Clinical pharmacology of selatogrel for self-administration by patients with suspected acute myocardial infarction

Expert Opin Drug Metab Toxicol. 2023 Jul-Dec;19(10):697-708. doi: 10.1080/17425255.2023.2266384. Epub 2023 Oct 27.

Abstract

Introduction: P2Y12 receptor antagonists (P2Y12 inhibitors) are well established for the treatment of coronary artery disease. The P2Y12 inhibitors currently commercially available present either pharmacokinetic limitations (due to delayed absorption, bioactivation requirement via CYP enzymes, or need of intravenous administration), pharmacodynamic (PD) limitations (limited % inhibition of platelet aggregation (IPA) or relevant PD interactions) or safety limitations (major bleeding in specific populations).

Areas covered: Selatogrel, a 2-phenylpyrimidine-4-carboxamide analog, is a potent, reversible, and selective P2Y12 inhibitor administered subcutaneously that is under development for the treatment of acute myocardial infarction (AMI) in patients with a recent history of AMI. In this review, the authors summarize the results from preclinical, phase 1, and phase 2 trials which showed that selatogrel provides rapid, pronounced, and reversible P2Y12 receptor inhibition with a favorable safety profile.

Expert opinion: These unique characteristics added to the limited potential to interact with co-medications and manageable PD interactions with other P2Y12 inhibitors provide a clear rationale for investigating the benefit of selatogrel as an emergency treatment to improve clinical outcomes in patients with AMI.

Keywords: Acute coronary syndrome; P2Y12 inhibitor; antiplatelet therapy; antithrombotic agent; selatogrel.

Publication types

  • Review

MeSH terms

  • Humans
  • Myocardial Infarction* / drug therapy
  • Myocardial Infarction* / etiology
  • Organophosphonates*
  • Percutaneous Coronary Intervention* / adverse effects
  • Platelet Aggregation Inhibitors / adverse effects
  • Purinergic P2Y Receptor Antagonists / adverse effects
  • Treatment Outcome

Substances

  • Platelet Aggregation Inhibitors
  • selatogrel
  • Purinergic P2Y Receptor Antagonists
  • Organophosphonates