lopinavir ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
HIV protease inhibitors 1601 192725-17-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lopinavir
  • aluviran
  • koletra
An HIV protease inhibitor used in a fixed-dose combination with RITONAVIR. It is also an inhibitor of CYTOCHROME P-450 CYP3A. There was some evidence of in vitro activity against SARS-CoV-2, but no clinical trial data was found to support use in the treatment of COVID-19.
  • Molecular weight: 628.81
  • Formula: C37H48N4O5
  • CLOGP: 6.09
  • LIPINSKI: 2
  • HAC: 9
  • HDO: 4
  • TPSA: 120
  • ALOGS: -5.51
  • ROTB: 15

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.80 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 2.20 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 24.22 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Sept. 15, 2000 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Exposure during pregnancy 914.41 25.30 389 5714 120626 50478395
Abortion spontaneous 514.92 25.30 192 5911 41580 50557441
Stillbirth 390.25 25.30 99 6004 5853 50593168
Abortion induced 284.18 25.30 85 6018 9259 50589762
Foetal exposure during pregnancy 272.95 25.30 108 5995 27251 50571770
Premature baby 224.28 25.30 84 6019 18253 50580768
Pregnancy 160.48 25.30 76 6027 29501 50569520
Premature labour 116.72 25.30 46 6057 11430 50587591
Live birth 107.21 25.30 48 6055 16360 50582661
Premature rupture of membranes 102.61 25.30 33 6070 4547 50594474
Foetal death 101.84 25.30 38 6065 8142 50590879
Viral mutation identified 86.78 25.30 23 6080 1606 50597415
Maternal exposure during pregnancy 84.47 25.30 100 6003 159678 50439343
Immune reconstitution inflammatory syndrome 81.20 25.30 29 6074 5487 50593534
Fanconi syndrome acquired 78.80 25.30 19 6084 904 50598117
Foetal growth restriction 68.89 25.30 27 6076 6600 50592421
Pre-eclampsia 67.18 25.30 28 6075 8016 50591005
Caesarean section 63.41 25.30 33 6070 15606 50583415
Virologic failure 59.73 25.30 17 6086 1547 50597474
Cushing's syndrome 53.58 25.30 13 6090 635 50598386
Anaemia 53.41 25.30 103 6000 252353 50346668
Patent ductus arteriosus 52.16 25.30 19 6084 3801 50595220
Drug interaction 51.79 25.30 89 6014 199532 50399489
Hepatic cytolysis 50.66 25.30 23 6080 8080 50590941
Viral load increased 50.60 25.30 14 6089 1149 50597872
Trisomy 21 49.37 25.30 11 6092 368 50598653
CD4 lymphocytes decreased 48.65 25.30 14 6089 1325 50597696
Drug resistance 46.97 25.30 29 6074 18960 50580061
Polydactyly 45.90 25.30 10 6093 301 50598720
Coarctation of the aorta 44.85 25.30 11 6092 562 50598459
Premature delivery 43.49 25.30 30 6073 23633 50575388
Gestational diabetes 42.95 25.30 20 6083 7445 50591576
Renal tubular acidosis 42.48 25.30 13 6090 1521 50597500
Ventricular septal defect 36.91 25.30 15 6088 4026 50594995
Maternal drugs affecting foetus 36.84 25.30 16 6087 5061 50593960
Drug ineffective 35.92 25.30 28 6075 819305 49779716
Placental disorder 34.89 25.30 11 6092 1419 50597602
Placenta praevia 34.86 25.30 10 6093 936 50598085
Fatigue 33.85 25.30 22 6081 707579 49891442
Metabolic acidosis 30.46 25.30 30 6073 38795 50560226
Renal tubular disorder 29.15 25.30 11 6092 2426 50596595
Cachexia 28.75 25.30 13 6090 4520 50594501
Hydrocephalus 28.07 25.30 13 6090 4775 50594246
Cardiac malposition 27.70 25.30 5 6098 55 50598966
Atrial septal defect 27.48 25.30 14 6089 6327 50592694
Congenital anomaly 26.23 25.30 9 6094 1512 50597509
Acquired immunodeficiency syndrome 25.90 25.30 5 6098 81 50598940
Blood HIV RNA increased 25.70 25.30 7 6096 542 50598479
Hyperlactacidaemia 25.59 25.30 10 6093 2423 50596598

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Lipodystrophy acquired 359.97 15.22 104 11562 2990 29559871
Mitochondrial toxicity 293.65 15.22 84 11582 2327 29560534
Exposure during pregnancy 256.35 15.22 104 11562 8450 29554411
Progressive external ophthalmoplegia 244.77 15.22 64 11602 1253 29561608
Eyelid ptosis 219.29 15.22 81 11585 5105 29557756
Immune reconstitution inflammatory syndrome 158.26 15.22 72 11594 7730 29555131
Foetal exposure during pregnancy 152.89 15.22 118 11548 33749 29529112
Diplopia 142.23 15.22 80 11586 13438 29549423
Premature baby 136.56 15.22 85 11581 17195 29545666
Kaposi's sarcoma 104.78 15.22 30 11636 832 29562029
Fanconi syndrome acquired 101.39 15.22 35 11631 1807 29561054
Renal tubular disorder 100.52 15.22 44 11622 4308 29558553
Congenital anomaly 72.19 15.22 25 11641 1303 29561558
Cushing's syndrome 72.15 15.22 19 11647 382 29562479
Viral load increased 65.08 15.22 26 11640 2023 29560838
Hyperlactacidaemia 64.85 15.22 28 11638 2650 29560211
Ophthalmoplegia 62.81 15.22 24 11642 1658 29561203
Hypertriglyceridaemia 59.59 15.22 37 11629 7438 29555423
Hyperlipidaemia 57.02 15.22 44 11622 12546 29550315
Trisomy 21 49.97 15.22 15 11651 492 29562369
CD4 lymphocytes decreased 49.79 15.22 20 11646 1578 29561283
Polydactyly 48.88 15.22 18 11648 1122 29561739
Osteonecrosis 45.99 15.22 40 11626 13479 29549382
Cerebral toxoplasmosis 45.08 15.22 18 11648 1398 29561463
Glycosuria 44.90 15.22 17 11649 1145 29561716
Acquired immunodeficiency syndrome 43.68 15.22 13 11653 414 29562447
Drug ineffective 43.16 15.22 48 11618 363122 29199739
Ventricular septal defect 42.92 15.22 23 11643 3506 29559355
Drug resistance 41.95 15.22 47 11619 21493 29541368
Viral mutation identified 41.29 15.22 20 11646 2468 29560393
Blood triglycerides increased 39.72 15.22 36 11630 12798 29550063
Mitochondrial cytopathy 39.50 15.22 10 11656 171 29562690
Drug interaction 39.41 15.22 168 11498 197217 29365644
Osteoporosis 38.94 15.22 33 11633 10736 29552125
Lipoatrophy 37.77 15.22 12 11654 477 29562384
Atypical mycobacterial infection 37.34 15.22 13 11653 688 29562173
Blood lactic acid increased 37.23 15.22 25 11641 5741 29557120
Hypophosphataemia 36.54 15.22 28 11638 7896 29554965
Fanconi syndrome 36.39 15.22 16 11650 1582 29561279
Hepatic failure 34.92 15.22 52 11614 31460 29531401
Liver disorder 33.96 15.22 48 11618 27701 29535160
HIV-associated neurocognitive disorder 33.88 15.22 10 11656 309 29562552
Proteinuria 33.40 15.22 36 11630 15768 29547093
Virologic failure 33.07 15.22 18 11648 2829 29560032
Osteomalacia 30.92 15.22 12 11654 864 29561997
Death 30.85 15.22 55 11611 342029 29220832
Oesophageal candidiasis 30.67 15.22 19 11647 3802 29559059
Kidney malformation 29.53 15.22 8 11658 180 29562681
Blood alkaline phosphatase increased 28.82 15.22 45 11621 28361 29534500
Febrile neutropenia 28.44 15.22 5 11661 112235 29450626
Anal cancer 28.39 15.22 9 11657 355 29562506
Gastroschisis 28.38 15.22 7 11659 107 29562754
Cytomegalovirus chorioretinitis 28.29 15.22 17 11649 3221 29559640
Cryptorchism 27.45 15.22 14 11652 1928 29560933
Hepatic cytolysis 26.98 15.22 24 11642 8323 29554538
Blood bilirubin increased 26.78 15.22 48 11618 33845 29529016
Porphyria non-acute 26.30 15.22 9 11657 452 29562409
Neonatal asphyxia 26.04 15.22 8 11658 284 29562577
HIV wasting syndrome 24.62 15.22 6 11660 87 29562774
HIV infection 24.25 15.22 11 11655 1170 29561691
Lactic acidosis 24.10 15.22 43 11623 30204 29532657
Cachexia 24.07 15.22 20 11646 6329 29556532
Encephalitis 23.85 15.22 20 11646 6410 29556451
Blood phosphorus decreased 22.74 15.22 14 11652 2771 29560090
Hepatic cirrhosis 22.30 15.22 28 11638 14416 29548445
Progressive multifocal leukoencephalopathy 22.28 15.22 22 11644 8697 29554164
Oesophageal atresia 22.26 15.22 8 11658 465 29562396
Pneumocystis jirovecii pneumonia 21.98 15.22 30 11636 16749 29546112
Hepatitis C 21.88 15.22 22 11644 8888 29553973
Opportunistic infection 21.82 15.22 11 11655 1478 29561383
HIV associated nephropathy 21.73 15.22 7 11659 291 29562570
Renal failure 21.36 15.22 98 11568 118501 29444360
Exomphalos 21.21 15.22 6 11660 159 29562702
Product dose omission issue 20.99 15.22 6 11660 96377 29466484
Stillbirth 20.76 15.22 6 11660 172 29562689
Maternal drugs affecting foetus 20.73 15.22 15 11651 3878 29558983
Fatigue 20.40 15.22 61 11605 316760 29246101
Femoral neck fracture 20.15 15.22 13 11653 2790 29560071
Gamma-glutamyltransferase increased 20.02 15.22 37 11629 26700 29536161
Lipohypertrophy 19.56 15.22 6 11660 212 29562649
Foetal distress syndrome 19.55 15.22 9 11657 990 29561871
Caesarean section 19.18 15.22 11 11655 1912 29560949
Castleman's disease 19.17 15.22 4 11662 27 29562834
Congenital hearing disorder 19.15 15.22 5 11661 97 29562764
Aspartate aminotransferase increased 18.78 15.22 59 11607 59666 29503195
CSF virus identified 18.58 15.22 4 11662 32 29562829
Immunoblastic lymphoma 18.44 15.22 3 11663 3 29562858
Lymphogranuloma venereum 17.98 15.22 3 11663 4 29562857
Anaemia neonatal 17.90 15.22 6 11660 283 29562578
Cortisol decreased 17.89 15.22 8 11658 823 29562038
Hodgkin's disease 17.70 15.22 8 11658 844 29562017
Segmented hyalinising vasculitis 17.52 15.22 4 11662 43 29562818
Drug abuse 17.34 15.22 5 11661 79878 29482983
Acute kidney injury 17.32 15.22 170 11496 265097 29297764
Completed suicide 17.25 15.22 7 11659 90239 29472622
Syphilis 16.84 15.22 6 11660 340 29562521
Cushingoid 16.77 15.22 11 11655 2427 29560434
Amylase increased 16.71 15.22 15 11651 5265 29557596
Adrenogenital syndrome 16.41 15.22 4 11662 58 29562803
Abdominal hernia 16.36 15.22 11 11655 2529 29560332
Dyspnoea 16.30 15.22 70 11596 326662 29236199
Disease progression 16.24 15.22 6 11660 81910 29480951
Trisomy 8 16.17 15.22 4 11662 62 29562799
Hyperphosphaturia 15.93 15.22 4 11662 66 29562795
Off label use 15.90 15.22 63 11603 300737 29262124
Central pain syndrome 15.82 15.22 4 11662 68 29562793
Cardiac murmur 15.64 15.22 16 11650 6597 29556264
Lymphadenopathy 15.51 15.22 32 11634 25017 29537844
Portal hypertension 15.38 15.22 12 11654 3474 29559387
CD4 lymphocytes increased 15.36 15.22 5 11661 215 29562646
Alanine aminotransferase increased 15.35 15.22 62 11604 70882 29491979
Blood pressure increased 15.33 15.22 5 11661 73798 29489063
Toxoplasmosis 15.31 15.22 8 11658 1159 29561702
Atrial septal defect 15.29 15.22 16 11650 6773 29556088

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Exposure during pregnancy 490.32 17.34 251 11355 77424 64409702
Abortion spontaneous 426.85 17.34 163 11443 24980 64462146
Lipodystrophy acquired 388.95 17.34 99 11507 3928 64483198
Mitochondrial toxicity 339.14 17.34 82 11524 2624 64484502
Stillbirth 300.69 17.34 79 11527 3554 64483572
Progressive external ophthalmoplegia 294.24 17.34 64 11542 1263 64485863
Abortion induced 223.12 17.34 71 11535 6317 64480809
Eyelid ptosis 221.76 17.34 78 11528 9447 64477679
Immune reconstitution inflammatory syndrome 212.00 17.34 81 11525 12389 64474737
Diplopia 149.87 17.34 80 11526 26685 64460441
Viral mutation identified 128.52 17.34 40 11566 3306 64483820
Drug resistance 127.12 17.34 79 11527 35023 64452103
Fanconi syndrome acquired 123.41 17.34 36 11570 2385 64484741
Pregnancy 99.21 17.34 56 11550 20809 64466317
Drug interaction 97.15 17.34 206 11400 361877 64125249
Viral load increased 92.45 17.34 29 11577 2458 64484668
Renal tubular disorder 91.46 17.34 36 11570 5951 64481175
Cushing's syndrome 89.91 17.34 23 11583 928 64486198
Live birth 87.62 17.34 42 11564 11162 64475964
Premature rupture of membranes 77.07 17.34 28 11578 3716 64483410
Hyperlactacidaemia 73.54 17.34 29 11577 4815 64482311
CD4 lymphocytes decreased 72.54 17.34 24 11582 2411 64484715
Foetal death 71.19 17.34 30 11576 5900 64481226
Ophthalmoplegia 66.21 17.34 23 11583 2679 64484447
Foetal exposure during pregnancy 58.30 17.34 24 11582 4452 64482674
Premature labour 57.87 17.34 28 11578 7592 64479534
Maternal exposure during pregnancy 55.58 17.34 77 11529 95807 64391319
Hypertriglyceridaemia 47.71 17.34 28 11578 11177 64475949
Virologic failure 46.55 17.34 19 11587 3447 64483679
Kaposi's sarcoma 46.54 17.34 13 11593 736 64486390
Caesarean section 44.94 17.34 27 11579 11247 64475879
Hepatic failure 43.94 17.34 52 11554 55342 64431784
Blood triglycerides increased 43.22 17.34 32 11574 18834 64468292
Renal tubular acidosis 42.31 17.34 17 11589 2962 64484164
Acquired immunodeficiency syndrome 39.72 17.34 9 11597 215 64486911
Drug ineffective 38.98 17.34 57 11549 840190 63646936
Cerebral toxoplasmosis 38.87 17.34 14 11592 1812 64485314
Placenta praevia 38.21 17.34 11 11595 695 64486431
Fanconi syndrome 38.06 17.34 15 11591 2486 64484640
Opportunistic infection 37.15 17.34 15 11591 2647 64484479
Pre-eclampsia 35.91 17.34 19 11587 6212 64480914
Blood lactic acid increased 34.10 17.34 22 11584 10379 64476747
Hypophosphataemia 33.79 17.34 25 11581 14695 64472431
Glycosuria 33.54 17.34 13 11593 2061 64485065
Portal hypertension 33.13 17.34 18 11588 6201 64480925
Cytomegalovirus chorioretinitis 31.23 17.34 16 11590 4896 64482230
HIV wasting syndrome 31.01 17.34 6 11600 64 64487062
Premature baby 30.96 17.34 14 11592 3258 64483868
Blood alkaline phosphatase increased 30.81 17.34 44 11562 56235 64430891
Lipoatrophy 30.28 17.34 9 11597 636 64486490
Renal failure 29.99 17.34 86 11520 181602 64305524
Mitochondrial cytopathy 29.90 17.34 8 11598 385 64486741
Gestational diabetes 29.28 17.34 16 11590 5574 64481552
Maternal drugs affecting foetus 29.23 17.34 11 11595 1609 64485517
Anaemia neonatal 29.16 17.34 5 11601 25 64487101
Hepatomegaly 28.66 17.34 24 11582 16858 64470268
Blood bilirubin increased 28.62 17.34 43 11563 57510 64429616
Osteonecrosis 28.39 17.34 30 11576 28199 64458927
Hepatic cytolysis 28.14 17.34 22 11584 14027 64473099
Neutropenia neonatal 27.85 17.34 5 11601 34 64487092
Atypical mycobacterial infection 27.73 17.34 10 11596 1298 64485828
Completed suicide 27.19 17.34 4 11602 224410 64262716
Pneumocystis jirovecii pneumonia 27.14 17.34 29 11577 27605 64459521
HIV associated nephropathy 27.09 17.34 7 11599 294 64486832
Premature delivery 26.66 17.34 24 11582 18565 64468561
Acute kidney injury 26.33 17.34 154 11452 449086 64038040
Aspartate aminotransferase increased 26.20 17.34 63 11543 119725 64367401
Hyperlipidaemia 25.96 17.34 26 11580 22950 64464176
Fatigue 25.63 17.34 61 11545 748669 63738457
Proteinuria 25.31 17.34 28 11578 27695 64459431
Anaemia 24.95 17.34 134 11472 378546 64108580
HIV viraemia 24.02 17.34 5 11601 79 64487047
Liver disorder 23.92 17.34 38 11568 53313 64433813
Gamma-glutamyltransferase increased 23.77 17.34 36 11570 48474 64438652
Joint swelling 23.57 17.34 5 11601 215377 64271749
Metabolic acidosis 23.25 17.34 44 11562 70914 64416212
Hepatotoxicity 22.99 17.34 32 11574 39930 64447196
Blood HIV RNA increased 22.93 17.34 9 11597 1475 64485651
Mycobacterium avium complex infection 22.66 17.34 12 11594 3928 64483198
Lactic acidosis 22.54 17.34 40 11566 61370 64425756
Pancreatitis 22.11 17.34 39 11567 59568 64427558
Cachexia 21.93 17.34 16 11590 9201 64477925
HIV-associated neurocognitive disorder 21.83 17.34 6 11600 320 64486806
Hepatosplenomegaly 21.82 17.34 13 11593 5330 64481796
Progressive multifocal leukoencephalopathy 21.28 17.34 21 11585 18211 64468915
CSF virus identified 21.09 17.34 4 11602 38 64487088
Death neonatal 20.91 17.34 4 11602 40 64487086
Immunoblastic lymphoma 20.79 17.34 3 11603 3 64487123
Anembryonic gestation 20.75 17.34 6 11600 385 64486741
Lymphadenopathy 20.58 17.34 33 11573 46653 64440473
Pulmonary tuberculosis 20.55 17.34 14 11592 7230 64479896
Lipohypertrophy 20.40 17.34 7 11599 785 64486341
Product dose omission issue 20.35 17.34 5 11601 194742 64292384
Adrenal suppression 20.34 17.34 8 11598 1319 64485807
Osteomalacia 19.97 17.34 8 11598 1383 64485743
Dyspnoea 19.79 17.34 65 11541 718609 63768517
Encephalitis 19.56 17.34 17 11589 12554 64474572
Fall 19.51 17.34 28 11578 416798 64070328
Multiple-drug resistance 19.48 17.34 13 11593 6489 64480637
Hepatitis C 19.41 17.34 16 11590 10999 64476127
Alanine aminotransferase increased 19.35 17.34 62 11544 138969 64348157
Urinary tract infection 18.93 17.34 9 11597 231587 64255539
Atypical mycobacterial lymphadenitis 18.71 17.34 3 11603 9 64487117
Hyperbilirubinaemia 18.64 17.34 21 11585 21184 64465942
Segmented hyalinising vasculitis 18.19 17.34 4 11602 83 64487043
Premature separation of placenta 17.89 17.34 7 11599 1137 64485989
Osteoporosis 17.53 17.34 29 11577 42051 64445075

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AR10 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
FDA MoA N0000000246 HIV Protease Inhibitors
FDA EPC N0000175889 Protease Inhibitor
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000190107 Organic Anion Transporting Polypeptide 1B1 Inhibitors
FDA MoA N0000190114 Cytochrome P450 3A Inhibitors
CHEBI has role CHEBI:35660 HIV protease inhibitors
CHEBI has role CHEBI:36044 antiviral drugs
CHEBI has role CHEBI:149553 anticoronaviral drug
MeSH PA D019380 Anti-HIV Agents
MeSH PA D000890 Anti-Infective Agents
MeSH PA D044966 Anti-Retroviral Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D065692 Cytochrome P-450 CYP3A Inhibitors
MeSH PA D065607 Cytochrome P-450 Enzyme Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D017320 HIV Protease Inhibitors
MeSH PA D065606 Metabolic Side Effects of Drugs and Substances
MeSH PA D011480 Protease Inhibitors
MeSH PA D000084762 Viral Protease Inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Human immunodeficiency virus infection indication 86406008 DOID:526
Coronavirus infection off-label use 186747009
Prevention of HIV Infection after Exposure off-label use
Hyperbilirubinemia contraindication 14783006 DOID:2741
Cirrhosis of liver contraindication 19943007 DOID:5082
Complete atrioventricular block contraindication 27885002
Hereditary factor VIII deficiency disease contraindication 28293008 DOID:12134
Torsades de pointes contraindication 31722008
Hereditary factor IX deficiency disease contraindication 41788008 DOID:12259
Hypokalemia contraindication 43339004
Conduction disorder of the heart contraindication 44808001
Chronic type B viral hepatitis contraindication 61977001
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Cardiomyopathy contraindication 85898001 DOID:0050700
Prolonged QT interval contraindication 111975006
Chronic hepatitis C contraindication 128302006
Structural disorder of heart contraindication 128599005
Liver function tests abnormal contraindication 166603001
Hypomagnesemia contraindication 190855004
Second degree atrioventricular block contraindication 195042002
Acute pancreatitis contraindication 197456007 DOID:2913
Disease of liver contraindication 235856003 DOID:409
Mixed hyperlipidemia contraindication 267434003
Hypertriglyceridemia contraindication 302870006
Breastfeeding (mother) contraindication 413712001
Myocardial ischemia contraindication 414795007 DOID:3393
Congenital long QT syndrome contraindication 442917000
First Degree Atrioventricular Heart Block contraindication




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.03 acidic
pKa2 12.72 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Multidrug resistance protein 1 Transporter IC50 4.99 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.07 CHEMBL
Pol polyprotein Enzyme INHIBITOR Ki 10.40 CHEMBL CHEMBL
Gag-Pol polyprotein Polyprotein WOMBAT-PK
CAAX prenyl protease 1 homolog Enzyme IC50 4.74 CHEMBL
Protease Enzyme IC50 7.60 CHEMBL
Protease Unclassified Ki 10.59 CHEMBL
Protease Unclassified Ki 10.54 CHEMBL

External reference:

IDSource
4021228 VUID
N0000179581 NUI
D01425 KEGG_DRUG
4021228 VANDF
C0674432 UMLSCUI
CHEBI:31781 CHEBI
AB1 PDB_CHEM_ID
CHEMBL729 ChEMBL_ID
D061466 MESH_DESCRIPTOR_UI
DB01601 DRUGBANK_ID
11504 IUPHAR_LIGAND_ID
7798 INN_ID
2494G1JF75 UNII
92727 PUBCHEM_CID
195088 RXNORM
15774 MMSL
d04716 MMSL
008874 NDDF
129475001 SNOMEDCT_US
387067003 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 0074-0522 TABLET, FILM COATED 100 mg ORAL NDA 32 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 0074-1575 TABLET, FILM COATED 100 mg ORAL NDA 32 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 0074-2605 TABLET, FILM COATED 200 mg ORAL NDA 32 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 0074-3956 SOLUTION 80 mg ORAL NDA 32 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 0074-6799 TABLET, FILM COATED 200 mg ORAL NDA 32 sections
Lopinavir-Ritonavir HUMAN PRESCRIPTION DRUG LABEL 2 0527-1947 SOLUTION 80 mg ORAL ANDA 27 sections
Lopinavir-Ritonavir HUMAN PRESCRIPTION DRUG LABEL 2 0527-1947 SOLUTION 80 mg ORAL ANDA 27 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 11819-342 TABLET, FILM COATED 200 mg ORAL NDA 27 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 21695-362 TABLET, FILM COATED 200 mg ORAL NDA 27 sections
Lopinavir and ritonavir HUMAN PRESCRIPTION DRUG LABEL 2 31722-556 TABLET, FILM COATED 200 mg ORAL ANDA 27 sections
Lopinavir and ritonavir HUMAN PRESCRIPTION DRUG LABEL 2 31722-603 TABLET, FILM COATED 100 mg ORAL ANDA 27 sections
Lopinavir and Ritonavir Human Prescription Drug Label 2 42385-933 TABLET, FILM COATED 100 mg ORAL ANDA 28 sections
Lopinavir and Ritonavir Human Prescription Drug Label 2 42385-934 TABLET, FILM COATED 200 mg ORAL ANDA 28 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 53808-0276 TABLET, FILM COATED 200 mg ORAL NDA 27 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 54868-5566 TABLET, FILM COATED 200 mg ORAL NDA 27 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 55289-947 TABLET, FILM COATED 200 mg ORAL NDA 27 sections
Lopinavir and Ritonavir HUMAN PRESCRIPTION DRUG LABEL 2 65015-299 GRANULE 40 mg ORAL Export only 1 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 66336-624 TABLET, FILM COATED 200 mg ORAL NDA 27 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 68071-2348 TABLET, FILM COATED 200 mg ORAL NDA 25 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 68258-1972 TABLET, FILM COATED 200 mg ORAL NDA 27 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 70518-0091 TABLET, FILM COATED 200 mg ORAL NDA 26 sections