Selatogrel: Potential to redefine timely anti‐platelet intervention

Acute coronary syndrome (ACS) encompasses a number of heart diseases that cause a sudden decrease in coronary perfusion, precipitating cardiomyocyte necrosis or heightened risk thereof. This pathology is a major burden of cardiovascular disease. The etiopathogenesis and clinical manifestation of ACS are predominantly attributable to myocardial hypoperfusion consequent, to coronary vessel occlusion, typically resulting from atherosclerotic plaque rupture and subsequent thrombosis. Dual antiplatelet therapy (DAPT), comprising aspirin and a P2Y<sub>12</sub> receptor antagonist, has long been the mainstay of ACS management. Notwithstanding, limitations in the pharmacokinetic (PK) and pharmacodynamic (PD) profiles of conventional DAPT agents persist. Selatogrel (ACT-246475), a novel P2Y<sub>12</sub> antagonist currently undergoing Phase III clinical trial, is poised to revolutionise ACS treatment. This highly selective and potent 2-phenylpyrimidine-4-carboxamide analogue is administered subcutaneously. As such, it affords immediate intervention in ACS patients. Importantly, selatogrel has a remarkably rapid onset of action and a favourable safety profile. These advantages render selatogrel a promising candidate for pre-hospital, self-administered ACS treatment, potentially optimising the reduction of total ischaemic time. Having successfully completed several Phase I and Phase II trials, selatogrel is currently undergoing Phase III evaluation to further elucidate its safety and efficacy. Subsequent investigations will serve to support or refine its therapeutic attributes.

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Publication Details

Journal
British Journal of Pharmacology
Published
2025-09-19
DOI
https://doi.org/10.1111/bph.70203
Citations
2
Primary Topic
Antiplatelet Therapy and Cardiovascular Diseases
Type
article
Field-Weighted Citation Impact
2.78
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article

Selatogrel: Potential to redefine timely anti‐platelet intervention

Ali H. Dakroub, Ali Hussein Eid, Philip A. Salem, Rudy N. Zalzal
2 citations
British Journal of Pharmacology
Antiplatelet Therapy and Cardiovascular Diseases
2.78
article

Selatogrel: Potential to redefine timely anti‐platelet intervention

Ali H. Dakroub, Ali Hussein Eid, Philip A. Salem, Rudy N. Zalzal
article en
2 citations

Abstract

Acute coronary syndrome (ACS) encompasses a number of heart diseases that cause a sudden decrease in coronary perfusion, precipitating cardiomyocyte necrosis or heightened risk thereof. This pathology is a major burden of cardiovascular disease. The etiopathogenesis and clinical manifestation of ACS are predominantly attributable to myocardial hypoperfusion consequent, to coronary vessel occlusion, typically resulting from atherosclerotic plaque rupture and subsequent thrombosis. Dual antiplatelet therapy (DAPT), comprising aspirin and a P2Y<sub>12</sub> receptor antagonist, has long been the mainstay of ACS management. Notwithstanding, limitations in the pharmacokinetic (PK) and pharmacodynamic (PD) profiles of conventional DAPT agents persist. Selatogrel (ACT-246475), a novel P2Y<sub>12</sub> antagonist currently undergoing Phase III clinical trial, is poised to revolutionise ACS treatment. This highly selective and potent 2-phenylpyrimidine-4-carboxamide analogue is administered subcutaneously. As such, it affords immediate intervention in ACS patients. Importantly, selatogrel has a remarkably rapid onset of action and a favourable safety profile. These advantages render selatogrel a promising candidate for pre-hospital, self-administered ACS treatment, potentially optimising the reduction of total ischaemic time. Having successfully completed several Phase I and Phase II trials, selatogrel is currently undergoing Phase III evaluation to further elucidate its safety and efficacy. Subsequent investigations will serve to support or refine its therapeutic attributes.

British Journal of PharmacologyVol. 182(22)
Cardiovascular Institute of the South (US), Mount Sinai Hospital (US), Qatar University (QA), American University of Beirut (LB), Icahn School of Medicine at Mount Sinai (US)
Openalex Percentile: Top 8%
Antiplatelet Therapy and Cardiovascular Diseases
2.78
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