Selatogrel: A Novel Subcutaneous P2Y12 Inhibitor

P2Y12 医学 替卡格雷 坎格雷洛 不利影响 急性冠脉综合征 肠内给药 药理学 药代动力学 临床试验 重症监护医学 氯吡格雷 内科学 阿司匹林 心肌梗塞 肠外营养
作者
Craig J. Beavers,Samuel. Aaron Effoe,Paul P. Dobesh
出处
期刊:Journal of Cardiovascular Pharmacology [Lippincott Williams & Wilkins]
卷期号:79 (2): 161-167 被引量:9
标识
DOI:10.1097/fjc.0000000000001079
摘要

Abstract: The use of a P2Y 12 inhibitor as a component of dual antiplatelet therapy in patients with an acute coronary syndrome (ACS) is well established. However, the P2Y 12 inhibitors currently available have pharmacokinetic limitations due to delayed absorption, lack of enteral access for administration with oral formulations, need for intravenous access with cangrelor, or need for metabolization to be ideal in the critical 3-hour window during an ACS. Selatogrel is a novel, potent, reversible, and selective 2-phenylprimdine-4-carboxamide administered subcutaneously under development. Results from preclinical, phase 1, and phase 2 trials have confirmed that the agent provides sustained and reversible P2Y 12 platelet inhibition with an acceptable safety profile. The most commonly reported adverse effects include minor bleeding and dyspnea. Phase 3 trials are being designed to understand the critical role this agent can play in upstream management of patients with ACS including a more defined understanding of the adverse effect profile, how to transition from this agent to an oral agent, who will be administering, and does this agent allow for a safe and quick transition to coronary artery bypass graft surgery if needed. Should it obtain approval, selatogrel has the potential to provide a unique and advantageous mechanism for P2Y 12 inhibition.
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