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Chemical compound
Aficamten
![](https://upload.wikimedia.org/wikipedia/commons/thumb/d/d8/Aficamten.svg/220px-Aficamten.svg.png) |
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Other names | CK-274 |
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N-[(1R)-5-(5-Ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl]-1-methylpyrazole-4-carboxamide
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CID | |
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ChEMBL | |
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Formula | C18H19N5O2 |
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Molar mass | 337.383 g·mol−1 |
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3D model (
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CCC1=NC(=NO1)C2=CC3=C(C=C2)[C@@H](CC3)NC(=O)C4=CN(N=C4)C
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InChI=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 Key:IOVAZWDIRCRMTM-OAHLLOKOSA-N
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Aficamten (CK-274) is a cardiac
myosin inhibitor
[1] developed by Cytokinetics for the treatment of obstructive
hypertrophic cardiomyopathy.
[2]
[3]
[4]
References
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^ 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. (14 October 2021).
"Discovery of Aficamten (CK-274), a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy". Journal of Medicinal Chemistry. 64 (19): 14142–14152.
doi:
10.1021/acs.jmedchem.1c01290.
ISSN
0022-2623.
PMID
34606259.
S2CID
238355647.
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^ 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 (2023).
"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. 14.
doi:
10.3389/fphar.2023.1227470.
PMC
10482267.
PMID
37680714.
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^ Sebastian, Sneha Annie; Padda, Inderbir; Lehr, Eric J.; Johal, Gurpreet (September 2023).
"Aficamten: A Breakthrough Therapy for Symptomatic Obstructive Hypertrophic Cardiomyopathy". American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions. 23 (5): 519–532.
doi:
10.1007/s40256-023-00599-0.
ISSN
1179-187X.
PMID
37526885.
S2CID
260348901.
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^ 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 (January 2023).
"Phase 2 Study of Aficamten in Patients With Obstructive Hypertrophic Cardiomyopathy". Journal of the American College of Cardiology. 81 (1): 34–45.
doi:
10.1016/j.jacc.2022.10.020.
hdl:
2158/1295661.
PMID
36599608.
S2CID
255472935.