lopinavir 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 ┬ÁM/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 1210.98 23.46 605 13223 124255 53210983
Abortion spontaneous 720.90 23.46 313 13515 46322 53288916
Off label use 581.72 23.46 658 13170 471554 52863684
Foetal exposure during pregnancy 522.97 23.46 229 13599 34486 53300752
Stillbirth 479.39 23.46 141 13687 6656 53328582
Abortion induced 414.79 23.46 141 13687 10685 53324553
Virologic failure 338.78 23.46 85 13743 2179 53333059
Viral mutation identified 331.03 23.46 82 13746 1992 53333246
Drug interaction 264.77 23.46 304 13524 219025 53116213
Foetal death 263.66 23.46 97 13731 9250 53325988
Maternal exposure during pregnancy 259.07 23.46 256 13572 155383 53179855
Premature baby 248.15 23.46 115 13713 19686 53315552
Immune reconstitution inflammatory syndrome 224.86 23.46 78 13750 6268 53328970
Drug resistance 219.64 23.46 106 13722 19856 53315382
Hypomania 200.37 23.46 67 13761 4815 53330423
Jaundice cholestatic 199.86 23.46 69 13759 5465 53329773
Live birth 193.45 23.46 89 13739 14970 53320268
Hepatotoxicity 162.42 23.46 97 13731 27783 53307455
Premature rupture of membranes 160.76 23.46 57 13771 4883 53330355
Pregnancy 159.18 23.46 100 13728 31341 53303897
Schizophrenia 155.11 23.46 68 13760 10211 53325027
Premature labour 152.34 23.46 71 13757 12291 53322947
Caesarean section 138.04 23.46 74 13754 17246 53317992
Blood HIV RNA increased 134.35 23.46 33 13795 772 53334466
Pathogen resistance 127.65 23.46 52 13776 6508 53328730
Fanconi syndrome acquired 119.93 23.46 32 13796 1049 53334189
Blood bilirubin increased 119.62 23.46 88 13740 35642 53299596
Viral load increased 114.54 23.46 33 13795 1442 53333796
HIV infection 112.78 23.46 27 13801 565 53334673
Premature delivery 112.35 23.46 75 13753 26029 53309209
Psychotic disorder 109.64 23.46 72 13756 24313 53310925
Ergot poisoning 107.93 23.46 22 13806 210 53335028
Treatment noncompliance 107.52 23.46 80 13748 32955 53302283
Lipodystrophy acquired 102.25 23.46 31 13797 1619 53333619
CD4 lymphocytes decreased 97.08 23.46 30 13798 1671 53333567
Skull malformation 87.63 23.46 20 13808 337 53334901
COVID-19 pneumonia 87.58 23.46 41 13787 7162 53328076
Spina bifida 81.39 23.46 22 13806 758 53334480
Long QT syndrome 77.65 23.46 30 13798 3266 53331972
Pain 77.62 23.46 28 13800 588370 52746868
Cholelithiasis 74.66 23.46 71 13757 40893 53294345
Human immunodeficiency virus transmission 68.80 23.46 13 13815 80 53335158
Fatigue 68.27 23.46 54 13774 730452 52604786
Genotype drug resistance test positive 68.17 23.46 18 13810 566 53334672
Electrocardiogram QT prolonged 67.36 23.46 78 13750 56325 53278913
COVID-19 67.34 23.46 64 13764 36824 53298414
Foetal growth restriction 66.70 23.46 34 13794 7140 53328098
Immunosuppressant drug level increased 65.89 23.46 27 13801 3428 53331810
Trisomy 21 64.50 23.46 16 13812 390 53334848
Normal newborn 60.93 23.46 32 13796 7147 53328091
Cushing's syndrome 59.06 23.46 17 13811 740 53334498
Cerebral ventricle dilatation 57.96 23.46 18 13810 1019 53334219
Portal hypertension 57.32 23.46 25 13803 3703 53331535
Hyperbilirubinaemia 55.45 23.46 35 13793 11034 53324204
Eosinophilia 54.93 23.46 45 13783 21290 53313948
Fall 54.57 23.46 13 13815 358427 52976811
Pre-eclampsia 52.71 23.46 31 13797 8616 53326622
Dyspnoea 49.03 23.46 48 13780 586184 52749054
Drug ineffective 46.21 23.46 89 13739 817156 52518082
Hepatocellular injury 45.41 23.46 47 13781 29939 53305299
Placental disorder 43.56 23.46 16 13812 1515 53333723
Patent ductus arteriosus 42.65 23.46 21 13807 4097 53331141
Hepatic cytolysis 42.19 23.46 26 13802 7859 53327379
Rash maculo-papular 42.14 23.46 45 13783 29704 53305534
Arnold-Chiari malformation 41.87 23.46 12 13816 514 53334724
Rickets 41.45 23.46 8 13820 56 53335182
Alopecia 41.02 23.46 6 13822 234577 53100661
Renal tubular dysfunction 40.47 23.46 11 13817 387 53334851
Renal tubular disorder 40.15 23.46 18 13810 2845 53332393
Vomiting 39.84 23.46 242 13586 496897 52838341
Hepatic enzyme increased 38.08 23.46 94 13734 126101 53209137
Placenta praevia 37.98 23.46 13 13815 1001 53334237
Arthralgia 37.89 23.46 35 13793 439748 52895490
Acquired immunodeficiency syndrome 37.27 23.46 8 13820 100 53335138
Peripheral swelling 36.66 23.46 5 13823 206103 53129135
Coarctation of the aorta 36.23 23.46 11 13817 577 53334661
Neural tube defect 36.22 23.46 9 13819 221 53335017
Anticoagulation drug level increased 36.10 23.46 9 13819 224 53335014
Urinary tract infection 35.89 23.46 9 13819 239894 53095344
Polydactyly 35.65 23.46 10 13818 396 53334842
Swelling 35.54 23.46 4 13824 191101 53144137
Gene mutation 35.00 23.46 13 13815 1270 53333968
Placental insufficiency 34.11 23.46 13 13815 1363 53333875
Pulmonary tuberculosis 33.75 23.46 19 13809 4862 53330376
Product dose omission issue 33.26 23.46 5 13823 191615 53143623
Ventricular septal defect 33.00 23.46 18 13810 4332 53330906
Mitochondrial cytopathy 32.70 23.46 9 13819 332 53334906
Atrial septal defect 32.49 23.46 21 13807 6893 53328345
Congenital anomaly 32.07 23.46 13 13815 1604 53333634
Gestational diabetes 31.95 23.46 22 13806 8017 53327221
Brachydactyly 31.62 23.46 7 13821 102 53335136
Anaemia 31.14 23.46 148 13680 276570 53058668
Dysmorphism 31.09 23.46 14 13814 2236 53333002
Renal tubular acidosis 31.07 23.46 13 13815 1738 53333500
Nephropathy toxic 30.68 23.46 22 13806 8550 53326688
Drug reaction with eosinophilia and systemic symptoms 30.48 23.46 40 13788 32760 53302478
Oligohydramnios 29.90 23.46 19 13809 6057 53329181
Cardiac malposition 29.55 23.46 6 13822 56 53335182
Hypertriglyceridaemia 29.26 23.46 19 13809 6285 53328953
Maternal drugs affecting foetus 28.94 23.46 18 13810 5528 53329710
Cerebral toxoplasmosis 28.79 23.46 10 13818 805 53334433
Constipation 28.61 23.46 8 13820 198404 53136834
Cholestasis of pregnancy 28.46 23.46 11 13817 1198 53334040
Transaminases increased 28.39 23.46 37 13791 30095 53305143
Pregnancy on contraceptive 28.11 23.46 11 13817 1238 53334000
Foetal malformation 28.09 23.46 7 13821 174 53335064
Hypophosphataemia 27.90 23.46 21 13807 8784 53326454
Pain in extremity 27.86 23.46 20 13808 285030 53050208
Hepatic displacement 26.86 23.46 5 13823 28 53335210
Congenital eye disorder 26.29 23.46 5 13823 32 53335206
Spinocerebellar disorder 25.90 23.46 5 13823 35 53335203
Hyperlactacidaemia 25.58 23.46 13 13815 2712 53332526
Mental disability 25.51 23.46 6 13822 116 53335122
Drug hypersensitivity 25.41 23.46 19 13809 265223 53070015
Benign hydatidiform mole 24.77 23.46 6 13822 132 53335106
Twin pregnancy 24.63 23.46 10 13818 1239 53333999
Threatened labour 24.28 23.46 9 13819 874 53334364
Therapeutic response unexpected 24.24 23.46 26 13802 17244 53317994
Meningitis cryptococcal 24.16 23.46 10 13818 1301 53333937
Dizziness 24.15 23.46 37 13791 372222 52963016
COVID-19 treatment 24.12 23.46 6 13822 148 53335090
Acute respiratory distress syndrome 24.11 23.46 30 13798 23302 53311936
Meningomyelocele 24.03 23.46 8 13820 566 53334672
Coronavirus infection 23.84 23.46 13 13815 3127 53332111
Abdominal discomfort 23.64 23.46 14 13814 221048 53114190

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
Off label use 1311.47 15.01 1392 24301 304928 32182905
Drug interaction 1192.77 15.01 1134 24559 217051 32270782
Depression 693.55 15.01 589 25104 96471 32391362
Lipodystrophy acquired 595.07 15.01 187 25506 3495 32484338
Mitochondrial toxicity 443.45 15.01 138 25555 2492 32485341
Foetal exposure during pregnancy 366.49 15.01 285 25408 41016 32446817
Eyelid ptosis 332.54 15.01 135 25558 5407 32482426
Immune reconstitution inflammatory syndrome 253.48 15.01 132 25561 9427 32478406
Long QT syndrome 228.92 15.01 84 25609 2547 32485286
Progressive external ophthalmoplegia 225.68 15.01 70 25623 1248 32486585
Hypertransaminasaemia 221.00 15.01 93 25600 4081 32483752
Virologic failure 209.30 15.01 87 25606 3700 32484133
Diplopia 199.82 15.01 131 25562 14381 32473452
Hypertriglyceridaemia 190.82 15.01 106 25587 8613 32479220
Exposure during pregnancy 187.88 15.01 107 25586 9122 32478711
Fanconi syndrome acquired 178.60 15.01 67 25626 2163 32485670
Premature baby 158.00 15.01 125 25568 18393 32469440
Drug-induced liver injury 150.85 15.01 136 25557 23927 32463906
Hepatic fibrosis 144.12 15.01 66 25627 3552 32484281
Viral mutation identified 142.43 15.01 62 25631 2957 32484876
Electrocardiogram QT prolonged 140.83 15.01 165 25528 39476 32448357
Loss of personal independence in daily activities 138.21 15.01 136 25557 26697 32461136
COVID-19 118.28 15.01 136 25557 31879 32455954
Drug effective for unapproved indication 107.16 15.01 41 25652 1398 32486435
Fanconi syndrome 97.83 15.01 41 25652 1779 32486054
Hyperbilirubinaemia 97.16 15.01 93 25600 17637 32470196
Renal tubular disorder 97.04 15.01 57 25636 5145 32482688
Pathogen resistance 96.04 15.01 71 25622 9439 32478394
HIV infection 95.59 15.01 41 25652 1885 32485948
Kaposi's sarcoma 93.99 15.01 34 25659 988 32486845
Viral load increased 93.62 15.01 47 25646 3103 32484730
Death 92.46 15.01 100 25593 382417 32105416
Trisomy 21 89.69 15.01 28 25665 510 32487323
Osteoporosis 84.60 15.01 73 25620 12109 32475724
Nephropathy toxic 83.80 15.01 72 25621 11874 32475959
Drug ineffective 76.33 15.01 116 25577 383361 32104472
COVID-19 pneumonia 72.50 15.01 58 25635 8662 32479171
Ophthalmoplegia 69.09 15.01 30 25663 1421 32486412
Volvulus 67.86 15.01 29 25664 1321 32486512
Drug resistance 64.49 15.01 85 25608 22880 32464953
Drug level increased 63.75 15.01 79 25614 20001 32467832
Extraocular muscle paresis 61.18 15.01 21 25672 521 32487312
Hyperlactacidaemia 60.82 15.01 35 25658 3039 32484794
Fatigue 60.62 15.01 116 25577 350585 32137248
Hepatocellular injury 58.05 15.01 85 25608 25233 32462600
Fall 57.14 15.01 43 25650 196158 32291675
Congenital anomaly 57.03 15.01 26 25667 1384 32486449
Febrile neutropenia 55.83 15.01 13 25680 119553 32368280
Cushing's syndrome 52.84 15.01 18 25675 436 32487397
Product dose omission issue 52.38 15.01 9 25684 102566 32385267
CD4 lymphocytes decreased 51.69 15.01 28 25665 2162 32485671
Acquired immunodeficiency syndrome 50.93 15.01 18 25675 488 32487345
Dyslipidaemia 49.32 15.01 42 25651 6841 32480992
Hyperlipidaemia 49.16 15.01 59 25634 14452 32473381
Osteoporotic fracture 48.34 15.01 22 25671 1166 32486667
Dyspnoea 47.92 15.01 138 25555 361907 32125926
Glycosuria 47.63 15.01 23 25670 1395 32486438
HIV-associated neurocognitive disorder 47.35 15.01 16 25677 378 32487455
Hypotension 47.21 15.01 61 25632 216049 32271784
Pneumonia 44.42 15.01 139 25554 355113 32132720
Mitochondrial cytopathy 43.27 15.01 13 25680 207 32487626
Osteonecrosis 42.81 15.01 59 25634 16563 32471270
Lipoatrophy 42.73 15.01 17 25676 644 32487189
Portal hypertension 42.51 15.01 31 25662 4033 32483800
Peripheral swelling 42.39 15.01 3 25690 68342 32419491
Proteinuria 42.31 15.01 60 25633 17295 32470538
Immunosuppressant drug level increased 42.29 15.01 34 25659 5111 32482722
Malignant neoplasm progression 42.08 15.01 6 25687 78490 32409343
Hypophosphataemia 42.02 15.01 43 25650 8832 32479001
Hepatic failure 41.57 15.01 89 25604 35591 32452242
Polydactyly 41.23 15.01 20 25673 1225 32486608
HIV associated nephropathy 40.20 15.01 14 25679 363 32487470
Cardiac failure congestive 40.04 15.01 9 25684 84843 32402990
Osteomalacia 39.89 15.01 18 25675 935 32486898
Liver injury 39.36 15.01 52 25641 14022 32473811
Coronavirus infection 38.12 15.01 28 25665 3684 32484149
Constipation 37.65 15.01 27 25666 126346 32361487
Hepatosplenomegaly 36.86 15.01 28 25665 3875 32483958
Cerebral toxoplasmosis 36.83 15.01 20 25673 1552 32486281
Blood triglycerides increased 36.32 15.01 51 25642 14568 32473265
CD4 lymphocytes increased 36.14 15.01 12 25681 268 32487565
Ventricular septal defect 35.59 15.01 27 25666 3730 32484103
Pain 35.02 15.01 59 25634 187497 32300336
Blood lactic acid increased 34.49 15.01 33 25660 6248 32481585
Blood pressure increased 34.40 15.01 10 25683 79344 32408489
Hepatic cytolysis 33.47 15.01 37 25656 8296 32479537
Hepatitis 33.43 15.01 64 25629 23629 32464204
Completed suicide 32.86 15.01 16 25677 92501 32395332
Muscle spasms 32.17 15.01 8 25685 70410 32417423
Portal fibrosis 31.78 15.01 12 25681 394 32487439
Gastroschisis 31.57 15.01 9 25684 118 32487715
Hyperferritinaemia 31.47 15.01 12 25681 405 32487428
Disease progression 30.88 15.01 15 25678 86847 32400986
Adrenogenital syndrome 30.79 15.01 8 25685 72 32487761
Low set ears 30.69 15.01 12 25681 434 32487399
Lipohypertrophy 30.49 15.01 11 25682 317 32487516
Cryptorchism 30.42 15.01 19 25674 1915 32485918
Blood bilirubin increased 29.40 15.01 82 25611 38702 32449131
Product use in unapproved indication 28.96 15.01 141 25552 87063 32400770
Atypical mycobacterial infection 28.73 15.01 14 25679 866 32486967
Maternal drugs affecting foetus 28.42 15.01 25 25668 4252 32483581
Cholestasis 27.62 15.01 64 25629 26969 32460864
Acute kidney injury 27.50 15.01 353 25340 293115 32194718
Bronchopulmonary aspergillosis 27.18 15.01 43 25650 13644 32474189
Liver disorder 27.09 15.01 70 25623 31584 32456249
Multiple-drug resistance 26.97 15.01 23 25670 3752 32484081
Anal cancer 26.94 15.01 11 25682 446 32487387
Urinary tract infection 26.73 15.01 15 25678 80056 32407777
Neonatal asphyxia 26.70 15.01 10 25683 321 32487512
Live birth 26.38 15.01 9 25684 219 32487614
Epistaxis 26.19 15.01 6 25687 55849 32431984
Oesophageal candidiasis 25.79 15.01 24 25669 4390 32483443
Inappropriate schedule of product administration 25.76 15.01 3 25690 45822 32442011
Taeniasis 25.76 15.01 7 25686 76 32487757
Drug ineffective for unapproved indication 25.31 15.01 42 25651 13870 32473963
Renal failure 25.08 15.01 187 25506 134291 32353542
Urticaria 24.95 15.01 8 25685 59606 32428227
Acute respiratory distress syndrome 24.94 15.01 59 25634 25194 32462639
Exomphalos 24.78 15.01 8 25685 163 32487670
Syphilis 24.01 15.01 11 25682 592 32487241
Congenital hearing disorder 23.68 15.01 7 25686 105 32487728
Kidney malformation 23.67 15.01 8 25685 189 32487644
HIV wasting syndrome 23.62 15.01 7 25686 106 32487727
Stillbirth 23.44 15.01 8 25685 195 32487638
Antiviral drug level above therapeutic 23.09 15.01 6 25687 54 32487779
Jaundice 22.79 15.01 69 25624 34089 32453744
Back pain 22.54 15.01 33 25660 111020 32376813
Oesophageal atresia 22.50 15.01 10 25683 501 32487332
Dizziness 22.10 15.01 88 25605 209530 32278303
Cortisol decreased 22.01 15.01 12 25681 938 32486895
Speech sound disorder 21.90 15.01 7 25686 138 32487695
Pneumocystis jirovecii pneumonia 21.89 15.01 47 25646 18823 32469010
Adrenal suppression 21.81 15.01 11 25682 733 32487100
Drug abuse 21.55 15.01 19 25674 80224 32407609
Splenomegaly 21.53 15.01 40 25653 14437 32473396
Mycobacterium avium complex infection 21.30 15.01 18 25675 2899 32484934
Eosinophilia 21.15 15.01 55 25638 24903 32462930
Endotracheal intubation 21.07 15.01 17 25676 2568 32485265
Transaminases increased 21.06 15.01 55 25638 24973 32462860
Somnolence 20.91 15.01 31 25662 103766 32384067
Small for dates baby 20.89 15.01 19 25674 3374 32484459
Feeling abnormal 20.63 15.01 11 25682 60412 32427421
Hepatic function abnormal 20.62 15.01 80 25613 44760 32443073
Cushingoid 20.56 15.01 17 25676 2657 32485176
Infection 20.50 15.01 22 25671 84693 32403140
Gamma-glutamyltransferase increased 20.36 15.01 62 25631 30720 32457113
Lymphadenopathy 20.26 15.01 57 25636 27025 32460808
Haemoglobin decreased 20.21 15.01 40 25653 119631 32368202
Renal tubular acidosis 20.13 15.01 15 25678 2017 32485816
COVID-19 treatment 20.11 15.01 8 25685 303 32487530
Burkitt's lymphoma 20.08 15.01 7 25686 182 32487651
Normal newborn 20.01 15.01 7 25686 184 32487649
Joint swelling 19.85 15.01 8 25685 51727 32436106
Lactic acidosis 19.85 15.01 65 25628 33471 32454362
Castleman's disease 19.77 15.01 5 25688 40 32487793
Rhabdomyolysis 19.69 15.01 105 25588 67160 32420673
Hepatic cirrhosis 19.65 15.01 42 25651 16767 32471066
Erythema 19.65 15.01 22 25671 83083 32404750
Porphyria non-acute 19.33 15.01 9 25684 503 32487330
ADAMTS13 activity decreased 19.23 15.01 6 25687 109 32487724
Faeces pale 19.10 15.01 13 25680 1516 32486317
Andersen-Tawil syndrome 19.04 15.01 4 25689 12 32487821
Mixed liver injury 19.01 15.01 16 25677 2564 32485269
Hyperreflexia 18.85 15.01 17 25676 2987 32484846
Therapeutic response unexpected 18.81 15.01 30 25663 9582 32478251
Blood alkaline phosphatase increased 18.77 15.01 62 25631 32070 32455763
Death neonatal 18.70 15.01 8 25685 365 32487468
Musculoskeletal toxicity 18.60 15.01 6 25687 122 32487711
Viral load decreased 18.59 15.01 5 25688 52 32487781
Neutrophil count decreased 18.57 15.01 7 25686 47132 32440701
Candida infection 18.52 15.01 41 25652 16762 32471071
Renal impairment 18.34 15.01 130 25563 91842 32395991
Low birth weight baby 18.27 15.01 25 25668 6969 32480864
Hepatomegaly 18.26 15.01 31 25662 10426 32477407
Protrusion tongue 18.25 15.01 7 25686 240 32487593
Foetal growth restriction 18.20 15.01 19 25674 3993 32483840
Pain in extremity 18.19 15.01 42 25651 118859 32368974
Encephalitis 18.13 15.01 25 25668 7019 32480814
Blood phosphorus decreased 18.08 15.01 17 25676 3149 32484684
Cytomegalovirus chorioretinitis 18.01 15.01 18 25675 3594 32484239
Cachexia 17.95 15.01 25 25668 7084 32480749
Psoriasis 17.92 15.01 7 25686 46116 32441717
Hepatotoxicity 17.83 15.01 44 25649 19293 32468540
Drug hypersensitivity 17.83 15.01 19 25674 73381 32414452
Pneumococcal infection 17.63 15.01 8 25685 421 32487412
Sickle cell disease 17.47 15.01 6 25687 149 32487684
Cellulitis 17.36 15.01 9 25684 50221 32437612
Loss of consciousness 17.35 15.01 24 25669 82683 32405150
Chest pain 17.31 15.01 46 25647 124091 32363742
Caesarean section 17.29 15.01 14 25679 2125 32485708
Wheezing 17.21 15.01 4 25689 36870 32450963
Anxiety 17.16 15.01 31 25662 95974 32391859
Arthralgia 17.14 15.01 60 25633 148388 32339445
Nephropathy 16.98 15.01 22 25671 5818 32482015
Prenatal screening test abnormal 16.96 15.01 4 25689 23 32487810
Hepatitis toxic 16.79 15.01 14 25679 2214 32485619
Delayed graft function 16.77 15.01 13 25680 1854 32485979
Cerebral ventricle dilatation 16.71 15.01 10 25683 933 32486900
Red blood cell schistocytes present 16.63 15.01 7 25686 307 32487526
Hospitalisation 16.59 15.01 9 25684 48962 32438871
Hepatitis cholestatic 16.55 15.01 26 25667 8199 32479634
Congenital abdominal hernia 16.54 15.01 4 25689 26 32487807
Therapeutic product effect incomplete 16.52 15.01 6 25687 41335 32446498
Blood pressure decreased 16.43 15.01 10 25683 51070 32436763
Confusional state 16.42 15.01 58 25635 143057 32344776
Ergot poisoning 16.39 15.01 5 25688 84 32487749
Acute hepatitis C 16.37 15.01 6 25687 181 32487652
Immunoblastic lymphoma 16.36 15.01 3 25690 3 32487830
Progressive multifocal leukoencephalopathy 16.31 15.01 28 25665 9503 32478330
Influenza 16.27 15.01 8 25685 46006 32441827
Cerebrovascular accident 16.22 15.01 27 25666 86293 32401540
Transient tachypnoea of the newborn 16.22 15.01 6 25687 186 32487647
Syncope 16.20 15.01 29 25664 90095 32397738
Pancreatitis acute 16.19 15.01 53 25640 27282 32460551
Anticoagulation drug level increased 16.03 15.01 8 25685 521 32487312
Dysmorphism 15.96 15.01 15 25678 2778 32485055
Chest discomfort 15.92 15.01 10 25683 50220 32437613
Opportunistic infection 15.90 15.01 12 25681 1645 32486188
Renal tubular necrosis 15.42 15.01 37 25656 15941 32471892
Visceral leishmaniasis 15.40 15.01 8 25685 567 32487266
Mitochondrial myopathy 15.19 15.01 6 25687 223 32487610
Oral candidiasis 15.16 15.01 31 25662 11996 32475837
Aspartate aminotransferase increased 15.09 15.01 97 25596 66332 32421501
Bilirubin conjugated increased 15.01 15.01 16 25677 3442 32484391

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 anti-virus drug
CHEBI has role CHEBI:149553 anti-coronaviral agents
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 (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

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
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
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