Synonyms: CK-274 | CK-3773274 | CK3773274
Compound class:
Synthetic organic
Comment: Aficamten (CK-3773274) is an orally administered cardiac myosin inhibitor that was developed by Cytokinetics as a potential treatment for hypertrophic cardiomyopathies [1-3]. It was designed to reduce the hypercontractility of cardiac sarcomeres that is thought to drive hypertrophy and fibrosis in heart muscle, by binding directly to a distinct and selective allosteric binding site on cardiac myosin.
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References |
1. Alsulami K, Marston S. (2020)
Small Molecules acting on Myofilaments as Treatments for Heart and Skeletal Muscle Diseases. Int J Mol Sci, 21 (24). [PMID:33339418] |
2. Argirò A, Zampieri M, Berteotti M, Marchi A, Tassetti L, Zocchi C, Iannone L, Bacchi B, Cappelli F, Stefàno P et al.. (2021)
Emerging Medical Treatment for Hypertrophic Cardiomyopathy. J Clin Med, 10 (5). [PMID:33804412] |
3. Chuang C, Collibee S, Ashcraft L, Wang W, Vander Wal M, Wang X, Hwee DT, Wu Y, Wang J, Chin ER et al.. (2021)
Discovery of Aficamten (CK-274), a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy. J Med Chem, 64 (19): 14142-14152. [PMID:34606259] |