lopinavir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| HIV protease inhibitors | 1601 | 192725-17-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.80 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 19, 2001 | EMA | ABBVIE DEUTSCHLAND GMBH CO. KG | |
| Sept. 15, 2000 | FDA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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:
| Source | Code | Description |
|---|---|---|
| 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|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |