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Lopinavir

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of women with high-grade and low-grade precancerous conditions. After three months of treatment, 82.6% of the women who had high-grade disease had normal cervical conditions, confirmed by smears and biopsies. Lopinavir has been shown to impair protein synthesis via AMP-activated protein kinase
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InChI=1S/C37H48N4O5/c1-25(2)34(41-20-12-19-38-37(41)45)36(44)39-30(21-28-15-7-5-8-16-28)23-32(42)31(22-29-17-9-6-10-18-29)40-33(43)24-46-35-26(3)13-11-14-27(35)4/h5-11,13-18,25,30-32,34,42H,12,19-24H2,1-4H3,(H,38,45)(H,39,44)(H,40,43)/t30-,31-,32-,34-/m0/s1
579: 796: 717:(CSF). Anecdotal reports state that lopinavir cannot be detected in the CSF; however, a study of paired CSF-plasma samples from 26 patients receiving lopinavir/ritonavir found lopinavir CSF levels above the 1659: 1633: 1551: 1653: 682:, especially among children living with HIV. Lopinavir and ritonavir can be taken as a tablet or an oral solution, a preferred option in children. In the early stages of 1843: 1848: 1075:"Screening of an FDA-approved compound library identifies four small-molecule inhibitors of Middle East respiratory syndrome coronavirus replication in cell culture" 1794: 1266: 2233: 153: 1430: 1800: 111: 1858: 1778: 1863: 1811: 1212: 776: 60: 1833: 1817: 678:
It was patented in 1995 and approved for medical use in 2000. Considered now as second-line therapy in the West, it is still prescribed in
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de Wilde AH, Jochmans D, Posthuma CC, Zevenhoven-Dobbe JC, van Nieuwkoop S, Bestebroer TM, et al. (August 2014).
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Kaletra (lopinavir/ritonavir) capsules; (lopinavir/ritonavir) oral solution. Prescribing information. April 2009
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injectable formulation of lopinavir is under clinical trial aiming at monthly dosing (NCT05850728).
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Side effects, interactions, and contraindications have only been evaluated in the drug combination
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Stecher C, Marinkov S, Mayr-Harting L, Katic A, Kastner MT, Rieder-Rommer FJ, et al. (2021).
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Capparelli EV, Holland D, Okamoto C, Gragg B, Durelle J, Marquie-Beck J, et al. (June 2005).
2209: 1805: 906:"Lopinavir concentrations in cerebrospinal fluid exceed the 50% inhibitory concentration for HIV" 772:. In this trial the medication was started typically around 13 days after the start of symptoms. 139: 2309: 1883: 1024:
Ammosova T, Platonov M, Ivanov A, Kont YS, Kumari N, Kehn-Hall K, et al. (November 2014).
243: 1991: 1026:"1E7-03, a low MW compound targeting host protein phosphatase-1, inhibits HIV-1 transcription" 818: 2080: 1893: 1773: 1643: 1242: 952: 750: 733: 330: 2319: 1963: 1789: 1638: 1396: 415: 395: 265: 1220: 8: 1898: 1757: 1629: 1547: 1346: 1225: 1179: 765: 714: 699: 672: 321: 171: 146: 922: 905: 736:(HPV). The study used the equivalent of one tablet twice a day applied topically to the 509: 486: 1152: 1125: 1101: 1074: 1050: 1025: 1001: 966: 935: 870: 845: 2040: 1703: 1157: 1106: 1055: 1006: 988: 927: 875: 824: 215: 202: 84: 70: 2065: 1147: 1137: 1096: 1086: 1045: 1037: 996: 978: 939: 917: 865: 857: 522: 225: 166: 2239: 355: 312:--4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide 2266: 2141: 2100: 1260: 253: 233: 2324: 2278: 2215: 1221: 892: 861: 844:
Perazzolo, Simone; Zhu; Lin, Weixian; Nguyen, Alexander; Ho, Rodney JY (2021).
983: 2288: 1981: 1731: 1566: 1452: 992: 660: 498: 1126:"A Trial of Lopinavir-Ritonavir in Adults Hospitalized with Severe Covid-19" 2035: 2025: 1606: 1596: 1414: 1371: 1366: 1361: 1323: 1303: 1233: 1161: 1110: 1059: 1010: 931: 879: 761: 161: 1142: 22: 2161: 2136: 2075: 2060: 2055: 1719: 1686: 1601: 1581: 1376: 1356: 1335: 1282: 1250: 1091: 78: 1072: 375: 2166: 2146: 2131: 2126: 2090: 2085: 1999: 1944: 1914: 1726: 1714: 1709: 1681: 1621: 1611: 1586: 1571: 1561: 1510: 1505: 1493: 1477: 1467: 1447: 1409: 1319: 1307: 1299: 687: 652: 601:
O=C(N(Cc1ccccc1)(O)C(NC(=O)(N2C(=O)NCCC2)C(C)C)Cc3ccccc3)COc4c(cccc4C)C
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HIV drug used to reverse effects of virus that causes cervical cancer
749:) activation, a mechanism that is similar to the antiviral effect of 668: 341: 278: 64: 1124:
Cao B, Wang Y, Wen D, Liu W, Wang J, Fan G, et al. (May 2020).
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Reports are contradictory regarding lopinavir penetration into the
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A 2014 study indicates that lopinavir is effective against the
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Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
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Elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil
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Darunavir/cobicistat/emtricitabine/tenofovir alafenamide
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Lopinavir is highly bound to plasma proteins (98–99%).
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virus in the hope of disturbing its protease activity.
2250: 843: 702:. They include nausea, vomiting, and stomach aches. 2286: 1801:Dolutegravir/emtricitabine/tenofovir alafenamide 686:pandemics, lopinavir was repurposed against the 354: 1859:Emtricitabine/rilpivirine/tenofovir alafenamide 1779:Bictegravir/emtricitabine/tenofovir alafenamide 816: 329: 1864:Emtricitabine/rilpivirine/tenofovir disoproxil 1350:(Integrase strand transfer inhibitors (INSTI)) 1812:Dolutegravir/lamivudine/tenofovir alafenamide 1206: 1123: 1834:Efavirenz/emtricitabine/tenofovir disoproxil 1818:Dolutegravir/lamivudine/tenofovir disoproxil 127: 955:University of Manchester, 17 February 2014. 760:replication in the low-micromolar range in 1829:Doravirine/lamivudine/tenofovir disoproxil 1213: 1199: 508: 485: 394: 38: 29: 1839:Efavirenz/lamivudine/tenofovir disoproxil 1151: 1141: 1100: 1090: 1049: 1000: 982: 921: 869: 414: 2106:Zinc finger protein transcription factor 481: 374: 83: 2287: 823:. John Wiley & Sons. p. 510. 810: 499: 196: 101: 1194: 1079:Antimicrobial Agents and Chemotherapy 797:"FDA Approved Drug Products: Kaletra" 454: 209: 118: 69: 1186:. U.S. National Library of Medicine. 886: 165: 1854:Emtricitabine/tenofovir alafenamide 1130:The New England Journal of Medicine 923:10.1097/01.aids.0000171409.38490.48 434: 345: 13: 1869:Emtricitabine/tenofovir disoproxil 14: 2336: 1172: 667:with another protease inhibitor, 2272: 2260: 2242:. Formerly or rarely used agent. 1879:Lamivudine/nevirapine/zidovudine 1763:Abacavir/dolutegravir/lamivudine 768:was found not to work in severe 539: 533: 2046:Epigallocatechin gallate (EGCG) 1889:Lamivudine/tenofovir disoproxil 1874:Lamivudine/nevirapine/stavudine 1117: 1030:British Journal of Pharmacology 817:Fischer J, Ganellin CR (2006). 756:Lopinavir was found to inhibit 705: 693: 626:Key:KJHKTHWMRKYKJE-SUGCFTRWSA-N 1769:Abacavir/lamivudine/zidovudine 1066: 1017: 958: 946: 897: 837: 789: 545: 527: 1: 820:Analogue-based Drug Discovery 782: 7: 1644:Tenofovir alafenamide (TAF) 727: 10: 2341: 1639:Tenofovir disoproxil (TDF) 862:10.1016/j.xphs.2020.11.019 659:class. It is used against 517:Chemical and physical data 2315:Drugs developed by AbbVie 2199: 2114: 2008: 1990: 1972: 1954: 1935: 1928: 1907: 1748: 1695: 1669: 1660:Discovery and development 1652: 1535: 1523: 1486: 1440: 1431:Discovery and development 1423: 1395: 1345: 1267:Discovery and development 1259: 1241: 984:10.3389/fmicb.2021.698603 971:Frontiers in Microbiology 634: 609: 589: 567: 554: 521: 516: 497: 465: 445: 425: 405: 385: 365: 340: 320: 292: 287: 277: 264: 252: 242: 232: 224: 186: 181: 152: 138: 91: 77: 59: 51: 46: 37: 28: 1956:Transcription inhibitors 1908:Pharmacokinetic boosters 1824:Dolutegravir/rilpivirine 1785:Cabotegravir/rilpivirine 1425:Protease Inhibitors (PI) 71:International Drug Names 2305:HIV protease inhibitors 2240:initial regimen options 1806:Dolutegravir/lamivudine 1283:Enfuvirtide (ENF, T-20) 1261:Entry/fusion inhibitors 1184:Drug Information Portal 2081:Portmanteau inhibitors 1974:Translation inhibitors 1884:Lamivudine/raltegravir 1654:Non-nucleoside (NNRTI) 1612:Islatravir (EFdA, ISL) 665:fixed-dose combination 2096:Synergistic enhancers 1894:Lamivudine/zidovudine 1774:Atazanavir/cobicistat 1750:Combined formulations 1587:Zidovudine (AZT, ZDV) 1525:Reverse-transcriptase 1397:Maturation inhibitors 1143:10.1056/NEJMoa2001282 751:protein phosphatase 1 734:human papilloma virus 1937:Uncoating inhibitors 1790:Darunavir/cobicistat 1630:Nucleotide analogues 1548:Nucleoside analogues 1347:Integrase inhibitors 1226:antiretroviral drugs 1092:10.1128/AAC.03011-14 1929:Experimental agents 1899:Lopinavir/ritonavir 1758:Abacavir/lamivudine 1732:Elsulfavirine (ESV) 1567:Emtricitabine (FTC) 1453:Fosamprenavir (FPV) 766:lopinavir/ritonavir 745:) and eEF2 kinase ( 724:in 77% of samples. 715:cerebrospinal fluid 700:lopinavir/ritonavir 673:lopinavir/ritonavir 205:(Prescription only) 25: 2300:Secondary alcohols 2226:Never to phase III 1372:Elvitegravir (EVG) 1367:Dolutegravir (DTG) 1362:Cabotegravir (CAB) 657:protease inhibitor 21: 2295:CYP3A4 inhibitors 2248: 2247: 2195: 2194: 2041:Diarylpyrimidines 1744: 1743: 1740: 1739: 1720:Rilpivirine (RPV) 1704:diarylpyrimidines 1687:Delavirdine (DLV) 1582:Zalcitabine (ddC) 1539:nucleotide (NRTI) 1519: 1518: 1377:Raltegravir (RAL) 1357:Bictegravir (BIC) 1336:Fostemsavir (FTR) 1251:Lenacapavir (LEN) 1243:Capsid inhibitors 1136:(19): 1787–1799. 1042:10.1111/bph.12863 646: 645: 580:Interactive image 467:CompTox Dashboard 213: 200: 121: 104: 16:Chemical compound 2332: 2277: 2276: 2265: 2264: 2263: 2256: 2066:Hydroxycarbamide 1933: 1932: 1727:Doravirine (DOR) 1715:Etravirine (ETR) 1710:Dapivirine (DPV) 1682:Nevirapine (NVP) 1667: 1666: 1572:Lamivudine (3TC) 1562:Didanosine (ddI) 1533: 1532: 1506:Tipranavir (TPV) 1494:Atazanavir (ATV) 1478:Saquinavir (SQV) 1468:Nelfinavir (NFV) 1448:Amprenavir (APV) 1438: 1437: 1320:Ibalizumab (IBA) 1215: 1208: 1201: 1192: 1191: 1187: 1166: 1165: 1155: 1145: 1121: 1115: 1114: 1104: 1094: 1070: 1064: 1063: 1053: 1021: 1015: 1014: 1004: 986: 962: 956: 950: 944: 943: 925: 901: 895: 890: 884: 883: 873: 856:(3): 1002–1017. 841: 835: 834: 814: 808: 807: 805: 803: 793: 642: 641: 582: 562: 547: 541: 535: 529: 512: 501: 490: 489: 475: 473: 458: 438: 418: 398: 378: 358: 348: 347: 333: 269: 211: 208: 198: 195: 169: 131: 120: 117: 114: 103: 100: 87: 73: 42: 33: 26: 24: 20: 2340: 2339: 2335: 2334: 2333: 2331: 2330: 2329: 2285: 2284: 2283: 2271: 2261: 2259: 2251: 2249: 2244: 2243: 2231: 2216:Clinical trials 2191: 2142:Dexelvucitabine 2110: 2101:Tre recombinase 2004: 1986: 1968: 1964:Tat antagonists 1950: 1924: 1903: 1736: 1691: 1677:Efavirenz (EFV) 1656: 1648: 1577:Stavudine (d4T) 1538: 1526: 1515: 1500:Darunavir (DRV) 1482: 1473:Ritonavir (RTV) 1463:Lopinavir (LPV) 1458:Indinavir (IDV) 1427: 1419: 1391: 1349: 1341: 1295:Maraviroc (MVC) 1263: 1255: 1237: 1222:Antiviral drugs 1219: 1178: 1175: 1170: 1169: 1122: 1118: 1071: 1067: 1036:(22): 5059–75. 1022: 1018: 963: 959: 951: 947: 902: 898: 891: 887: 842: 838: 831: 815: 811: 801: 799: 795: 794: 790: 785: 730: 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692: 661:HIV infections 644: 643: 632: 631: 629: 628: 625: 623: 620: 612: 611: 610: 607: 606: 604: 603: 600: 592: 591: 590: 587: 586: 584: 583: 575: 573: 565: 564: 558: 552: 551: 548: 542: 536: 530: 525: 519: 518: 514: 513: 503: 495: 494: 492: 491: 478: 476: 463: 462: 460: 459: 451: 449: 443: 442: 440: 439: 431: 429: 423: 422: 420: 419: 411: 409: 403: 402: 400: 399: 391: 389: 383: 382: 380: 379: 371: 369: 363: 362: 360: 359: 351: 349: 338: 337: 335: 334: 326: 324: 318: 317: 315: 314: 303: 295: 294: 293: 290: 289: 285: 284: 281: 275: 274: 271: 262: 261: 256: 250: 249: 246: 240: 239: 236: 230: 229: 222: 221: 219: 218: 206: 192: 190: 184: 183: 179: 178: 176: 175: 172:with ritonavir 158: 156: 150: 149: 144: 142:administration 136: 135: 133: 132: 115: 97: 95: 89: 88: 81: 75: 74: 67: 57: 56: 53: 49: 48: 44: 43: 35: 34: 15: 9: 6: 4: 3: 2: 2337: 2326: 2323: 2321: 2318: 2316: 2313: 2311: 2310:Phenol ethers 2308: 2306: 2303: 2301: 2298: 2296: 2293: 2292: 2290: 2280: 2275: 2270: 2268: 2258: 2257: 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526: 524: 520: 515: 511: 507: 504: 502: 500:ECHA InfoCard 496: 488: 484: 483:DTXSID8046456 480: 479: 477: 468: 464: 457: 453: 452: 450: 448: 444: 437: 433: 432: 430: 428: 424: 417: 413: 412: 410: 408: 404: 397: 393: 392: 390: 388: 384: 377: 373: 372: 370: 368: 364: 357: 353: 352: 350: 343: 339: 332: 328: 327: 325: 323: 319: 311: 307: 302: 301: 298: 291: 286: 282: 280: 276: 272: 270: 263: 260: 257: 255: 251: 247: 245: 241: 237: 235: 231: 227: 223: 217: 207: 204: 194: 193: 191: 189: 185: 180: 173: 168: 163: 160: 159: 157: 155: 151: 148: 145: 143: 137: 130: 125: 116: 113: 108: 99: 98: 96: 94: 90: 86: 82: 80: 76: 72: 68: 66: 62: 58: 54: 50: 47:Clinical data 45: 41: 36: 32: 27: 19: 2236: 2036:Cyanovirin-N 2026:Calanolide A 1702: 1696:2 generation 1670:1 generation 1657: 1628: 1607:Elvucitabine 1597:Apricitabine 1546: 1487:2 generation 1462: 1441:1 generation 1428: 1415:Fipravirimat 1329: 1324:Semzuvolimab 1313: 1304:Cenicriviroc 1288: 1276: 1264: 1183: 1133: 1129: 1119: 1082: 1078: 1068: 1033: 1029: 1019: 974: 970: 960: 948: 913: 909: 899: 888: 853: 849: 839: 819: 812: 800:. Retrieved 791: 774: 755: 753:inhibitors. 731: 712: 709: 706:Pharmacology 697: 694:Side effects 677: 648: 647: 636:   309: 305: 283:Mostly fecal 273:5 to 6 hours 266:Elimination 188:Legal status 182:Legal status 93:License data 18: 2320:Pyrimidones 2237:recommended 2212:from market 2162:Lersivirine 2137:Capravirine 2076:Miltefosine 2061:Griffithsin 2056:Fosdevirine 1602:Censavudine 1232:(primarily 1180:"Lopinavir" 850:J Pharm Sci 777:long-acting 764:. In 2020, 563: g·mol 506:100.281.362 331:192725-17-0 288:Identifiers 79:MedlinePlus 52:Other names 2289:Categories 2167:Lodenosine 2147:Droxinavir 2132:Brecanavir 2127:Atevirdine 2091:Seliciclib 2086:Scytovirin 2000:Elipovimab 1945:TRIM5alpha 1622:Stampidine 1527:inhibitors 1511:TMC-310911 1410:BMS-955176 1308:Leronlimab 1300:Vicriviroc 977:: 698603. 783:References 688:SARS-CoV-2 653:retroviral 651:is an anti 568:3D model ( 556:Molar mass 416:2494G1JF75 387:ChemSpider 322:CAS Number 297:IUPAC name 254:Metabolism 2222:Phase III 2210:Withdrawn 2187:Telinavir 2182:Palinavir 2177:Mozenavir 2157:Emivirine 2152:Lasinavir 2122:Aplaviroc 2051:Foscarnet 2031:Ceragenin 1592:Amdoxovir 1405:Bevirimat 1382:BI 224436 993:1664-302X 669:ritonavir 649:Lopinavir 456:ChEMBL729 279:Excretion 268:half-life 140:Routes of 129:Lopinavir 65:Drugs.com 23:Lopinavir 2267:Medicine 2172:Loviride 1162:32187464 1111:24841269 1060:25073485 1011:34335531 932:15905676 880:33248057 802:30 April 770:COVID-19 758:MERS-CoV 738:cervices 728:Research 684:COVID-19 639:(verify) 367:DrugBank 170:) ( 154:ATC code 147:By mouth 124:DailyMed 2279:Viruses 2253:Portals 2071:KP-1461 1617:Racivir 1387:MK-2048 1153:7121492 1102:4136071 1051:4253456 1002:8320725 940:3162858 871:7689305 655:of the 561:628.814 523:Formula 376:DB01601 342:PubChem 238:Unknown 164: ( 162:J05AR10 126::  109::  85:a602015 55:ABT-378 2205:WHO-EM 2021:BIT225 2016:Abzyme 1947:(gene) 1634:NtRTIs 1529:(RTIs) 1160:  1150:  1109:  1099:  1058:  1048:  1009:  999:  991:  938:  930:  878:  868:  827:  594:SMILES 447:ChEMBL 436:D01425 248:98-99% 216:℞-only 214: 201: 122:  112:by INN 105:  2325:Ureas 2009:Other 1992:BNAbs 1552:NRTIs 1331:gp120 936:S2CID 747:eEF2K 663:as a 614:InChI 570:JSmol 396:83706 356:92727 259:Liver 2234:DHHS 1290:CCR5 1278:gp41 1158:PMID 1107:PMID 1056:PMID 1007:PMID 989:ISSN 928:PMID 910:AIDS 876:PMID 825:ISBN 804:2004 743:AMPK 680:LMIC 427:KEGG 407:UNII 228:data 61:AHFS 1315:CD4 1234:J05 1230:HIV 1148:PMC 1138:doi 1134:382 1097:PMC 1087:doi 1046:PMC 1038:doi 1034:171 997:PMC 979:doi 918:doi 866:PMC 858:doi 854:110 675:). 472:EPA 346:CID 203:POM 167:WHO 107:EMA 2291:: 2218:: 1322:, 1306:, 1302:, 1224:: 1182:. 1156:. 1146:. 1132:. 1128:. 1105:. 1095:. 1083:58 1081:. 1077:. 1054:. 1044:. 1032:. 1028:. 1005:. 995:. 987:. 975:12 973:. 969:. 934:. 926:. 914:19 912:. 908:. 874:. 864:. 852:. 848:. 775:A 721:50 719:IC 537:48 531:37 308:)- 304:(2 210:US 197:UK 119:US 102:EU 2255:: 2232:° 1820:° 1814:° 1808:° 1797:° 1781:° 1765:° 1662:) 1658:( 1636:: 1632:/ 1554:: 1550:/ 1502:° 1496:° 1433:) 1429:( 1338:) 1334:( 1326:) 1318:( 1310:) 1293:( 1285:) 1281:( 1269:) 1265:( 1236:) 1214:e 1207:t 1200:v 1164:. 1140:: 1113:. 1089:: 1062:. 1040:: 1013:. 981:: 942:. 920:: 882:. 860:: 833:. 806:. 741:( 671:( 572:) 549:5 546:O 543:4 540:N 534:H 528:C 474:) 470:( 310:N 306:S 212:: 199:: 174:) 63:/

Index



AHFS
Drugs.com
International Drug Names
MedlinePlus
a602015
License data
EMA
by INN
DailyMed
Lopinavir
Routes of
administration

By mouth
ATC code
J05AR10
WHO
with ritonavir
Legal status
POM
℞-only
Pharmacokinetic
Bioavailability
Protein binding
Metabolism
Liver
Elimination half-life
Excretion
IUPAC name
CAS Number

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