292: 288: 284: 280: 278: 274: 270: 266: 260: 250: 247: 237: 236: 234: 232: 228: 223: 215: 210: 207: 206: 204: 202: 198: 195: 192: 190: 184: 178: 169: 168: 166: 164: 158: 151: 146: 137: 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: 2734:Hepatotoxins 2714:Carboxamides 2655: 2455:Cyanovirin-N 2445:Calanolide A 2121: 2115:2 generation 2089:1 generation 2076: 2047: 2026:Elvucitabine 2016:Apricitabine 1965: 1906:2 generation 1896: 1860:1 generation 1847: 1834:Fipravirimat 1748: 1743:Semzuvolimab 1732: 1723:Cenicriviroc 1707: 1695: 1683: 1602: 1599:"Saquinavir" 1581:the original 1576: 1567: 1534: 1530: 1517: 1505:. Retrieved 1501: 1492: 1481:the original 1468: 1456:. Retrieved 1447: 1438: 1426:. Retrieved 1420:. The Body. 1411: 1402: 1397: 1385:. Retrieved 1380: 1371: 1359:. Retrieved 1355: 1345: 1333:. Retrieved 1316: 1312: 1278:AIDS Therapy 1277: 1270: 1235: 1231: 1221: 1209:. Retrieved 1205:the original 1200: 1191: 1171: 1164: 1140: 1133: 1121:. Retrieved 1113:"Saquinavir" 1078:. Retrieved 1073: 1064: 1055: 1045: 1033:. Retrieved 1028: 1019: 982: 979:Formulations 970: 944: 924: 913:. Retrieved 908: 875: 863: 852: 845: 841: 825: 822:Side effects 805: 802:Medical uses 797: 793:HIV protease 774: 749: 745: 744: 733:   535:NIAID ChemDB 357: 353: 314:Elimination 231:Legal status 225:Legal status 114:License data 29: 2656:recommended 2631:from market 2581:Lersivirine 2556:Capravirine 2495:Miltefosine 2480:Griffithsin 2475:Fosdevirine 2021:Censavudine 1651:(primarily 1428:20 February 1406:inhibitors. 1197:"Fortovase" 1123:5 September 781:heart block 660: g·mol 379:127779-20-8 336:Identifiers 100:MedlinePlus 73:Other names 64:Trade names 2749:Quinolines 2708:Categories 2586:Lodenosine 2566:Droxinavir 2551:Brecanavir 2546:Atevirdine 2510:Seliciclib 2505:Scytovirin 2419:Elipovimab 2364:TRIM5alpha 2041:Stampidine 1946:inhibitors 1930:TMC-310911 1829:BMS-955176 1727:Leronlimab 1719:Vicriviroc 1458:28 January 1387:29 October 1361:28 October 1335:8 November 1211:28 January 1080:28 January 1035:28 January 1011:References 915:28 October 866:omeprazole 746:Saquinavir 665:3D model ( 653:Molar mass 555:PDB ligand 484:L3JE09KZ2F 455:ChemSpider 415:IUPHAR/BPS 370:CAS Number 345:IUPAC name 321:9–15 hours 301:Metabolism 150:Saquinavir 34:Saquinavir 2641:Phase III 2629:Withdrawn 2606:Telinavir 2601:Palinavir 2596:Mozenavir 2576:Emivirine 2571:Lasinavir 2541:Aplaviroc 2470:Foscarnet 2450:Ceragenin 2011:Amdoxovir 1824:Bevirimat 1801:BI 224436 1502:Drugs.com 1201:Drugs.com 1029:Drugs.com 993:ritonavir 967:Economics 952:ritonavir 939:indinavir 935:ritonavir 882:Proteases 848:ritonavir 828:diarrhoea 812:ritonavir 762:ritonavir 524:ChEMBL114 327:Excretion 316:half-life 187:Routes of 161:Pregnancy 92:Monograph 86:Drugs.com 2686:Medicine 2591:Loviride 1559:28468973 1551:22663249 1422:Archived 1329:Archived 1325:21637182 1262:44506039 1254:16791014 1156:Archived 1117:Archived 1074:DailyMed 989:mesylate 808:HIV/AIDS 770:by mouth 758:HIV/AIDS 750:Invirase 736:(verify) 435:DrugBank 283:boosting 201:ATC code 194:By mouth 176: B1 163:category 145:DailyMed 18:Invirase 2698:Viruses 2672:Portals 2490:KP-1461 2036:Racivir 1806:MK-2048 893:History 658:670.855 620:Formula 444:DB01232 390:PubChem 217:) 211: ( 209:J05AE01 147::  130::  106:a696001 2624:WHO-EM 2440:BIT225 2435:Abzyme 2366:(gene) 2053:NtRTIs 1948:(RTIs) 1557:  1549:  1507:9 July 1323:  1285:  1260:  1252:  1179:  1148:  832:nausea 691:SMILES 544:000640 515:ChEMBL 504:D00429 464:390016 404:441243 307:CYP3A4 259:â„ž-only 257: 244: 143:  133:by INN 126:  2428:Other 2411:BNAbs 1971:NRTIs 1750:gp120 1555:S2CID 1527:(PDF) 1484:(PDF) 1477:(PDF) 1452:(FDA) 1448:U.S. 1258:S2CID 927:Roche 887:HIV-1 711:InChI 667:JSmol 562:ROC ( 2653:DHHS 1709:CCR5 1697:gp41 1547:PMID 1509:2020 1460:2020 1430:2013 1389:2020 1363:2020 1337:2013 1321:PMID 1283:ISBN 1250:PMID 1232:AIDS 1213:2020 1177:ISBN 1146:ISBN 1125:2015 1082:2020 1037:2020 937:and 917:2020 565:PDBe 495:KEGG 475:UNII 424:4813 271:data 82:AHFS 1734:CD4 1653:J05 1649:HIV 1539:doi 1381:NIH 1240:doi 858:3A4 814:or 764:or 588:EPA 394:CID 295:98% 214:WHO 128:EMA 76:SQV 2710:: 2637:: 1741:, 1725:, 1721:, 1643:: 1601:. 1575:. 1553:. 1545:. 1533:. 1529:. 1500:. 1446:. 1379:. 1354:. 1327:. 1317:60 1315:. 1311:. 1297:^ 1256:. 1248:. 1236:20 1234:. 1230:. 1199:. 1154:. 1090:^ 1072:. 1054:. 1027:. 975:. 958:. 907:. 880:. 868:. 830:, 795:. 783:, 779:, 772:. 634:50 628:38 568:, 356:)- 352:(2 253:US 246:S4 240:AU 172:AU 140:US 123:EU 2674:: 2651:° 2239:° 2233:° 2227:° 2216:° 2200:° 2184:° 2081:) 2077:( 2055:: 2051:/ 1973:: 1969:/ 1921:° 1915:° 1852:) 1848:( 1757:) 1753:( 1745:) 1737:( 1729:) 1712:( 1704:) 1700:( 1688:) 1684:( 1655:) 1633:e 1626:t 1619:v 1561:. 1541:: 1535:9 1511:. 1462:. 1432:. 1391:. 1365:. 1339:. 1291:. 1264:. 1242:: 1215:. 1185:. 1127:. 1084:. 1039:. 999:; 919:. 669:) 646:5 643:O 640:6 637:N 631:H 625:C 590:) 586:( 574:) 358:N 354:S 285:) 255:: 242:: 174:: 84:/ 20:)

Index

Invirase


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

Text is available under the Creative Commons Attribution-ShareAlike License. Additional terms may apply.

↑