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Elinogrel: Competitive, reversible, direct-acting oral and i.v. P2Y12 ADP receptor antagonist

Description

Elinogrel is a novel, small molecule antiplatelet compound in the P2Y12ADP receptor antagonist class. It inhibits the ADP receptor (P2Y12) on platelets to block platelet aggregation and prevent thrombosis.

Key Characteristics

  • Elinogrel is the only compound in the P2Y12ADP receptor antagonist class with an i.v. and oral formulation, offering the potential to be used in acute and chronic indications. The i.v. formulation provides immediate onset and high levels of platelet inhibition, which is critical in the acute setting. It may be transitioned easily to the oral formulation, which similarly provides high levels of inhibition of platelet aggregation, for chronic use.
  • Elinogrel is fast-acting and direct, requiring no metabolism for activation. As a result, elinogrel avoids the issue of delayed action and wide inter-patient variability seen with thienopyridines (e.g., clopidogrel [Plavix®]).
  • Elinogrel has predictable reversibility, which may be advantageous for patients undergoing emergency or elective surgical procedures in which rapid restoration of platelet function is critical to reduce bleeding.

Potential Indications

  • Prevention of death, myocardial infarction and stroke in patients with acute coronary syndrome (ACS)
  • Prevention of major cardiovascular events, such as myocardial infarction and stroke, in patients with chronic coronary heart disease (CHD)

Clinical Development

Portola, in collaboration with Novartis, evaluated the efficacy and safety of i.v. and oral formulations of elinogrel in the Phase 2 INNOVATE-PCI study in approximately 650 patients undergoing non-urgent percutaneous coronary intervention (PCI). In August 2010, results were presented during the Hot Line II – Coronary Artery Disease late-breaker session at the European Society of Cardiology (ESC) Congress. The data showed that the trial achieved its objectives. The i.v. and oral elinogrel regimen provided more rapid and greater antiplatelet activity than clopidogrel (Plavix®) without a significant increase in the risk of TIMI major and minor bleeding, and was generally well tolerated.