tirofiban Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 14, 1998 | FDA | MEDICURE |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
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:48676 | fibrin modulating drug |
| CHEBI has role | CHEBI:50433 | platelet glycoprotein-IIb/IIIa receptor antagonist |
| CHEBI has role | CHEBI:50249 | anticoagulant |
Drug Use (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 |
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)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 12.5MG BASE/50ML (EQ 0.25MG BASE/ML) | AGGRASTAT | MEDICURE | N020912 | May 14, 1998 | DISCN | INJECTABLE | INJECTION | 6770660 | May 1, 2023 | A DOSING REGIMEN OF AGGRASTAT (TIROFIBAN HYDROCHLORIDE)(25MCG/KG FOLLOWED BY 0.15MCG/KG/MIN INFUSION) TO REDUCE THE RATE OF THROMBOTIC CORONARY EVENTS ASSOCIATED WITH ACUTE CORONARY SYNDROME (ACS) IN PATIENTS WITH NON-ST ELEVATION ACS |
| EQ 3.75MG BASE/15ML (EQ 0.25MG BASE/ML) | AGGRASTAT | MEDICURE | N020912 | Aug. 31, 2016 | RX | SOLUTION | INJECTION | 6770660 | May 1, 2023 | A DOSING REGIMEN OF AGGRASTAT (TIROFIBAN HYDROCHLORIDE)(25MCG/KG FOLLOWED BY 0.15MCG/KG/MIN INFUSION) TO REDUCE THE RATE OF THROMBOTIC CORONARY EVENTS ASSOCIATED WITH ACUTE CORONARY SYNDROME (ACS) IN PATIENTS WITH NON-ST ELEVATION ACS |
| EQ 12.5MG BASE/250ML (EQ 0.05MG BASE/ML) | AGGRASTAT | MEDICURE | N020913 | April 20, 2000 | RX | INJECTABLE | INJECTION | 6770660 | May 1, 2023 | A DOSING REGIMEN OF AGGRASTAT (TIROFIBAN HYDROCHLORIDE)(25MCG/KG FOLLOWED BY 0.15MCG/KG/MIN INFUSION) TO REDUCE THE RATE OF THROMBOTIC CORONARY EVENTS ASSOCIATED WITH ACUTE CORONARY SYNDROME (ACS) IN PATIENTS WITH NON-ST ELEVATION ACS |
| EQ 25MG BASE/500ML (EQ 0.05MG BASE/ML) | AGGRASTAT | MEDICURE | N020913 | May 14, 1998 | DISCN | INJECTABLE | INJECTION | 6770660 | May 1, 2023 | A DOSING REGIMEN OF AGGRASTAT (TIROFIBAN HYDROCHLORIDE)(25MCG/KG FOLLOWED BY 0.15MCG/KG/MIN INFUSION) TO REDUCE THE RATE OF THROMBOTIC CORONARY EVENTS ASSOCIATED WITH ACUTE CORONARY SYNDROME (ACS) IN PATIENTS WITH NON-ST ELEVATION ACS |
| EQ 5MG BASE/100ML (EQ 0.05MG BASE/ML) | AGGRASTAT | MEDICURE | N020913 | May 17, 2002 | RX | INJECTABLE | INJECTION | 6770660 | May 1, 2023 | A DOSING REGIMEN OF AGGRASTAT (TIROFIBAN HYDROCHLORIDE)(25MCG/KG FOLLOWED BY 0.15MCG/KG/MIN INFUSION) TO REDUCE THE RATE OF THROMBOTIC CORONARY EVENTS ASSOCIATED WITH ACUTE CORONARY SYNDROME (ACS) IN PATIENTS WITH NON-ST ELEVATION ACS |
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 |
|---|---|
| D000077466 | MESH_DESCRIPTOR_UI |
| 4024116 | VUID |
| N0000022121 | NUI |
| C0247025 | UMLSCUI |
| D01029 | KEGG_DRUG |
| 6H925F8O5J | UNII |
| 150915-40-5 | SECONDARY_CAS_RN |
| 108981004 | SNOMEDCT_US |
| d04315 | MMSL |
| 73137 | RXNORM |
| 386953003 | SNOMEDCT_US |
| 4024116 | VANDF |
| 007531 | NDDF |
| CHEMBL916 | ChEMBL_ID |
| DB00775 | DRUGBANK_ID |
| CHEMBL1704 | ChEMBL_ID |
| 7345 | INN_ID |
| AGG | PDB_CHEM_ID |
| CHEBI:9605 | CHEBI |
| CHEMBL3189072 | ChEMBL_ID |
| 60947 | PUBCHEM_CID |
| 6586 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| AGGRASTAT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25208-001 | INJECTION, SOLUTION | 3.75 mg | INTRAVENOUS | NDA | 16 sections |
| AGGRASTAT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25208-002 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | NDA | 16 sections |