P2Y12R antagonists in antithrombotic therapy: a patent and literature review (2019-present).

Abstract

Introduction: P2Y₁₂ receptor (P2Y₁₂R) is a G protein-coupled receptor that plays a crucial role in regulating platelet activation and aggregation. P2Y₁₂R is involved in various processes such as renal fibrosis, cancer, ischemic disease, and related complications, making it an appealing target for therapeutic interventions. Over the past decade, the discovery and development of P2Y₁₂R antagonists have significantly advanced, offering novel treatment options that improve clinical outcomes.

Areas covered: This review covers P2Y₁₂R antagonists reported in patents issued in the online databases of the World Intellectual Property Organization and the European Patent Office from 2019 to 2024. This review introduces the development of existing antagonists and evaluates the therapeutic potential of these compounds.

Expert opinion: Reversible P2Y₁₂R antagonists offer a potentially safer alternative to the currently dominant irreversible antagonists on the market, as they allow for more controlled platelet inhibition and can reduce the toxicity and adverse effects associated with conventional drugs. Importantly, the integration of computational drug design and molecular docking studies in the discovery and optimization of P2Y₁₂R antagonists represents a significant advancement in precision medicine. This not only provides valuable structural scaffolds but also stimulates novel ideas for developing promising drugs that are both safe and efficacious.