Aficamten

Catalog No: 25110

CAS Number: 2364554-48-1

Purity: 98% Min.

Aficamten, also known as CK-3773274 and CK-274, is a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy. Aficamten was designed to provide a predicted human half-life (t1/2) appropriate for once a day (qd) dosing, to reach steady state within two weeks, to have no substantial cytochrome P450 induction or inhibition, and to have a wide therapeutic window in vivo with a clear pharmacokinetic/pharmacodynamic relationship. In a phase I clinical trial, aficamten demonstrated a human t1/2 similar to predictions and was able to reach steady state concentration within the desired two-week window.

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Chemical Information

Name	Aficamten
Iupac Chemical Name	N-[(1R)-5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl]-1-methyl-1H-pyrazole-4-carboxamide
Synonyms	Aficamten; CK-3773274; CK3773274; CK 3773274; CK-274; CK274; CK 274;
Molecular Formula	C18H19N5O2
Molecular Weight	337.38
Smile	O=C(C1=CN(C)N=C1)N[C@@H]2CCC3=C2C=CC(C4=NOC(CC)=N4)=C3
InChiKey	IOVAZWDIRCRMTM-OAHLLOKOSA-N
InChi	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
CAS Number	2364554-48-1
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Formulation	Off-white solid
Purity	98% Min.
Storage	Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years).
Solubility	Soluble in DMSO
Handling
Shipping Condition	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
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Targets
Mechanism
Cell study
Animal study
Clinical study

1: Chuang C, Collibee S, Ashcraft L, Wang W, Vander Wal M, Wang X, Hwee DT, Wu Y, Wang J, Chin ER, Cremin P, Zamora J, Hartman J, Schaletzky J, Wehri E, Robertson LA, Malik FI, Morgan BP. Discovery of Aficamten (CK-274), a Next- Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy. J Med Chem. 2021 Oct 14;64(19):14142-14152. doi: 10.1021/acs.jmedchem.1c01290. Epub 2021 Oct 4. PMID: 34606259.

2: Lehman SJ, Crocini C, Leinwand LA. Targeting the sarcomere in inherited cardiomyopathies. Nat Rev Cardiol. 2022 Jun;19(6):353-363. doi: 10.1038/s41569-022-00682-0. Epub 2022 Mar 18. PMID: 35304599; PMCID: PMC9119933.

3: Maron MS, Masri A, Choudhury L, Olivotto I, Saberi S, Wang A, Garcia-Pavia P, Lakdawala NK, Nagueh SF, Rader F, Tower-Rader A, Turer AT, Coats C, Fifer MA, Owens A, Solomon SD, Watkins H, Barriales-Villa R, Kramer CM, Wong TC, Paige SL, Heitner SB, Kupfer S, Malik FI, Meng L, Wohltman A, Abraham T; REDWOOD-HCM Steering Committee and Investigators. Phase 2 Study of Aficamten in Patients With Obstructive Hypertrophic Cardiomyopathy. J Am Coll Cardiol. 2023 Jan 3;81(1):34-45. doi: 10.1016/j.jacc.2022.10.020. PMID: 36599608.

4: Kawana M, Spudich JA, Ruppel KM. Hypertrophic cardiomyopathy: Mutations to mechanisms to therapies. Front Physiol. 2022 Sep 26;13:975076. doi: 10.3389/fphys.2022.975076. Erratum in: Front Physiol. 2022 Dec 12;13:1111059. PMID: 36225299; PMCID: PMC9548533.

5: Morelli C, Ingrasciotta G, Jacoby D, Masri A, Olivotto I. Sarcomere protein modulation: The new frontier in cardiovascular medicine and beyond. Eur J Intern Med. 2022 Aug;102:1-7. doi: 10.1016/j.ejim.2022.04.020. Epub 2022 May 6. PMID: 35534374.

6: Masri A, Olivotto I. Cardiac Myosin Inhibitors as a Novel Treatment Option for Obstructive Hypertrophic Cardiomyopathy: Addressing the Core of the Matter. J Am Heart Assoc. 2022 May 3;11(9):e024656. doi: 10.1161/JAHA.121.024656. Epub 2022 May 3. PMID: 35502770; PMCID: PMC9238628.

7: Malik FI, Robertson LA, Armas DR, Robbie EP, Osmukhina A, Xu D, Li H, Solomon SD. A Phase 1 Dose-Escalation Study of the Cardiac Myosin Inhibitor Aficamten in Healthy Participants. JACC Basic Transl Sci. 2022 Aug 10;7(8):763-775. doi: 10.1016/j.jacbts.2022.04.008. PMID: 36061336; PMCID: PMC9436819.

8: Sharpe AN, Oldach MS, Rivas VN, Kaplan JL, Walker AL, Kovacs SL, Hwee DT, Cremin P, Morgan BP, Malik FI, Harris SP, Stern JA. Effects of Aficamten on cardiac contractility in a feline translational model of hypertrophic cardiomyopathy. Sci Rep. 2023 Jan 2;13(1):32. doi: 10.1038/s41598-022-26630-z. PMID: 36593243; PMCID: PMC9807554.

9: Mozzini C, Pagani M. THE HEART FAILURE KNIGHTS. Curr Probl Cardiol. 2023 May 25:101834. doi: 10.1016/j.cpcardiol.2023.101834. Epub ahead of print. PMID: 37244515.

10: Nair A, Xie L, Silva Enciso JE. Myosin Inhibitors: The Next Generation. J Am Coll Cardiol. 2023 Jan 3;81(1):46-48. doi: 10.1016/j.jacc.2022.10.018. PMID: 36599609.

11: Papp Z. Moderating the Myosin Motor to Treat Hypertrophic Cardiomyopathy. JACC Basic Transl Sci. 2022 Aug 22;7(8):776-778. doi: 10.1016/j.jacbts.2022.06.006. PMID: 36061334; PMCID: PMC9436807.

12: Sharpe AN, Oldach MS, Kaplan JL, Rivas V, Kovacs SL, Hwee DT, Morgan BP, Malik FI, Harris SP, Stern JA. Pharmacokinetics of a single dose of Aficamten (CK-274) on cardiac contractility in a A31P MYBPC3 hypertrophic cardiomyopathy cat model. J Vet Pharmacol Ther. 2023 Jan;46(1):52-61. doi: 10.1111/jvp.13103. Epub 2022 Nov 16. PMID: 36382714; PMCID: PMC10099566.

13: Mathai S, Williams L. Left ventricular outflow tract obstruction in hypertrophic cardiomyopathy and the impact of mavacamten. Ther Adv Chronic Dis. 2022 Nov 15;13:20406223221136074. doi: 10.1177/20406223221136074. PMID: 36407022; PMCID: PMC9666864.

14: Autore C, Bariani R, Bauce B, Biagini E, Canepa M, Castelletti S, Crotti L, Limongelli G, Merlo M, Monda E, Pio Loco Detto Gava C, Parisi V, Tini G, Imazio M. From the phenotype to precision medicine: an update on the cardiomyopathies diagnostic workflow. J Cardiovasc Med (Hagerstown). 2023 May 1;24(Suppl 2):e178-e186. doi: 10.2459/JCM.0000000000001424. PMID: 37186568.

15: Packard E, de Feria A, Peshin S, Reza N, Owens AT. Contemporary Therapies and Future Directions in the Management of Hypertrophic Cardiomyopathy. Cardiol Ther. 2022 Dec;11(4):491-507. doi: 10.1007/s40119-022-00283-5. Epub 2022 Oct 15. PMID: 36243823; PMCID: PMC9652179.

16: Altibi A, Alani A, Zhao Y, Masri A. Baseline and Longitudinal Imaging of Hypertrophic Cardiomyopathy in the Era of Emerging Therapeutics. Curr Cardiol Rep. 2023 Jun;25(6):583-595. doi: 10.1007/s11886-023-01883-w. Epub 2023 Apr 27. PMID: 37103749.

17: Rosenzveig A, Garg N, Rao SJ, Kanwal AK, Kanwal A, Aronow WS, Martinez MW. Current and emerging pharmacotherapy for the management of hypertrophic cardiomyopathy. Expert Opin Pharmacother. 2023 Jun 4:1-12. doi: 10.1080/14656566.2023.2219840. Epub ahead of print. PMID: 37272195.

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Aficamten

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