molecules of the month

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…