Thiotepa
- Atc Codes:L01AC01
- CAS Codes:52-24-4
- PHARMGKB ID:52-24-4
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Thio-Tepa; France: Thiotepa; Germany: Thiotepa; Italy: Thioplex; Latvia: Tiofosfamīds; Luxembourg: Ledertepa; Netherlands: Ledertepa; UK: Thiotepa.
North America
USA: Thiotepa.
Asia
Japan: Tespamin.
Drug combinations
Chemistry
Thiotepa: C~6~H~12~N~3~PS. Mw: 189.22. (1) Aziridine,1,1′,1»-phosphinothioylidynetris-; (2) Tris(1-aziridinyl)phosphine sulfide. CAS-52-24-4.
Pharmacologic Category
Antineoplastic Agents; Alkylating Agents. (ATC-Code: L01AC01).
Mechanism of action
Reacts with DNA phosphate groups to produce cross-linking of DNA strands leading to inhibition of DNA, RNA, and protein synthesis. It is presumed that aziridine rings open and react as nitrogen mustard. Reactivity enhanced at lower pH.
Therapeutic use
Treatment of superficial tumors of bladder. Palliative treatment of adenocarcinoma of breast or ovary. Lymphomas and sarcomas. Controlling intracavitary effusions caused by metastatic tumors. CNS leukemia/lymphoma, CNS metastases.
Pregnancy and lactiation implications
Animal studies demonstrated teratogenicity and fetal loss. There are no adequate, well-controlled studies in pregnant women. May cause harm if administered during pregnancy. Enters breast milk (not recommended in nursing women).
Unlabeled use
Contraindications
Hypersensitivity to thiotepa or any component of the formulation. Pregnancy.
Warnings and precautions
May be mutagenic and teratogenic. Myelosuppression common (use with caution in bone marrow damage). Potentially carcinogenic (myelodysplastic syndromes and acute leukemias reported). Use with caution in hepatic and renal impairment.