321:
32:
297:
Antiretroviral protease inhibitors act by binding to the catalytic site of HIV protease, preventing cleavage of viral polyprotein precursor proteins into functional viral proteins required for viral replication. Most ARPIs are peptide-like molecules which resemble the substrate of the viral protease.
491:
The sixteenth FDA-approved antiretroviral. It was the first protease inhibitor approved for twice-a-day dosing instead of needing to be taken every eight hours. The convenient dosing came at a price, as the dose required is 1,200 mg, delivered in 8 very large gel capsules. Production was
948:
Madruga JV, Berger D, McMurchie M, et al. (Jul 2007). "Efficacy and safety of darunavir-ritonavir compared with that of lopinavir-ritonavir at 48 weeks in treatment-experienced, HIV-infected patients in TITAN: a randomised controlled phase III trial".
406:
AbbVie was part of Abbott
Laboratories when patent was granted. As well as being a protease inhibitor in its own right, ritonavir inhibits the breakdown of other protease inhibitors. This property makes it very useful in drug combinations.
317:, were approved in late 1995–1996. Within 2 years, annual deaths from AIDS in the United States fell from over 50,000 to approximately 18,000 Prior to this the annual death rate had been increasing by approximately 20% each year.
581:
of amprenavir. The human body metabolizes fosamprenavir in order to form amprenavir, which is the active ingredient. That metabolization increases the duration that amprenavir is available, making fosamprenavir a
552:
Atazanavir was the first PI approved for once-daily dosing. It appears to be less likely to cause lipodystrophy and elevated cholesterol as side effects. It may also not be cross-resistant with other PIs.
1644:
1618:
1536:
929:. Developed by the DHHS Panel on Antiretroviral Guidelines for Adults and Adolescents—A Working Group of the Office of AIDS Research Advisory Council (OARAC). July 14, 2016
278:, of the development of drug-resistant mutated viruses. To reduce this risk, it is common to use several different drugs together that are each aimed at different targets.
1638:
1828:
1833:
1779:
1251:
2218:
1415:
729:
1785:
1843:
1763:
244:
1848:
1163:
1046:
2377:
1796:
1197:
795:"Exploring the Binding Mechanism of PF-07321332 SARS-CoV-2 Protease Inhibitor through Molecular Dynamics and Binding Free Energy Simulations"
1818:
1802:
753:
724:
2990:
2518:
2171:
2166:
324:
The number of people in the U.S. dying of HIV fell by 60% in the 2 years following the introduction of the first HIV protease inhibitors
2441:
1813:
1823:
2257:
2090:
281:
In addition to those non-human proteases listed above, inhibitors of human proteases may be used to treat cancer. See the articles
1734:
923:
1137:
Capaldini, L. (1997). "Protease inhibitors' metabolic side effects: cholesterol, triglycerides, blood sugar, and "Crix belly"".
1074:
2934:
2189:
2080:
650:
combination for first-line therapy. Darunavir is the first drug in a long time that did not come with a price increase. It
2579:
1838:
1175:
3324:
3168:
3127:
1853:
282:
52:
3093:
2564:
1190:
907:
3285:
2951:
2206:
1863:
1747:
642:
recommended treatment option for treatment-naĂŻve and treatment-experienced adults and adolescents. Several ongoing
3199:
2983:
1873:
1858:
1521:
1509:
719:
1017:"Retaining Efficacy Against Evasive HIV: Darunavir analog to AIDS-virus shapeshifters: Resistance may be futile"
3245:
3152:
1753:
111:) and blocking proteolytic cleavage of protein precursors that are necessary for the production of infectious
3339:
3173:
2235:
754:"The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances"
3413:
3372:
3364:
2250:
1183:
375:
240:
20:
320:
3268:
3258:
3240:
3181:
3085:
1958:
3122:
3064:
3027:
2976:
46:
3388:
3211:
3077:
3344:
3206:
2554:
2030:
1940:
1921:
1808:
1769:
694:
646:
trials are showing a high efficiency for the darunavir/ritonavir combination being superior to the
118:
Protease inhibitors that have been developed and are currently used in clinical practice include:
3319:
3297:
3263:
3022:
2939:
2691:
2243:
2194:
1790:
586:
version of amprenavir and thus reduces the number of pills required versus standard amprenavir.
492:
discontinued by the manufacturer
December 31, 2004, as it has been superseded by fosamprenavir.
3280:
3250:
3216:
3189:
3101:
3017:
2803:
2788:
2574:
2569:
1868:
1098:"Protease inhibitor-associated diabetes mellitus: A potential cause of morbidity and mortality"
992:
677:, and ritonavir, which inhibits the metabolism of nirmatrelvir, thereby prolonging its effect.
1976:
3329:
2750:
2745:
2695:
2559:
2065:
1878:
1758:
1628:
1227:
623:
448:
359:
2549:
1948:
1774:
1623:
1381:
698:
599:
537:
286:
1205:
1016:
924:"Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents"
8:
3194:
3109:
1883:
1742:
1614:
1532:
1331:
1210:
878:
854:, Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases, 2012,
714:
647:
643:
521:
302:
123:
3032:
2740:
2645:
974:
821:
794:
962:
103:. These protease inhibitors prevent viral replication by selectively binding to viral
3302:
2901:
2025:
1688:
1142:
1119:
1114:
1097:
966:
903:
855:
826:
779:
777:
187:
978:
3037:
3003:
2760:
2050:
1109:
1028:
958:
816:
806:
674:
2968:
2224:
3307:
3114:
2281:
2277:
2126:
2085:
1245:
566:
476:
88:
1166:
of the development of protease inhibitors by
Hoffman La Roche, Abbott, and Merck
274:
Given the specificity of the target of these drugs there is the risk, like with
3160:
3147:
3054:
2945:
2885:
2464:
2269:
2200:
1206:
847:
690:
420:
126:
108:
2265:
1032:
629:
543:
511:
482:
454:
426:
397:
365:
3407:
3290:
2478:
1966:
1716:
1551:
1437:
686:
558:
150:
654:
two other approved drugs of its type, and is matching the price of a third.
2999:
2860:
2855:
2825:
2799:
2784:
2774:
2611:
2533:
2431:
2382:
2352:
2273:
2020:
2010:
1591:
1581:
1399:
1356:
1351:
1346:
1308:
1288:
1218:
1146:
1123:
970:
859:
830:
670:
651:
583:
263:
258:
223:
1047:"First doses of Paxlovid, Pfizer's new COVID pill, are released to states"
669:, was approved in December 2021 to treat COVID-19. It is a combination of
3137:
2906:
2880:
2875:
2835:
2830:
2794:
2779:
2769:
2714:
2700:
2682:
2620:
2601:
2593:
2451:
2406:
2401:
2347:
2342:
2337:
2332:
2312:
2290:
2146:
2121:
2060:
2045:
2040:
1704:
1671:
1586:
1566:
1361:
1341:
1320:
1267:
1235:
811:
505:
391:
253:
218:
213:
203:
96:
80:
1003:
852:
LiverTox: Clinical and
Research Information on Drug-Induced Liver Injury
2916:
2911:
2845:
2732:
2677:
2672:
2667:
2663:
2655:
2625:
2528:
2523:
2513:
2508:
2488:
2473:
2446:
2436:
2426:
2416:
2372:
2367:
2362:
2357:
2327:
2322:
2317:
2151:
2131:
2116:
2111:
2075:
2070:
1984:
1929:
1899:
1711:
1699:
1694:
1666:
1606:
1596:
1571:
1556:
1546:
1495:
1490:
1478:
1462:
1452:
1432:
1394:
1304:
1292:
1284:
991:
Liz
Highleyman, Patient Advocates Commend Pricing of New PI Darunavir,
778:
Programme on
International Nonproprietary Names (INN) (February 2023).
591:
529:
468:
440:
351:
306:
275:
233:
228:
208:
180:
175:
165:
140:
135:
1169:
3230:
2870:
2840:
2710:
2705:
2650:
2636:
2493:
2483:
2421:
2299:
2266:
2161:
2141:
2136:
2106:
2035:
2015:
1904:
1661:
1576:
1561:
1484:
1457:
1447:
1442:
1389:
1366:
1279:
702:
615:
497:
412:
383:
314:
310:
190:
170:
160:
155:
145:
104:
2411:
2156:
1541:
666:
524:). AbbVie was part of Abbott Laboratories when patent was granted.
100:
92:
84:
947:
780:"Pre-stems: Suffixes used in the selection of INN - February 2023"
701:. This lipodystrophy is colloquially known as "Crix belly", after
2865:
2503:
2498:
2055:
1601:
1371:
578:
520:
Is only marketed as a fixed-dose combination with ritonavir (see
3069:
2850:
2820:
2005:
2000:
902:(69 ed.). Pharmaceutical Pr. March 31, 2015. p. 426.
112:
16:
Class of antiviral drugs used to treat HIV/AIDS and hepatitis C
3354:
1315:
639:
1077:. DailyMed, US National Library of Medicine. 18 October 2023
993:
http://www.hivandhepatitis.com/recent/2006/ad1/063006_a.html
2461:
2392:
2303:
1829:
Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
1274:
1262:
194:
1834:
Elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil
1299:
1214:
1051:
793:
Ahmad B, Batool M, Ain QU, Kim MS, Choi S (August 2021).
1780:
Darunavir/cobicistat/emtricitabine/tenofovir alafenamide
660:
1004:
Darunavir - first molecule to treat drug-resistant HIV
292:
730:
Discovery and development of HIV-protease inhibitors
2998:
673:, a protease inhibitor targeted to the SARS-CoV-2
792:
3405:
1786:Dolutegravir/emtricitabine/tenofovir alafenamide
879:"HIV Surveillance --- United States, 1981--2008"
1844:Emtricitabine/rilpivirine/tenofovir alafenamide
1764:Bictegravir/emtricitabine/tenofovir alafenamide
1102:Journal of Acquired Immune Deficiency Syndromes
245:severe acute respiratory syndrome coronavirus 2
1849:Emtricitabine/rilpivirine/tenofovir disoproxil
1335:(Integrase strand transfer inhibitors (INSTI))
41:needs attention from an expert in Pharmacology
2984:
2251:
1797:Dolutegravir/lamivudine/tenofovir alafenamide
1191:
374:The first protease inhibitor approved by the
301:Protease inhibitors were the second class of
1819:Efavirenz/emtricitabine/tenofovir disoproxil
1803:Dolutegravir/lamivudine/tenofovir disoproxil
725:Discovery and development of NS5A inhibitors
685:Protease inhibitors can cause a syndrome of
305:developed. The first members of this class,
799:International Journal of Molecular Sciences
748:
746:
744:
2991:
2977:
2258:
2244:
1814:Doravirine/lamivudine/tenofovir disoproxil
1198:
1184:
1172:US Department of Health and Human Services
1824:Efavirenz/lamivudine/tenofovir disoproxil
1136:
1113:
820:
810:
665:A drug combination targeting SARS-CoV-2,
2091:Zinc finger protein transcription factor
1014:
741:
319:
3406:
1095:
55:may be able to help recruit an expert.
2972:
2239:
1179:
661:Non-antiretroviral antiviral activity
19:For natural protease inhibitors, see
916:
892:
842:
840:
786:
25:
2580:Sofosbuvir/velpatasvir/voxilaprevir
1839:Emtricitabine/tenofovir alafenamide
610:Also known as tipranavir disodium.
13:
1854:Emtricitabine/tenofovir disoproxil
1075:"Paxlovid: Drug label information"
293:Antiretroviral protease inhibitors
283:matrix metalloproteinase inhibitor
87:. Some of the most well known are
14:
3425:
2565:Ombitasvir/paritaprevir/ritonavir
1156:
837:
376:U.S. Food and Drug Administration
2227:. Formerly or rarely used agent.
1864:Lamivudine/nevirapine/zidovudine
1748:Abacavir/dolutegravir/lamivudine
1115:10.1097/00126334-200303010-00001
243:(including, but not limited to,
30:
2031:Epigallocatechin gallate (EGCG)
1874:Lamivudine/tenofovir disoproxil
1859:Lamivudine/nevirapine/stavudine
1130:
1089:
1067:
1039:
1021:Chemical & Engineering News
1008:
997:
720:Reverse-transcriptase inhibitor
680:
197:protease inhibitors—class stem
1754:Abacavir/lamivudine/zidovudine
985:
941:
871:
771:
1:
2306:protease inhibitors (–previr)
1170:HIV/AIDS Treatment Guidelines
963:10.1016/S0140-6736(07)61049-6
900:British National Formulary 69
735:
83:that act by interfering with
782:. World Health Organization.
638:As of 2016, darunavir is an
241:3-chymotrypsin-like protease
85:enzymes that cleave proteins
21:Protease inhibitor (biology)
7:
1629:Tenofovir alafenamide (TAF)
848:"Protease Inhibitors (HIV)"
759:. World Health Organization
708:
43:. The specific problem is:
10:
3430:
3169:Dihydropteroate synthetase
3028:Non-competitive inhibition
1624:Tenofovir disoproxil (TDF)
47:Template:Enzyme inhibition
18:
3389:Steroidogenesis inhibitor
3381:
3353:
3229:
3136:
3053:
3046:
3010:
2929:
2894:
2813:
2759:
2731:
2724:
2634:
2610:
2592:
2542:
2460:
2391:
2298:
2289:
2184:
2099:
1993:
1975:
1957:
1939:
1920:
1913:
1892:
1733:
1680:
1654:
1645:Discovery and development
1637:
1520:
1508:
1471:
1425:
1416:Discovery and development
1408:
1380:
1330:
1252:Discovery and development
1244:
1226:
1033:10.1021/cen-v084n034.p009
3325:Matrix metalloproteinase
3128:Ribonucleotide reductase
3023:Uncompetitive inhibition
2692:neuraminidase inhibitors
2555:Glecaprevir/pibrentasvir
1941:Transcription inhibitors
1893:Pharmacokinetic boosters
1809:Dolutegravir/rilpivirine
1770:Cabotegravir/rilpivirine
1410:Protease Inhibitors (PI)
695:diabetes mellitus type 2
247:) inhibitors—class stem
53:WikiProject Pharmacology
3094:Dihydrofolate reductase
2225:initial regimen options
1791:Dolutegravir/lamivudine
1268:Enfuvirtide (ENF, T-20)
1246:Entry/fusion inhibitors
45:non-antiviral types in
3190:Nucleotidyltransferase
3018:Competitive inhibition
2895:Multiple/Unknown/Other
2664:adamantane derivatives
2575:Sofosbuvir/velpatasvir
2570:Sofosbuvir/daclatasvir
2066:Portmanteau inhibitors
1959:Translation inhibitors
1869:Lamivudine/raltegravir
1639:Non-nucleoside (NNRTI)
1597:Islatravir (EFdA, ISL)
325:
129:inhibitors—class stem
3200:Reverse transcriptase
2763:inhibitors (–trelvir)
2751:Peginterferon alfa-2b
2746:Peginterferon alfa-2a
2560:Ledipasvir/sofosbuvir
2081:Synergistic enhancers
1879:Lamivudine/zidovudine
1759:Atazanavir/cobicistat
1735:Combined formulations
1572:Zidovudine (AZT, ZDV)
1510:Reverse-transcriptase
1382:Maturation inhibitors
630:U.S. patent 6,248,775
544:U.S. patent 5,849,911
512:U.S. patent 5,914,332
483:U.S. patent 5,585,397
455:U.S. patent 5,484,926
427:U.S. patent 5,413,999
398:U.S. patent 5,541,206
366:U.S. patent 5,196,438
323:
91:widely used to treat
3246:Acetylcholinesterase
3153:Thymidylate synthase
2550:Elbasvir/grazoprevir
1922:Uncoating inhibitors
1775:Darunavir/cobicistat
1615:Nucleotide analogues
1533:Nucleoside analogues
1332:Integrase inhibitors
1211:antiretroviral drugs
812:10.3390/ijms22179124
624:Janssen Therapeutics
600:Boehringer Ingelheim
538:Bristol-Myers Squibb
303:antiretroviral drugs
287:proteasome inhibitor
3414:Protease inhibitors
3340:Histone deacetylase
3174:Farnesyltransferase
2467:inhibitors (–buvir)
2395:inhibitors (–asvir)
1914:Experimental agents
1884:Lopinavir/ritonavir
1743:Abacavir/lamivudine
1717:Elsulfavirine (ESV)
1552:Emtricitabine (FTC)
1438:Fosamprenavir (FPV)
1139:AIDS Treatment News
1096:Fantry, LE (2003).
715:The Proteolysis Map
648:lopinavir/ritonavir
522:lopinavir/ritonavir
356:Invirase, Fortovase
73:Protease inhibitors
3373:Carbonic anhydrase
3365:Dopa decarboxylase
3033:Suicide inhibition
2956:Never to phase III
2814:RNA pol inhibitors
2741:Interferon alfa 2b
2646:Baloxavir marboxil
2211:Never to phase III
1357:Elvitegravir (EVG)
1352:Dolutegravir (DTG)
1347:Cabotegravir (CAB)
1055:. 23 December 2021
517:September 15, 2000
326:
3401:
3400:
3397:
3396:
3269:Alpha-glucosidase
3259:Polygalacturonase
3241:Phosphodiesterase
3182:GABA transaminase
3086:Monoamine oxidase
3070:HMG-CoA reductase
3004:enzyme inhibition
2966:
2965:
2925:
2924:
2588:
2587:
2543:Combination drugs
2233:
2232:
2180:
2179:
2026:Diarylpyrimidines
1729:
1728:
1725:
1724:
1705:Rilpivirine (RPV)
1689:diarylpyrimidines
1672:Delavirdine (DLV)
1567:Zalcitabine (ddC)
1524:nucleotide (NRTI)
1504:
1503:
1362:Raltegravir (RAL)
1342:Bictegravir (BIC)
1321:Fostemsavir (FTR)
1236:Lenacapavir (LEN)
1228:Capsid inhibitors
1015:Borman S (2006).
658:
657:
449:Hoffmann–La Roche
360:Hoffmann–La Roche
343:FDA approval date
188:Hepatitis C virus
70:
69:
3421:
3123:Xanthine oxidase
3065:Aldose reductase
3051:
3050:
3038:Mixed inhibition
2993:
2986:
2979:
2970:
2969:
2729:
2728:
2725:Multiple/general
2296:
2295:
2260:
2253:
2246:
2237:
2236:
2051:Hydroxycarbamide
1918:
1917:
1712:Doravirine (DOR)
1700:Etravirine (ETR)
1695:Dapivirine (DPV)
1667:Nevirapine (NVP)
1652:
1651:
1557:Lamivudine (3TC)
1547:Didanosine (ddI)
1518:
1517:
1491:Tipranavir (TPV)
1479:Atazanavir (ATV)
1463:Saquinavir (SQV)
1453:Nelfinavir (NFV)
1433:Amprenavir (APV)
1423:
1422:
1305:Ibalizumab (IBA)
1200:
1193:
1186:
1177:
1176:
1151:
1150:
1134:
1128:
1127:
1117:
1093:
1087:
1086:
1084:
1082:
1071:
1065:
1064:
1062:
1060:
1043:
1037:
1036:
1012:
1006:
1001:
995:
989:
983:
982:
945:
939:
938:
936:
934:
928:
920:
914:
913:
896:
890:
889:
887:
885:
875:
869:
868:
867:
866:
844:
835:
834:
824:
814:
790:
784:
783:
775:
769:
768:
766:
764:
758:
750:
675:3C-like protease
632:
574:October 20, 2003
546:
514:
485:
457:
429:
400:
371:December 6, 1995
368:
328:
327:
65:
62:
56:
34:
33:
26:
3429:
3428:
3424:
3423:
3422:
3420:
3419:
3418:
3404:
3403:
3402:
3393:
3377:
3349:
3225:
3212:Tyrosine kinase
3132:
3042:
3006:
2997:
2967:
2962:
2961:
2946:Clinical trials
2921:
2890:
2809:
2755:
2720:
2630:
2606:
2584:
2538:
2456:
2387:
2285:
2264:
2234:
2229:
2228:
2216:
2201:Clinical trials
2176:
2127:Dexelvucitabine
2095:
2086:Tre recombinase
1989:
1971:
1953:
1949:Tat antagonists
1935:
1909:
1888:
1721:
1676:
1662:Efavirenz (EFV)
1641:
1633:
1562:Stavudine (d4T)
1523:
1511:
1500:
1485:Darunavir (DRV)
1467:
1458:Ritonavir (RTV)
1448:Lopinavir (LPV)
1443:Indinavir (IDV)
1412:
1404:
1376:
1334:
1326:
1280:Maraviroc (MVC)
1248:
1240:
1222:
1207:Antiviral drugs
1204:
1159:
1154:
1135:
1131:
1094:
1090:
1080:
1078:
1073:
1072:
1068:
1058:
1056:
1045:
1044:
1040:
1013:
1009:
1002:
998:
990:
986:
957:(9581): 49–58.
946:
942:
932:
930:
926:
922:
921:
917:
910:
898:
897:
893:
883:
881:
877:
876:
872:
864:
862:
846:
845:
838:
791:
787:
776:
772:
762:
760:
756:
752:
751:
742:
738:
711:
683:
663:
628:
567:GlaxoSmithKline
542:
510:
481:
477:GlaxoSmithKline
453:
425:
421:Merck & Co.
396:
364:
295:
272:
113:viral particles
89:antiviral drugs
66:
60:
57:
51:
35:
31:
24:
17:
12:
11:
5:
3427:
3417:
3416:
3399:
3398:
3395:
3394:
3392:
3391:
3385:
3383:
3379:
3378:
3376:
3375:
3368:
3367:
3360:
3358:
3351:
3350:
3348:
3347:
3345:Beta-lactamase
3342:
3335:
3334:
3333:
3332:
3327:
3322:
3312:
3311:
3310:
3305:
3295:
3294:
3293:
3288:
3272:
3271:
3266:
3261:
3254:
3253:
3248:
3243:
3236:
3234:
3227:
3226:
3224:
3223:
3222:
3221:
3220:
3219:
3207:Protein kinase
3204:
3203:
3202:
3197:
3185:
3184:
3177:
3176:
3171:
3164:
3163:
3156:
3155:
3150:
3143:
3141:
3134:
3133:
3131:
3130:
3125:
3118:
3117:
3112:
3105:
3104:
3097:
3096:
3089:
3088:
3081:
3080:
3073:
3072:
3067:
3060:
3058:
3055:Oxidoreductase
3048:
3044:
3043:
3041:
3040:
3035:
3030:
3025:
3020:
3014:
3012:
3008:
3007:
2996:
2995:
2988:
2981:
2973:
2964:
2963:
2960:
2959:
2958:
2957:
2954:
2943:
2937:
2931:
2930:
2927:
2926:
2923:
2922:
2920:
2919:
2914:
2909:
2904:
2898:
2896:
2892:
2891:
2889:
2888:
2886:Valopicitabine
2883:
2878:
2873:
2868:
2863:
2858:
2853:
2848:
2843:
2838:
2833:
2828:
2823:
2817:
2815:
2811:
2810:
2808:
2807:
2797:
2792:
2782:
2777:
2772:
2766:
2764:
2757:
2756:
2754:
2753:
2748:
2743:
2737:
2735:
2726:
2722:
2721:
2719:
2718:
2708:
2703:
2687:
2686:
2680:
2675:
2659:
2658:
2653:
2648:
2642:
2640:
2632:
2631:
2629:
2628:
2616:
2614:
2608:
2607:
2605:
2604:
2598:
2596:
2590:
2589:
2586:
2585:
2583:
2582:
2577:
2572:
2567:
2562:
2557:
2552:
2546:
2544:
2540:
2539:
2537:
2536:
2531:
2526:
2521:
2516:
2511:
2506:
2501:
2496:
2491:
2486:
2481:
2476:
2470:
2468:
2465:RNA polymerase
2458:
2457:
2455:
2454:
2449:
2444:
2439:
2434:
2429:
2424:
2419:
2414:
2409:
2404:
2398:
2396:
2389:
2388:
2386:
2385:
2380:
2375:
2370:
2365:
2360:
2355:
2350:
2345:
2340:
2335:
2330:
2325:
2320:
2315:
2309:
2307:
2293:
2287:
2286:
2263:
2262:
2255:
2248:
2240:
2231:
2230:
2215:
2214:
2213:
2212:
2209:
2198:
2192:
2186:
2185:
2182:
2181:
2178:
2177:
2175:
2174:
2169:
2164:
2159:
2154:
2149:
2144:
2139:
2134:
2129:
2124:
2119:
2114:
2109:
2103:
2101:
2097:
2096:
2094:
2093:
2088:
2083:
2078:
2073:
2068:
2063:
2058:
2053:
2048:
2043:
2038:
2033:
2028:
2023:
2018:
2013:
2008:
2003:
1997:
1995:
1991:
1990:
1988:
1987:
1981:
1979:
1973:
1972:
1970:
1969:
1963:
1961:
1955:
1954:
1952:
1951:
1945:
1943:
1937:
1936:
1934:
1933:
1926:
1924:
1915:
1911:
1910:
1908:
1907:
1902:
1900:Cobicistat (c)
1896:
1894:
1890:
1889:
1887:
1886:
1881:
1876:
1871:
1866:
1861:
1856:
1851:
1846:
1841:
1836:
1831:
1826:
1821:
1816:
1811:
1806:
1800:
1794:
1788:
1783:
1777:
1772:
1767:
1761:
1756:
1751:
1745:
1739:
1737:
1731:
1730:
1727:
1726:
1723:
1722:
1720:
1719:
1714:
1709:
1708:
1707:
1702:
1697:
1684:
1682:
1678:
1677:
1675:
1674:
1669:
1664:
1658:
1656:
1649:
1635:
1634:
1632:
1631:
1626:
1610:
1609:
1604:
1599:
1594:
1589:
1584:
1579:
1574:
1569:
1564:
1559:
1554:
1549:
1544:
1542:Abacavir (ABC)
1528:
1526:
1522:Nucleoside and
1515:
1506:
1505:
1502:
1501:
1499:
1498:
1493:
1488:
1482:
1475:
1473:
1469:
1468:
1466:
1465:
1460:
1455:
1450:
1445:
1440:
1435:
1429:
1427:
1420:
1406:
1405:
1403:
1402:
1397:
1392:
1386:
1384:
1378:
1377:
1375:
1374:
1369:
1364:
1359:
1354:
1349:
1344:
1338:
1336:
1328:
1327:
1325:
1324:
1312:
1296:
1282:
1271:
1258:
1256:
1242:
1241:
1239:
1238:
1232:
1230:
1224:
1223:
1203:
1202:
1195:
1188:
1180:
1174:
1173:
1167:
1158:
1157:External links
1155:
1153:
1152:
1129:
1088:
1066:
1038:
1007:
996:
984:
940:
915:
908:
891:
870:
836:
785:
770:
739:
737:
734:
733:
732:
727:
722:
717:
710:
707:
691:hyperlipidemia
682:
679:
662:
659:
656:
655:
636:
633:
626:
621:
618:
612:
611:
608:
605:
602:
597:
594:
588:
587:
575:
572:
569:
564:
563:Lexiva, Telzir
561:
555:
554:
550:
547:
540:
535:
532:
526:
525:
518:
515:
508:
503:
500:
494:
493:
489:
488:April 15, 1999
486:
479:
474:
471:
465:
464:
461:
460:March 14, 1997
458:
451:
446:
443:
437:
436:
433:
432:March 13, 1996
430:
423:
418:
415:
409:
408:
404:
401:
394:
389:
386:
380:
379:
372:
369:
362:
357:
354:
348:
347:
344:
341:
338:
335:
332:
294:
291:
285:(–mastat) and
271:
270:
268:
267:
266:
261:
256:
238:
237:
236:
231:
226:
221:
216:
211:
206:
185:
184:
183:
178:
173:
168:
163:
158:
153:
148:
143:
138:
127:HIV-1 protease
124:Antiretroviral
120:
109:HIV-1 protease
68:
67:
38:
36:
29:
15:
9:
6:
4:
3:
2:
3426:
3415:
3412:
3411:
3409:
3390:
3387:
3386:
3384:
3382:Miscellaneous
3380:
3374:
3370:
3369:
3366:
3362:
3361:
3359:
3356:
3352:
3346:
3343:
3341:
3337:
3336:
3331:
3328:
3326:
3323:
3321:
3320:Enkephalinase
3318:
3317:
3316:
3313:
3309:
3306:
3304:
3301:
3300:
3299:
3298:Endopeptidase
3296:
3292:
3289:
3287:
3284:
3283:
3282:
3278:
3274:
3273:
3270:
3267:
3265:
3264:Neuraminidase
3262:
3260:
3256:
3255:
3252:
3249:
3247:
3244:
3242:
3238:
3237:
3235:
3232:
3228:
3218:
3215:
3214:
3213:
3210:
3209:
3208:
3205:
3201:
3198:
3196:
3193:
3192:
3191:
3187:
3186:
3183:
3179:
3178:
3175:
3172:
3170:
3166:
3165:
3162:
3158:
3157:
3154:
3151:
3149:
3145:
3144:
3142:
3139:
3135:
3129:
3126:
3124:
3120:
3119:
3116:
3113:
3111:
3107:
3106:
3103:
3099:
3098:
3095:
3091:
3090:
3087:
3083:
3082:
3079:
3075:
3074:
3071:
3068:
3066:
3062:
3061:
3059:
3056:
3052:
3049:
3045:
3039:
3036:
3034:
3031:
3029:
3026:
3024:
3021:
3019:
3016:
3015:
3013:
3009:
3005:
3001:
2994:
2989:
2987:
2982:
2980:
2975:
2974:
2971:
2955:
2953:
2950:
2949:
2947:
2944:
2941:
2938:
2936:
2933:
2932:
2928:
2918:
2915:
2913:
2910:
2908:
2905:
2903:
2900:
2899:
2897:
2893:
2887:
2884:
2882:
2879:
2877:
2874:
2872:
2869:
2867:
2864:
2862:
2859:
2857:
2854:
2852:
2849:
2847:
2844:
2842:
2839:
2837:
2834:
2832:
2829:
2827:
2824:
2822:
2819:
2818:
2816:
2812:
2805:
2801:
2798:
2796:
2793:
2790:
2786:
2783:
2781:
2778:
2776:
2773:
2771:
2768:
2767:
2765:
2762:
2758:
2752:
2749:
2747:
2744:
2742:
2739:
2738:
2736:
2734:
2730:
2727:
2723:
2716:
2712:
2709:
2707:
2704:
2702:
2698:
2697:
2696:release phase
2693:
2689:
2688:
2684:
2681:
2679:
2676:
2674:
2670:
2669:
2668:M2 inhibitors
2665:
2661:
2660:
2657:
2654:
2652:
2649:
2647:
2644:
2643:
2641:
2638:
2633:
2627:
2624:
2622:
2618:
2617:
2615:
2613:
2609:
2603:
2600:
2599:
2597:
2595:
2591:
2581:
2578:
2576:
2573:
2571:
2568:
2566:
2563:
2561:
2558:
2556:
2553:
2551:
2548:
2547:
2545:
2541:
2535:
2532:
2530:
2527:
2525:
2522:
2520:
2517:
2515:
2512:
2510:
2507:
2505:
2502:
2500:
2497:
2495:
2492:
2490:
2487:
2485:
2482:
2480:
2479:Bemnifosbuvir
2477:
2475:
2472:
2471:
2469:
2466:
2463:
2459:
2453:
2450:
2448:
2445:
2443:
2440:
2438:
2435:
2433:
2430:
2428:
2425:
2423:
2420:
2418:
2415:
2413:
2410:
2408:
2405:
2403:
2400:
2399:
2397:
2394:
2390:
2384:
2381:
2379:
2376:
2374:
2371:
2369:
2366:
2364:
2361:
2359:
2356:
2354:
2351:
2349:
2346:
2344:
2341:
2339:
2336:
2334:
2331:
2329:
2326:
2324:
2321:
2319:
2316:
2314:
2311:
2310:
2308:
2305:
2301:
2297:
2294:
2292:
2288:
2283:
2279:
2275:
2271:
2268:
2261:
2256:
2254:
2249:
2247:
2242:
2241:
2238:
2226:
2223:
2220:
2210:
2208:
2205:
2204:
2202:
2199:
2196:
2193:
2191:
2188:
2187:
2183:
2173:
2170:
2168:
2165:
2163:
2160:
2158:
2155:
2153:
2150:
2148:
2145:
2143:
2140:
2138:
2135:
2133:
2130:
2128:
2125:
2123:
2120:
2118:
2115:
2113:
2110:
2108:
2105:
2104:
2102:
2100:Failed agents
2098:
2092:
2089:
2087:
2084:
2082:
2079:
2077:
2074:
2072:
2069:
2067:
2064:
2062:
2059:
2057:
2054:
2052:
2049:
2047:
2044:
2042:
2039:
2037:
2034:
2032:
2029:
2027:
2024:
2022:
2019:
2017:
2014:
2012:
2009:
2007:
2004:
2002:
1999:
1998:
1996:
1992:
1986:
1983:
1982:
1980:
1978:
1974:
1968:
1967:Trichosanthin
1965:
1964:
1962:
1960:
1956:
1950:
1947:
1946:
1944:
1942:
1938:
1931:
1928:
1927:
1925:
1923:
1919:
1916:
1912:
1906:
1905:Ritonavir (r)
1903:
1901:
1898:
1897:
1895:
1891:
1885:
1882:
1880:
1877:
1875:
1872:
1870:
1867:
1865:
1862:
1860:
1857:
1855:
1852:
1850:
1847:
1845:
1842:
1840:
1837:
1835:
1832:
1830:
1827:
1825:
1822:
1820:
1817:
1815:
1812:
1810:
1807:
1804:
1801:
1798:
1795:
1792:
1789:
1787:
1784:
1781:
1778:
1776:
1773:
1771:
1768:
1765:
1762:
1760:
1757:
1755:
1752:
1749:
1746:
1744:
1741:
1740:
1738:
1736:
1732:
1718:
1715:
1713:
1710:
1706:
1703:
1701:
1698:
1696:
1693:
1692:
1691:
1690:
1686:
1685:
1683:
1679:
1673:
1670:
1668:
1665:
1663:
1660:
1659:
1657:
1653:
1650:
1648:
1646:
1640:
1636:
1630:
1627:
1625:
1622:
1620:
1616:
1612:
1611:
1608:
1605:
1603:
1600:
1598:
1595:
1593:
1590:
1588:
1585:
1583:
1580:
1578:
1575:
1573:
1570:
1568:
1565:
1563:
1560:
1558:
1555:
1553:
1550:
1548:
1545:
1543:
1540:
1538:
1534:
1530:
1529:
1527:
1525:
1519:
1516:
1513:
1507:
1497:
1494:
1492:
1489:
1486:
1483:
1480:
1477:
1476:
1474:
1470:
1464:
1461:
1459:
1456:
1454:
1451:
1449:
1446:
1444:
1441:
1439:
1436:
1434:
1431:
1430:
1428:
1424:
1421:
1419:
1417:
1411:
1407:
1401:
1398:
1396:
1393:
1391:
1388:
1387:
1385:
1383:
1379:
1373:
1370:
1368:
1365:
1363:
1360:
1358:
1355:
1353:
1350:
1348:
1345:
1343:
1340:
1339:
1337:
1333:
1329:
1322:
1318:
1317:
1313:
1310:
1306:
1302:
1301:
1297:
1294:
1290:
1286:
1283:
1281:
1277:
1276:
1272:
1269:
1265:
1264:
1260:
1259:
1257:
1255:
1253:
1247:
1243:
1237:
1234:
1233:
1231:
1229:
1225:
1220:
1216:
1213:used against
1212:
1208:
1201:
1196:
1194:
1189:
1187:
1182:
1181:
1178:
1171:
1168:
1165:
1164:brief history
1161:
1160:
1148:
1144:
1140:
1133:
1125:
1121:
1116:
1111:
1107:
1103:
1099:
1092:
1076:
1070:
1054:
1053:
1048:
1042:
1034:
1030:
1026:
1022:
1018:
1011:
1005:
1000:
994:
988:
980:
976:
972:
968:
964:
960:
956:
952:
944:
925:
919:
911:
909:9780857111562
905:
901:
895:
880:
874:
861:
857:
853:
849:
843:
841:
832:
828:
823:
818:
813:
808:
804:
800:
796:
789:
781:
774:
755:
749:
747:
745:
740:
731:
728:
726:
723:
721:
718:
716:
713:
712:
706:
704:
700:
699:kidney stones
696:
692:
688:
687:lipodystrophy
678:
676:
672:
668:
653:
649:
645:
641:
637:
635:June 23, 2006
634:
631:
627:
625:
622:
619:
617:
614:
613:
609:
607:June 22, 2005
606:
603:
601:
598:
595:
593:
590:
589:
585:
580:
576:
573:
570:
568:
565:
562:
560:
559:Fosamprenavir
557:
556:
551:
549:June 20, 2003
548:
545:
541:
539:
536:
533:
531:
528:
527:
523:
519:
516:
513:
509:
507:
504:
501:
499:
496:
495:
490:
487:
484:
480:
478:
475:
472:
470:
467:
466:
462:
459:
456:
452:
450:
447:
444:
442:
439:
438:
434:
431:
428:
424:
422:
419:
416:
414:
411:
410:
405:
403:March 1, 1996
402:
399:
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390:
387:
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382:
381:
377:
373:
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363:
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345:
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336:
333:
330:
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318:
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284:
279:
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269:
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186:
182:
179:
177:
174:
172:
169:
167:
164:
162:
159:
157:
154:
152:
151:Fosamprenavir
149:
147:
144:
142:
139:
137:
134:
133:
132:
128:
125:
122:
121:
119:
116:
114:
110:
106:
102:
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90:
86:
82:
78:
74:
64:
54:
50:
48:
42:
39:This article
37:
28:
27:
22:
3314:
3281:Exopeptidase
3276:
3251:Ribonuclease
3217:Janus kinase
3102:Lipoxygenase
3078:5α-Reductase
3000:Pharmacology
2861:Molnupiravir
2856:Mericitabine
2826:Deuremidevir
2800:Simnotrelvir
2785:Nirmatrelvir
2775:Ibuzatrelvir
2761:3CL protease
2690:
2662:
2619:
2612:Picornavirus
2534:Uprifosbuvir
2432:Pibrentasvir
2383:Voxilaprevir
2353:Paritaprevir
2221:
2021:Cyanovirin-N
2011:Calanolide A
1687:
1681:2 generation
1655:1 generation
1642:
1613:
1592:Elvucitabine
1582:Apricitabine
1531:
1472:2 generation
1426:1 generation
1413:
1409:
1400:Fipravirimat
1314:
1309:Semzuvolimab
1298:
1289:Cenicriviroc
1273:
1261:
1249:
1141:(277): 1–4.
1138:
1132:
1108:(3): 243–4.
1105:
1101:
1091:
1079:. Retrieved
1069:
1057:. Retrieved
1050:
1041:
1024:
1020:
1010:
999:
987:
954:
950:
943:
931:. Retrieved
918:
899:
894:
882:. Retrieved
873:
863:, retrieved
851:
805:(17): 9124.
802:
798:
788:
773:
761:. Retrieved
705:(Crixivan).
684:
681:Side effects
671:nirmatrelvir
664:
584:slow release
300:
296:
280:
273:
264:Simnotrelvir
259:Nirmatrelvir
248:
224:Paritaprevir
198:
130:
117:
76:
72:
71:
61:January 2020
58:
44:
40:
3330:Oxytocinase
3138:Transferase
2942:from market
2907:Merimepodib
2881:Triazavirin
2876:Taribavirin
2836:Galidesivir
2831:Favipiravir
2795:Rupintrivir
2780:Lufotrelvir
2770:Ensitrelvir
2715:Laninamivir
2701:Oseltamivir
2683:Rimantadine
2621:viral entry
2602:Bulevirtide
2594:Hepatitis D
2452:Velpatasvir
2407:Daclatasvir
2402:Coblopasvir
2378:Vedroprevir
2348:Narlaprevir
2343:Grazoprevir
2338:Glecaprevir
2333:Faldaprevir
2313:Asunaprevir
2291:Hepatitis C
2272:(primarily
2222:recommended
2197:from market
2147:Lersivirine
2122:Capravirine
2061:Miltefosine
2046:Griffithsin
2041:Fosdevirine
1587:Censavudine
1217:(primarily
1059:23 December
652:leapfrogged
276:antibiotics
254:Ensitrelvir
219:Glecaprevir
214:Grazoprevir
204:Asunaprevir
97:hepatitis C
81:medications
2917:Presatovir
2912:Moroxydine
2846:Remdesivir
2804:+ritonavir
2789:+ritonavir
2733:Interferon
2678:Amantadine
2673:Adapromine
2656:Umifenovir
2626:Pleconaril
2529:Radalbuvir
2524:TMC-647055
2514:Sofosbuvir
2509:Setrobuvir
2489:Deleobuvir
2474:Beclabuvir
2447:Samatasvir
2437:Ravidasvir
2427:Ombitasvir
2417:Ledipasvir
2373:Vaniprevir
2368:Telaprevir
2363:Sovaprevir
2358:Simeprevir
2328:Danoprevir
2323:Ciluprevir
2318:Boceprevir
2270:antivirals
2152:Lodenosine
2132:Droxinavir
2117:Brecanavir
2112:Atevirdine
2076:Seliciclib
2071:Scytovirin
1985:Elipovimab
1930:TRIM5alpha
1607:Stampidine
1512:inhibitors
1496:TMC-310911
1395:BMS-955176
1293:Leronlimab
1285:Vicriviroc
933:5 November
884:8 November
865:2024-06-20
763:5 November
736:References
592:Tipranavir
530:Atazanavir
469:Amprenavir
441:Nelfinavir
352:Saquinavir
334:Trade name
307:saquinavir
289:(–zomib).
234:Telaprevir
229:Simeprevir
209:Boceprevir
181:Tipranavir
176:Saquinavir
166:Nelfinavir
141:Atazanavir
136:Amprenavir
3231:Hydrolase
3195:Integrase
3110:Aromatase
3047:Substrate
2952:Phase III
2940:Withdrawn
2871:Ribavirin
2841:GS-441524
2711:Peramivir
2706:Zanamivir
2651:Pimodivir
2637:influenza
2519:Tegobuvir
2494:Filibuvir
2484:Dasabuvir
2422:Odalasvir
2267:RNA virus
2207:Phase III
2195:Withdrawn
2172:Telinavir
2167:Palinavir
2162:Mozenavir
2142:Emivirine
2137:Lasinavir
2107:Aplaviroc
2036:Foscarnet
2016:Ceragenin
1577:Amdoxovir
1390:Bevirimat
1367:BI 224436
1027:(34): 9.
703:indinavir
644:phase III
616:Darunavir
498:Lopinavir
473:Agenerase
413:Indinavir
384:Ritonavir
315:indinavir
311:ritonavir
171:Ritonavir
161:Lopinavir
156:Indinavir
146:Darunavir
105:proteases
3408:Category
3277:Protease
2442:Ruzasvir
2412:Elbasvir
2157:Loviride
1147:11364559
1124:12626882
979:26084893
971:17617272
860:31644200
831:34502033
709:See also
667:Paxlovid
620:Prezista
445:Viracept
417:Crixivan
249:–trelvir
101:COVID-19
93:HIV/AIDS
3303:Trypsin
2866:NITD008
2504:IDX-184
2499:GS-6620
2276:, also
2056:KP-1461
1602:Racivir
1372:MK-2048
1081:14 June
822:8430524
596:Aptivus
579:prodrug
534:Reyataz
502:Kaletra
378:(FDA).
337:Company
199:–previr
3357:(EC 4)
3233:(EC 3)
3140:(EC 2)
3100:1.13
3057:(EC 1)
2935:WHO-EM
2851:MK-608
2821:CMX521
2639:agents
2190:WHO-EM
2006:BIT225
2001:Abzyme
1932:(gene)
1619:NtRTIs
1514:(RTIs)
1145:
1122:
977:
969:
951:Lancet
906:
858:
829:
819:
697:, and
506:AbbVie
392:AbbVie
388:Norvir
346:Notes
340:Patent
313:, and
131:–navir
107:(e.g.
79:) are
3355:Lyase
3315:Mixed
3308:Renin
3286:DPP-4
3121:1.17
3115:COX-2
3108:1.14
3011:Class
2902:EICAR
2635:Anti-
2282:D06BB
2278:S01AD
1994:Other
1977:BNAbs
1537:NRTIs
1316:gp120
975:S2CID
927:(PDF)
757:(PDF)
640:OARAC
3371:4.2
3363:4.1
3338:3.5
3275:3.4
3257:3.2
3239:3.1
3188:2.7
3180:2.6
3167:2.5
3161:PARP
3159:2.4
3148:COMT
3146:2.1
3092:1.5
3084:1.4
3076:1.3
3063:1.1
2462:NS5B
2393:NS5A
2280:and
2219:DHHS
1275:CCR5
1263:gp41
1143:PMID
1120:PMID
1083:2024
1061:2021
967:PMID
935:2016
904:ISBN
886:2013
856:PMID
827:PMID
765:2016
331:Name
99:and
3291:ACE
2300:NS3
2274:J05
1300:CD4
1219:J05
1215:HIV
1110:doi
1052:NPR
1029:doi
959:doi
955:370
817:PMC
807:doi
191:NS3
77:PIs
3410::
3279::
3002::
2948::
2713:,
2304:4A
2203::
1307:,
1291:,
1287:,
1209::
1162:A
1118:.
1106:32
1104:.
1100:.
1049:.
1025:84
1023:.
1019:.
973:.
965:.
953:.
850:,
839:^
825:.
815:.
803:22
801:.
797:.
743:^
693:,
689:,
577:A
463:—
435:—
309:,
195:4A
115:.
95:,
2992:e
2985:t
2978:v
2806:)
2802:(
2791:)
2787:(
2717:)
2699:(
2694:/
2685:)
2671:(
2666:/
2623::
2302:/
2284:)
2259:e
2252:t
2245:v
2217:°
1805:°
1799:°
1793:°
1782:°
1766:°
1750:°
1647:)
1643:(
1621::
1617:/
1539::
1535:/
1487:°
1481:°
1418:)
1414:(
1323:)
1319:(
1311:)
1303:(
1295:)
1278:(
1270:)
1266:(
1254:)
1250:(
1221:)
1199:e
1192:t
1185:v
1149:.
1126:.
1112::
1085:.
1063:.
1035:.
1031::
981:.
961::
937:.
912:.
888:.
833:.
809::
767:.
604:—
571:—
193:/
75:(
63:)
59:(
49:.
23:.
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