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Tauromustine (TCNU) is a **novel water-soluble nitrosourea derivative** based on the endogenous amino acid taurine. It functions as an **alkylating agent** and exhibits antineoplastic activity by inducing DNA cross-linking, which inhibits DNA and RNA synthesis, leading to cell death. TCNU was developed for **oral administration** and investigated primarily for refractory and advanced cancers, with initial studies reporting activity in colorectal cancer, melanoma, lung, renal, and stomach cancers. The drug’s dose-limiting toxicity is myelosuppression—most notably thrombocytopenia—and the most common side effects are gastrointestinal, specifically nausea and vomiting.
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