42:
444:(HAART), is composed of two or more types of antiretroviral drugs. Combination therapy decreases the likelihood that drug resistance will occur, because it is unlikely that the HIV-1 strains will be able to mutate enough to become resistant to all drugs being used in the combination. Combination therapy increases the length of lives of patients with HIV-1, and can greatly reduce the possibility for transmission of the virus.
2356:
2344:
473:(NRTI) that is a synthetic fluoro derivative of thiacytidine. Within the cell, emtricitabine becomes phosphorylated, which forms emtricitabine 5′-triphosphate within the cell. This allows for the drug to compete with the viral and host substrate and ultimately causes a termination of DNA chain elongation. Underlying
487:
of tenofovir that functions as a nucleotide reverse transcriptase inhibitor (NtRTI). Other prodrugs for tenofovir have been tested, but TAF is more efficient at refining HIV-1 therapy. It converts intracellularly to TFV diphosphate, which is a metabolite in HIV target cells. Thus, TAF has higher
459:(INSTI). Bictegravir is different from other INSTIs because it contains a bridged bicyclic ring and a distinct benzyl tail with a 2,4,6-trifluorobenzyl group. This contributes to an increase in plasma protein binding and a reduction of activation of the
410:
for the treatment of human immunodeficiency virus 1 (HIV 1) infection in people weighing at least 14 kilograms (31 lb) without present or past evidence of viral resistance to the integrase inhibitor class, emtricitabine or tenofovir.
488:
active metabolite concentrations and lower plasma TFV than other
Tenofovir prodrugs. TAF is metabolized primarily with the kidneys, and has a lower dosage than other prodrugs, so it is less detrimental to the renal elimination system.
1132:
Mayer KH, Gelman M, Holmes J, Kraft J, Melbourne K, Mimiaga MJ (May 2022). "Safety and
Tolerability of Once Daily Coformulated Bictegravir, Emtricitabine, and Tenofovir Alafenamide for Postexposure Prophylaxis After Sexual Exposure".
1741:
1178:"An open-label evaluation of safety and tolerability of coformulated bictegravir/emtricitabine/tenofovir alafenamide for post-exposure prophylaxis following potential exposure to human immunodeficiency virus-1"
252:
1925:
1930:
463:(PXR). These changes minimize interactions between drugs, lower clearance, and increase solubility. Bictegravir was found to be less drug resistant than other drugs in the same class.
1876:
398:
in 2019. As of 2024, it is recommended as a first-line choice of antiretroviral therapy in several countries, including the
European Union, the United Kingdom and the United States.
1348:
434:
Bictegravir/emtricitabine/tenofovir alafenamide is an example of a combination drug that can be taken as a complete regimen for the treatment of the human immunodeficiency virus.
2315:
207:
1512:
477:(HBV) can interact with emtricitabine to cause significant liver damage, but it does not have a significant detrimental effect on the liver when given to patients without HBV.
394:
It was approved for use in 2018 in
Australia, the European Union and the United States and in 2019 in New Zealand and the United Kingdom; a generic version was approved by the
758:
384:
2376:
1882:
865:
1940:
1945:
711:
1893:
1294:
105:
836:
557:
1915:
1899:
1910:
978:
470:
83:
71:
1920:
1072:
2187:
712:"U.S. Food and Drug Administration Approves Gilead's Biktarvy (Bictegravir, Emtricitabine, Tenofovir Alafenamide) for Treatment of HIV-1 Infection"
500:(PEP) for preventing HIV infection after exposure and has shown positive early results. However, it has not been approved for this use as of 2024.
1831:
682:
672:
Text was copied from this source which is copyright
European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
2286:
2177:
1106:
921:"Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile"
441:
115:
543:
1935:
456:
1950:
1506:
1287:
395:
1960:
1844:
689:
624:
1970:
1955:
1735:
1715:
1633:
1618:
1606:
894:
237:
137:
41:
1850:
814:
1080:
1007:
2334:
1272:
1280:
517:
2303:
1227:"Bictegravir/Emtricitabine/Tenofovir Alafenamide for HIV-1: What is the Hidden Potential of This Emerging Treatment?"
156:
659:
497:
368:
33:
2127:
2037:
1905:
1866:
2291:
1887:
843:
193:
810:
1965:
1084:
365:
2162:
1975:
1855:
1725:
1324:
480:
388:
78:
1033:"Tenofovir alafenamide: A novel prodrug of tenofovir for the treatment of Human Immunodeficiency Virus"
837:"BHIVA guidelines on antiretroviral treatment for adults living with HIV-1 2022 (2023 interim update)"
1871:
1720:
1478:
1980:
1839:
1711:
1629:
1428:
1307:
460:
437:
316:
200:
59:
1158:
167:
729:
2268:
2263:
2122:
1785:
1258:
1207:
1150:
1054:
950:
474:
289:
276:
264:
95:
999:
683:"Australian Public Assessment Report for Bictegravir / Emtricitabine / Tenofovir alafenamide"
655:
586:"Biktarvy 50 mg/200 mg/25 mg film-coated tablets - Summary of Product Characteristics (SmPC)"
325:
2147:
1248:
1238:
1197:
1189:
1142:
1044:
940:
932:
2348:
2223:
2182:
1342:
968:
715:
919:
Tsiang M, Jones GS, Goldsmith J, Mulato A, Hansen D, Kan E, et al. (December 2016).
1253:
1226:
625:"Biktarvy- bictegravir sodium, emtricitabine, and tenofovir alafenamide fumarate tablet"
426:
Adverse drug reactions include, but are not limited to, diarrhea, nausea, and headache.
2360:
2297:
2073:
2055:
2018:
1303:
1202:
1177:
945:
920:
558:"Drug and medical device highlights 2018: Helping you maintain and improve your health"
759:"Bictegravir-emtricitabine-tenofovir alafenamide for the treatment of HIV-1 in adults"
2370:
2063:
1813:
1648:
1534:
1162:
585:
562:
518:"Bictegravir / emtricitabine / tenofovir alafenamide (Biktarvy) Use During Pregnancy"
466:
420:
380:
379:, a human immunodeficiency virus type 1 (HIV-1) integrase strand transfer inhibitor;
129:
66:
1049:
1032:
866:"Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV"
2117:
2107:
1688:
1678:
1496:
1453:
1448:
1443:
1405:
1385:
1315:
788:
220:
215:
1193:
1146:
2243:
2218:
2157:
2142:
2137:
1801:
1768:
1683:
1663:
1458:
1438:
1417:
1364:
1332:
762:
452:
376:
123:
54:
2248:
2228:
2213:
2208:
2172:
2167:
2081:
2026:
1996:
1808:
1796:
1791:
1763:
1703:
1693:
1668:
1653:
1643:
1592:
1587:
1575:
1559:
1549:
1529:
1491:
1401:
1389:
1381:
784:
2258:
2238:
2233:
2203:
2132:
2112:
2045:
2001:
1758:
1673:
1658:
1581:
1554:
1544:
1539:
1486:
1463:
1376:
1107:"Boston study finds Biktarvy useful for HIV post-exposure prophylaxis (PEP)"
407:
109:
1262:
1211:
1154:
1058:
954:
1176:
Liu A, Xin R, Zhang H, Dai L, Wu RE, Wang X, et al. (November 2022).
496:
Bictegravir/emtricitabine/tenofovir alafenamide has been investigated for
2253:
1638:
936:
785:"Hetero launches TAFFIC, the latest 3-in-1 single pill for HIV treatment"
372:
151:
1243:
17:
2321:
2152:
1698:
1468:
973:
872:
736:
484:
2355:
2102:
2097:
345:
1412:
1371:
1359:
336:
295:
270:
1276:
283:
146:
1396:
1311:
391:, an HIV-1 nucleoside analog reverse transcriptase inhibitor.
1926:
Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
246:
178:
1931:
Elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil
1877:
Darunavir/cobicistat/emtricitabine/tenofovir alafenamide
259:
2332:
2196:
2090:
2072:
2054:
2036:
2017:
2010:
1989:
1830:
1777:
1751:
1734:
1617:
1605:
1568:
1522:
1505:
1477:
1427:
1341:
1323:
895:"FDA-Approved HIV Medicines Understanding HIV/AIDS"
335:
315:
310:
236:
231:
206:
192:
166:
136:
122:
104:
94:
89:
77:
65:
53:
48:
1073:"Tenofovir Alafenamide Information for Providers"
1031:Ray AS, Fordyce MW, Hitchcock MJ (January 2016).
385:nucleoside analog reverse transcriptase inhibitor
1883:Dolutegravir/emtricitabine/tenofovir alafenamide
619:
617:
615:
613:
611:
609:
607:
1941:Emtricitabine/rilpivirine/tenofovir alafenamide
1861:Bictegravir/emtricitabine/tenofovir alafenamide
1135:Journal of Acquired Immune Deficiency Syndromes
650:
648:
646:
358:Bictegravir/emtricitabine/tenofovir alafenamide
324:
34:Bictegravir/emtricitabine/tenofovir alafenamide
1946:Emtricitabine/rilpivirine/tenofovir disoproxil
1432:(Integrase strand transfer inhibitors (INSTI))
1894:Dolutegravir/lamivudine/tenofovir alafenamide
1288:
1225:Januszka JE, Drwiega EN, Badowski ME (2023).
8:
1916:Efavirenz/emtricitabine/tenofovir disoproxil
1900:Dolutegravir/lamivudine/tenofovir disoproxil
155:
32:
303:In general: ℞ (Prescription only)
2014:
1911:Doravirine/lamivudine/tenofovir disoproxil
1748:
1614:
1519:
1295:
1281:
1273:
979:United States National Library of Medicine
544:"Regulatory Decision Summary for Biktarvy"
471:nucleoside reverse transcriptase inhibitor
423:about acute exacerbations of hepatitis B.
84:nucleoside reverse transcriptase inhibitor
72:nucleoside reverse transcriptase inhibitor
1921:Efavirenz/lamivudine/tenofovir disoproxil
1252:
1242:
1201:
1048:
944:
419:The US FDA prescription label contains a
2188:Zinc finger protein transcription factor
2377:Fixed dose combination (antiretroviral)
2339:
509:
128:
31:
1026:
1024:
925:Antimicrobial Agents and Chemotherapy
114:
7:
1000:"Emtricitabine Dosage, Side Effects"
811:"Initial Regimens: ART-naïve Adults"
442:highly active antiretroviral therapy
219:
1936:Emtricitabine/tenofovir alafenamide
457:integrase strand transfer inhibitor
344:
1951:Emtricitabine/tenofovir disoproxil
25:
396:Drugs Controller General of India
2354:
2342:
2324:. Formerly or rarely used agent.
1961:Lamivudine/nevirapine/zidovudine
1845:Abacavir/dolutegravir/lamivudine
690:Therapeutic Goods Administration
40:
2128:Epigallocatechin gallate (EGCG)
1971:Lamivudine/tenofovir disoproxil
1956:Lamivudine/nevirapine/stavudine
1050:10.1016/j.antiviral.2015.11.009
27:Fixed dose combination HIV drug
1851:Abacavir/lamivudine/zidovudine
875:. 21 September 2022. p. 6
815:European AIDS Clinical Society
1:
1081:National Institutes of Health
1008:National Institutes of Health
1194:10.1097/CM9.0000000000002494
1147:10.1097/QAI.0000000000002912
360:, sold under the brand name
1726:Tenofovir alafenamide (TAF)
730:"BIKTARVY Data Sheet v 8.0"
2393:
1721:Tenofovir disoproxil (TDF)
2281:
1742:Discovery and development
1513:Discovery and development
1349:Discovery and development
846:. 28 May 2023. p. 16
660:European Medicines Agency
498:post-exposure prophylaxis
369:antiretroviral medication
39:
2038:Transcription inhibitors
1990:Pharmacokinetic boosters
1906:Dolutegravir/rilpivirine
1867:Cabotegravir/rilpivirine
1507:Protease Inhibitors (PI)
2322:initial regimen options
1888:Dolutegravir/lamivudine
1365:Enfuvirtide (ENF, T-20)
1343:Entry/fusion inhibitors
1182:Chinese Medical Journal
844:British HIV Association
2163:Portmanteau inhibitors
2056:Translation inhibitors
1966:Lamivudine/raltegravir
1736:Non-nucleoside (NNRTI)
1694:Islatravir (EFdA, ISL)
440:for HIV, often called
366:fixed-dose combination
2178:Synergistic enhancers
1976:Lamivudine/zidovudine
1856:Atazanavir/cobicistat
1832:Combined formulations
1669:Zidovudine (AZT, ZDV)
1607:Reverse-transcriptase
1479:Maturation inhibitors
481:Tenofovir alafenamide
389:tenofovir alafenamide
371:for the treatment of
79:Tenofovir alafenamide
2019:Uncoating inhibitors
1872:Darunavir/cobicistat
1712:Nucleotide analogues
1630:Nucleoside analogues
1429:Integrase inhibitors
1308:antiretroviral drugs
937:10.1128/AAC.01474-16
2011:Experimental agents
1981:Lopinavir/ritonavir
1840:Abacavir/lamivudine
1814:Elsulfavirine (ESV)
1649:Emtricitabine (FTC)
1535:Fosamprenavir (FPV)
1244:10.2147/HIV.S385877
1087:on 2 September 2020
524:. 16 September 2019
461:pregnane X receptor
438:Combination therapy
430:Combination therapy
406:The combination is
279:(Prescription only)
255:(Prescription only)
60:integrase inhibitor
36:
2308:Never to phase III
1454:Elvitegravir (EVG)
1449:Dolutegravir (DTG)
1444:Cabotegravir (CAB)
1113:. 24 February 2022
1037:Antiviral Research
791:. 17 December 2019
718:. 7 February 2018.
546:. 23 October 2014.
2330:
2329:
2277:
2276:
2123:Diarylpyrimidines
1826:
1825:
1822:
1821:
1802:Rilpivirine (RPV)
1786:diarylpyrimidines
1769:Delavirdine (DLV)
1664:Zalcitabine (ddC)
1621:nucleotide (NRTI)
1601:
1600:
1459:Raltegravir (RAL)
1439:Bictegravir (BIC)
1418:Fostemsavir (FTR)
1333:Lenacapavir (LEN)
1325:Capsid inhibitors
1188:(22): 2725–2729.
931:(12): 7086–7097.
787:(Press release).
714:(Press release).
566:. 14 October 2020
475:hepatitis B virus
355:
354:
299:
287:
274:
262:
250:
182:
149:
16:(Redirected from
2384:
2359:
2358:
2347:
2346:
2345:
2338:
2148:Hydroxycarbamide
2015:
1809:Doravirine (DOR)
1797:Etravirine (ETR)
1792:Dapivirine (DPV)
1764:Nevirapine (NVP)
1749:
1654:Lamivudine (3TC)
1644:Didanosine (ddI)
1615:
1588:Tipranavir (TPV)
1576:Atazanavir (ATV)
1560:Saquinavir (SQV)
1550:Nelfinavir (NFV)
1530:Amprenavir (APV)
1520:
1402:Ibalizumab (IBA)
1297:
1290:
1283:
1274:
1267:
1266:
1256:
1246:
1222:
1216:
1215:
1205:
1173:
1167:
1166:
1129:
1123:
1122:
1120:
1118:
1103:
1097:
1096:
1094:
1092:
1083:. Archived from
1069:
1063:
1062:
1052:
1028:
1019:
1018:
1016:
1014:
996:
990:
989:
987:
985:
965:
959:
958:
948:
916:
910:
909:
907:
905:
891:
885:
884:
882:
880:
870:
862:
856:
855:
853:
851:
841:
833:
827:
826:
824:
822:
807:
801:
800:
798:
796:
781:
775:
774:
772:
770:
755:
749:
748:
746:
744:
739:. 24 August 2023
734:
726:
720:
719:
708:
702:
701:
699:
697:
687:
679:
673:
671:
669:
667:
652:
641:
640:
638:
636:
621:
602:
601:
599:
597:
592:. 25 August 2020
582:
576:
575:
573:
571:
554:
548:
547:
540:
534:
533:
531:
529:
514:
348:
328:
297:
294:
285:
282:
272:
269:
261:
258:
248:
245:
223:
180:
177:
159:
148:
145:
132:
118:
44:
37:
35:
21:
2392:
2391:
2387:
2386:
2385:
2383:
2382:
2381:
2367:
2366:
2365:
2353:
2343:
2341:
2333:
2331:
2326:
2325:
2313:
2298:Clinical trials
2273:
2224:Dexelvucitabine
2192:
2183:Tre recombinase
2086:
2068:
2050:
2046:Tat antagonists
2032:
2006:
1985:
1818:
1773:
1759:Efavirenz (EFV)
1738:
1730:
1659:Stavudine (d4T)
1620:
1608:
1597:
1582:Darunavir (DRV)
1564:
1555:Ritonavir (RTV)
1545:Lopinavir (LPV)
1540:Indinavir (IDV)
1509:
1501:
1473:
1431:
1423:
1377:Maraviroc (MVC)
1345:
1337:
1319:
1304:Antiviral drugs
1301:
1271:
1270:
1224:
1223:
1219:
1175:
1174:
1170:
1131:
1130:
1126:
1116:
1114:
1105:
1104:
1100:
1090:
1088:
1071:
1070:
1066:
1030:
1029:
1022:
1012:
1010:
998:
997:
993:
983:
981:
969:"Emtricitabine"
967:
966:
962:
918:
917:
913:
903:
901:
893:
892:
888:
878:
876:
868:
864:
863:
859:
849:
847:
839:
835:
834:
830:
820:
818:
809:
808:
804:
794:
792:
783:
782:
778:
768:
766:
757:
756:
752:
742:
740:
732:
728:
727:
723:
716:Gilead Sciences
710:
709:
705:
695:
693:
692:. 1 August 2019
685:
681:
680:
676:
665:
663:
656:"Biktarvy EPAR"
654:
653:
644:
634:
632:
631:. 8 August 2019
623:
622:
605:
595:
593:
584:
583:
579:
569:
567:
556:
555:
551:
542:
541:
537:
527:
525:
516:
515:
511:
506:
494:
450:
432:
417:
404:
351:
331:
306:
227:
195:
188:
169:
162:
28:
23:
22:
15:
12:
11:
5:
2390:
2388:
2380:
2379:
2369:
2368:
2364:
2363:
2351:
2328:
2327:
2312:
2311:
2310:
2309:
2306:
2295:
2289:
2283:
2282:
2279:
2278:
2275:
2274:
2272:
2271:
2266:
2261:
2256:
2251:
2246:
2241:
2236:
2231:
2226:
2221:
2216:
2211:
2206:
2200:
2198:
2194:
2193:
2191:
2190:
2185:
2180:
2175:
2170:
2165:
2160:
2155:
2150:
2145:
2140:
2135:
2130:
2125:
2120:
2115:
2110:
2105:
2100:
2094:
2092:
2088:
2087:
2085:
2084:
2078:
2076:
2070:
2069:
2067:
2066:
2060:
2058:
2052:
2051:
2049:
2048:
2042:
2040:
2034:
2033:
2031:
2030:
2023:
2021:
2012:
2008:
2007:
2005:
2004:
1999:
1997:Cobicistat (c)
1993:
1991:
1987:
1986:
1984:
1983:
1978:
1973:
1968:
1963:
1958:
1953:
1948:
1943:
1938:
1933:
1928:
1923:
1918:
1913:
1908:
1903:
1897:
1891:
1885:
1880:
1874:
1869:
1864:
1858:
1853:
1848:
1842:
1836:
1834:
1828:
1827:
1824:
1823:
1820:
1819:
1817:
1816:
1811:
1806:
1805:
1804:
1799:
1794:
1781:
1779:
1775:
1774:
1772:
1771:
1766:
1761:
1755:
1753:
1746:
1732:
1731:
1729:
1728:
1723:
1707:
1706:
1701:
1696:
1691:
1686:
1681:
1676:
1671:
1666:
1661:
1656:
1651:
1646:
1641:
1639:Abacavir (ABC)
1625:
1623:
1619:Nucleoside and
1612:
1603:
1602:
1599:
1598:
1596:
1595:
1590:
1585:
1579:
1572:
1570:
1566:
1565:
1563:
1562:
1557:
1552:
1547:
1542:
1537:
1532:
1526:
1524:
1517:
1503:
1502:
1500:
1499:
1494:
1489:
1483:
1481:
1475:
1474:
1472:
1471:
1466:
1461:
1456:
1451:
1446:
1441:
1435:
1433:
1425:
1424:
1422:
1421:
1409:
1393:
1379:
1368:
1355:
1353:
1339:
1338:
1336:
1335:
1329:
1327:
1321:
1320:
1302:
1300:
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1679:Apricitabine
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1523:1 generation
1510:
1497:Fipravirimat
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1406:Semzuvolimab
1395:
1386:Cenicriviroc
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1085:the original
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415:Side effects
405:
402:Medical uses
393:
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357:
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326:2097023-87-3
238:Legal status
232:Legal status
138:License data
29:
2319:recommended
2294:from market
2244:Lersivirine
2219:Capravirine
2158:Miltefosine
2143:Griffithsin
2138:Fosdevirine
1684:Censavudine
1314:(primarily
1237:: 705–711.
879:22 February
850:22 February
821:22 February
795:22 February
769:22 February
763:NHS England
743:22 February
696:22 February
666:22 February
483:(TAF) is a
469:(FTC) is a
453:Bictegravir
383:, an HIV-1
377:bictegravir
311:Identifiers
124:MedlinePlus
96:Trade names
55:Bictegravir
2249:Lodenosine
2229:Droxinavir
2214:Brecanavir
2209:Atevirdine
2173:Seliciclib
2168:Scytovirin
2082:Elipovimab
2027:TRIM5alpha
1704:Stampidine
1609:inhibitors
1593:TMC-310911
1492:BMS-955176
1390:Leronlimab
1382:Vicriviroc
1117:27 January
504:References
448:Components
317:CAS Number
2304:Phase III
2292:Withdrawn
2269:Telinavir
2264:Palinavir
2259:Mozenavir
2239:Emivirine
2234:Lasinavir
2204:Aplaviroc
2133:Foscarnet
2113:Ceragenin
1674:Amdoxovir
1487:Bevirimat
1464:BI 224436
1163:245822499
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596:26 August
522:Drugs.com
408:indicated
194:Routes of
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116:Monograph
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1231:HIV/AIDS
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629:DailyMed
570:17 April
492:Research
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362:Biktarvy
208:ATC code
201:By mouth
183: B3
170:category
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152:DailyMed
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2153:KP-1461
1699:Racivir
1469:MK-2048
1203:9944392
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485:prodrug
364:, is a
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1360:gp41
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1119:2024
1093:2018
1055:PMID
1015:2018
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951:PMID
906:2018
881:2024
852:2024
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797:2024
771:2024
745:2024
698:2024
668:2024
637:2020
598:2020
572:2024
530:2020
337:KEGG
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1312:HIV
1249:PMC
1239:doi
1198:PMC
1190:doi
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