Eptifibatide is a synthetic cyclic heptapeptide and potent platelet glycoprotein IIb/IIIa (GP IIb/IIIa) receptor antagonist. It inhibits platelet aggregation by preventing fibrinogen, von Willebrand factor and other adhesive ligands from binding to the platelet GP IIb/IIIa receptor.
Eptifibatide is used as an antiplatelet pharmaceutical ingredient in the management of acute coronary syndrome (ACS) and in patients undergoing percutaneous coronary intervention (PCI), including intracoronary stenting.
Eptifibatide is a synthetic cyclic peptide containing six amino-acid residues and one mercaptopropionyl residue. An intramolecular disulfide bond forms the cyclic structure that is important for its pharmacological activity.
The chemical formula of eptifibatide is C₃₅H₄₉N₁₁O₉S₂, with a molecular weight of approximately 831.97 g/mol. Its CAS Registry Number is 188627-80-7.
Eptifibatide reversibly inhibits platelet aggregation by selectively blocking the platelet GP IIb/IIIa receptor. This prevents fibrinogen, von Willebrand factor and other adhesive proteins from binding to activated platelets. Consequently, platelet aggregation is inhibited. The effect is reversible after discontinuation because eptifibatide dissociates from the platelet receptor.
Eptifibatide is associated with:
Current U.S. labeling identifies eptifibatide injection as a platelet aggregation inhibitor for ACS and patients undergoing PCI.
Eptifibatide is a peptide-based active pharmaceutical ingredient rather than a conventional low-molecular-weight chemical API. Therefore, its quality characterization includes peptide identity, molecular mass, purity, related substances and other peptide-specific analytical parameters.
USP's current material describes an eptifibatide drug-substance monograph based on validated analytical methods, including liquid chromatographic procedures for assay and eptifibatide-related impurities.
Eptifibatide finished pharmaceutical products are supplied as a sterile, clear, colourless solution for intravenous use. U.S. labeling describes presentations including 2 mg/mL and 0.75 mg/mL strengths.
Pharmaceutical-grade Eptifibatide should be evaluated using validated analytical procedures appropriate for peptide drug substances. Important quality attributes can include identity, assay/content, related peptides and impurities, water content, residual solvents/reagents, elemental impurities and other approved specification parameters.
A qualified Eptifibatide API supplier should provide appropriate Certificate of Analysis (CoA), specification documentation, Safety Data Sheet (SDS/MSDS), batch traceability and applicable regulatory documentation.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |
| Melting Point | 150°C – 154°C |