Aficamten Explained

Synonyms:	CK-274
Cas Number:	2364554-48-1
Pubchem:	139331495
Unii:	B1I77MH6K1
Chemspiderid:	114935503
Chembl:	4847050
Stdinchi:	1S/C18H19N5O2/c1-3-16-21-17(22-25-16)12-4-6-14-11(8-12)5-7-15(14)20-18(24)13-9-19-23(2)10-13/h4,6,8-10,15H,3,5,7H2,1-2H3,(H,20,24)/t15-/m1/s1
Stdinchikey:	IOVAZWDIRCRMTM-OAHLLOKOSA-N
Smiles:	CCC1=NC(=NO1)C2=CC3=C(C=C2)[C@@H](CC3)NC(=O)C4=CN(N=C4)C
Iupac Name:	N-[(1''R'')-5-(5-Ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1''H''-inden-1-yl]-1-methylpyrazole-4-carboxamide
C:	18
H:	19
N:	5
O:	2

Aficamten (CK-274) is a cardiac myosin inhibitor^[1] developed by Cytokinetics for the treatment of obstructive hypertrophic cardiomyopathy.^{[2] [3] [4]}

Notes and References

1. Chuang . Chihyuan . Collibee . Scott . Ashcraft . Luke . Wang . Wenyue . Vander Wal . Mark . Wang . Xiaolin . Hwee . Darren T. . Wu . Yangsong . Wang . Jingying . Chin . Eva R. . Cremin . Peadar . Zamora . Jeanelle . Hartman . James . Schaletzky . Julia . Wehri . Eddie . Robertson . Laura A. . Malik . Fady I. . Morgan . Bradley P. . Discovery of Aficamten (CK-274), a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy . Journal of Medicinal Chemistry . 14 October 2021 . 64 . 19 . 14142–14152 . 10.1021/acs.jmedchem.1c01290 . 34606259 . 238355647 . en . 0022-2623. free .
2. Zhao . Xue . Liu . Hongzhong . Tian . Wei . Fang . Ligang . Yu . Mengyang . Wu . Xiaofei . Liu . Aijing . Wan . Ruijie . Li . Li . Luo . Jinghui . Li . Yuqiong . Liu . Bo . He . Yu . Chen . Xiaowen . Li . Yuan . Xu . Donghong . Wang . Hongyun . Han . Xiaohong . Safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple doses of aficamten in healthy Chinese participants: a randomized, double-blind, placebo-controlled, phase 1 study . Frontiers in Pharmacology . 2023 . 14 . 10.3389/fphar.2023.1227470 . 37680714 . 10482267 . en . free .
3. Sebastian . Sneha Annie . Padda . Inderbir . Lehr . Eric J. . Johal . Gurpreet . Aficamten: A Breakthrough Therapy for Symptomatic Obstructive Hypertrophic Cardiomyopathy . American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions . September 2023 . 23 . 5 . 519–532 . 10.1007/s40256-023-00599-0 . 37526885 . 260348901 . 1179-187X.
4. Maron . Martin S. . Masri . Ahmad . Choudhury . Lubna . Olivotto . Iacopo . Saberi . Sara . Wang . Andrew . Garcia-Pavia . Pablo . Lakdawala . Neal K. . Nagueh . Sherif F. . Rader . Florian . Tower-Rader . Albree . Turer . Aslan T. . Coats . Caroline . Fifer . Michael A. . Owens . Anjali . Solomon . Scott D. . Watkins . Hugh . Barriales-Villa . Roberto . Kramer . Christopher M. . Wong . Timothy C. . Paige . Sharon L. . Heitner . Stephen B. . Kupfer . Stuart . Malik . Fady I. . Meng . Lisa . Wohltman . Amy . Abraham . Theodore . Phase 2 Study of Aficamten in Patients With Obstructive Hypertrophic Cardiomyopathy . Journal of the American College of Cardiology . January 2023 . 81 . 1 . 34–45 . 10.1016/j.jacc.2022.10.020. 36599608 . 255472935 . free . 2158/1295661 . free .