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tirofiban 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| fibrinogen receptor antagonists (glycoprotein IIb/IIIa receptor antagonists) | 2680 | 144494-65-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a reversible antagonist of fibrinogen binding to the GP IIb/IIIa receptor, the major platelet surface receptor involved in platelet aggregation, when administered intravenously inhibits ex vivo platelet aggregation in a dose- and concentration-dependent manner
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 10 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 65 % | Benet LZ, Broccatelli F, Oprea TI |
| BA (Bioavailability) | 0 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.34 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 3 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.36 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.60 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PRKDC,TEK,TGFBR1,ZAP70 | 23 | |||
| kinase-selectivity-class | AXL,CDK4,EIF2AK3,GRK2,TEK | 5 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 14, 1998 | FDA | MEDICURE |
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 |
|---|---|---|---|---|---|---|
| Thrombocytopenia | 147.12 | 89.70 | 56 | 636 | 208669 | 90419086 |
| Angina pectoris | 95.41 | 89.70 | 27 | 665 | 39133 | 90588622 |
| Vascular stent thrombosis | 89.81 | 89.70 | 14 | 678 | 1102 | 90626653 |
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 |
|---|---|---|---|---|---|---|
| Thrombocytopenia | 289.76 | 56.87 | 127 | 1046 | 190152 | 42430010 |
| Cerebral haemorrhage | 78.15 | 56.87 | 32 | 1141 | 38934 | 42581228 |
| Vascular stent thrombosis | 56.95 | 56.87 | 14 | 1159 | 3228 | 42616934 |
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 |
|---|---|---|---|---|---|---|
| Thrombocytopenia | 387.14 | 59.31 | 159 | 1598 | 348726 | 110238816 |
| Vascular stent thrombosis | 135.61 | 59.31 | 27 | 1730 | 4134 | 110583408 |
| Pulmonary alveolar haemorrhage | 93.27 | 59.31 | 27 | 1730 | 20123 | 110567419 |
| Cerebral haemorrhage | 93.25 | 59.31 | 36 | 1721 | 64932 | 110522610 |
| Coronary artery stenosis | 84.46 | 59.31 | 23 | 1734 | 13735 | 110573807 |
| Myocardial infarction | 79.65 | 59.31 | 45 | 1712 | 192038 | 110395504 |
| Cardiogenic shock | 75.99 | 59.31 | 30 | 1727 | 57308 | 110530234 |
| Acute myocardial infarction | 68.17 | 59.31 | 31 | 1726 | 83746 | 110503796 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | B01AC17 | BLOOD AND BLOOD FORMING ORGANS ANTITHROMBOTIC AGENTS ANTITHROMBOTIC AGENTS Platelet aggregation inhibitors excl. heparin |
| FDA PE | N0000008832 | Decreased Platelet Aggregation |
| FDA EPC | N0000175578 | Platelet Aggregation Inhibitor |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D005343 | Fibrinolytic Agents |
| MeSH PA | D006401 | Hematologic Agents |
| MeSH PA | D010975 | Platelet Aggregation Inhibitors |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:48676 | fibrin modulating drug |
| CHEBI has role | CHEBI:50249 | anticoagulant |
| CHEBI has role | CHEBI:50433 | platelet glycoprotein-IIb/IIIa receptor antagonist |
| CHEBI has role | CHEBI:145947 | antiatherosclerotic agent |
Related Drugs by ATC class:
B01AC Platelet aggregation inhibitors excl. heparin 24 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Non-Q wave myocardial infarction | indication | 314207007 | |
| Acute coronary syndrome | indication | 394659003 | |
| Percutaneous coronary intervention | indication | 415070008 | |
| Intracranial hemorrhage | contraindication | 1386000 | |
| Acute pericarditis | contraindication | 15555002 | |
| Arteriovenous malformation | contraindication | 24551003 | |
| Acute nephropathy | contraindication | 58574008 | |
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| Neoplasm of brain | contraindication | 126952004 | DOID:1319 |
| Bleeding | contraindication | 131148009 | |
| Lithotripsy | contraindication | 133864008 | |
| Cerebrovascular accident | contraindication | 230690007 | |
| Arterial aneurysm | contraindication | 233981004 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Dissection of aorta | contraindication | 308546005 | |
| Surgical procedure | contraindication | 387713003 | |
| Traumatic injury | contraindication | 417746004 | |
| Hypertensive urgency | contraindication | 443482000 | |
| Hemorrhagic Diabetic Retinopathy | contraindication | ||
| Hemodialysis with High-Flux Membrane | 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 | 3.02 | acidic |
| pKa2 | 13.5 | acidic |
| pKa3 | 10.31 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Integrin alpha-IIb/beta-3 | Adhesion | INHIBITOR | IC50 | 7.96 | SCIENTIFIC LITERATURE | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| 4024116 | VUID |
| N0000022121 | NUI |
| D01029 | KEGG_DRUG |
| 150915-40-5 | SECONDARY_CAS_RN |
| 4021109 | VANDF |
| 4024116 | VANDF |
| C0247025 | UMLSCUI |
| CHEBI:9605 | CHEBI |
| AGG | PDB_CHEM_ID |
| CHEMBL916 | ChEMBL_ID |
| CHEMBL3189072 | ChEMBL_ID |
| D000077466 | MESH_DESCRIPTOR_UI |
| DB00775 | DRUGBANK_ID |
| 6586 | IUPHAR_LIGAND_ID |
| 7345 | INN_ID |
| GGX234SI5H | UNII |
| 60947 | PUBCHEM_CID |
| 187024 | RXNORM |
| 11701 | MMSL |
| 252483 | MMSL |
| 5588 | MMSL |
| d04315 | MMSL |
| 007531 | NDDF |
| 007532 | NDDF |
| 108981004 | SNOMEDCT_US |
| 1269173006 | SNOMEDCT_US |
| 386953003 | SNOMEDCT_US |
| 412321006 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Tirofiban Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 14789-101 | INJECTION | 50 ug | INTRAVENOUS | ANDA | 25 sections |
| Tirofiban Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 14789-102 | INJECTION | 50 ug | INTRAVENOUS | ANDA | 25 sections |
| Tirofiban Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25021-417 | INJECTION, SOLUTION | 50 ug | INTRAVENOUS | ANDA | 28 sections |
| AGGRASTAT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25208-001 | INJECTION, SOLUTION | 3.75 mg | INTRAVENOUS | NDA | 25 sections |
| AGGRASTAT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25208-002 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | NDA | 25 sections |
| AGGRASTAT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25208-901 | INJECTION, SOLUTION | 3.75 mg | INTRAVENOUS | NDA | 25 sections |
| AGGRASTAT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25208-902 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | NDA | 25 sections |
| Tirofiban | Human Prescription Drug Label | 1 | 55150-429 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | ANDA | 25 sections |
| Tirofiban | Human Prescription Drug Label | 1 | 55150-430 | INJECTION, SOLUTION | 12.50 mg | INTRAVENOUS | ANDA | 25 sections |
| Tirofiban hydrochloride | Human Prescription Drug Label | 1 | 68083-145 | INJECTION, SOLUTION | 12.50 mg | INTRAVENOUS | ANDA | 25 sections |