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

Martine Géhin, Robert F. Storey, Corine Bernaud, Jasper Dingemanse

2023Expert Opinion on Drug Metabolism & Toxicology13 citationsDOIOpen Access PDF

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.

Topics & Concepts

P2Y12PharmacodynamicsMedicinePharmacologyMyocardial infarctionPharmacokineticsCoronary artery diseasePlatelet aggregationClinical pharmacologyClopidogrelPlateletInternal medicineAntiplatelet Therapy and Cardiovascular DiseasesAtrial Fibrillation Management and OutcomesAcute Myocardial Infarction Research
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