Chemistry, pharmacology and pharmacokinetics of N,N',N' -triethylenethiophosphoramide (ThioTEPA)
| Autor: | M. J. van Maanen, C.J.M. Smeets, Jos H. Beijnen |
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| Rok vydání: | 2000 |
| Předmět: |
Drug
Chromatography Gas Magnetic Resonance Spectroscopy media_common.quotation_subject ThioTEPA Pharmacology law.invention Carboplatin Broad spectrum Urinary excretion Pharmacokinetics law Antineoplastic Combined Chemotherapy Protocols medicine Animals Humans Radiology Nuclear Medicine and imaging Antineoplastic Agents Alkylating Cyclophosphamide Biotransformation Chromatography High Pressure Liquid media_common Clinical pharmacology Molecular Structure business.industry General Medicine Alkylating Activity Oncology Mechanism of action medicine.symptom business Thiotepa medicine.drug |
| Zdroj: | Cancer treatment reviews. 26(4) |
| ISSN: | 0305-7372 |
| Popis: | N,N′,N′′ -triethylenethiophosphoramide (thioTEPA) is a trifunctional alkylating agent with a broad spectrum of antitumour activity developed in the 1950s. The drug is now experiencing renewed interest as it appears to be one of the most effective anticancer drugs in high dose regimens. Despite many years of experience with thioTEPA, pharmacologic data are incomplete and controversy remains with respect to the dose-dependent pharmacokinetics of thioTEPA. In recent years greater insight has been obtained into the metabolism of thioTEPA, but there is still a gap between the total urinary excretion of thioTEPA and metabolites and the alkylating activity. In vivo and in vitro studies show that alkylation of DNA by thioTEPA can follow two pathways, but it remains unclear which pathway represents the precise mechanism of action. The currently available sensitive analytical methods for thioTEPA and its metabolites can be used to elucidate the many questions that still exist even so many years after its introduction. An overview is given of the chemistry, pharmacology, clinical use and toxicity of thioTEPA as well as its pharmacokinetics and analytical methods for thioTEPA and its metabolites. |
| Databáze: | OpenAIRE |
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