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| Primary information |
|---|
| ID | 10364 |
| Therapeutic ID | Th1052 |
| Protein Name | Eptifibatide |
| Sequence | >Th1052_Eptifibatide
CXGDWPC |
| Molecular Weight | 831.962 |
| Chemical Formula | C35H49N11O9S2 |
| Isoelectric Point | NA |
| Hydrophobicity | -2.3 |
| Melting point | NA |
| Half-life | Approximately 2.5 hours |
| Description | Synthetic cyclic hexapeptide that binds to platelet receptor glycoprotein and inhibits platelet aggregation. |
| Indication/Disease | For treatment of myocardial infarction and acute coronary syndrome. |
| Pharmacodynamics | Eptifibatide is an anti-coagulant that selectively blocks the platelet glycoprotein IIb/IIIa receptor. Eptifibatide is a cyclic heptapeptide derived from a protein found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarus barbouri). It belongs to the class of the so called arginin-glycin-aspartat-mimetics and reversibly binds to platelets. |
| Mechanism of Action | Eptifibatide inhibits platelet aggregation by reversibly binding to the platelet receptor glycoprotein (GP) IIb/IIIa of human platelets, thus preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands. Inhibition of platelet aggregation occurs in a dose- and concentration-dependent manner. |
| Toxicity | Eptifibatide was not lethal to rats, rabbits, or monkeys when administered by continuous Intravenous infusion for 90 minutes at a total dose of 45 mg/kg (about 2 to 5 times the recommended maximum daily human dose on a body surface area basis). |
| Metabolism | No major metabolites have been detected in human plasma. Deamidated eptifibatide and other, more polar metabolites have been detected in urine. |
| Absorption | The mean absolute bioavailability following a single subcutaneous injection to healthy female volunteers is about 40%. |
| NA |
| Clearance | 56 mL/kg/h [patients with coronary artery disease] |
| Categories | Amino Acids, Peptides, and Proteins, Antiplatelet agents, Blood and Blood Forming Organs, Decreased Platelet Aggregation, Hematologic Agents, Peptides, Peptides, Cyclic, Platelet Aggregation Inhibitors Excl. Heparin |
| Patents Number | US5767251 |
| Date of Issue | 16-Jun-1998 |
| Date of Expiry | 16-Jun-2015 |
| Drug Interaction | NA |
| Target | NA |
| Brand Name | NA |
| Company | NA |
| Brand Description | NA |
| Prescribed For | NA |
| Chemical Name | NA |
| Formulation | NA |
| Physical Appearance | NA |
| Route of Administration | NA |
| Recommended Dosage | NA |
| Contraindication | NA |
| Side Effects | NA |
| Useful Link 1 | NA |
| Useful Link 2 | NA |
| Remarks | NA |