amprenavir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| HIV protease inhibitors | 200 | 161814-49-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
; RN refers to (3S-(3R*(1S*,2R*)))-isomer; fosamprenavir is a prodrug
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.20 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.04 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 1 % | 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 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 20, 2000 | EMA | ||
| April 15, 1999 | FDA | GLAXOSMITHKLINE |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J05AE05 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Protease inhibitors |
| FDA MoA | N0000000246 | HIV Protease Inhibitors |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D019380 | Anti-HIV Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D044966 | Anti-Retroviral Agents |
| MeSH PA | D000904 | Antibiotics, Antitubercular |
| MeSH PA | D000995 | Antitubercular 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 |
| FDA MoA | N0000182141 | Cytochrome P450 3A4 Inhibitors |
| FDA MoA | N0000185506 | Cytochrome P450 3A4 Inducers |
| FDA MoA | N0000191264 | P-Glycoprotein Inducers |
| CHEBI has role | CHEBI:35660 | HIV protease inhibitors |
| CHEBI has role | CHEBI:36044 | antiviral drugs |
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 |
| Prevention of HIV Infection after Exposure | off-label use | ||
| Acquired hemolytic anemia | contraindication | 4854004 | |
| 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 | |
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| 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 |
| Familial hypercholesterolemia - homozygous | contraindication | 238078005 | |
| Hypertriglyceridemia | contraindication | 302870006 | |
| Cardiovascular event risk | contraindication | 395112001 | |
| Autoimmune hemolytic anemia | contraindication | 413603009 | DOID:718 |
| 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 | |
| Vitamin K Deficiency Induced Hypoprothrombinemia | 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 | 13.6 | acidic |
| pKa2 | 1.64 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Thromboxane-A synthase | Enzyme | IC50 | 5.17 | DRUG MATRIX | |||||
| Cathepsin D | Enzyme | IC50 | 4.82 | CHEMBL | |||||
| Cytochrome P450 3A4 | Enzyme | IC50 | 6 | DRUG MATRIX | |||||
| Pol polyprotein | Enzyme | INHIBITOR | Ki | 10.40 | CHEMBL | CHEMBL | |||
| Gag-Pol polyprotein | Polyprotein | WOMBAT-PK | |||||||
| Protease | Enzyme | Ki | 10.44 | CHEMBL | |||||
| Protease | Unclassified | Ki | 10.52 | CHEMBL | |||||
| Protease | Unclassified | Ki | 9.82 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021158 | VUID |
| N0000148609 | NUI |
| D00894 | KEGG_DRUG |
| 228655 | RXNORM |
| C0754188 | UMLSCUI |
| CHEBI:40050 | CHEBI |
| 478 | PDB_CHEM_ID |
| CHEMBL116 | ChEMBL_ID |
| DB00701 | DRUGBANK_ID |
| C095108 | MESH_SUPPLEMENTAL_RECORD_UI |
| 12681 | IUPHAR_LIGAND_ID |
| 7751 | INN_ID |
| 5S0W860XNR | UNII |
| 65016 | PUBCHEM_CID |
| 29919 | MMSL |
| 8067 | MMSL |
| d04428 | MMSL |
| 116088006 | SNOMEDCT_US |
| 387006009 | SNOMEDCT_US |
| 4021158 | VANDF |
| 007752 | NDDF |
Pharmaceutical products:
None