332:
43:
308:
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.
502:
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
959:
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".
417:
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.
1655:
328:, 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.
592:
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
563:
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.
1839:
1844:
1790:
1262:
2229:
1426:
740:
940:. 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
289:, 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.
1796:
1854:
1774:
255:
1859:
1807:
1208:
1829:
1813:
735:
3001:
1824:
1834:
2268:
2101:
1745:
1174:
1057:
2945:
2200:
2091:
806:"Exploring the Binding Mechanism of PF-07321332 SARS-CoV-2 Protease Inhibitor through Molecular Dynamics and Binding Free Energy Simulations"
63:
764:
2590:
1849:
335:
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
3335:
3179:
3138:
1864:
293:
3104:
2575:
1201:
918:
331:
292:
In addition to those non-human proteases listed above, inhibitors of human proteases may be used to treat cancer. See the articles
3296:
1874:
1758:
934:
1148:
Capaldini, L. (1997). "Protease inhibitors' metabolic side effects: cholesterol, triglycerides, blood sugar, and "Crix belly"".
1085:
3210:
2994:
1884:
1869:
1649:
1629:
1547:
1532:
1520:
730:
3256:
3163:
1764:
661:
combination for first-line therapy. Darunavir is the first drug in a long time that did not come with a price increase. It
3350:
3184:
1186:
3424:
3383:
3375:
2261:
1194:
386:
251:
31:
3279:
3269:
3251:
3192:
3096:
2962:
2217:
3133:
3075:
3038:
2987:
653:
recommended treatment option for treatment-naĂŻve and treatment-experienced adults and adolescents. Several ongoing
57:
3399:
3222:
3088:
1028:"Retaining Efficacy Against Evasive HIV: Darunavir analog to AIDS-virus shapeshifters: Resistance may be futile"
3355:
3217:
2565:
2041:
1951:
1819:
1780:
705:
122:) and blocking proteolytic cleavage of protein precursors that are necessary for the production of infectious
2246:
765:"The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances"
3330:
3308:
3274:
3033:
2950:
2702:
2254:
2205:
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3227:
3200:
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2580:
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459:
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610:
548:
297:
3205:
3120:
1894:
1753:
1625:
1543:
1342:
1221:
725:
658:
657:
trials are showing a high efficiency for the darunavir/ritonavir combination being superior to the
532:
313:
134:
129:
Protease inhibitors that have been developed and are currently used in clinical practice include:
3043:
2751:
2656:
2388:
985:
597:
version of amprenavir and thus reduces the number of pills required versus standard amprenavir.
503:
discontinued by the manufacturer
December 31, 2004, as it has been superseded by fosamprenavir.
2529:
2182:
2177:
1109:"Protease inhibitor-associated diabetes mellitus: A potential cause of morbidity and mortality"
1003:
688:, and ritonavir, which inhibits the metabolism of nirmatrelvir, thereby prolonging its effect.
3313:
2912:
2452:
2036:
1699:
1153:
1130:
977:
914:
866:
837:
198:
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1120:
1039:
969:
827:
817:
685:
3318:
3125:
2137:
2096:
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1027:
935:"Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents"
577:
487:
99:
889:
865:, Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases, 2012,
3171:
3158:
3065:
2956:
2896:
2706:
2475:
2280:
2211:
1987:
1969:
1932:
1217:
832:
805:
701:
654:
431:
137:
119:
17:
973:
114:. These protease inhibitors prevent viral replication by selectively binding to viral
3418:
3301:
2489:
1977:
1727:
1562:
1448:
1125:
1108:
790:
697:
569:
161:
989:
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2836:
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2021:
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681:
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274:
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234:
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2301:
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2056:
2051:
1715:
1682:
1597:
1577:
1372:
1352:
1331:
1278:
1246:
1177:
of the development of protease inhibitors by
Hoffman La Roche, Abbott, and Merck
516:
402:
285:
Given the specificity of the target of these drugs there is the risk, like with
264:
229:
224:
214:
107:
91:
858:
2927:
2922:
2856:
2743:
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2674:
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2519:
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1995:
1940:
1910:
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554:
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244:
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151:
146:
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2310:
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2046:
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1959:
1915:
1672:
1587:
1572:
1495:
1468:
1458:
1453:
1400:
1377:
1290:
713:
665:
two other approved drugs of its type, and is matching the price of a third.
626:
508:
423:
394:
325:
321:
201:
181:
171:
166:
156:
115:
1157:
1134:
981:
870:
841:
1058:"First doses of Paxlovid, Pfizer's new COVID pill, are released to states"
680:, was approved in December 2021 to treat COVID-19. It is a combination of
2422:
2167:
1552:
822:
677:
111:
103:
95:
1014:
863:
LiverTox: Clinical and
Research Information on Drug-Induced Liver Injury
2876:
2514:
2509:
2235:
2066:
1612:
1382:
1002:
Liz
Highleyman, Patient Advocates Commend Pricing of New PI Darunavir,
789:
Programme on
International Nonproprietary Names (INN) (February 2023).
589:
1180:
3080:
2861:
2831:
2016:
2011:
123:
535:). AbbVie was part of Abbott Laboratories when patent was granted.
3365:
1326:
791:"Pre-stems: Suffixes used in the selection of INN - February 2023"
712:. This lipodystrophy is colloquially known as "Crix belly", after
650:
330:
531:
Is only marketed as a fixed-dose combination with ritonavir (see
2472:
2403:
2314:
1285:
1273:
205:
2983:
2250:
1190:
913:(69 ed.). Pharmaceutical Pr. March 31, 2015. p. 426.
27:
Class of antiviral drugs used to treat HIV/AIDS and hepatitis C
1310:
1225:
1062:
36:
1088:. DailyMed, US National Library of Medicine. 18 October 2023
1004:
http://www.hivandhepatitis.com/recent/2006/ad1/063006_a.html
1840:
Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
1845:
Elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil
804:
Ahmad B, Batool M, Ain QU, Kim MS, Choi S (August 2021).
1791:
Darunavir/cobicistat/emtricitabine/tenofovir alafenamide
1015:
Darunavir - first molecule to treat drug-resistant HIV
741:
Discovery and development of HIV-protease inhibitors
3392:
3364:
3240:
3147:
3064:
3057:
3021:
2905:
2824:
2770:
2742:
2735:
2645:
2621:
2603:
2553:
2471:
2402:
2309:
2300:
2110:
2004:
1986:
1968:
1950:
1931:
1924:
1903:
1744:
1691:
1665:
1648:
1531:
1519:
1482:
1436:
1419:
1391:
1341:
1255:
1237:
684:, a protease inhibitor targeted to the SARS-CoV-2
1797:Dolutegravir/emtricitabine/tenofovir alafenamide
890:"HIV Surveillance --- United States, 1981--2008"
1855:Emtricitabine/rilpivirine/tenofovir alafenamide
1775:Bictegravir/emtricitabine/tenofovir alafenamide
1113:Journal of Acquired Immune Deficiency Syndromes
256:severe acute respiratory syndrome coronavirus 2
1860:Emtricitabine/rilpivirine/tenofovir disoproxil
1346:(Integrase strand transfer inhibitors (INSTI))
52:needs attention from an expert in Pharmacology
2995:
2262:
1808:Dolutegravir/lamivudine/tenofovir alafenamide
1202:
385:The first protease inhibitor approved by the
312:Protease inhibitors were the second class of
8:
1830:Efavirenz/emtricitabine/tenofovir disoproxil
1814:Dolutegravir/lamivudine/tenofovir disoproxil
736:Discovery and development of NS5A inhibitors
696:Protease inhibitors can cause a syndrome of
316:developed. The first members of this class,
810:International Journal of Molecular Sciences
759:
757:
755:
3061:
3002:
2988:
2980:
2739:
2306:
2269:
2255:
2247:
1928:
1825:Doravirine/lamivudine/tenofovir disoproxil
1662:
1528:
1433:
1209:
1195:
1187:
1183:US Department of Health and Human Services
1835:Efavirenz/lamivudine/tenofovir disoproxil
1124:
831:
821:
676:A drug combination targeting SARS-CoV-2,
2102:Zinc finger protein transcription factor
338:
751:
66:may be able to help recruit an expert.
672:Non-antiretroviral antiviral activity
30:For natural protease inhibitors, see
7:
853:
851:
2591:Sofosbuvir/velpatasvir/voxilaprevir
1850:Emtricitabine/tenofovir alafenamide
621:Also known as tipranavir disodium.
1865:Emtricitabine/tenofovir disoproxil
1086:"Paxlovid: Drug label information"
304:Antiretroviral protease inhibitors
294:matrix metalloproteinase inhibitor
98:. Some of the most well known are
25:
2576:Ombitasvir/paritaprevir/ritonavir
387:U.S. Food and Drug Administration
2238:. Formerly or rarely used agent.
1875:Lamivudine/nevirapine/zidovudine
1759:Abacavir/dolutegravir/lamivudine
1126:10.1097/00126334-200303010-00001
254:(including, but not limited to,
41:
2042:Epigallocatechin gallate (EGCG)
1885:Lamivudine/tenofovir disoproxil
1870:Lamivudine/nevirapine/stavudine
1032:Chemical & Engineering News
731:Reverse-transcriptase inhibitor
208:protease inhibitors—class stem
1765:Abacavir/lamivudine/zidovudine
1:
2317:protease inhibitors (–previr)
1181:HIV/AIDS Treatment Guidelines
974:10.1016/S0140-6736(07)61049-6
911:British National Formulary 69
94:that act by interfering with
793:. World Health Organization.
649:As of 2016, darunavir is an
252:3-chymotrypsin-like protease
96:enzymes that cleave proteins
32:Protease inhibitor (biology)
1640:Tenofovir alafenamide (TAF)
859:"Protease Inhibitors (HIV)"
770:. World Health Organization
54:. The specific problem is:
3441:
3180:Dihydropteroate synthetase
3039:Non-competitive inhibition
1635:Tenofovir disoproxil (TDF)
58:Template:Enzyme inhibition
29:
3400:Steroidogenesis inhibitor
2940:
2195:
1656:Discovery and development
1427:Discovery and development
1263:Discovery and development
1044:10.1021/cen-v084n034.p009
3336:Matrix metalloproteinase
3139:Ribonucleotide reductase
3034:Uncompetitive inhibition
2703:neuraminidase inhibitors
2566:Glecaprevir/pibrentasvir
1952:Transcription inhibitors
1904:Pharmacokinetic boosters
1820:Dolutegravir/rilpivirine
1781:Cabotegravir/rilpivirine
1421:Protease Inhibitors (PI)
706:diabetes mellitus type 2
258:) inhibitors—class stem
64:WikiProject Pharmacology
3105:Dihydrofolate reductase
2236:initial regimen options
1802:Dolutegravir/lamivudine
1279:Enfuvirtide (ENF, T-20)
1257:Entry/fusion inhibitors
56:non-antiviral types in
18:HIV protease inhibitors
3201:Nucleotidyltransferase
3029:Competitive inhibition
2906:Multiple/Unknown/Other
2675:adamantane derivatives
2586:Sofosbuvir/velpatasvir
2581:Sofosbuvir/daclatasvir
2077:Portmanteau inhibitors
1970:Translation inhibitors
1880:Lamivudine/raltegravir
1650:Non-nucleoside (NNRTI)
1608:Islatravir (EFdA, ISL)
336:
140:inhibitors—class stem
3211:Reverse transcriptase
2774:inhibitors (–trelvir)
2762:Peginterferon alfa-2b
2757:Peginterferon alfa-2a
2571:Ledipasvir/sofosbuvir
2092:Synergistic enhancers
1890:Lamivudine/zidovudine
1770:Atazanavir/cobicistat
1746:Combined formulations
1583:Zidovudine (AZT, ZDV)
1521:Reverse-transcriptase
1393:Maturation inhibitors
641:U.S. patent 6,248,775
555:U.S. patent 5,849,911
523:U.S. patent 5,914,332
494:U.S. patent 5,585,397
466:U.S. patent 5,484,926
438:U.S. patent 5,413,999
409:U.S. patent 5,541,206
377:U.S. patent 5,196,438
334:
102:widely used to treat
3257:Acetylcholinesterase
3164:Thymidylate synthase
2561:Elbasvir/grazoprevir
1933:Uncoating inhibitors
1786:Darunavir/cobicistat
1626:Nucleotide analogues
1544:Nucleoside analogues
1343:Integrase inhibitors
1222:antiretroviral drugs
823:10.3390/ijms22179124
635:Janssen Therapeutics
611:Boehringer Ingelheim
549:Bristol-Myers Squibb
314:antiretroviral drugs
298:proteasome inhibitor
3425:Protease inhibitors
3351:Histone deacetylase
3185:Farnesyltransferase
2478:inhibitors (–buvir)
2406:inhibitors (–asvir)
1925:Experimental agents
1895:Lopinavir/ritonavir
1754:Abacavir/lamivudine
1728:Elsulfavirine (ESV)
1563:Emtricitabine (FTC)
1449:Fosamprenavir (FPV)
1150:AIDS Treatment News
1107:Fantry, LE (2003).
726:The Proteolysis Map
659:lopinavir/ritonavir
533:lopinavir/ritonavir
367:Invirase, Fortovase
84:Protease inhibitors
3384:Carbonic anhydrase
3376:Dopa decarboxylase
3044:Suicide inhibition
2967:Never to phase III
2825:RNA pol inhibitors
2752:Interferon alfa 2b
2657:Baloxavir marboxil
2222:Never to phase III
1368:Elvitegravir (EVG)
1363:Dolutegravir (DTG)
1358:Cabotegravir (CAB)
1066:. 23 December 2021
528:September 15, 2000
337:
3412:
3411:
3408:
3407:
3280:Alpha-glucosidase
3270:Polygalacturonase
3252:Phosphodiesterase
3193:GABA transaminase
3097:Monoamine oxidase
3081:HMG-CoA reductase
3015:enzyme inhibition
2977:
2976:
2936:
2935:
2599:
2598:
2554:Combination drugs
2244:
2243:
2191:
2190:
2037:Diarylpyrimidines
1740:
1739:
1736:
1735:
1716:Rilpivirine (RPV)
1700:diarylpyrimidines
1683:Delavirdine (DLV)
1578:Zalcitabine (ddC)
1535:nucleotide (NRTI)
1515:
1514:
1373:Raltegravir (RAL)
1353:Bictegravir (BIC)
1332:Fostemsavir (FTR)
1247:Lenacapavir (LEN)
1239:Capsid inhibitors
1026:Borman S (2006).
669:
668:
460:Hoffmann–La Roche
371:Hoffmann–La Roche
354:FDA approval date
199:Hepatitis C virus
81:
80:
16:(Redirected from
3432:
3134:Xanthine oxidase
3076:Aldose reductase
3062:
3049:Mixed inhibition
3004:
2997:
2990:
2981:
2740:
2736:Multiple/general
2307:
2271:
2264:
2257:
2248:
2062:Hydroxycarbamide
1929:
1723:Doravirine (DOR)
1711:Etravirine (ETR)
1706:Dapivirine (DPV)
1678:Nevirapine (NVP)
1663:
1568:Lamivudine (3TC)
1558:Didanosine (ddI)
1529:
1502:Tipranavir (TPV)
1490:Atazanavir (ATV)
1474:Saquinavir (SQV)
1464:Nelfinavir (NFV)
1444:Amprenavir (APV)
1434:
1316:Ibalizumab (IBA)
1211:
1204:
1197:
1188:
1162:
1161:
1145:
1139:
1138:
1128:
1104:
1098:
1097:
1095:
1093:
1082:
1076:
1075:
1073:
1071:
1054:
1048:
1047:
1023:
1017:
1012:
1006:
1000:
994:
993:
956:
950:
949:
947:
945:
939:
931:
925:
924:
907:
901:
900:
898:
896:
886:
880:
879:
878:
877:
855:
846:
845:
835:
825:
801:
795:
794:
786:
780:
779:
777:
775:
769:
761:
686:3C-like protease
643:
585:October 20, 2003
557:
525:
496:
468:
440:
411:
382:December 6, 1995
379:
339:
76:
73:
67:
45:
44:
37:
21:
3440:
3439:
3435:
3434:
3433:
3431:
3430:
3429:
3415:
3414:
3413:
3404:
3388:
3360:
3236:
3223:Tyrosine kinase
3143:
3053:
3017:
3008:
2978:
2973:
2972:
2957:Clinical trials
2932:
2901:
2820:
2766:
2731:
2641:
2617:
2595:
2549:
2467:
2398:
2296:
2275:
2245:
2240:
2239:
2227:
2212:Clinical trials
2187:
2138:Dexelvucitabine
2106:
2097:Tre recombinase
2000:
1982:
1964:
1960:Tat antagonists
1946:
1920:
1899:
1732:
1687:
1673:Efavirenz (EFV)
1652:
1644:
1573:Stavudine (d4T)
1534:
1522:
1511:
1496:Darunavir (DRV)
1478:
1469:Ritonavir (RTV)
1459:Lopinavir (LPV)
1454:Indinavir (IDV)
1423:
1415:
1387:
1345:
1337:
1291:Maraviroc (MVC)
1259:
1251:
1233:
1218:Antiviral drugs
1215:
1170:
1165:
1147:
1146:
1142:
1106:
1105:
1101:
1091:
1089:
1084:
1083:
1079:
1069:
1067:
1056:
1055:
1051:
1025:
1024:
1020:
1013:
1009:
1001:
997:
968:(9581): 49–58.
958:
957:
953:
943:
941:
937:
933:
932:
928:
921:
909:
908:
904:
894:
892:
888:
887:
883:
875:
873:
857:
856:
849:
803:
802:
798:
788:
787:
783:
773:
771:
767:
763:
762:
753:
749:
722:
694:
674:
639:
578:GlaxoSmithKline
553:
521:
492:
488:GlaxoSmithKline
464:
436:
432:Merck & Co.
407:
375:
306:
283:
124:viral particles
100:antiviral drugs
77:
71:
68:
62:
46:
42:
35:
28:
23:
22:
15:
12:
11:
5:
3438:
3436:
3428:
3427:
3417:
3416:
3410:
3409:
3406:
3405:
3403:
3402:
3396:
3394:
3390:
3389:
3387:
3386:
3379:
3378:
3371:
3369:
3362:
3361:
3359:
3358:
3356:Beta-lactamase
3353:
3346:
3345:
3344:
3343:
3338:
3333:
3323:
3322:
3321:
3316:
3306:
3305:
3304:
3299:
3283:
3282:
3277:
3272:
3265:
3264:
3259:
3254:
3247:
3245:
3238:
3237:
3235:
3234:
3233:
3232:
3231:
3230:
3218:Protein kinase
3215:
3214:
3213:
3208:
3196:
3195:
3188:
3187:
3182:
3175:
3174:
3167:
3166:
3161:
3154:
3152:
3145:
3144:
3142:
3141:
3136:
3129:
3128:
3123:
3116:
3115:
3108:
3107:
3100:
3099:
3092:
3091:
3084:
3083:
3078:
3071:
3069:
3066:Oxidoreductase
3059:
3055:
3054:
3052:
3051:
3046:
3041:
3036:
3031:
3025:
3023:
3019:
3018:
3009:
3007:
3006:
2999:
2992:
2984:
2975:
2974:
2971:
2970:
2969:
2968:
2965:
2954:
2948:
2942:
2941:
2938:
2937:
2934:
2933:
2931:
2930:
2925:
2920:
2915:
2909:
2907:
2903:
2902:
2900:
2899:
2897:Valopicitabine
2894:
2889:
2884:
2879:
2874:
2869:
2864:
2859:
2854:
2849:
2844:
2839:
2834:
2828:
2826:
2822:
2821:
2819:
2818:
2808:
2803:
2793:
2788:
2783:
2777:
2775:
2768:
2767:
2765:
2764:
2759:
2754:
2748:
2746:
2737:
2733:
2732:
2730:
2729:
2719:
2714:
2698:
2697:
2691:
2686:
2670:
2669:
2664:
2659:
2653:
2651:
2643:
2642:
2640:
2639:
2627:
2625:
2619:
2618:
2616:
2615:
2609:
2607:
2601:
2600:
2597:
2596:
2594:
2593:
2588:
2583:
2578:
2573:
2568:
2563:
2557:
2555:
2551:
2550:
2548:
2547:
2542:
2537:
2532:
2527:
2522:
2517:
2512:
2507:
2502:
2497:
2492:
2487:
2481:
2479:
2476:RNA polymerase
2469:
2468:
2466:
2465:
2460:
2455:
2450:
2445:
2440:
2435:
2430:
2425:
2420:
2415:
2409:
2407:
2400:
2399:
2397:
2396:
2391:
2386:
2381:
2376:
2371:
2366:
2361:
2356:
2351:
2346:
2341:
2336:
2331:
2326:
2320:
2318:
2304:
2298:
2297:
2276:
2274:
2273:
2266:
2259:
2251:
2242:
2241:
2226:
2225:
2224:
2223:
2220:
2209:
2203:
2197:
2196:
2193:
2192:
2189:
2188:
2186:
2185:
2180:
2175:
2170:
2165:
2160:
2155:
2150:
2145:
2140:
2135:
2130:
2125:
2120:
2114:
2112:
2108:
2107:
2105:
2104:
2099:
2094:
2089:
2084:
2079:
2074:
2069:
2064:
2059:
2054:
2049:
2044:
2039:
2034:
2029:
2024:
2019:
2014:
2008:
2006:
2002:
2001:
1999:
1998:
1992:
1990:
1984:
1983:
1981:
1980:
1974:
1972:
1966:
1965:
1963:
1962:
1956:
1954:
1948:
1947:
1945:
1944:
1937:
1935:
1926:
1922:
1921:
1919:
1918:
1913:
1911:Cobicistat (c)
1907:
1905:
1901:
1900:
1898:
1897:
1892:
1887:
1882:
1877:
1872:
1867:
1862:
1857:
1852:
1847:
1842:
1837:
1832:
1827:
1822:
1817:
1811:
1805:
1799:
1794:
1788:
1783:
1778:
1772:
1767:
1762:
1756:
1750:
1748:
1742:
1741:
1738:
1737:
1734:
1733:
1731:
1730:
1725:
1720:
1719:
1718:
1713:
1708:
1695:
1693:
1689:
1688:
1686:
1685:
1680:
1675:
1669:
1667:
1660:
1646:
1645:
1643:
1642:
1637:
1621:
1620:
1615:
1610:
1605:
1600:
1595:
1590:
1585:
1580:
1575:
1570:
1565:
1560:
1555:
1553:Abacavir (ABC)
1539:
1537:
1533:Nucleoside and
1526:
1517:
1516:
1513:
1512:
1510:
1509:
1504:
1499:
1493:
1486:
1484:
1480:
1479:
1477:
1476:
1471:
1466:
1461:
1456:
1451:
1446:
1440:
1438:
1431:
1417:
1416:
1414:
1413:
1408:
1403:
1397:
1395:
1389:
1388:
1386:
1385:
1380:
1375:
1370:
1365:
1360:
1355:
1349:
1347:
1339:
1338:
1336:
1335:
1323:
1307:
1293:
1282:
1269:
1267:
1253:
1252:
1250:
1249:
1243:
1241:
1235:
1234:
1216:
1214:
1213:
1206:
1199:
1191:
1185:
1184:
1178:
1169:
1168:External links
1166:
1164:
1163:
1140:
1099:
1077:
1049:
1018:
1007:
995:
951:
926:
919:
902:
881:
847:
796:
781:
750:
748:
745:
744:
743:
738:
733:
728:
721:
718:
702:hyperlipidemia
693:
690:
673:
670:
667:
666:
647:
644:
637:
632:
629:
623:
622:
619:
616:
613:
608:
605:
599:
598:
586:
583:
580:
575:
574:Lexiva, Telzir
572:
566:
565:
561:
558:
551:
546:
543:
537:
536:
529:
526:
519:
514:
511:
505:
504:
500:
499:April 15, 1999
497:
490:
485:
482:
476:
475:
472:
471:March 14, 1997
469:
462:
457:
454:
448:
447:
444:
443:March 13, 1996
441:
434:
429:
426:
420:
419:
415:
412:
405:
400:
397:
391:
390:
383:
380:
373:
368:
365:
359:
358:
355:
352:
349:
346:
343:
305:
302:
296:(–mastat) and
282:
281:
279:
278:
277:
272:
267:
249:
248:
247:
242:
237:
232:
227:
222:
217:
196:
195:
194:
189:
184:
179:
174:
169:
164:
159:
154:
149:
138:HIV-1 protease
135:Antiretroviral
131:
120:HIV-1 protease
79:
78:
49:
47:
40:
26:
24:
14:
13:
10:
9:
6:
4:
3:
2:
3437:
3426:
3423:
3422:
3420:
3401:
3398:
3397:
3395:
3393:Miscellaneous
3391:
3385:
3381:
3380:
3377:
3373:
3372:
3370:
3367:
3363:
3357:
3354:
3352:
3348:
3347:
3342:
3339:
3337:
3334:
3332:
3331:Enkephalinase
3329:
3328:
3327:
3324:
3320:
3317:
3315:
3312:
3311:
3310:
3309:Endopeptidase
3307:
3303:
3300:
3298:
3295:
3294:
3293:
3289:
3285:
3284:
3281:
3278:
3276:
3275:Neuraminidase
3273:
3271:
3267:
3266:
3263:
3260:
3258:
3255:
3253:
3249:
3248:
3246:
3243:
3239:
3229:
3226:
3225:
3224:
3221:
3220:
3219:
3216:
3212:
3209:
3207:
3204:
3203:
3202:
3198:
3197:
3194:
3190:
3189:
3186:
3183:
3181:
3177:
3176:
3173:
3169:
3168:
3165:
3162:
3160:
3156:
3155:
3153:
3150:
3146:
3140:
3137:
3135:
3131:
3130:
3127:
3124:
3122:
3118:
3117:
3114:
3110:
3109:
3106:
3102:
3101:
3098:
3094:
3093:
3090:
3086:
3085:
3082:
3079:
3077:
3073:
3072:
3070:
3067:
3063:
3060:
3056:
3050:
3047:
3045:
3042:
3040:
3037:
3035:
3032:
3030:
3027:
3026:
3024:
3020:
3016:
3012:
3005:
3000:
2998:
2993:
2991:
2986:
2985:
2982:
2966:
2964:
2961:
2960:
2958:
2955:
2952:
2949:
2947:
2944:
2943:
2939:
2929:
2926:
2924:
2921:
2919:
2916:
2914:
2911:
2910:
2908:
2904:
2898:
2895:
2893:
2890:
2888:
2885:
2883:
2880:
2878:
2875:
2873:
2870:
2868:
2865:
2863:
2860:
2858:
2855:
2853:
2850:
2848:
2845:
2843:
2840:
2838:
2835:
2833:
2830:
2829:
2827:
2823:
2816:
2812:
2809:
2807:
2804:
2801:
2797:
2794:
2792:
2789:
2787:
2784:
2782:
2779:
2778:
2776:
2773:
2769:
2763:
2760:
2758:
2755:
2753:
2750:
2749:
2747:
2745:
2741:
2738:
2734:
2727:
2723:
2720:
2718:
2715:
2713:
2709:
2708:
2707:release phase
2704:
2700:
2699:
2695:
2692:
2690:
2687:
2685:
2681:
2680:
2679:M2 inhibitors
2676:
2672:
2671:
2668:
2665:
2663:
2660:
2658:
2655:
2654:
2652:
2649:
2644:
2638:
2635:
2633:
2629:
2628:
2626:
2624:
2620:
2614:
2611:
2610:
2608:
2606:
2602:
2592:
2589:
2587:
2584:
2582:
2579:
2577:
2574:
2572:
2569:
2567:
2564:
2562:
2559:
2558:
2556:
2552:
2546:
2543:
2541:
2538:
2536:
2533:
2531:
2528:
2526:
2523:
2521:
2518:
2516:
2513:
2511:
2508:
2506:
2503:
2501:
2498:
2496:
2493:
2491:
2490:Bemnifosbuvir
2488:
2486:
2483:
2482:
2480:
2477:
2474:
2470:
2464:
2461:
2459:
2456:
2454:
2451:
2449:
2446:
2444:
2441:
2439:
2436:
2434:
2431:
2429:
2426:
2424:
2421:
2419:
2416:
2414:
2411:
2410:
2408:
2405:
2401:
2395:
2392:
2390:
2387:
2385:
2382:
2380:
2377:
2375:
2372:
2370:
2367:
2365:
2362:
2360:
2357:
2355:
2352:
2350:
2347:
2345:
2342:
2340:
2337:
2335:
2332:
2330:
2327:
2325:
2322:
2321:
2319:
2316:
2312:
2308:
2305:
2303:
2299:
2294:
2290:
2286:
2282:
2279:
2272:
2267:
2265:
2260:
2258:
2253:
2252:
2249:
2237:
2234:
2231:
2221:
2219:
2216:
2215:
2213:
2210:
2207:
2204:
2202:
2199:
2198:
2194:
2184:
2181:
2179:
2176:
2174:
2171:
2169:
2166:
2164:
2161:
2159:
2156:
2154:
2151:
2149:
2146:
2144:
2141:
2139:
2136:
2134:
2131:
2129:
2126:
2124:
2121:
2119:
2116:
2115:
2113:
2111:Failed agents
2109:
2103:
2100:
2098:
2095:
2093:
2090:
2088:
2085:
2083:
2080:
2078:
2075:
2073:
2070:
2068:
2065:
2063:
2060:
2058:
2055:
2053:
2050:
2048:
2045:
2043:
2040:
2038:
2035:
2033:
2030:
2028:
2025:
2023:
2020:
2018:
2015:
2013:
2010:
2009:
2007:
2003:
1997:
1994:
1993:
1991:
1989:
1985:
1979:
1978:Trichosanthin
1976:
1975:
1973:
1971:
1967:
1961:
1958:
1957:
1955:
1953:
1949:
1942:
1939:
1938:
1936:
1934:
1930:
1927:
1923:
1917:
1916:Ritonavir (r)
1914:
1912:
1909:
1908:
1906:
1902:
1896:
1893:
1891:
1888:
1886:
1883:
1881:
1878:
1876:
1873:
1871:
1868:
1866:
1863:
1861:
1858:
1856:
1853:
1851:
1848:
1846:
1843:
1841:
1838:
1836:
1833:
1831:
1828:
1826:
1823:
1821:
1818:
1815:
1812:
1809:
1806:
1803:
1800:
1798:
1795:
1792:
1789:
1787:
1784:
1782:
1779:
1776:
1773:
1771:
1768:
1766:
1763:
1760:
1757:
1755:
1752:
1751:
1749:
1747:
1743:
1729:
1726:
1724:
1721:
1717:
1714:
1712:
1709:
1707:
1704:
1703:
1702:
1701:
1697:
1696:
1694:
1690:
1684:
1681:
1679:
1676:
1674:
1671:
1670:
1668:
1664:
1661:
1659:
1657:
1651:
1647:
1641:
1638:
1636:
1633:
1631:
1627:
1623:
1622:
1619:
1616:
1614:
1611:
1609:
1606:
1604:
1601:
1599:
1596:
1594:
1591:
1589:
1586:
1584:
1581:
1579:
1576:
1574:
1571:
1569:
1566:
1564:
1561:
1559:
1556:
1554:
1551:
1549:
1545:
1541:
1540:
1538:
1536:
1530:
1527:
1524:
1518:
1508:
1505:
1503:
1500:
1497:
1494:
1491:
1488:
1487:
1485:
1481:
1475:
1472:
1470:
1467:
1465:
1462:
1460:
1457:
1455:
1452:
1450:
1447:
1445:
1442:
1441:
1439:
1435:
1432:
1430:
1428:
1422:
1418:
1412:
1409:
1407:
1404:
1402:
1399:
1398:
1396:
1394:
1390:
1384:
1381:
1379:
1376:
1374:
1371:
1369:
1366:
1364:
1361:
1359:
1356:
1354:
1351:
1350:
1348:
1344:
1340:
1333:
1329:
1328:
1324:
1321:
1317:
1313:
1312:
1308:
1305:
1301:
1297:
1294:
1292:
1288:
1287:
1283:
1280:
1276:
1275:
1271:
1270:
1268:
1266:
1264:
1258:
1254:
1248:
1245:
1244:
1242:
1240:
1236:
1231:
1227:
1224:used against
1223:
1219:
1212:
1207:
1205:
1200:
1198:
1193:
1192:
1189:
1182:
1179:
1176:
1175:brief history
1172:
1171:
1167:
1159:
1155:
1151:
1144:
1141:
1136:
1132:
1127:
1122:
1118:
1114:
1110:
1103:
1100:
1087:
1081:
1078:
1065:
1064:
1059:
1053:
1050:
1045:
1041:
1037:
1033:
1029:
1022:
1019:
1016:
1011:
1008:
1005:
999:
996:
991:
987:
983:
979:
975:
971:
967:
963:
955:
952:
936:
930:
927:
922:
920:9780857111562
916:
912:
906:
903:
891:
885:
882:
872:
868:
864:
860:
854:
852:
848:
843:
839:
834:
829:
824:
819:
815:
811:
807:
800:
797:
792:
785:
782:
766:
760:
758:
756:
752:
746:
742:
739:
737:
734:
732:
729:
727:
724:
723:
719:
717:
715:
711:
710:kidney stones
707:
703:
699:
698:lipodystrophy
691:
689:
687:
683:
679:
671:
664:
660:
656:
652:
648:
646:June 23, 2006
645:
642:
638:
636:
633:
630:
628:
625:
624:
620:
618:June 22, 2005
617:
614:
612:
609:
606:
604:
601:
600:
596:
591:
587:
584:
581:
579:
576:
573:
571:
570:Fosamprenavir
568:
567:
562:
560:June 20, 2003
559:
556:
552:
550:
547:
544:
542:
539:
538:
534:
530:
527:
524:
520:
518:
515:
512:
510:
507:
506:
501:
498:
495:
491:
489:
486:
483:
481:
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458:
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450:
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439:
435:
433:
430:
427:
425:
422:
421:
416:
414:March 1, 1996
413:
410:
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404:
401:
398:
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393:
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388:
384:
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378:
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366:
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333:
329:
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197:
193:
190:
188:
185:
183:
180:
178:
175:
173:
170:
168:
165:
163:
162:Fosamprenavir
160:
158:
155:
153:
150:
148:
145:
144:
143:
139:
136:
133:
132:
130:
127:
125:
121:
117:
113:
109:
105:
101:
97:
93:
89:
85:
75:
65:
61:
59:
53:
50:This article
48:
39:
38:
33:
19:
3325:
3292:Exopeptidase
3287:
3262:Ribonuclease
3228:Janus kinase
3113:Lipoxygenase
3089:5α-Reductase
3011:Pharmacology
2872:Molnupiravir
2867:Mericitabine
2837:Deuremidevir
2811:Simnotrelvir
2796:Nirmatrelvir
2786:Ibuzatrelvir
2772:3CL protease
2701:
2673:
2630:
2623:Picornavirus
2545:Uprifosbuvir
2443:Pibrentasvir
2394:Voxilaprevir
2364:Paritaprevir
2232:
2032:Cyanovirin-N
2022:Calanolide A
1698:
1692:2 generation
1666:1 generation
1653:
1624:
1603:Elvucitabine
1593:Apricitabine
1542:
1483:2 generation
1437:1 generation
1424:
1420:
1411:Fipravirimat
1325:
1320:Semzuvolimab
1309:
1300:Cenicriviroc
1284:
1272:
1260:
1152:(277): 1–4.
1149:
1143:
1119:(3): 243–4.
1116:
1112:
1102:
1090:. Retrieved
1080:
1068:. Retrieved
1061:
1052:
1035:
1031:
1021:
1010:
998:
965:
961:
954:
942:. Retrieved
929:
910:
905:
893:. Retrieved
884:
874:, retrieved
862:
816:(17): 9124.
813:
809:
799:
784:
772:. Retrieved
716:(Crixivan).
695:
692:Side effects
682:nirmatrelvir
675:
595:slow release
311:
307:
291:
284:
275:Simnotrelvir
270:Nirmatrelvir
259:
235:Paritaprevir
209:
141:
128:
87:
83:
82:
72:January 2020
69:
55:
51:
3341:Oxytocinase
3149:Transferase
2953:from market
2918:Merimepodib
2892:Triazavirin
2887:Taribavirin
2847:Galidesivir
2842:Favipiravir
2806:Rupintrivir
2791:Lufotrelvir
2781:Ensitrelvir
2726:Laninamivir
2712:Oseltamivir
2694:Rimantadine
2632:viral entry
2613:Bulevirtide
2605:Hepatitis D
2463:Velpatasvir
2418:Daclatasvir
2413:Coblopasvir
2389:Vedroprevir
2359:Narlaprevir
2354:Grazoprevir
2349:Glecaprevir
2344:Faldaprevir
2324:Asunaprevir
2302:Hepatitis C
2283:(primarily
2233:recommended
2208:from market
2158:Lersivirine
2133:Capravirine
2072:Miltefosine
2057:Griffithsin
2052:Fosdevirine
1598:Censavudine
1228:(primarily
1070:23 December
663:leapfrogged
287:antibiotics
265:Ensitrelvir
230:Glecaprevir
225:Grazoprevir
215:Asunaprevir
108:hepatitis C
92:medications
2928:Presatovir
2923:Moroxydine
2857:Remdesivir
2815:+ritonavir
2800:+ritonavir
2744:Interferon
2689:Amantadine
2684:Adapromine
2667:Umifenovir
2637:Pleconaril
2540:Radalbuvir
2535:TMC-647055
2525:Sofosbuvir
2520:Setrobuvir
2500:Deleobuvir
2485:Beclabuvir
2458:Samatasvir
2448:Ravidasvir
2438:Ombitasvir
2428:Ledipasvir
2384:Vaniprevir
2379:Telaprevir
2374:Sovaprevir
2369:Simeprevir
2339:Danoprevir
2334:Ciluprevir
2329:Boceprevir
2281:antivirals
2163:Lodenosine
2143:Droxinavir
2128:Brecanavir
2123:Atevirdine
2087:Seliciclib
2082:Scytovirin
1996:Elipovimab
1941:TRIM5alpha
1618:Stampidine
1523:inhibitors
1507:TMC-310911
1406:BMS-955176
1304:Leronlimab
1296:Vicriviroc
944:5 November
895:8 November
876:2024-06-20
774:5 November
747:References
603:Tipranavir
541:Atazanavir
480:Amprenavir
452:Nelfinavir
363:Saquinavir
345:Trade name
318:saquinavir
300:(–zomib).
245:Telaprevir
240:Simeprevir
220:Boceprevir
192:Tipranavir
187:Saquinavir
177:Nelfinavir
152:Atazanavir
147:Amprenavir
3242:Hydrolase
3206:Integrase
3121:Aromatase
3058:Substrate
2963:Phase III
2951:Withdrawn
2882:Ribavirin
2852:GS-441524
2722:Peramivir
2717:Zanamivir
2662:Pimodivir
2648:influenza
2530:Tegobuvir
2505:Filibuvir
2495:Dasabuvir
2433:Odalasvir
2278:RNA virus
2218:Phase III
2206:Withdrawn
2183:Telinavir
2178:Palinavir
2173:Mozenavir
2153:Emivirine
2148:Lasinavir
2118:Aplaviroc
2047:Foscarnet
2027:Ceragenin
1588:Amdoxovir
1401:Bevirimat
1378:BI 224436
1038:(34): 9.
714:indinavir
655:phase III
627:Darunavir
509:Lopinavir
484:Agenerase
424:Indinavir
395:Ritonavir
326:indinavir
322:ritonavir
182:Ritonavir
172:Lopinavir
167:Indinavir
157:Darunavir
116:proteases
3419:Category
3288:Protease
2453:Ruzasvir
2423:Elbasvir
2168:Loviride
1158:11364559
1135:12626882
990:26084893
982:17617272
871:31644200
842:34502033
720:See also
678:Paxlovid
631:Prezista
456:Viracept
428:Crixivan
260:–trelvir
112:COVID-19
104:HIV/AIDS
3314:Trypsin
2877:NITD008
2515:IDX-184
2510:GS-6620
2287:, also
2067:KP-1461
1613:Racivir
1383:MK-2048
1092:14 June
833:8430524
607:Aptivus
590:prodrug
545:Reyataz
513:Kaletra
389:(FDA).
348:Company
210:–previr
3368:(EC 4)
3244:(EC 3)
3151:(EC 2)
3111:1.13
3068:(EC 1)
2946:WHO-EM
2862:MK-608
2832:CMX521
2650:agents
2201:WHO-EM
2017:BIT225
2012:Abzyme
1943:(gene)
1630:NtRTIs
1525:(RTIs)
1156:
1133:
988:
980:
962:Lancet
917:
869:
840:
830:
708:, and
517:AbbVie
403:AbbVie
399:Norvir
357:Notes
351:Patent
324:, and
142:–navir
118:(e.g.
90:) are
3366:Lyase
3326:Mixed
3319:Renin
3297:DPP-4
3132:1.17
3126:COX-2
3119:1.14
3022:Class
2913:EICAR
2646:Anti-
2293:D06BB
2289:S01AD
2005:Other
1988:BNAbs
1548:NRTIs
1327:gp120
986:S2CID
938:(PDF)
768:(PDF)
651:OARAC
3382:4.2
3374:4.1
3349:3.5
3286:3.4
3268:3.2
3250:3.1
3199:2.7
3191:2.6
3178:2.5
3172:PARP
3170:2.4
3159:COMT
3157:2.1
3103:1.5
3095:1.4
3087:1.3
3074:1.1
2473:NS5B
2404:NS5A
2291:and
2230:DHHS
1286:CCR5
1274:gp41
1154:PMID
1131:PMID
1094:2024
1072:2021
978:PMID
946:2016
915:ISBN
897:2013
867:PMID
838:PMID
776:2016
342:Name
110:and
3302:ACE
2311:NS3
2285:J05
1311:CD4
1230:J05
1226:HIV
1121:doi
1063:NPR
1040:doi
970:doi
966:370
828:PMC
818:doi
202:NS3
88:PIs
3421::
3290::
3013::
2959::
2724:,
2315:4A
2214::
1318:,
1302:,
1298:,
1220::
1173:A
1129:.
1117:32
1115:.
1111:.
1060:.
1036:84
1034:.
1030:.
984:.
976:.
964:.
861:,
850:^
836:.
826:.
814:22
812:.
808:.
754:^
704:,
700:,
588:A
474:—
446:—
320:,
206:4A
126:.
106:,
3003:e
2996:t
2989:v
2817:)
2813:(
2802:)
2798:(
2728:)
2710:(
2705:/
2696:)
2682:(
2677:/
2634::
2313:/
2295:)
2270:e
2263:t
2256:v
2228:°
1816:°
1810:°
1804:°
1793:°
1777:°
1761:°
1658:)
1654:(
1632::
1628:/
1550::
1546:/
1498:°
1492:°
1429:)
1425:(
1334:)
1330:(
1322:)
1314:(
1306:)
1289:(
1281:)
1277:(
1265:)
1261:(
1232:)
1210:e
1203:t
1196:v
1160:.
1137:.
1123::
1096:.
1074:.
1046:.
1042::
992:.
972::
948:.
923:.
899:.
844:.
820::
778:.
615:—
582:—
204:/
86:(
74:)
70:(
60:.
34:.
20:)
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