ZE66-0205

ZE66-0205 is a novel, orally bioavailable small molecule that functions as a targeted protein degrader of mucosa-associated lymphoid tissue lymphoma translocation 1 protein (MALT1). MALT1 is a key component of the CBM complex (CARD11, BCL10, and MALT1), which mediates B-cell receptor signaling and activates the NF-κB pathway—critical for survival in certain aggressive B-cell malignancies such as diffuse large B-cell lymphoma (DLBCL) and chronic lymphocytic leukemia (CLL). Unlike traditional allosteric inhibitors that only block the protease activity of MALT1, ZE66-0205 induces degradation of the entire MALT1 protein, thereby inhibiting both its scaffolding and protease functions. Preclinical studies have demonstrated potent in vitro and in vivo efficacy against DLBCL models—including those resistant to Bruton's tyrosine kinase inhibitors—by degrading CBM target proteins and suppressing downstream NF-κB signaling. The drug is being developed by Eilean Therapeutics for treatment of B-cell malignancies[1][2][3][4][5].

Other names

MALT1 degrader Eilean TherapeuticsMALT-1 degrader Eilean TherapeuticsMALT 1 degrader Eilean Therapeutics