mezigdomide

Mezigdomide is an oral small molecule drug classified as a cereblon E3 ligase modulator (CELMoD). It acts by binding to cereblon (CRBN), the substrate recognition component of the CRL4–CRBN E3 ubiquitin ligase complex, thereby altering its conformation and recruiting novel protein substrates for selective proteasomal degradation. This leads to rapid and deep degradation of key lymphoid transcription factors, notably Ikaros family zinc finger protein 1 (IKZF1) and Ikaros family zinc finger protein 3 (IKZF3), which play critical roles in hematopoietic cell development and multiple myeloma pathobiology. The resulting effects include immunomodulation—such as T-cell activation—and antineoplastic activity through downregulation of proteins essential for cancer cell proliferation. Mezigdomide has demonstrated high potency in degrading these targets compared to other CELMoDs, even overcoming resistance due to cereblon down-regulation or mutation. It is being developed primarily for relapsed or refractory multiple myeloma, including patients previously treated with other immunomodulatory agents[1][2][4][5][6].

Other names

mezigdomideMezigdomide [USAN]2259648-80-9UNII-LA88IH4O02UNII-LA-88IH4O02UNII-LA 88IH4O02