sarmustine

Sarmustine (SarCNU) is an alkylating agent of the chloroethylnitrosourea class with antineoplastic activity. It selectively accumulates in some tumor cells and forms covalent linkages with nucleophilic centers in DNA. This leads to depurination, base pair miscoding, strand scission, and DNA-DNA cross-linking—mechanisms that result in cytotoxicity. Sarmustine is a small molecule that can cross the blood-brain-tumor barrier and has been investigated primarily for brain tumors (malignant glioma), colorectal cancer (recurrent or metastatic), and other solid tumors. It is administered orally and was found to be more effective than BCNU against human gliomas in preclinical studies but showed unexpected pulmonary toxicity during clinical trials[1][4][6].

Brand names

SarCNU

Other names

sarcnu2-chloroethyl-3-sarcosinamide-1-nitrosoureasarcosinamide chloroethyl nitrosoureaN-chlorothylnitrosourea sarcosinamide1-(carbamoylmethyl)-3-(2-chloroethyl)-1-methyl-3-nitrosourea