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| Primary information |
|---|
| ID | 10363 |
| 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 | 55 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 | US6706681 |
| Date of Issue | 16-Mar-2004 |
| Date of Expiry | 16-Mar-2021 |
| Drug Interaction | NA |
| Target | Lutropin-choriogonadotropic hormone receptor,Follicle-stimulating hormone receptor, Integrin beta-3, Voltage-dependent N-type calcium channel (Protein Group) |
| Brand Name | INTEGRILIN |
| Company | Schering-Plough/Essex |
| Brand Description | Schering-Plough/Essex |
| Prescribed For | Acute Coronary Syndrome (ACS), Percutaneous Coronary Intervention (PCI) |
| Chemical Name | N6-(aminoiminomethyl)-N2-(3-mercapto-1-oxopropyl)-Llysylglycyl-L-α-aspartyl-L-tryptophyl-L-prolyl-L-cysteinamide, cyclic (1→6)-disulfide. |
| Formulation | Each 10-mL vial contains 2 mg/mL of INTEGRILIN and each 100-mL vial contains either 0.75 mg/mL of INTEGRILIN or 2 mg/mL of INTEGRILIN. Each vial of either size also contains 5.25 mg/mL citric acid and sodium hydroxide to adjust the pH to 5.35. |
| Physical Appearance | INTEGRILIN Injection is a clear, colorless, Sterile, non-pyrogenic solution of Eptifibatide |
| Route of Administration | Injection Solution for Intravenous Use |
| Recommended Dosage | Dosage in Acute Coronary Syndrome (ACS): 180 mcg/kg intravenous (IV) bolus as soon as possible after diagnosis, followed by continuous infusion of 2 mcg/kg/min Dosage in 180 mcg/kg IV bolus immediately before PCI followed by continuous infusion of 2 mcg/kg/min and a second bolus of 180 mcg/kg (given 10 minutes after the first bolus). |
| Contraindication | 1. Severe hypertension (systolic blood pressure > 200 mm Hg or diastolic blood pressure > 110 mm Hg) not adequately controlled onantihypertensive therapy. 2. History of stroke within 30 days or any history of hemorrhagic stroke. 3. Current or planned administration of another parenteral GP IIb/IIIa inhibitor. 4.Hypersensitivity to INTEGRILIN or any component of the product (hypersensitivity reactions that occurred included anaphylaxis and urticaria). |
| Side Effects | Bleeding, Intracranial Hemorrhage and Stroke, Immunogenicity/Thrombocytopenia. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |