Eptifibatide;? Sequence?

Product Name Eptifibatide;?
Sequence? Mpr-Har-Gly-Asp-Trp-Pro-Cys-NH2
Cas No. 148031-34-9
Molecular Formula C35H49N11O9S2
Molecular Weight 832.4
Appearance White slightly yellwish powder
Specific Rotation[20/D] -75.0~-95.0°(C=1,1%HAc) ?
Amino Acids composition ± 10%
Peptide Purity (By HPLC) ≥98% by area integration
Related Substance (By HPLC) Total Impurities (%)≤2.0%? Largest Single Impurity (%)≤ 1.0%
Water Content (Karl Fischer) ≤8.0%
Peptide Content(N determination) ≥80%
Acetate Content ≤15%
IR spectrum in accordance


Brief introduction:

Eptifibatide (Integrilin, Millennium Pharmaceuticals, also co-promoted by Schering-Plough/Essex), is an antiplatelet drug of the glycoprotein IIb/IIIa inhibitor class.[1] Eptifibatide is a cyclic heptapeptide derived from a protein found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarius barbouri).

It belongs to the class of the so-called arginin-glycin-aspartat-mimetics and reversibly binds to platelets. Eptifibatide has a short half-life. The drug is the third inhibitor of GPIIb/IIIa that has found broad acceptance after the specific antibody abciximab and the non-peptide tirofiban entered the global market.

Indications

Eptifibatide is used to reduce the risk of acute cardiac ischemic events (death and/or myocardial infarction) in patients with unstable angina or non-ST-segment-elevation (e.g., non-Q-wave) myocardial infarction (i.e., non-ST-segment elevation acute coronary syndromes) both in patients who are to receive non surgery (conservative) medical treatment and those undergoing percutaneous coronary intervention (PCI).

The drug is usually applied together with aspirin or clopidogrel and (low molecular weight or unfractionated) heparin. Additionally, the usual supportive treatment consisting of applications of nitrates, beta-blockers, opioid analgesics and/or benzodiazepines should be employed as indicated. Angiographic evaluation and other intensive diagnostic procedures may be considered a first line task before initiating therapy with eptifibatide.

The drug should exclusively be used in hospitalized patients both because of the serious degree of patients' illness and because of the possible side-effects of eptifibatide.




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