act-246475 and Acute-Coronary-Syndrome

Platelet P2Y. Selatogrel, formerly known as ACT-246475, is a novel, potent, reversible, and selective non-thienopyridine antagonist of the P2Y. Advantages of subcutaneous administration of selatogrel are fast onset of action, easy administration and the fecal excretion not requiring dose adjustment based on renal function. These characteristics may translate into an advantage in the peri-procedural setting and in emergency and/or unconscious patients. Selatogrel may represent a viable alternative to intravenous P2Y

Topics: Acute Coronary Syndrome; Animals; Drug Development; Humans; Injections, Subcutaneous; Organophosphonates; Percutaneous Coronary Intervention; Purinergic P2Y Receptor Antagonists; Pyrimidines; Thrombosis

The use of a P2Y12 inhibitor as a component of dual antiplatelet therapy in patients with an acute coronary syndrome (ACS) is well established. However, the P2Y12 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 P2Y12 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 P2Y12 inhibition.

Topics: Acute Coronary Syndrome; Adenosine Monophosphate; Humans; Organophosphonates; Percutaneous Coronary Intervention; Platelet Aggregation Inhibitors; Purinergic P2Y Receptor Antagonists; Pyrimidines

Topics: Acute Coronary Syndrome; Blood Platelets; Clinical Trials, Phase I as Topic; Clinical Trials, Phase II as Topic; Humans; Injections, Subcutaneous; Organophosphonates; Platelet Aggregation Inhibitors; Purinergic P2Y Receptor Antagonists; Pyrimidines