chlorozotocin

Chlorozotocin is a water-soluble chloroethyl nitrosourea derivative and an analog of streptozocin. As an alkylating agent, it functions by attaching alkyl groups to DNA, resulting in interstrand cross-links and DNA strand breaks that interfere with DNA replication and transcription, ultimately leading to cell death. It was specifically developed to incorporate a glucose moiety to enhance uptake by certain cells and potentially reduce myelosuppression compared to other nitrosoureas like carmustine (BCNU). While it demonstrated activity in preclinical models, clinical trials in various solid tumors, including colorectal cancer and melanoma, showed limited efficacy and significant side effects such as thrombocytopenia and renal toxicity (azotemia).

Other names

2-[3-(2-chloroethyl)-3-nitrosoureido]-2-deoxy-D-glucopyranoseChlorozotocine