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
March 19, 2001 EMA ABBVIE DEUTSCHLAND GMBH CO. KG
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 935.20 26.84 402 5911 155145 63327564
Abortion spontaneous 592.47 26.84 209 6104 46986 63435723
Stillbirth 396.83 26.84 99 6214 6651 63476058
Abortion induced 297.10 26.84 86 6227 10156 63472553
Foetal exposure during pregnancy 291.09 26.84 112 6201 31850 63450859
Premature baby 233.73 26.84 85 6228 20650 63462059
Pregnancy 161.60 26.84 77 6236 36759 63445950
Premature labour 121.50 26.84 46 6267 12458 63470251
Premature rupture of membranes 106.07 26.84 33 6280 4960 63477749
Live birth 98.58 26.84 49 6264 25581 63457128
Maternal exposure during pregnancy 98.39 26.84 115 6198 219947 63262762
Foetal death 98.09 26.84 38 6275 10942 63471767
Caesarean section 97.91 26.84 43 6270 16989 63465720
Hepatic cytolysis 92.14 26.84 40 6273 15367 63467342
Viral mutation identified 88.78 26.84 23 6290 1787 63480922
Immune reconstitution inflammatory syndrome 83.90 26.84 29 6284 6055 63476654
Fanconi syndrome acquired 80.26 26.84 19 6294 1017 63481692
Foetal growth restriction 70.52 26.84 27 6286 7526 63475183
Pre-eclampsia 68.97 26.84 28 6285 9105 63473604
Cushing's syndrome 60.60 26.84 14 6299 673 63482036
Virologic failure 60.04 26.84 17 6296 1845 63480864
Drug interaction 56.78 26.84 90 6223 229041 63253668
Anaemia 56.53 26.84 103 6210 293327 63189382
Patent ductus arteriosus 53.76 26.84 19 6294 4231 63478478
Trisomy 21 51.03 26.84 11 6302 384 63482325
Viral load increased 50.97 26.84 14 6299 1360 63481349
CD4 lymphocytes decreased 50.44 26.84 14 6299 1413 63481296
Polydactyly 47.51 26.84 10 6303 311 63482398
Drug resistance 47.08 26.84 29 6284 22904 63459805
Coarctation of the aorta 46.85 26.84 11 6302 568 63482141
Ultrasound antenatal screen 44.96 26.84 9 6304 217 63482492
Gestational diabetes 44.39 26.84 20 6293 8376 63474333
Renal tubular acidosis 43.70 26.84 13 6300 1679 63481030
Maternal drugs affecting foetus 42.78 26.84 17 6296 5225 63477484
Premature delivery 42.04 26.84 30 6283 30251 63452458
Ventricular septal defect 38.55 26.84 15 6298 4363 63478346
Drug ineffective 38.33 26.84 29 6284 1044736 62437973
Placental disorder 36.44 26.84 11 6302 1493 63481216
Fatigue 36.08 26.84 22 6291 888006 62594703
Placenta praevia 35.98 26.84 10 6303 1014 63481695
Aspartate aminotransferase increased 33.43 26.84 43 6270 90234 63392475
Metabolic acidosis 31.57 26.84 30 6283 45039 63437670
Hydrops foetalis 31.15 26.84 8 6305 600 63482109
Renal tubular disorder 30.19 26.84 11 6302 2671 63480038
Trisomy 18 29.80 26.84 6 6307 149 63482560
Hydrocephalus 29.21 26.84 13 6300 5287 63477422
Atrial septal defect 28.85 26.84 14 6299 6924 63475785
Cardiac malposition 28.50 26.84 5 6308 57 63482652
Cachexia 28.25 26.84 13 6300 5713 63476996
Alanine aminotransferase increased 27.36 26.84 42 6271 103728 63378981

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 407.05 15.74 113 11911 3231 34941676
Mitochondrial toxicity 336.73 15.74 93 11931 2606 34942301
Exposure during pregnancy 283.53 15.74 109 11915 8825 34936082
Progressive external ophthalmoplegia 282.48 15.74 71 11953 1364 34943543
Eyelid ptosis 255.66 15.74 90 11934 5676 34939231
Foetal exposure during pregnancy 191.24 15.74 134 11890 37967 34906940
Immune reconstitution inflammatory syndrome 162.91 15.74 73 11951 8686 34936221
Diplopia 160.22 15.74 89 11935 16754 34928153
Premature baby 137.28 15.74 85 11939 19548 34925359
Kaposi's sarcoma 108.13 15.74 30 11994 853 34944054
Renal tubular disorder 103.58 15.74 44 11980 4599 34940308
Fanconi syndrome acquired 103.42 15.74 35 11989 1956 34942951
Trisomy 18 75.49 15.74 22 12002 749 34944158
Congenital anomaly 74.37 15.74 25 11999 1368 34943539
Cushing's syndrome 74.18 15.74 19 12005 394 34944513
Ultrasound antenatal screen 73.21 15.74 20 12004 536 34944371
Cleft lip and palate 71.84 15.74 22 12002 890 34944017
Ophthalmoplegia 71.26 15.74 26 11998 1814 34943093
Hyperlactacidaemia 65.34 15.74 28 11996 2988 34941919
Hydrops foetalis 64.43 15.74 20 12004 847 34944060
Viral load increased 63.25 15.74 26 11998 2501 34942406
Hypertriglyceridaemia 60.09 15.74 37 11987 8411 34936496
Hyperlipidaemia 56.77 15.74 44 11980 14485 34930422
CD4 lymphocytes decreased 50.78 15.74 20 12004 1721 34943186
Polydactyly 50.19 15.74 18 12006 1195 34943712
Trisomy 21 49.83 15.74 15 12009 572 34944335
Drug resistance 48.68 15.74 52 11972 25875 34919032
Drug ineffective 48.08 15.74 52 11972 456699 34488208
Cerebral toxoplasmosis 47.51 15.74 19 12005 1702 34943205
Osteonecrosis 47.39 15.74 40 11984 14850 34930057
Glycosuria 46.13 15.74 17 12007 1220 34943687
Drug interaction 45.16 15.74 175 11849 225771 34719136
Ventricular septal defect 43.17 15.74 23 12001 3978 34940929
Acquired immunodeficiency syndrome 42.95 15.74 13 12011 505 34944402
Hepatic cytolysis 42.19 15.74 37 11987 14459 34930448
Blood triglycerides increased 40.92 15.74 36 11988 14123 34930784
Fanconi syndrome 40.69 15.74 17 12007 1703 34943204
Viral mutation identified 40.63 15.74 20 12004 2934 34941973
Mitochondrial cytopathy 40.27 15.74 10 12014 182 34944725
Osteoporosis 40.25 15.74 34 11990 12634 34932273
Caesarean section 40.10 15.74 18 12006 2146 34942761
Lipoatrophy 38.86 15.74 12 12012 499 34944408
Abortion spontaneous 37.34 15.74 11 12013 389 34944518
Blood lactic acid increased 36.83 15.74 25 11999 6703 34938204
Hepatic failure 36.73 15.74 52 11972 34479 34910428
Aspartate aminotransferase increased 36.06 15.74 75 11949 67708 34877199
Atypical mycobacterial infection 36.00 15.74 13 12011 880 34944027
HIV-associated neurocognitive disorder 34.49 15.74 10 12014 334 34944573
Liver disorder 32.62 15.74 48 11976 32949 34911958
Proteinuria 32.56 15.74 36 11988 18606 34926301
Death 32.04 15.74 55 11969 397994 34546913
Virologic failure 32.00 15.74 18 12006 3462 34941445
Osteomalacia 31.99 15.74 12 12012 905 34944002
Hypophosphataemia 31.79 15.74 28 11996 10998 34933909
Febrile neutropenia 30.93 15.74 5 12019 136844 34808063
Oesophageal candidiasis 30.61 15.74 19 12005 4377 34940530
Kidney malformation 30.44 15.74 8 12016 184 34944723
Blood alkaline phosphatase increased 30.31 15.74 45 11979 31130 34913777
Alanine aminotransferase increased 29.35 15.74 77 11947 80738 34864169
Cytomegalovirus chorioretinitis 28.83 15.74 17 12007 3572 34941335
Cryptorchism 28.61 15.74 14 12010 2027 34942880
Blood bilirubin increased 28.60 15.74 49 11975 38247 34906660
Anal cancer 27.47 15.74 9 12015 454 34944453
Porphyria non-acute 26.99 15.74 9 12015 480 34944427
Hepatitis C 26.44 15.74 24 12000 9806 34935101
Gastroschisis 26.44 15.74 7 12017 166 34944741
Neonatal asphyxia 25.58 15.74 8 12016 347 34944560
HIV wasting syndrome 25.37 15.74 6 12018 88 34944819
HIV infection 24.37 15.74 11 12013 1328 34943579
Cachexia 24.30 15.74 20 12004 7166 34937741
Encephalitis 24.08 15.74 20 12004 7257 34937650
Lactic acidosis 24.02 15.74 43 11981 34729 34910178
Product dose omission issue 23.67 15.74 6 12018 119705 34825202
Renal failure 23.50 15.74 98 11926 130459 34814448
Pneumocystis jirovecii pneumonia 22.93 15.74 31 11993 19679 34925228
Blood phosphorus decreased 22.79 15.74 14 12010 3167 34941740
Progressive multifocal leukoencephalopathy 22.72 15.74 22 12002 9742 34935165
Oesophageal atresia 22.69 15.74 8 12016 505 34944402
Gamma-glutamyltransferase increased 22.61 15.74 38 11986 29193 34915714
Maternal drugs affecting foetus 22.34 15.74 15 12009 3950 34940957
Opportunistic infection 22.13 15.74 11 12013 1647 34943260
HIV associated nephropathy 21.91 15.74 7 12017 326 34944581
Stillbirth 21.38 15.74 6 12018 178 34944729
Hepatic cirrhosis 21.32 15.74 28 11996 17286 34927621
Fatigue 20.98 15.74 62 11962 370591 34574316
Exomphalos 20.42 15.74 6 12018 210 34944697
Disease progression 20.27 15.74 6 12018 108071 34836836
Foetal distress syndrome 19.90 15.74 9 12015 1091 34943816
Femoral neck fracture 19.81 15.74 13 12011 3294 34941613
Castleman's disease 19.72 15.74 4 12020 27 34944880
Congenital hearing disorder 19.69 15.74 5 12019 100 34944807
CSF virus identified 19.12 15.74 4 12020 32 34944875
Lipohypertrophy 18.93 15.74 6 12018 272 34944635
Immunoblastic lymphoma 18.85 15.74 3 12021 3 34944904
Acute kidney injury 18.64 15.74 173 11851 304815 34640092
Hodgkin's disease 18.49 15.74 8 12016 873 34944034
Lymphogranuloma venereum 18.39 15.74 3 12021 4 34944903
Anaemia neonatal 18.16 15.74 6 12018 311 34944596
Segmented hyalinising vasculitis 17.82 15.74 4 12020 46 34944861
Drug abuse 17.70 15.74 6 12018 99090 34845817
Cushingoid 17.07 15.74 11 12013 2703 34942204
Abdominal hernia 16.96 15.74 11 12013 2733 34942174
Amylase increased 16.89 15.74 15 12009 5953 34938954
Adrenogenital syndrome 16.77 15.74 4 12020 61 34944846
Dyspnoea 16.63 15.74 70 11954 376712 34568195
Jaundice 16.61 15.74 35 11989 31847 34913060
Cortisol decreased 16.61 15.74 8 12016 1119 34943788
Blood pressure increased 16.32 15.74 5 12019 88097 34856810
Syphilis 16.29 15.74 6 12018 430 34944477
Central pain syndrome 16.20 15.74 4 12020 71 34944836
Trisomy 8 16.15 15.74 4 12020 72 34944835
Atrial septal defect 15.98 15.74 16 12008 7376 34937531
Hyperphosphaturia 15.95 15.74 4 12020 76 34944831
CD4 lymphocytes increased 15.90 15.74 5 12019 221 34944686
Completed suicide 15.78 15.74 7 12017 98161 34846746

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 523.67 17.96 189 11950 29318 79702931
Exposure during pregnancy 515.71 17.96 268 11871 100864 79631385
Lipodystrophy acquired 443.95 17.96 108 12031 4217 79728032
Mitochondrial toxicity 388.23 17.96 91 12048 3023 79729226
Progressive external ophthalmoplegia 339.59 17.96 71 12068 1374 79730875
Stillbirth 307.13 17.96 79 12060 3876 79728373
Eyelid ptosis 258.32 17.96 87 12052 10957 79721292
Abortion induced 231.53 17.96 72 12067 7037 79725212
Immune reconstitution inflammatory syndrome 220.61 17.96 82 12057 13759 79718490
Diplopia 170.97 17.96 89 12050 33377 79698872
Drug resistance 138.60 17.96 84 12055 42129 79690120
Viral mutation identified 129.50 17.96 40 12099 3818 79728431
Foetal exposure during pregnancy 129.02 17.96 44 12095 5746 79726503
Fanconi syndrome acquired 125.56 17.96 36 12103 2658 79729591
Ultrasound antenatal screen 122.85 17.96 27 12112 666 79731583
Hydrops foetalis 114.33 17.96 26 12113 752 79731497
Drug interaction 111.15 17.96 214 11925 414969 79317280
Trisomy 18 109.47 17.96 24 12115 585 79731664
Cleft lip and palate 106.21 17.96 24 12115 674 79731575
Cushing's syndrome 97.75 17.96 24 12115 971 79731278
Pregnancy 97.41 17.96 57 12082 26794 79705455
Renal tubular disorder 94.50 17.96 36 12103 6450 79725799
Caesarean section 92.93 17.96 43 12096 12492 79719757
Viral load increased 92.37 17.96 29 12110 2919 79729330
Hepatic cytolysis 83.90 17.96 52 12087 27099 79705150
Premature rupture of membranes 79.36 17.96 28 12111 4041 79728208
Live birth 76.57 17.96 43 12096 18701 79713548
Ophthalmoplegia 76.28 17.96 25 12114 2887 79729362
CD4 lymphocytes decreased 74.63 17.96 24 12115 2610 79729639
Hyperlactacidaemia 74.19 17.96 29 12110 5566 79726683
Aspartate aminotransferase increased 72.29 17.96 97 12042 138544 79593705
Maternal exposure during pregnancy 71.91 17.96 96 12043 136442 79595807
Foetal death 67.22 17.96 30 12109 8014 79724235
Premature labour 59.76 17.96 28 12111 8362 79723887
Alanine aminotransferase increased 57.74 17.96 95 12044 162475 79569774
Hypertriglyceridaemia 48.72 17.96 28 12111 12712 79719537
Kaposi's sarcoma 48.52 17.96 13 12126 746 79731503
Hepatic failure 46.80 17.96 52 12087 61160 79671089
Virologic failure 46.14 17.96 19 12120 4172 79728077
Blood triglycerides increased 44.89 17.96 32 12107 21008 79711241
Drug ineffective 44.47 17.96 60 12079 1080853 78651396
Fanconi syndrome 42.13 17.96 16 12123 2840 79729409
Renal tubular acidosis 41.89 17.96 17 12122 3597 79728652
Cerebral toxoplasmosis 41.33 17.96 15 12124 2347 79729902
Placenta praevia 39.30 17.96 11 12128 744 79731505
Acquired immunodeficiency syndrome 38.40 17.96 9 12130 298 79731951
Opportunistic infection 38.09 17.96 15 12124 2935 79729314
Pre-eclampsia 36.71 17.96 19 12120 7022 79725227
Glycosuria 34.98 17.96 13 12126 2175 79730074
Portal hypertension 33.70 17.96 18 12121 7090 79725159
Renal failure 33.61 17.96 86 12053 200882 79531367
Blood lactic acid increased 33.38 17.96 22 12117 12722 79719527
Blood alkaline phosphatase increased 32.31 17.96 44 12095 63620 79668629
Cytomegalovirus chorioretinitis 32.08 17.96 16 12123 5474 79726775
HIV wasting syndrome 31.52 17.96 6 12133 70 79732179
Premature baby 31.27 17.96 14 12125 3766 79728483
Lipoatrophy 31.18 17.96 9 12130 680 79731569
Blood bilirubin increased 30.96 17.96 44 12095 66188 79666061
Mitochondrial cytopathy 30.89 17.96 8 12131 402 79731847
Hypophosphataemia 30.80 17.96 25 12114 19888 79712361
Maternal drugs affecting foetus 30.62 17.96 11 12128 1672 79730577
Osteonecrosis 30.16 17.96 30 12109 31065 79701184
Gestational diabetes 30.02 17.96 16 12123 6277 79725972
Acute kidney injury 30.02 17.96 157 11982 519247 79213002
Anaemia neonatal 30.00 17.96 5 12134 25 79732224
Hepatomegaly 29.84 17.96 24 12115 18850 79713399
Pneumocystis jirovecii pneumonia 29.04 17.96 30 12109 32478 79699771
Fatigue 28.62 17.96 62 12077 929665 78802584
Neutropenia neonatal 28.56 17.96 5 12134 35 79732214
Joint swelling 28.14 17.96 5 12134 288641 79443608
HIV associated nephropathy 27.47 17.96 7 12132 330 79731919
Hyperlipidaemia 26.84 17.96 26 12113 26067 79706182
Atypical mycobacterial infection 26.56 17.96 10 12129 1733 79730516
Gamma-glutamyltransferase increased 26.56 17.96 37 12102 54643 79677606
Anaemia 26.02 17.96 135 12004 444880 79287369
Proteinuria 25.50 17.96 28 12111 32474 79699775
Premature delivery 25.31 17.96 24 12115 23443 79708806
Completed suicide 24.52 17.96 4 12135 245763 79486486
HIV viraemia 23.84 17.96 5 12134 98 79732151
Metabolic acidosis 23.76 17.96 44 12095 82485 79649764
Lactic acidosis 23.45 17.96 40 12099 70319 79661930
Pancreatitis 22.88 17.96 39 12100 68536 79663713
Mycobacterium avium complex infection 22.80 17.96 12 12127 4588 79727661
Blood HIV RNA increased 22.67 17.96 9 12130 1799 79730450
Product dose omission issue 22.63 17.96 5 12134 247532 79484717
HIV-associated neurocognitive disorder 22.37 17.96 6 12133 346 79731903
Hepatosplenomegaly 22.30 17.96 13 12126 6056 79726193
Progressive multifocal leukoencephalopathy 22.08 17.96 21 12118 20579 79711670
CSF virus identified 21.76 17.96 4 12135 38 79732211
Cachexia 21.69 17.96 16 12123 11067 79721182
Pulmonary tuberculosis 21.63 17.96 14 12125 7851 79724398
Lymphadenopathy 21.46 17.96 33 12106 53214 79679035
Anembryonic gestation 21.37 17.96 6 12133 410 79731839
Immunoblastic lymphoma 21.29 17.96 3 12136 3 79732246
Adrenal suppression 21.22 17.96 8 12131 1391 79730858
Hepatotoxicity 20.94 17.96 32 12107 51320 79680929
Lipohypertrophy 20.80 17.96 7 12132 877 79731372
Osteomalacia 20.79 17.96 8 12131 1472 79730777
Pain 20.74 17.96 48 12091 703754 79028495
Hepatitis C 20.65 17.96 16 12123 11909 79720340
Liver function test abnormal 20.63 17.96 36 12103 64439 79667810
Swelling 20.58 17.96 4 12135 216707 79515542
Dyspnoea 20.35 17.96 65 12074 856960 78875289
Liver disorder 20.08 17.96 38 12101 72379 79659870
Encephalitis 19.66 17.96 17 12122 14743 79717506
Hyperbilirubinaemia 19.02 17.96 21 12118 24497 79707752
Urinary tract infection 19.01 17.96 9 12130 274503 79457746
Segmented hyalinising vasculitis 18.72 17.96 4 12135 86 79732163
Jaundice 18.67 17.96 31 12108 53318 79678931
Alopecia 18.63 17.96 6 12133 231349 79500900
Premature separation of placenta 18.45 17.96 7 12132 1239 79731010
Atypical mycobacterial lymphadenitis 18.35 17.96 3 12136 13 79732236
Fall 18.06 17.96 29 12110 487600 79244649

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
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
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 0074-0522 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 0074-1575 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 0074-2605 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 0074-3956 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 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
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