Mavacamten CAS# 1642288-47-8 玛伐凯泰

Mavacamten (MYK-461) is a first-in-class, selective small-molecule inhibitor of cardiac myosin ATPase developed for hypertrophic cardiomyopathy. In preclinical studies, it reduced myosin-actin cross-bridge formation with an IC50 of ~0.3 µM, leading to decreased sarcomere contractility without affecting calcium transients. In isolated cardiomyocytes and engineered heart tissues, mavacamten dose-dependently lowered contractile force while preserving relaxation. In mouse models of hypertrophic cardiomyopathy, chronic administration reduced left ventricular hypertrophy, myocardial fibrosis, and improved diastolic function. Pharmacokinetic studies in animals showed good oral bioavailability and predictable exposure. These findings supported its therapeutic potential as a modulator of cardiac hypercontractility.