|Drug class||Alkylating agent|
|Main uses||Cancer, pterygium.|
|Side effects||Low blood cells, graft-versus-host disease, blood in the urine, mucosal inflammation|
|Intravenous, intracavitary, intravesical|
|Metabolism||Liver (CYP2B, CYP3A)|
|Elimination half-life||1.5–4.1 hours|
6 hours for thiotepa
8 hours for TEPA
|Chemical and physical data|
|Molar mass||189.22 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Thiotepa, sold under the brand name Tepadina, is a medication primarily used to treat cancer. This includes bladder, breast, ovarian, and lymphoma. Such use; however, is not recommended by Scotland. Other uses include, as an eye drop, for pterygium.
Common side effects include low blood cells, graft-versus-host disease, blood in the urine, and mucosal inflammation. Other side effects may include further cancer and anaphylaxis. Use in pregnancy may harm the baby. It is an alkylating agent and works by giving cells that divide rapidly.
Thiotepa was approved for medical use in the United States in 1959. It was approved in Europe in 2010, though has been used for decades before this. In the United States it costs about 3,600 USD for 100 mg.
Thiotepa is used in combination with other chemotherapy agents to treat cancer. 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. These diseases include Hodgkin's disease and leukaemia. Thiotepa is also used with high-dose chemotherapy with HPCT support to treat certain solid tumors in adult and children.
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.
Thiotepa is given into the bladder for bladder cancer.
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]
It is an organophosphorus compound with the formula SP(NC2H4)3. It is an analog of N,N′,N′′-triethylenephosphoramide (TEPA), which contains tetrahedral phosphorus and is structurally akin to phosphate. It is manufactured by heating aziridine with thiophosphoryl chloride.
Thiotepa was developed by the American Cyanamid company in the early 1950s and reported to media outlets in 1953. In 1959, thiotepa was registered with the Food and Drug Administration (FDA) as a drug therapy for several solid cancers.
On January 29, 2007, the European Medicines Agency (EMA) designated thiotepa as an orphan drug. On April 2, 2007, the United States FDA designated thiotepa as a conditioning treatment for use prior to hematopoietic stem cell transplantation. Adienne Pharma & Biotech (Italy), the owner of thiotepa (Tepadina) applied for these designations.
Society and culture
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