molecules of the month


selective KIT inhibitor

Ph I. for advanced GIST

HTS of ELF library (~450K cmpds) for sel. KITV654A inhibition

J. Med. Chem., February 2, 2023

Merck Healthcare KGaA, Darmstadt, DE

M4205, selective KIT inhibitor, Ph I. for advanced GIST, MERCK HEALTHCARE KGAA, DARMSTADT, DE
6 mins read

A KIT-selective, non-classical hinge binder-containing kinase inhibitor with best-in-class potential for the treatment of GIST. M4205 (IDRX-42) is a highly selective inhibitor of KIT, a class III receptor tyrosine kinase. KIT has been difficult to target effectively due to its high propensity for both mutations in the KIT gene, and secondary mutations within the ATP-binding pocket leading to 5% recurrence in primary disease and up to 90% recurrence for locally advanced disease. The molecule is another interesting example of selectivity being achieved with non-classical hinge binder with only one strong hydrogen-bonding interaction. M4205 is currently in a Ph. I FIH trial, with the intention to treat gastrointestinal stromal tumors (GISTs), one of the most common ​​mesenchymal neoplasms in the GI…

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