eragidomide

Eragidomide (CC-90009) is a novel, clinical-stage small molecule that acts as a cereblon (CRBN) E3 ligase modulator (CELMoD). It functions as a molecular glue, promoting the selective ubiquitination and proteasomal degradation of GSPT1 (G1 to S phase transition 1, also known as eRF3A), via recruitment to the CUL4-DDB1-CRBN-RBX1 E3 ubiquitin ligase complex. This targeted protein degradation leads to activation of the integrated stress response and induction of apoptosis in acute myeloid leukemia (AML) cells. Eragidomide has demonstrated potent antileukemic activity in preclinical models and is currently under investigation in phase I clinical trials for relapsed or refractory AML[2][3][5][6][8].

Other names

eragidomidecereblon modulator 1