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molecules of the month

reldesemtiv

second gen. oral troponin activator

Ph. III candidate for ALS (300 mg BID)

from HTS in muscle assay and reducing BP

Journal of Medicinal Chemistry

Cytokinetics, South San Francisco, CA

Chemical structure of molecule reldesemtiv
2 mins read

The Cytokinetics second generation troponin activator, reldesemtiv, is intended to treat muscle weakness by directly activating skeletal muscle. A high concentration of free drug is expected to be needed due to the large amount of fast skeletal muscle troponin in the body, making safety and selectivity critical. Reldesemtiv demonstrated robust activity in a Ph. I PD assessment of muscle response (with a maximum conc. reached at 4000 mg dose of 26 μM) and a reduction in decrease of ALSFRS-R scores in a Ph. II study for ALS patients with more advanced disease across all dose groups, supporting its advancement to a Ph. III trial despite the primary endpoint of slow upright vital capacity not being achieved. The molecule looks quite different from its…


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