Thiotepa (INN[6]), sold under the brand name Tepadina, is a medication used to treat cancer.[4][5][7]
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| Trade names | Tepadina | ||
| AHFS/Drugs.com | Monograph | ||
| MedlinePlus | a682821 | ||
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| Routes of administration | Intravenous, intracavitary, intravesical | ||
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| Metabolism | Liver (CYP2B6, CYP3A) | ||
| Elimination half-life | 1.5–4.1 hours | ||
| Excretion | Kidney 6 hours for thiotepa 8 hours for TEPA | ||
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| ECHA InfoCard | 100.000.124  | ||
| Chemical and physical data | |||
| Formula | C6H12N3PS | ||
| Molar mass | 189.22 g·mol−1 | ||
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Thiotepa is an organophosphorus compound with the formula (C2H4N)3PS.[8] It is an analogofN,N′,N″-triethylenephosphoramide (TEPA), which contains tetrahedral phosphorus and is structurally akin to phosphate. It is manufactured by heating aziridine with thiophosphoryl chloride.[citation needed]
Thiotepa is indicated for use in combination with other chemotherapy agents to treat cancer.[4][5][7] This can be with or without total body irradiation (TBI), as a conditioning treatment prior to allogeneic or autologous hematopoietic progenitor cell transplantation (HPCT) in hematological diseases in adults and children.[5][7] These diseases include Hodgkin's disease and leukaemia.[7] Thiotepa is also used with high-dose chemotherapy with HPCT support to treat certain solid tumors in adult and children.[5][7]
Thiotepa is used in the palliation of many neoplastic diseases. The best results are found in the treatment of adenocarcinoma of the breast, adenocarcinoma of the ovary, papillary thyroid cancer and bladder cancer. Thiotepa is used to control intracavitary effusions caused by serosal neoplastic deposits.[7]
Thiotepa is used as intravesical chemotherapy in bladder cancer.[9]
It may be used prophylactically to prevent seeding of tumor cells at cystoscopic biopsy; as an adjunctive agent at the time of biopsy; or as a therapeutic agent to prevent recurrence after cystoscopic resection of bladder tumor (transurethral resection of bladder tumor, TURBT).[medical citation needed] Efficacy in tumor control may reach 55%.[medical citation needed] The main toxicity of this therapy is bone marrow suppression due to systemic absorption of the drug.[medical citation needed]
The main side effect of thiotepa is bone marrow suppression resulting in leukopenia, thrombocytopenia and anemia.[10] Liver and lung toxicity may also occur.[medical citation needed]
Thiotepa was developed by the American Cyanamid company in the early 1950s and reported to media outlets in 1953.[11] In 1959, thiotepa was registered with the Food and Drug Administration (FDA) as a drug therapy for several solid cancers.[12]
In January 2007, the European Medicines Agency (EMA) designated thiotepa as an orphan drug. In April 2007, the United States FDA designated thiotepa as a conditioning treatment for use prior to hematopoietic stem cell transplantation.[13]
In 2024 The (FDA) approved the New Drug Application (NDA) for Tepylute, a ready-to-dilute formulation of thiotepa to treat breast and ovarian cancer.[14] [15]
