Thiotepa (preferred international nonproprietary name)

Thiotepa is a synthetic small molecule alkylating agent used in cancer chemotherapy. It contains three reactive aziridine rings, allowing it to cross-link DNA by covalently attaching to nucleobases, thereby disrupting DNA replication and inducing apoptosis in rapidly dividing cells. It is primarily used as a cytostatic agent in the treatment of breast, ovarian, and bladder cancers, and as part of conditioning regimens for stem cell and bone marrow transplantation. The primary therapeutic target of thiotepa is DNA, not a protein or receptor, and its main toxicity is myelosuppression due to cytotoxic effects on bone marrow cells

Other names

N,N',N''-triethylenethiophosphoramideThiophosphamideThiophosphoramideTriethylenethiophosphoramideTriethylenethiophosphorotriamideTris(1-aziridinyl)phosphine sulfideThioplexTepadina®Tepylute®TEPATriaziridinylphosphine sulfide

Alkylation of DNA (introduces alkyl groups at the N7 position of guanine and other nucleobases, resulting in cross-linking and disruption of DNA replication and transcription)