RODRIGO SOUZA
Biocatalysis and Organic Synthesis Group, Chemistry Institute, Federal University
of Rio de Janeiro, Rio de Janeiro, Brazils

This month we will present synthetic strategies towards the synthesis of mavacamten, used to treat obstructive hypertrophic cardiomyopathy by selective inhibition of cardiac myosin. Hypertrophic cardiomyopathy (HCM) is a condition in which the heart becomes thickened without an obvious cause, resulting in the heart being less able to pump blood effectively and also may cause electrical conduction problems.

Mavacamten is sold under the brand name Camzyos and was initially developed by MyoKardia, a California-based clinical-stage biopharmaceutical company discovering and developing targeted therapies for the treatment of serious cardiovascular diseases. In 2020, MyoKardia was acquired by Bristol Myers Squib for $13.1 billion, including the first-in-class mavacamten (formerly MYK-461) which is expected to achieve around $958 million in sales by 2025.

One strategy can be found over literature to the synthesis of mavacamten, starting from couplin ... ...