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First developed in the 1950s, thiotepa is a highly toxic antineoplastic that is pharmacologically similar to nitrogen mustard and which has also been used as an insect sterilant. It has broad antitumor activity, with the most consistent results in the treatment of adenocarcinoma of the breast and ovary, as well as superficial tumors of the bladder and certain lymphomas. Due to its mechanism of action as a cytotoxic agent via alkylation of DNA bonds, it is highly toxic to dividing cells, most notably of the hematopoietic system. Thiotepa is mutagenic, an animal teratogen (Pregnancy Category D), and, according to the National Toxicology Program, a known human carcinogen (NTP, 2011).




Beilke, L. D. (2014). Thiotepa. In Encyclopedia of Toxicology: Third Edition (pp. 551–552). Elsevier.

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