2-chloroethyl-3-sarcosinamide-1-nitrosourea (SarCNU) is an alkylating chloroethylnitrosourea with antineoplastic activity. It is a selective cytotoxin that enters cells via the extraneuronal transporter for monoamine transmitters (EMT). Both in vitro and in vivo studies demonstrated that SarCNU was more effective than BCNU against human gliomas. Selectively accumulating in some tumor cells, SarCNU forms covalent linkages with nucleophilic centers in DNA, causing depurination, base pair miscoding, strand scission, and DNA-DNA cross-linking, which may result in cytotoxicity. SarCNU crosses the blood-brain-tumour-barrier and is taken orally. Phase II trial of SarCNU in malignant glioma revealed unexpected pulmonary toxicity. SarCNU was not FDA approved for orphan indication of malignant glioma.