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Aggrastat (TIROFIBAN)
Aggrastat works by blocking the integrin alpha-IIb/beta-3 receptor on platelets, preventing them from aggregating and forming blood clots.
Aggrastat (Tirofiban) is a small molecule platelet aggregation inhibitor that targets the integrin alpha-IIb/beta-3 receptor. It was originally developed by Medicure and is currently owned by the same company. Aggrastat is used to treat acute coronary syndrome, non-Q wave myocardial infarction, and percutaneous coronary intervention. The drug is off-patent and has multiple generic manufacturers. Key safety considerations include its short half-life of 1.6 hours and negligible bioavailability.
At a glance
| Generic name | TIROFIBAN |
|---|---|
| Sponsor | Medicure |
| Drug class | Platelet Aggregation Inhibitor |
| Target | Integrin alpha-IIb/beta-3 |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | FDA-approved |
| First approval | 1998 |
Mechanism of action
Tirofiban hydrochloride is reversible antagonist of fibrinogen binding to the GP IIb/IIIa receptor, the major platelet surface receptor involved in platelet aggregation. When administered intravenously, tirofiban hydrochloride inhibits ex vivo platelet aggregation in dose- and concentration-dependent manner.When given according to the PRISM-PLUS regimen of 0.4 mcg/kg/min over 30 minutes followed by 0.1 mcg/kg/min maintenance infusion, 90% inhibition of platelet aggregation is attained by the end of the 30-minute infusion. When given according to the recommended regimen of 25 mcg/kg followed by 0.15 mcg/kg/min maintenance infusion, 90% inhibition of platelet aggregation is attained within 10 minutes. Platelet aggregation inhibition is reversible following cessation of the infusion of tirofiban hydrochloride.
Approved indications
- Acute coronary syndrome
- Non-Q wave myocardial infarction
- Percutaneous coronary intervention
Common side effects
- Major Bleeding
- Minor Bleeding
- Transfusions
- Edema/swelling
- Pain, pelvic
- Reaction, vasovagal
- Bradycardia
- Dissection, coronary artery
- Pain, leg
- Dizziness
- Sweating
- Thrombocytopenia
Key clinical trials
- Induced Suppression of Platelet Activity in Aneurysmal Subarachnoid Hemorrhage Management-2 (iSPASM-2) (PHASE1,PHASE2)
- Tirofiban After Successful MT Recanalization in AIS (PHASE2,PHASE3)
- Efficacy and Safety of Tirofiban for Patients With BAD (BRANT) (PHASE3)
- ATILA Project: Aspirin Versus Tirofiban in Endovascular Treatment for Patients With Acute Ischemic Stroke Due to Tandem Lesion (PHASE4)
- HR-MRI-Directed Tirofiban Therapy for Late-Window Acute Ischemic Stroke (TIAN) (PHASE3)
- Study on Tirofiban With Aspirin in the Treatment of Acute Penetrating Artery Territory Infarction (PHASE4)
- Intravenous Tirofiban After Bridging Therapy for Acute Stroke With Atherosclerotic Large Artery Occlusion (PHASE3)
- Prospective Registry of Endovascular Thrombectomy for eXtra-Large Ischemic Stroke
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Aggrastat CI brief — competitive landscape report
- Aggrastat updates RSS · CI watch RSS
- Medicure portfolio CI