andromustine

Andromustine is a cytostatic alkylating agent consisting of a conjugate between the nitrogen mustard chlorambucil and the androgen epiandrosterone. Developed by Kureha Corporation, it was primarily investigated for the treatment of breast cancer, particularly cases that are hormone-sensitive. The compound functions as a prodrug; once inside the target cells, it is believed to release chlorambucil, which then acts as a DNA alkylator. By forming interstrand and intrastrand cross-links in DNA, it interferes with replication and transcription, ultimately triggering apoptosis in rapidly dividing malignant cells. The incorporation of the epiandrosterone moiety was intended to enhance the uptake of the cytotoxic agent into androgen-receptor-expressing tissues, thereby improving the therapeutic index and reducing the systemic side effects typically associated with non-targeted alkylating agents.

Other names

Andro-chlorambucilEpiandrosterone chlorambucil ester3β-hydroxy-5α-androstan-17-one 3-(4-(bis(2-chloroethyl)amino)phenyl)butyrate