Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C15H19N3O2 |
Molecular Weight | 273.3303 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)N1C(=O)NC(N[C@@H](C)C2=CC=CC=C2)=CC1=O
InChI
InChIKey=RLCLASQCAPXVLM-NSHDSACASA-N
InChI=1S/C15H19N3O2/c1-10(2)18-14(19)9-13(17-15(18)20)16-11(3)12-7-5-4-6-8-12/h4-11,16H,1-3H3,(H,17,20)/t11-/m0/s1
MYK-461 (also known as Mavacamten) is a small-molecule modulator of cardiac myosin that targets the underlying sarcomere hypercontractility of hypertrophic cardiomyopathy, one of the most prevalent heritable cardiovascular disorders. Studies on isolated cells and muscle fibers, as well as intact animals, have shown that MYK-461 inhibits sarcomere force production, thereby reducing cardiac contractility. In Phase II clinical trials MYK-461 reduces left ventricular outflow tract obstruction and improve exercise capacity and symptoms in patients with obstructive hypertrophic cardiomyopathy. Phase III clinical trials are currently ongoing.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: cardiac myosin ATPase Sources: https://www.ncbi.nlm.nih.gov/pubmed/26912705 |
0.3 µM [IC50] |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/31035291
10 to 20 mg/day
Route of Administration:
Oral
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FDA ORPHAN DRUG |
515015
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ACTIVE MOIETY