==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb

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1363 details
Primary information
ThPP IDTh1052
Therapeutic Peptide/Protein NameEptifibatide
SequenceMpr-Har-Gly-Asp-Trp-Pro-Cys-NH2. view full sequnce in fasta
Functional ClassificationN.A.
Molecular Weight831.962
Chemical FormulaC35H49N11O9S2
Isoelectric PointN.A.
Hydrophobicity-2.3
Melting Point (℃)N.A.
Half LifeMean terminal half-life 29 ± 6 hr (initial half-life is 4.5± 0.5 hr)
DescriptionSynthetic cyclic hexapeptide that binds to platelet receptor glycoprotein and inhibits platelet aggregation.
Indication/DiseaseFor treatment of myocardial infarction and acute coronary syndrome.
PharmacodynamicsEptifibatide 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 ActionEptifibatide 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.
ToxicityEptifibatide 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).
MetabolismNo major metabolites have been detected in human plasma. Deamidated eptifibatide and other, more polar metabolites have been detected in urine.
AbsorptionThe mean absolute bioavailability following a single subcutaneous injection to healthy female volunteers is about 40%.
Volume of DistributionN.A.
Clearance55 mL/kg/h [patients with coronary artery disease]
CategoriesPlatelet Aggregation Inhibitors
Patents NumberUS6706681
Date of Issue17/03/05
Date of Expiry17/03/25
Drug InteractionN.A.
TargetLutropin-choriogonadotropic hormone receptor,Follicle-stimulating hormone receptor
Information of corresponding available drug in the market
Brand NameINTEGRILIN
CompanySchering-Plough/Essex
Brand DiscriptionINTEGRILIN 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 forAcute Coronary Syndrome (ACS), Percutaneous Coronary Intervention (PCI)
Chemical NameN6-(aminoiminomethyl)-N2-(3-mercapto-1-oxopropyl)-Llysylglycyl-L-α-aspartyl-L-tryptophyl-L-prolyl-L-cysteinamide, cyclic (1→6)-disulfide.
FormulationEach 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 AppearnceINTEGRILIN Injection is a clear, colorless, Sterile, non-pyrogenic solution  of Eptifibatide
Route of AdministrationInjection Solution for Intravenous Use
Recommended DosageDosage 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).
Contraindication1. 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 EffectsBleeding, Intracranial Hemorrhage and Stroke, Immunogenicity/Thrombocytopenia.
Useful LinkGuojie 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 ID12411291, 19636680, 12500432, 24222836, 23696756, 18393952, 18172631, 11562343, 10973767
3-D StructureN.A.