M4112

M4112 is an oral, potent, and selective small molecule inhibitor that targets both indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase 2 (TDO2). By inhibiting these enzymes involved in tryptophan metabolism along the kynurenine pathway, M4112 has potential immunomodulating and antineoplastic activities. It was developed as a first-in-class dual IDO1/TDO2 inhibitor for the treatment of advanced solid tumors. Preclinical studies demonstrated its ability to decrease the kynurenine:tryptophan ratio in tumor models. In a phase I clinical trial in patients with advanced solid tumors (NCT03306420), M4112 showed initial target engagement but did not result in sustained reduction of plasma kynurenine levels at steady state. The drug was generally well tolerated with no serious safety concerns identified[1][2][3][4].