AIMZ-938

AIMZ-938 (also known as CEU-938) is a novel, preclinical-stage cytochrome P450 1A1 (CYP1A1)-dependent prodrug developed by Université Laval for the treatment of breast cancer. Chemically, it is a member of the phenyl 4-(2-oxo-3-alkylimidazolidin-1-yl)benzenesulfonate (PAIB-SO) class, specifically 3,5-dichlorophenyl 4-(2-oxo-3-pentylimidazolidin-1-yl)benzenesulfonate. AIMZ-938 is selectively bioactivated within CYP1A1-expressing breast cancer cells via N-dealkylation to release its highly cytotoxic active metabolite, CEU-700. CEU-700 acts as a potent antimitotic agent by binding to the colchicine-binding site on tubulin and disrupting microtubule dynamics, leading to G2/M cell-cycle arrest. This localized activation spares normal tissues that lack CYP1A1 expression, minimizing chemotherapy-associated systemic toxicities. Preclinical studies in mouse models have demonstrated that AIMZ-938 is well-tolerated, has a favorable half-life, and exhibits robust antitumor efficacy comparable to paclitaxel in breast cancer xenografts.

Other names

3,5-dichlorophenyl 4-(2-oxo-3-pentylimidazolidin-1-yl)benzenesulfonatephenyl 4-(2-oxo-3-alkylimidazolidin-1-yl)benzenesulfonate