A database of FDA approved therapeutic peptides and proteins
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1363 details |
| Primary information | |
|---|---|
| ThPP ID | Th1052 |
| Therapeutic Peptide/Protein Name | Eptifibatide |
| Sequence | Mpr-Har-Gly-Asp-Trp-Pro-Cys-NH2. view full sequnce in fasta |
| Functional Classification | N.A. |
| Molecular Weight | 831.962 |
| Chemical Formula | C35H49N11O9S2 |
| Isoelectric Point | N.A. |
| Hydrophobicity | -2.3 |
| Melting Point (℃) | N.A. |
| Half Life | Mean terminal half-life 29 ± 6 hr (initial half-life is 4.5± 0.5 hr) |
| 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%. |
| Volume of Distribution | N.A. |
| Clearance | 55 mL/kg/h [patients with coronary artery disease] |
| Categories | Platelet Aggregation Inhibitors |
| Patents Number | US6706681 |
| Date of Issue | 17/03/05 |
| Date of Expiry | 17/03/25 |
| Drug Interaction | N.A. |
| Target | Lutropin-choriogonadotropic hormone receptor,Follicle-stimulating hormone receptor |
| Information of corresponding available drug in the market | |
| Brand Name | INTEGRILIN |
| Company | Schering-Plough/Essex |
| Brand Discription | INTEGRILIN Injection is a clear, colorless, sterile, non-pyrogenic solution for intravenous (IV) use with an empirical formula of C35H49N11O9S2 and a molecular weight of 831.96. |
| 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. |
| Physcial Appearnce | 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 | Guojie Ho, Antoinette Paone, Luciano Forni, Catherine De Tollenaere, Brice Bonnet, Christine Devijver, “Processes for preparing eptifibatide.†U.S. Patent US20060036071, issued February 16, 2006. |
| PubMed ID | 12411291, 19636680, 12500432, 24222836, 23696756, 18393952, 18172631, 11562343, 10973767 |
| 3-D Structure | N.A. |