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 1154.78 22.57 568 12120 107644 46565730
Abortion spontaneous 684.30 22.57 300 12388 43346 46630028
Stillbirth 479.27 22.57 141 12547 6350 46667024
Foetal exposure during pregnancy 464.11 22.57 206 12482 30541 46642833
Abortion induced 403.96 22.57 138 12550 10122 46663252
Off label use 337.22 22.57 461 12227 379380 46293994
Viral mutation identified 309.15 22.57 77 12611 1822 46671552
Virologic failure 293.28 22.57 75 12613 1980 46671394
Maternal exposure during pregnancy 278.55 22.57 227 12461 102322 46571052
Foetal death 261.82 22.57 96 12592 8647 46664727
Premature baby 230.88 22.57 108 12580 18004 46655370
Drug resistance 216.55 22.57 102 12586 17266 46656108
Drug interaction 214.07 22.57 269 12419 202825 46470549
Immune reconstitution inflammatory syndrome 209.69 22.57 73 12615 5652 46667722
Hypomania 168.61 22.57 58 12630 4330 46669044
Pregnancy 168.42 22.57 100 12588 27037 46646337
Jaundice cholestatic 168.42 22.57 60 12628 4969 46668405
Live birth 164.59 22.57 72 12616 10258 46663116
Premature rupture of membranes 156.60 22.57 55 12633 4368 46669006
Hepatotoxicity 144.42 22.57 88 12600 24921 46648453
Premature labour 142.78 22.57 67 12621 11232 46662142
Blood HIV RNULL increased 138.00 22.57 33 12655 654 46672720
Schizophrenia 134.16 22.57 59 12629 8509 46664865
Caesarean section 129.36 22.57 71 12617 16532 46656842
Fanconi syndrome acquired 121.90 22.57 32 12656 937 46672437
Viral load increased 115.28 22.57 33 12655 1342 46672032
HIV infection 111.46 22.57 27 12661 566 46672808
Ergot poisoning 107.17 22.57 22 12666 207 46673167
Pathogen resistance 102.27 22.57 44 12644 6016 46667358
Blood bilirubin increased 99.58 22.57 79 12609 34105 46639269
Lipodystrophy acquired 99.30 22.57 30 12658 1475 46671899
CD4 lymphocytes decreased 97.31 22.57 30 12658 1580 46671794
Psychotic disorder 89.88 22.57 63 12625 22558 46650816
Treatment noncompliance 89.37 22.57 70 12618 29661 46643713
Skull malformation 87.02 22.57 20 12668 331 46673043
Spina bifida 83.87 22.57 22 12666 642 46672732
Long QT syndrome 78.24 22.57 30 12658 3050 46670324
COVID-19 pneumonia 76.45 22.57 30 12658 3245 46670129
Premature delivery 75.20 22.57 56 12632 22013 46651361
Genotype drug resistance test positive 68.40 22.57 18 12670 532 46672842
Human immunodeficiency virus transmission 68.19 22.57 13 12675 80 46673294
Immunosuppressant drug level increased 65.99 22.57 27 12661 3255 46670119
Foetal growth restriction 65.09 22.57 33 12655 6534 46666840
Trisomy 21 63.79 22.57 16 12672 389 46672985
Normal newborn 61.96 22.57 31 12657 5970 46667404
Pain 59.12 22.57 28 12660 476920 46196454
Cholelithiasis 58.64 22.57 62 12626 38619 46634755
Portal hypertension 57.81 22.57 25 12663 3458 46669916
Cushing's syndrome 57.74 22.57 17 12671 764 46672610
Cerebral ventricle dilatation 57.71 22.57 18 12670 985 46672389
COVID-19 56.38 22.57 44 12644 18531 46654843
Eosinophilia 55.05 22.57 44 12644 19173 46654201
Fatigue 52.60 22.57 53 12635 608644 46064730
Fall 51.60 22.57 13 12675 329084 46344290
Hepatic enzyme increased 51.40 22.57 85 12603 81702 46591672
Pre-eclampsia 50.96 22.57 30 12658 7964 46665410
Hyperbilirubinaemia 50.85 22.57 33 12655 10405 46662969
Drug ineffective 46.04 22.57 71 12617 677767 45995607
Hepatocellular injury 45.95 22.57 48 12640 29474 46643900
Dyspnoea 44.36 22.57 45 12643 515503 46157871
Placental disorder 44.11 22.57 16 12672 1393 46671981
Patent ductus arteriosus 42.98 22.57 21 12667 3841 46669533
Arnold-Chiari malformation 42.77 22.57 12 12676 453 46672921
Renal tubular disorder 41.92 22.57 18 12670 2447 46670927
Placenta praevia 38.75 22.57 13 12675 898 46672476
Anticoagulation drug level increased 37.69 22.57 9 12679 177 46673197
Rash maculo-papular 37.56 22.57 42 12646 27832 46645542
Neural tube defect 37.04 22.57 9 12679 191 46673183
Coarctation of the aorta 36.42 22.57 11 12677 540 46672834
Polydactyly 35.97 22.57 10 12678 365 46673009
Urinary tract infection 35.87 22.57 8 12680 220258 46453116
Vomiting 34.86 22.57 226 12462 452568 46220806
Placental insufficiency 33.93 22.57 13 12675 1318 46672056
Drug hypersensitivity 33.88 22.57 12 12676 243813 46429561
Ventricular septal defect 33.48 22.57 18 12670 4016 46669358
Pulmonary tuberculosis 33.47 22.57 19 12669 4712 46668662
Atrial septal defect 33.27 22.57 21 12667 6311 46667063
Mitochondrial cytopathy 33.24 22.57 9 12679 297 46673077
Gestational diabetes 33.15 22.57 22 12666 7197 46666177
Dysmorphism 32.67 22.57 14 12674 1893 46671481
Congenital anomaly 31.83 22.57 13 12675 1559 46671815
Electrocardiogram QT prolonged 31.76 22.57 53 12635 51272 46622102
Renal tubular acidosis 31.75 22.57 13 12675 1570 46671804
Acquired immunodeficiency syndrome 31.55 22.57 7 12681 98 46673276
Oligohydramnios 30.93 22.57 19 12669 5446 46667928
Hypertriglyceridaemia 30.18 22.57 19 12669 5685 46667689
Anaemia 29.88 22.57 143 12545 255636 46417738
Product dose omission issue 29.79 22.57 5 12683 168515 46504859
Cerebral toxoplasmosis 29.46 22.57 10 12678 716 46672658
Pain in extremity 29.28 22.57 17 12671 258663 46414711
Cardiac malposition 29.27 22.57 6 12682 56 46673318
Foetal malformation 28.93 22.57 7 12681 146 46673228
Pregnancy on contraceptive 28.90 22.57 11 12677 1096 46672278
Cholestasis of pregnancy 28.73 22.57 11 12677 1113 46672261
Maternal drugs affecting foetus 28.24 22.57 18 12670 5500 46667874
Transaminases increased 27.83 22.57 36 12652 27725 46645649
Arthralgia 27.83 22.57 35 12653 364568 46308806
Hyperlactacidaemia 27.55 22.57 13 12675 2202 46671172
Peripheral swelling 27.26 22.57 5 12683 158066 46515308
Hepatic displacement 26.63 22.57 5 12683 28 46673346
Alopecia 26.22 22.57 6 12682 162408 46510966
Congenital eye disorder 26.06 22.57 5 12683 32 46673342
Spinocerebellar disorder 25.67 22.57 5 12683 35 46673339
Mental disability 25.53 22.57 6 12682 110 46673264
Constipation 25.16 22.57 8 12680 174089 46499285
Meningomyelocele 24.81 22.57 8 12680 488 46672886
Twin pregnancy 24.72 22.57 10 12678 1171 46672203
Benign hydatidiform mole 24.71 22.57 6 12682 127 46673247
Coronavirus infection 24.69 22.57 13 12675 2781 46670593
Hypertransaminasaemia 24.65 22.57 14 12674 3474 46669900
Meningitis cryptococcal 24.60 22.57 10 12678 1185 46672189
Threatened labour 24.50 22.57 9 12679 812 46672562
Renal tubular dysfunction 24.16 22.57 7 12681 297 46673077
COVID-19 treatment 23.57 22.57 6 12682 155 46673219
Disseminated Bacillus Calmette-Guerin infection 23.30 22.57 4 12684 12 46673362
Fanconi syndrome 23.13 22.57 9 12679 951 46672423
Toxoplasmosis 23.11 22.57 10 12678 1384 46671990
Amniotic cavity disorder 23.06 22.57 4 12684 13 46673361
Hydrocephalus 22.73 22.57 15 12673 4862 46668512
Metabolic acidosis 22.60 22.57 39 12649 38741 46634633
Congenital acrochordon 22.60 22.57 5 12683 69 46673305

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 842.41 14.49 998 22378 248292 29680810
Drug interaction 579.55 14.49 742 22634 198826 29730276
Lipodystrophy acquired 570.07 14.49 179 23197 3381 29925721
Mitochondrial toxicity 430.11 14.49 133 23243 2381 29926721
Foetal exposure during pregnancy 371.29 14.49 273 23103 36598 29892504
Eyelid ptosis 325.37 14.49 130 23246 5058 29924044
Depression 300.60 14.49 361 23015 90076 29839026
Immune reconstitution inflammatory syndrome 258.26 14.49 131 23245 8970 29920132
Progressive external ophthalmoplegia 216.60 14.49 67 23309 1199 29927903
Hypertransaminasaemia 214.96 14.49 89 23287 3796 29925306
Virologic failure 196.05 14.49 79 23297 3140 29925962
Diplopia 195.19 14.49 126 23250 13646 29915456
Exposure during pregnancy 191.50 14.49 108 23268 9153 29919949
Long QT syndrome 191.03 14.49 71 23305 2262 29926840
Hypertriglyceridaemia 191.00 14.49 103 23273 7995 29921107
Fanconi syndrome acquired 183.25 14.49 67 23309 2036 29927066
Premature baby 150.90 14.49 116 23260 16575 29912527
Viral mutation identified 144.73 14.49 60 23316 2566 29926536
Drug-induced liver injury 144.20 14.49 125 23251 21149 29907953
Hepatic fibrosis 139.29 14.49 64 23312 3516 29925586
Drug effective for unapproved indication 118.44 14.49 41 23335 1058 29928044
Renal tubular disorder 99.75 14.49 57 23319 4949 29924153
Fanconi syndrome 99.31 14.49 41 23335 1734 29927368
Kaposi's sarcoma 94.21 14.49 34 23342 994 29928108
Hyperbilirubinaemia 94.05 14.49 89 23287 16853 29912249
Trisomy 21 93.94 14.49 28 23348 439 29928663
Pathogen resistance 92.98 14.49 66 23310 8344 29920758
Viral load increased 92.53 14.49 45 23331 2809 29926293
Osteoporosis 91.77 14.49 72 23304 10591 29918511
HIV infection 91.54 14.49 38 23338 1630 29927472
Death 83.37 14.49 94 23282 357189 29571913
COVID-19 pneumonia 83.30 14.49 49 23327 4491 29924611
COVID-19 73.76 14.49 80 23296 17798 29911304
Volvulus 69.90 14.49 29 23347 1242 29927860
Drug resistance 66.01 14.49 80 23296 20053 29909049
Hyperlactacidaemia 63.82 14.49 34 23342 2572 29926530
Drug ineffective 63.74 14.49 105 23271 340282 29588820
Nephropathy toxic 63.10 14.49 58 23318 10581 29918521
Congenital anomaly 62.19 14.49 27 23349 1295 29927807
Ophthalmoplegia 59.29 14.49 26 23350 1278 29927824
Hepatocellular injury 57.03 14.49 84 23292 25387 29903715
Cushing's syndrome 52.76 14.49 18 23358 444 29928658
Extraocular muscle paresis 52.72 14.49 18 23358 445 29928657
Osteoporotic fracture 51.35 14.49 22 23354 1021 29928081
Acquired immunodeficiency syndrome 50.88 14.49 18 23358 496 29928606
CD4 lymphocytes decreased 50.67 14.49 27 23349 2043 29927059
Glycosuria 49.62 14.49 23 23353 1288 29927814
Fall 49.01 14.49 42 23334 181830 29747272
Hyperlipidaemia 48.44 14.49 57 23319 13850 29915252
Loss of personal independence in daily activities 46.74 14.49 70 23306 21465 29907637
Osteonecrosis 46.32 14.49 60 23316 16075 29913027
Febrile neutropenia 46.23 14.49 13 23363 106680 29822422
HIV-associated neurocognitive disorder 45.75 14.49 15 23361 326 29928776
Electrocardiogram QT prolonged 45.61 14.49 92 23284 35743 29893359
Fatigue 45.46 14.49 116 23260 320557 29608545
Hypophosphataemia 45.14 14.49 43 23333 8202 29920900
HIV associated nephropathy 44.91 14.49 14 23362 257 29928845
Proteinuria 44.73 14.49 59 23317 16086 29913016
Lipoatrophy 44.62 14.49 17 23359 580 29928522
Portal hypertension 44.20 14.49 31 23345 3842 29925260
Product dose omission issue 43.94 14.49 9 23367 91622 29837480
Mitochondrial cytopathy 43.84 14.49 13 23363 200 29928902
Polydactyly 41.62 14.49 20 23356 1215 29927887
Osteomalacia 40.94 14.49 18 23358 890 29928212
Dyspnoea 40.31 14.49 130 23246 333165 29595937
Liver injury 40.19 14.49 49 23327 12351 29916751
Coronavirus infection 39.93 14.49 28 23348 3470 29925632
Hypotension 39.20 14.49 60 23316 200505 29728597
Cardiac failure congestive 39.03 14.49 9 23367 84398 29844704
Hepatosplenomegaly 38.50 14.49 28 23348 3673 29925429
Cerebral toxoplasmosis 38.30 14.49 20 23356 1452 29927650
Hepatitis 37.98 14.49 65 23311 22291 29906811
Pneumonia 37.97 14.49 134 23242 334172 29594930
Ventricular septal defect 37.40 14.49 27 23349 3502 29925600
Completed suicide 36.46 14.49 16 23360 99476 29829626
Peripheral swelling 36.41 14.49 3 23373 61071 29868031
CD4 lymphocytes increased 36.29 14.49 12 23364 268 29928834
Dyslipidaemia 35.48 14.49 32 23344 5695 29923407
Blood triglycerides increased 35.44 14.49 49 23327 13968 29915134
Malignant neoplasm progression 34.86 14.49 7 23369 72280 29856822
Cryptorchism 33.15 14.49 19 23357 1658 29927444
Hyperferritinaemia 32.74 14.49 12 23364 367 29928735
Blood bilirubin increased 32.00 14.49 81 23295 36555 29892547
Portal fibrosis 31.90 14.49 12 23364 395 29928707
Gastroschisis 31.75 14.49 9 23367 117 29928985
Low set ears 31.40 14.49 12 23364 413 29928689
Lipohypertrophy 30.69 14.49 11 23365 315 29928787
Adrenogenital syndrome 30.60 14.49 8 23368 75 29929027
Atypical mycobacterial infection 30.20 14.49 14 23362 784 29928318
Liver disorder 29.46 14.49 69 23307 29653 29899449
Hepatic failure 29.45 14.49 75 23301 33968 29895134
Cholestasis 29.32 14.49 62 23314 24888 29904214
Constipation 29.26 14.49 27 23349 112879 29816223
Syphilis 28.96 14.49 11 23365 372 29928730
Blood pressure increased 28.93 14.49 10 23366 71918 29857184
Kidney malformation 28.73 14.49 8 23368 97 29929005
Maternal drugs affecting foetus 28.71 14.49 25 23351 4248 29924854
Pain 27.98 14.49 58 23318 172583 29756519
Muscle spasms 27.88 14.49 8 23368 64830 29864272
Anal cancer 27.48 14.49 11 23365 429 29928673
Oesophageal candidiasis 27.02 14.49 24 23352 4186 29924916
Neonatal asphyxia 26.88 14.49 10 23366 319 29928783
Urinary tract infection 26.73 14.49 12 23364 73647 29855455
Renal failure 26.60 14.49 182 23194 128784 29800318
Disease progression 26.02 14.49 15 23361 79859 29849243
Eosinophilia 25.96 14.49 55 23321 22105 29906997
Taeniasis 25.85 14.49 7 23369 76 29929026
Blood lactic acid increased 25.64 14.49 27 23349 5803 29923299
Pneumocystis jirovecii pneumonia 25.50 14.49 47 23329 17073 29912029
Jaundice 25.48 14.49 69 23307 32417 29896685
Exomphalos 24.93 14.49 8 23368 162 29928940
Lymphadenopathy 24.60 14.49 57 23319 24319 29904783
Drug abuse 24.55 14.49 17 23359 82055 29847047
Congenital hearing disorder 24.09 14.49 7 23369 100 29929002
Stillbirth 24.05 14.49 8 23368 182 29928920
Acute kidney injury 23.96 14.49 322 23054 273520 29655582
Acute respiratory distress syndrome 23.82 14.49 55 23321 23417 29905685
Epistaxis 23.79 14.49 6 23370 52975 29876127
Adrenal suppression 23.63 14.49 11 23365 622 29928480
HIV wasting syndrome 23.53 14.49 7 23369 109 29928993
Multiple-drug resistance 23.46 14.49 19 23357 2922 29926180
Oesophageal atresia 23.34 14.49 10 23366 464 29928638
Lactic acidosis 23.19 14.49 65 23311 31148 29897954
Antiviral drug level above therapeutic 23.17 14.49 6 23370 54 29929048
Sickle cell disease 23.12 14.49 7 23369 116 29928986
Speech sound disorder 22.78 14.49 6 23370 58 29929044
Transaminases increased 22.75 14.49 54 23322 23403 29905699
Gamma-glutamyltransferase increased 22.68 14.49 62 23314 29288 29899814
Mycobacterium avium complex infection 22.66 14.49 18 23358 2693 29926409
Cortisol decreased 22.54 14.49 12 23364 906 29928196
Small for dates baby 22.02 14.49 19 23357 3189 29925913
Musculoskeletal toxicity 21.84 14.49 6 23370 69 29929033
Hepatic function abnormal 21.64 14.49 77 23299 41868 29887234
Hepatic cirrhosis 21.45 14.49 42 23334 15957 29913145
Urticaria 21.26 14.49 8 23368 54598 29874504
Inappropriate schedule of product administration 21.02 14.49 3 23373 39725 29889377
Rhabdomyolysis 20.46 14.49 101 23275 63479 29865623
Dysmorphism 20.39 14.49 15 23361 2002 29927100
Burkitt's lymphoma 20.24 14.49 7 23369 180 29928922
Encephalitis 20.15 14.49 25 23351 6411 29922691
Normal newborn 20.10 14.49 7 23369 184 29928918
Splenomegaly 20.07 14.49 37 23339 13443 29915659
Blood alkaline phosphatase increased 19.98 14.49 62 23314 31425 29897677
ADAMTS13 activity decreased 19.96 14.49 6 23370 97 29929005
Endotracheal intubation 19.91 14.49 16 23360 2434 29926668
Hyperreflexia 19.86 14.49 17 23359 2822 29926280
Castleman's disease 19.83 14.49 5 23371 40 29929062
Porphyria non-acute 19.81 14.49 9 23367 481 29928621
Cytomegalovirus chorioretinitis 19.73 14.49 18 23358 3250 29925852
Cushingoid 19.70 14.49 16 23360 2471 29926631
Faeces pale 19.65 14.49 13 23363 1464 29927638
Live birth 19.64 14.49 7 23369 197 29928905
Cachexia 19.62 14.49 25 23351 6586 29922516
Hepatomegaly 19.47 14.49 31 23345 10016 29919086
Renal tubular acidosis 19.44 14.49 14 23362 1808 29927294
Immunosuppressant drug level increased 19.31 14.49 21 23355 4681 29924421
Andersen-Tawil syndrome 19.09 14.49 4 23372 12 29929090
Blood phosphorus decreased 19.09 14.49 17 23359 2975 29926127
Hepatotoxicity 18.94 14.49 43 23333 18102 29911000
Death neonatal 18.93 14.49 8 23368 359 29928743
Back pain 18.77 14.49 32 23344 102564 29826538
Viral load decreased 18.66 14.49 5 23371 52 29929050
Opportunistic infection 18.63 14.49 12 23364 1292 29927810
Protrusion tongue 18.62 14.49 7 23369 230 29928872
Cerebral ventricle dilatation 18.34 14.49 10 23366 792 29928310
Foetal growth restriction 18.31 14.49 18 23358 3567 29925535
Feeling abnormal 18.00 14.49 11 23365 56745 29872357
Haemoglobin decreased 17.90 14.49 39 23337 114059 29815043
Somnolence 17.87 14.49 30 23346 96733 29832369
Aspartate aminotransferase increased 17.81 14.49 97 23279 63325 29865777
Progressive multifocal leukoencephalopathy 17.72 14.49 28 23348 8985 29920117
Hepatitis toxic 17.69 14.49 14 23362 2083 29927019
Hepatitis cholestatic 17.66 14.49 26 23350 7846 29921256
Pancreatitis acute 17.62 14.49 52 23324 25643 29903459
Infection 17.60 14.49 21 23355 78053 29851049
Caesarean section 17.46 14.49 14 23362 2123 29926979
Anxiety 17.40 14.49 27 23349 89844 29839258
COVID-19 treatment 17.02 14.49 7 23369 293 29928809
Prenatal screening test abnormal 17.01 14.49 4 23372 23 29929079
Renal tubular necrosis 16.88 14.49 37 23339 15214 29913888
Nephrocalcinosis 16.85 14.49 8 23368 473 29928629
Acute hepatitis C 16.77 14.49 6 23370 171 29928931
Visceral leishmaniasis 16.62 14.49 8 23368 488 29928614
Congenital abdominal hernia 16.59 14.49 4 23372 26 29929076
Red blood cell schistocytes present 16.58 14.49 7 23369 313 29928789
Transient tachypnoea of the newborn 16.51 14.49 6 23370 179 29928923
Joint swelling 16.48 14.49 8 23368 46938 29882164
Drug level increased 16.46 14.49 41 23335 18313 29910789
Ergot poisoning 16.45 14.49 5 23371 84 29929018
Immunoblastic lymphoma 16.39 14.49 3 23373 3 29929099
Cellulitis 16.38 14.49 8 23368 46776 29882326
Anogenital warts 16.36 14.49 8 23368 505 29928597
Anticoagulation drug level increased 16.24 14.49 8 23368 513 29928589
Deep vein thrombosis 16.22 14.49 14 23362 60487 29868615
Metabolic acidosis 16.20 14.49 65 23311 37396 29891706
Pneumococcal infection 15.96 14.49 7 23369 344 29928758
Drug hypersensitivity 15.90 14.49 18 23358 68501 29860601
Dizziness 15.50 14.49 89 23287 194820 29734282
Nephropathy 15.32 14.49 20 23356 5396 29923706
Psoriasis 15.30 14.49 7 23369 42499 29886603
Lymphocytic infiltration 15.28 14.49 8 23368 584 29928518
Neutrophil count decreased 15.27 14.49 7 23369 42447 29886655
Erythema 15.25 14.49 23 23353 77428 29851674
Loss of consciousness 15.22 14.49 24 23352 79351 29849751
Renal impairment 15.13 14.49 115 23261 84069 29845033
CD4 lymphocytes abnormal 14.94 14.49 5 23371 116 29928986
Lymphogranuloma venereum 14.86 14.49 3 23373 7 29929095
Segmented hyalinising vasculitis 14.80 14.49 4 23372 43 29929059
Oral candidiasis 14.76 14.49 29 23347 11042 29918060
CSF virus identified 14.72 14.49 4 23372 44 29929058
Urticarial vasculitis 14.56 14.49 4 23372 46 29929056

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
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
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

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

External reference:

IDSource
4021228 VUID
N0000179581 NUI
D01425 KEGG_DRUG
4021228 VANDF
C0674432 UMLSCUI
CHEBI:31781 CHEBI
AB1 PDB_CHEM_ID
CHEMBL729 ChEMBL_ID
92727 PUBCHEM_CID
D061466 MESH_DESCRIPTOR_UI
DB01601 DRUGBANK_ID
11504 IUPHAR_LIGAND_ID
7798 INN_ID
2494G1JF75 UNII
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 26 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 0074-1575 TABLET, FILM COATED 100 mg ORAL NDA 26 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 0074-2605 TABLET, FILM COATED 200 mg ORAL NDA 26 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 0074-3956 SOLUTION 80 mg ORAL NDA 26 sections
Kaletra HUMAN PRESCRIPTION DRUG LABEL 2 0074-6799 TABLET, FILM COATED 200 mg ORAL NDA 26 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