lopinavir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 0 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC 17
kinase-selectivity-class AXL,GRK2,PDK4 3
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 18.450 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Sept. 15, 2000 FDA
March 19, 2001 EMA ABBVIE DEUTSCHLAND GMBH CO. KG

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 884.82 28.99 404 6390 238006 90383647
Abortion spontaneous 622.27 28.99 209 6585 53847 90567806
Stillbirth 414.95 28.99 99 6695 7344 90614309
Abortion induced 303.83 28.99 85 6709 11803 90609850
Foetal exposure during pregnancy 289.54 28.99 112 6682 42863 90578790
Premature baby 237.54 28.99 84 6710 24993 90596660
Pregnancy 141.34 28.99 76 6718 61971 90559682
Premature labour 131.14 28.99 46 6748 13330 90608323
Premature rupture of membranes 111.77 28.99 33 6761 5525 90616128
Caesarean section 106.01 28.99 43 6751 18534 90603119
Viral mutation identified 97.71 28.99 24 6770 2001 90619652
Immune reconstitution inflammatory syndrome 95.95 28.99 31 6763 6988 90614665
Foetal death 85.14 28.99 38 6756 20685 90600968
Fanconi syndrome acquired 81.69 28.99 19 6775 1255 90620398
Maternal exposure during pregnancy 79.25 28.99 115 6679 359948 90261705
Hepatic cytolysis 73.51 28.99 39 6755 30877 90590776
Foetal growth restriction 72.25 28.99 27 6767 9353 90612300
Pre-eclampsia 71.46 28.99 28 6766 11020 90610633
Virologic failure 71.17 28.99 19 6775 2205 90619448
Live birth 64.82 28.99 51 6743 79056 90542597
Anaemia 63.92 28.99 103 6691 352699 90268954
Schizophrenia 63.35 28.99 28 6766 14886 90606767
Drug interaction 63.25 28.99 90 6704 276363 90345290
Cushing's syndrome 59.97 28.99 13 6781 623 90621030
Patent ductus arteriosus 57.67 28.99 19 6775 4550 90617103
Hypomania 55.61 28.99 22 6772 8875 90612778
CD4 lymphocytes decreased 53.24 28.99 14 6780 1533 90620120
Viral load increased 53.16 28.99 14 6780 1542 90620111
Trisomy 21 52.51 28.99 11 6783 447 90621206
Drug resistance 52.21 28.99 31 6763 30418 90591235
Polydactyly 50.20 28.99 10 6784 315 90621338
Coarctation of the aorta 49.12 28.99 11 6783 613 90621040
Premature delivery 47.74 28.99 32 6762 38730 90582923
Ultrasound antenatal screen 47.50 28.99 9 6785 217 90621436
Hepatotoxicity 47.43 28.99 34 6760 45808 90575845
Gestational diabetes 45.37 28.99 20 6774 10562 90611091
Maternal drugs affecting foetus 43.98 28.99 16 6778 5139 90616514
Cardiac murmur 43.38 28.99 23 6771 18171 90603482
Aspartate aminotransferase increased 40.41 28.99 44 6750 102893 90518760
Ventricular septal defect 39.59 28.99 15 6779 5392 90616261
Placental disorder 38.76 28.99 11 6783 1600 90620053
Drug ineffective 38.22 28.99 29 6765 1384269 89237384
Portal hypertension 37.91 28.99 14 6780 4687 90616966
Placenta praevia 37.85 28.99 10 6784 1115 90620538
Cholelithiasis 36.97 28.99 31 6763 52475 90569178
Cachexia 36.09 28.99 15 6779 6863 90614790
Renal tubular acidosis 34.82 28.99 11 6783 2304 90619349
Fatigue 34.70 28.99 22 6772 1154001 89467652
Alanine aminotransferase increased 33.83 28.99 43 6751 118295 90503358
Jaundice cholestatic 33.67 28.99 16 6778 10027 90611626
Hydrops foetalis 33.33 28.99 8 6786 605 90621048
Trisomy 18 31.57 28.99 6 6788 147 90621506
Renal tubular disorder 31.31 28.99 11 6783 3196 90618457
Blood bilirubin increased 31.29 28.99 26 6768 43444 90578209
Hydrocephalus 31.00 28.99 13 6781 6081 90615572
Cardiac malposition 30.60 28.99 5 6789 49 90621604
Atrial septal defect 30.33 28.99 14 6780 8220 90613433
Asthma-chronic obstructive pulmonary disease overlap syndrome 30.22 28.99 12 6782 4887 90616766
Total lung capacity increased 29.93 28.99 12 6782 5009 90616644
Metabolic acidosis 29.51 28.99 28 6766 55648 90566005

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 429.14 15.96 114 12057 3336 42605828
Mitochondrial toxicity 342.34 15.96 90 12081 2525 42606639
Exposure during pregnancy 315.63 15.96 111 12060 8437 42600727
Progressive external ophthalmoplegia 296.80 15.96 71 12100 1340 42607824
Eyelid ptosis 259.34 15.96 90 12081 6571 42602593
Foetal exposure during pregnancy 187.56 15.96 134 12037 47177 42561987
Immune reconstitution inflammatory syndrome 162.44 15.96 72 12099 10071 42599093
Diplopia 157.37 15.96 88 12083 20228 42588936
Premature baby 141.51 15.96 86 12085 23067 42586097
Kaposi's sarcoma 116.78 15.96 30 12141 765 42608399
Renal tubular disorder 109.12 15.96 44 12127 4865 42604299
Fanconi syndrome acquired 104.41 15.96 34 12137 2036 42607128
Congenital anomaly 80.52 15.96 26 12145 1515 42607649
Cushing's syndrome 78.77 15.96 19 12152 371 42608793
Trisomy 18 77.03 15.96 22 12149 843 42608321
Ultrasound antenatal screen 76.61 15.96 20 12151 544 42608620
Cleft lip and palate 75.41 15.96 22 12149 910 42608254
Ophthalmoplegia 71.45 15.96 26 12145 2174 42606990
Hydrops foetalis 67.25 15.96 20 12151 885 42608279
Viral load increased 63.64 15.96 26 12145 2971 42606193
Drug ineffective 61.62 15.96 54 12117 630143 41979021
Hypertriglyceridaemia 60.26 15.96 37 12134 10089 42599075
Hyperlactacidaemia 59.50 15.96 28 12143 4488 42604676
Drug interaction 55.72 15.96 185 11986 266814 42342350
Polydactyly 53.17 15.96 18 12153 1216 42607948
Trisomy 21 52.72 15.96 15 12156 567 42608597
Osteonecrosis 51.71 15.96 40 12131 15825 42593339
CD4 lymphocytes decreased 48.92 15.96 19 12152 1902 42607262
Hyperlipidaemia 48.83 15.96 44 12127 21472 42587692
Glycosuria 47.52 15.96 17 12154 1353 42607811
Drug resistance 46.43 15.96 53 12118 34195 42574969
Acquired immunodeficiency syndrome 45.59 15.96 13 12158 495 42608669
Ventricular septal defect 45.15 15.96 23 12148 4376 42604788
Blood lactic acid increased 44.36 15.96 28 12143 8011 42601153
Mitochondrial cytopathy 43.87 15.96 10 12161 151 42609013
Cerebral toxoplasmosis 43.86 15.96 18 12153 2080 42607084
Abortion spontaneous 43.86 15.96 12 12159 392 42608772
Caesarean section 43.79 15.96 18 12153 2088 42607076
Blood triglycerides increased 43.13 15.96 36 12135 15860 42593304
Lipoatrophy 42.71 15.96 12 12159 433 42608731
Viral mutation identified 41.88 15.96 20 12151 3311 42605853
Fanconi syndrome 39.59 15.96 16 12155 1778 42607386
Osteoporosis 38.88 15.96 33 12138 14873 42594291
Hepatic failure 38.74 15.96 51 12120 38049 42571115
Aspartate aminotransferase increased 37.79 15.96 74 12097 77089 42532075
Febrile neutropenia 36.32 15.96 5 12166 185698 42423466
HIV-associated neurocognitive disorder 36.22 15.96 10 12161 338 42608826
Osteomalacia 34.60 15.96 12 12159 872 42608292
Blood alkaline phosphatase increased 34.19 15.96 45 12126 33552 42575612
Alanine aminotransferase increased 33.11 15.96 76 12095 88330 42520834
Atypical mycobacterial infection 32.98 15.96 13 12158 1353 42607811
Virologic failure 32.81 15.96 18 12153 3976 42605188
Kidney malformation 31.92 15.96 8 12163 184 42608980
Proteinuria 31.87 15.96 36 12135 22947 42586217
Blood bilirubin increased 31.79 15.96 49 12122 42203 42566961
Liver disorder 31.28 15.96 47 12124 39597 42569567
Cryptorchism 31.19 15.96 14 12157 2013 42607151
Death 29.72 15.96 56 12115 471129 42138035
Hepatitis C 29.69 15.96 24 12147 10109 42599055
Oesophageal candidiasis 29.53 15.96 19 12152 5616 42603548
Anal cancer 29.08 15.96 9 12162 456 42608708
Hepatic cytolysis 28.95 15.96 37 12134 26807 42582357
Porphyria non-acute 28.55 15.96 9 12162 485 42608679
Off label use 28.41 15.96 91 12080 638244 41970920
Cytomegalovirus chorioretinitis 27.81 15.96 17 12154 4594 42604570
Renal failure 27.60 15.96 97 12074 143629 42465535
Gastroschisis 27.34 15.96 7 12164 176 42608988
HIV wasting syndrome 27.16 15.96 6 12165 78 42609086
Product dose omission issue 26.18 15.96 6 12165 154359 42454805
Cachexia 25.46 15.96 20 12151 8084 42601080
Maternal drugs affecting foetus 25.35 15.96 15 12156 3824 42605340
HIV infection 25.24 15.96 11 12160 1474 42607690
Progressive multifocal leukoencephalopathy 25.01 15.96 23 12148 11513 42597651
Neonatal asphyxia 24.74 15.96 8 12163 468 42608696
Oesophageal atresia 23.91 15.96 8 12163 521 42608643
Disease progression 23.54 15.96 6 12165 143650 42465514
Gamma-glutamyltransferase increased 23.49 15.96 37 12134 32460 42576704
Encephalitis 23.32 15.96 20 12151 9138 42600026
HIV associated nephropathy 22.77 15.96 7 12164 347 42608817
Hepatic cirrhosis 22.58 15.96 28 12143 19674 42589490
Opportunistic infection 22.11 15.96 11 12160 1990 42607174
Stillbirth 21.93 15.96 6 12165 196 42608968
Lactic acidosis 21.65 15.96 43 12128 45218 42563946
Pneumocystis jirovecii pneumonia 21.51 15.96 31 12140 25150 42584014
Exomphalos 21.50 15.96 6 12165 211 42608953
Hypophosphataemia 21.22 15.96 28 12143 20917 42588247
Blood phosphorus decreased 21.04 15.96 13 12158 3580 42605584
Foetal distress syndrome 20.86 15.96 9 12162 1177 42607987
Congenital hearing disorder 20.76 15.96 5 12166 97 42609067
Castleman's disease 20.46 15.96 4 12167 27 42609137
Hodgkin's disease 20.41 15.96 8 12163 820 42608344
Portal hypertension 19.94 15.96 14 12157 4773 42604391
Depression suicidal 19.67 15.96 12 12159 3233 42605931
CSF virus identified 19.55 15.96 4 12167 35 42609129
Lipohypertrophy 19.52 15.96 6 12165 297 42608867
Immunoblastic lymphoma 19.41 15.96 3 12168 3 42609161
Fatigue 19.39 15.96 62 12109 435579 42173585
Femoral neck fracture 19.16 15.96 13 12158 4196 42604968
Psychomotor skills impaired 18.89 15.96 14 12157 5190 42603974
Tearfulness 18.83 15.96 12 12159 3488 42605676
Segmented hyalinising vasculitis 18.80 15.96 4 12167 43 42609121
COVID-19 18.69 15.96 5 12166 115943 42493221
Acute kidney injury 18.64 15.96 173 11998 367164 42242000
CD4 lymphocytes increased 18.43 15.96 5 12166 158 42609006
Adrenogenital syndrome 18.32 15.96 4 12167 49 42609115
Jaundice 17.93 15.96 34 12137 34555 42574609
Lymphogranuloma venereum 17.87 15.96 3 12168 7 42609157
Depressive symptom 17.78 15.96 12 12159 3841 42605323
Abdominal hernia 17.76 15.96 11 12160 3044 42606120
Amylase increased 17.75 15.96 15 12156 6714 42602450
Anaemia neonatal 17.71 15.96 6 12165 406 42608758
Atrial septal defect 17.58 15.96 16 12155 7903 42601261
Dysmorphism 16.93 15.96 11 12160 3305 42605859
Trisomy 8 16.89 15.96 4 12167 72 42609092
Psychiatric decompensation 16.79 15.96 12 12159 4210 42604954
Cushingoid 16.61 15.96 11 12160 3411 42605753
Cortisol decreased 16.49 15.96 8 12163 1370 42607794
Hyperphosphaturia 16.35 15.96 4 12167 83 42609081
Lymphadenopathy 16.32 15.96 32 12139 33333 42575831
Hypospadias 16.20 15.96 11 12160 3556 42605608

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
Abortion spontaneous 550.91 19.08 190 12575 34092 110542442
Lipodystrophy acquired 474.16 19.08 109 12656 4415 110572119
Exposure during pregnancy 463.80 19.08 270 12495 167154 110409380
Mitochondrial toxicity 393.10 19.08 88 12677 3157 110573377
Progressive external ophthalmoplegia 360.41 19.08 71 12694 1349 110575185
Stillbirth 322.92 19.08 79 12686 4185 110572349
Eyelid ptosis 265.89 19.08 87 12678 13240 110563294
Abortion induced 238.26 19.08 71 12694 7948 110568586
Immune reconstitution inflammatory syndrome 226.24 19.08 81 12684 16145 110560389
Diplopia 172.42 19.08 88 12677 41806 110534728
Drug resistance 145.35 19.08 87 12678 56287 110520247
Viral mutation identified 139.43 19.08 41 12724 4378 110572156
Drug interaction 138.52 19.08 224 12541 499959 110076575
Fanconi syndrome acquired 131.18 19.08 36 12729 2998 110573536
Ultrasound antenatal screen 129.79 19.08 27 12738 679 110575855
Foetal exposure during pregnancy 125.84 19.08 43 12722 7462 110569072
Hydrops foetalis 121.39 19.08 26 12739 755 110575779
Trisomy 18 115.62 19.08 24 12741 597 110575937
Cleft lip and palate 111.69 19.08 24 12741 708 110575826
Caesarean section 103.63 19.08 44 12721 13773 110562761
Cushing's syndrome 100.57 19.08 23 12742 907 110575627
Renal tubular disorder 99.45 19.08 36 12729 7393 110569141
Viral load increased 96.29 19.08 29 12736 3361 110573173
Premature rupture of membranes 83.37 19.08 28 12737 4609 110571925
Aspartate aminotransferase increased 82.63 19.08 97 12668 159839 110416695
Ophthalmoplegia 78.21 19.08 25 12740 3525 110573009
Pregnancy 76.07 19.08 56 12709 51011 110525523
CD4 lymphocytes decreased 74.07 19.08 23 12742 2951 110573583
Hyperlactacidaemia 70.93 19.08 29 12736 8257 110568277
Alanine aminotransferase increased 68.86 19.08 95 12670 183678 110392856
Premature labour 64.79 19.08 28 12737 9144 110567390
Hepatic cytolysis 61.65 19.08 51 12714 55002 110521532
Blood bilirubin increased 60.44 19.08 58 12707 75914 110500620
Portal hypertension 59.81 19.08 26 12739 8611 110567923
Foetal death 55.43 19.08 30 12735 16015 110560519
Virologic failure 55.27 19.08 21 12744 4931 110571603
Kaposi's sarcoma 53.10 19.08 13 12752 689 110575845
Hepatic failure 51.90 19.08 51 12714 68688 110507846
Hypertriglyceridaemia 49.75 19.08 28 12737 16126 110560408
Drug ineffective 49.51 19.08 62 12703 1520478 109056056
Blood triglycerides increased 49.19 19.08 32 12733 23894 110552640
Maternal exposure during pregnancy 47.13 19.08 96 12669 254787 110321747
Schizophrenia 46.87 19.08 30 12735 21796 110554738
Hepatotoxicity 45.94 19.08 46 12719 63354 110513180
Hypomania 43.59 19.08 22 12743 10188 110566346
Blood lactic acid increased 42.26 19.08 25 12740 15796 110560738
Placenta praevia 41.75 19.08 11 12754 784 110575750
Renal failure 41.48 19.08 85 12680 226489 110350045
Fanconi syndrome 39.55 19.08 15 12750 3504 110573030
Acquired immunodeficiency syndrome 39.50 19.08 9 12756 349 110576185
Opportunistic infection 39.45 19.08 15 12750 3528 110573006
Blood alkaline phosphatase increased 38.23 19.08 44 12721 70891 110505643
Pre-eclampsia 37.99 19.08 19 12746 8631 110567903
Cerebral toxoplasmosis 37.52 19.08 14 12751 3128 110573406
Live birth 37.28 19.08 43 12722 69441 110507093
Glycosuria 36.15 19.08 13 12752 2617 110573917
Acute kidney injury 36.11 19.08 157 12608 635273 109941261
Renal tubular acidosis 35.30 19.08 15 12750 4700 110571834
Osteonecrosis 35.17 19.08 30 12735 33711 110542823
Joint swelling 34.58 19.08 5 12760 442840 110133694
Lipoatrophy 34.39 19.08 9 12756 625 110575909
Maternal drugs affecting foetus 34.03 19.08 11 12754 1606 110574928
Mitochondrial cytopathy 33.39 19.08 8 12757 387 110576147
Anaemia 33.25 19.08 138 12627 546948 110029586
Hepatomegaly 33.05 19.08 24 12741 21390 110555144
HIV wasting syndrome 32.95 19.08 6 12759 73 110576461
Pneumocystis jirovecii pneumonia 32.80 19.08 32 12733 42703 110533831
Cytomegalovirus chorioretinitis 32.32 19.08 16 12749 7112 110569422
Gestational diabetes 31.77 19.08 16 12749 7373 110569161
Premature baby 31.62 19.08 14 12751 4841 110571693
Cholelithiasis 30.30 19.08 37 12728 63385 110513149
Anaemia neonatal 30.20 19.08 5 12760 33 110576501
Neutropenia neonatal 29.94 19.08 5 12760 35 110576499
Psychotic disorder 29.83 19.08 33 12732 50904 110525630
Progressive multifocal leukoencephalopathy 29.78 19.08 24 12741 24932 110551602
Gamma-glutamyltransferase increased 29.67 19.08 36 12729 61273 110515261
Mycobacterium avium complex infection 29.07 19.08 14 12751 5863 110570671
HIV associated nephropathy 28.89 19.08 7 12758 355 110576179
Cachexia 28.23 19.08 18 12747 12987 110563547
Fatigue 27.94 19.08 62 12703 1215896 109360638
Swelling 27.31 19.08 4 12761 351037 110225497
Proteinuria 27.10 19.08 28 12737 39990 110536544
Liver function test abnormal 26.32 19.08 36 12729 68914 110507620
Tearfulness 26.02 19.08 14 12751 7381 110569153
Hyperlipidaemia 25.94 19.08 26 12739 35822 110540712
Hypophosphataemia 25.75 19.08 25 12740 33157 110543377
Premature delivery 25.52 19.08 24 12741 30608 110545926
Depression suicidal 25.41 19.08 12 12753 4812 110571722
Atypical mycobacterial infection 24.94 19.08 10 12755 2708 110573826
Total lung capacity increased 24.74 19.08 12 12753 5100 110571434
Alopecia 24.46 19.08 6 12759 364747 110211787
HIV viraemia 24.30 19.08 5 12760 119 110576415
Hepatosplenomegaly 24.07 19.08 13 12752 6906 110569628
Metabolic acidosis 23.91 19.08 42 12723 99702 110476832
Lymphadenopathy 23.87 19.08 33 12732 63802 110512732
Hepatitis C 23.86 19.08 16 12749 12557 110563977
Psychomotor skills impaired 23.83 19.08 13 12752 7045 110569489
Varices oesophageal 23.56 19.08 13 12752 7202 110569332
Lactic acidosis 23.44 19.08 40 12725 92771 110483763
Blood HIV RNA increased 23.42 19.08 9 12756 2179 110574355
Psychiatric decompensation 23.38 19.08 12 12753 5753 110570781
Pain 23.32 19.08 47 12718 954908 109621626
Pulmonary tuberculosis 23.26 19.08 14 12751 9125 110567409
Pancreatitis 23.22 19.08 40 12725 93493 110483041
HIV-associated neurocognitive disorder 23.13 19.08 6 12759 402 110576132
CSF virus identified 22.87 19.08 4 12761 38 110576496
Anembryonic gestation 22.77 19.08 6 12759 428 110576106
Osteomalacia 22.40 19.08 8 12757 1579 110574955
Asthma-chronic obstructive pulmonary disease overlap syndrome 22.30 19.08 12 12753 6332 110570202
Product dose omission issue 22.16 19.08 5 12760 321777 110254757
Immunoblastic lymphoma 22.12 19.08 3 12762 3 110576531
Anticoagulation drug level increased 21.96 19.08 7 12758 978 110575556
Adrenal suppression 21.88 19.08 8 12757 1688 110574846
Lipohypertrophy 21.81 19.08 7 12758 999 110575535
Jaundice cholestatic 21.70 19.08 16 12749 14592 110561942
Jaundice 21.22 19.08 30 12735 59206 110517328
Stomatitis 21.20 19.08 3 12762 270239 110306295
Encephalitis 20.14 19.08 17 12748 18822 110557712
Hyperbilirubinaemia 19.94 19.08 21 12744 30650 110545884
Lung neoplasm 19.60 19.08 12 12753 8064 110568470
Porphyria non-acute 19.46 19.08 6 12759 751 110575783
Segmented hyalinising vasculitis 19.40 19.08 4 12761 96 110576438
Depressive symptom 19.15 19.08 12 12753 8402 110568132

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
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D011480 Protease Inhibitors
MeSH PA D017320 HIV Protease Inhibitors
MeSH PA D019380 Anti-HIV Agents
MeSH PA D065607 Cytochrome P-450 Enzyme Inhibitors
MeSH PA D065692 Cytochrome P-450 CYP3A Inhibitors
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:33231 antitubercular agent
CHEBI has role CHEBI:33281 antimicrobial agent
CHEBI has role CHEBI:35441 antiinfective agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35660 HIV protease inhibitor
CHEBI has role CHEBI:36044 antiviral drug
CHEBI has role CHEBI:50864 insulin-sensitizing drug
CHEBI has role CHEBI:64946 anti-HIV agent
CHEBI has role CHEBI:149553 anticoronaviral agent

Related Drugs by ATC class:

J05AR Antivirals for treatment of HIV infections, combinations 19 drugs
abacaviratazanavirbictegravircobicistatdarunavirdolutegravirdoravirineefavirenzelvitegraviremtricitabinelamivudinenevirapine show all 19 →

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




🐶 Veterinary Drug Use

None

🐶 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
ATP-binding cassette sub-family G member 2 Transporter IC50 5.12 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
Replicase polyprotein 1ab Enzyme IC50 5.04 CHEMBL
Protease Enzyme Ki 10.59 CHEMBL
Protease Enzyme 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 0074-3008 TABLET, FILM COATED 100 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 0074-4014 TABLET, FILM COATED 200 mg ORAL NDA 32 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 0074-6799 TABLET, FILM COATED 200 mg ORAL NDA 32 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 33342-163 TABLET, FILM COATED 100 mg ORAL ANDA 28 sections
Lopinavir and Ritonavir Human Prescription Drug Label 2 33342-164 TABLET, FILM COATED 200 mg ORAL ANDA 28 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
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
Lopinavir and Ritonavir HUMAN PRESCRIPTION DRUG LABEL 2 68071-2949 TABLET, FILM COATED 200 mg ORAL ANDA 28 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