Stem definition | Drug id | CAS RN |
---|---|---|
HIV protease inhibitors | 1240 | 226700-79-4 |
Dose | Unit | Route |
---|---|---|
1.40 | g | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
S (Water solubility) | 0.31 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 0 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 67.81 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Date | Agency | Company | Orphan |
---|---|---|---|
Oct. 20, 2003 | FDA | VIIV HLTHCARE |
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 |
---|---|---|---|---|---|---|
Viral mutation identified | 91.16 | 46.94 | 17 | 714 | 1882 | 46683449 |
Exposure during pregnancy | 89.18 | 46.94 | 40 | 691 | 108172 | 46577159 |
Drug resistance | 70.85 | 46.94 | 21 | 710 | 17347 | 46667984 |
Abortion spontaneous | 66.08 | 46.94 | 25 | 706 | 43621 | 46641710 |
Lipodystrophy acquired | 56.71 | 46.94 | 11 | 720 | 1494 | 46683837 |
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 | 90.54 | 25.62 | 25 | 2077 | 3535 | 29946841 |
Virologic failure | 56.75 | 25.62 | 17 | 2085 | 3202 | 29947174 |
Immune reconstitution inflammatory syndrome | 46.18 | 25.62 | 19 | 2083 | 9082 | 29941294 |
Hypertriglyceridaemia | 44.84 | 25.62 | 18 | 2084 | 8080 | 29942296 |
Heart transplant rejection | 42.24 | 25.62 | 11 | 2091 | 1242 | 29949134 |
Viral mutation identified | 38.33 | 25.62 | 12 | 2090 | 2614 | 29947762 |
Mitochondrial cytopathy | 36.07 | 25.62 | 7 | 2095 | 206 | 29950170 |
Hyperlactacidaemia | 34.28 | 25.62 | 11 | 2091 | 2595 | 29947781 |
Myositis | 31.16 | 25.62 | 15 | 2087 | 10362 | 29940014 |
Drug resistance | 29.28 | 25.62 | 18 | 2084 | 20115 | 29930261 |
Adrenogenital syndrome | 28.79 | 25.62 | 5 | 2097 | 78 | 29950298 |
Portal hypertension | 26.35 | 25.62 | 10 | 2092 | 3863 | 29946513 |
Hypercholesterolaemia | 25.94 | 25.62 | 12 | 2090 | 7580 | 29942796 |
Source | Code | Description |
---|---|---|
ATC | J05AE07 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Protease inhibitors |
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 | D004791 | Enzyme Inhibitors |
MeSH PA | D017320 | HIV Protease Inhibitors |
MeSH PA | D011480 | Protease Inhibitors |
MeSH PA | D000084762 | Viral Protease Inhibitors |
FDA EPC | N0000175889 | Protease Inhibitor |
CHEBI has role | CHEBI:50266 | prodrugs |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Human immunodeficiency virus infection | indication | 86406008 | DOID:526 |
Prevention of HIV Infection after Exposure | off-label use | ||
Hypercholesterolemia | contraindication | 13644009 | |
Myocardial infarction | contraindication | 22298006 | DOID:5844 |
Hereditary factor VIII deficiency disease | contraindication | 28293008 | DOID:12134 |
Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
Hereditary factor IX deficiency disease | contraindication | 41788008 | DOID:12259 |
Hemolytic anemia | contraindication | 61261009 | DOID:583 |
Chronic type B viral hepatitis | contraindication | 61977001 | |
Lipodystrophy | contraindication | 71325002 | DOID:811 |
Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
Hyperglycemia | contraindication | 80394007 | DOID:4195 |
Kidney stone | contraindication | 95570007 | |
Chronic hepatitis C | contraindication | 128302006 | |
Liver function tests abnormal | contraindication | 166603001 | |
Disease of liver | contraindication | 235856003 | DOID:409 |
Hypertriglyceridemia | contraindication | 302870006 | |
Cardiovascular event risk | contraindication | 395112001 | |
Breastfeeding (mother) | contraindication | 413712001 | |
Disorder of coronary artery | contraindication | 414024009 | |
Obesity | contraindication | 414916001 | DOID:9970 |
Ketoacidosis in diabetes mellitus | contraindication | 420422005 | DOID:1837 |
Smokes tobacco daily | contraindication | 449868002 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 1.13 | acidic |
pKa2 | 6.35 | acidic |
pKa3 | 1.8 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Pol polyprotein | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
Gag-Pol polyprotein | Polyprotein | WOMBAT-PK |
ID | Source |
---|---|
4021412 | VUID |
N0000148827 | NUI |
D02497 | KEGG_DRUG |
226700-81-8 | SECONDARY_CAS_RN |
4021412 | VANDF |
C1176315 | UMLSCUI |
CHEBI:82941 | CHEBI |
CHEMBL1664 | ChEMBL_ID |
CHEMBL1200734 | ChEMBL_ID |
DB01319 | DRUGBANK_ID |
131536 | PUBCHEM_CID |
C426859 | MESH_SUPPLEMENTAL_RECORD_UI |
8011 | INN_ID |
WOU1621EEG | UNII |
358262 | RXNORM |
17646 | MMSL |
262160 | MMSL |
64492 | MMSL |
d04901 | MMSL |
004510 | NDDF |
004511 | NDDF |
407017006 | SNOMEDCT_US |
407018001 | SNOMEDCT_US |
412393004 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Fosamprenavir Calcium | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-3520 | TABLET, FILM COATED | 700 mg | ORAL | ANDA | 27 sections |
LEXIVA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-207 | TABLET, FILM COATED | 700 mg | ORAL | NDA | 26 sections |
LEXIVA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-208 | SUSPENSION | 50 mg | ORAL | NDA | 26 sections |
LEXIVA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53808-0281 | TABLET, FILM COATED | 700 mg | ORAL | NDA | 26 sections |
LEXIVA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53808-1010 | TABLET, FILM COATED | 700 mg | ORAL | NDA | 25 sections |
Fosamprenavir Calcium | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63304-583 | TABLET, COATED | 700 mg | ORAL | ANDA | 25 sections |