The radiomimetic action of thiotepa is believed to occur through the Chemistry, pharmacology and pharmacokinetics of N,N′,N ... but it remains unclear which pathway represents the precise mechanism of action. Thiotepa may cause fetal harm when administered to a pregnant woman, based on its mechanism of action and animal studies. It is chemically and pharmacologically related to nitrogen mustards. After administration, thiotepa converts into ethylenimine groups. ♦Thiotepa (thy-oh-tep'-ah) Triethylene, Thio-Tepa, TESPA, TSPA Pregnancy Category D Mechanism of Action An alkylating agent that alters DNA replication, RNA transcription, and nucleic acid formation, resulting in cell death. Indications Carcinoma of the bladder, ovaries, and breast; brain tumors; Hodgkin's disease; non-Hodgkin's lymphoma; lymphosarcoma; malignant effusions. Thiotepa is a polyfunctional, organophosphorus alkylating agent and a stable derivative of N,N',N''-triethylenephosphoramide (TEPA), with antineoplastic activity. Discuss the potential hazard to the fetus if thiotepa is used during pregnancy or if a patient becomes pregnant while taking this drug. What are the generic drug sources for thiotepa and what is the scope of freedom to operate?. Dactinomycin, also known as actinomycin D, is a chemotherapy medication used to treat a number of types of cancer. Thiotepa belongs to a class of drugs called alkylating agents. What is the mechanism of action? Alkylating agent that produces crosslinking of DNA strands by reacting with phosphate groups to inhibit protein synthesis, DNA, and RNA. The DNA damage caused by thiotepa results in cell death. ... What are the possible late side effects of treatment with thiotepa? Mechanism Of Action. The radiomimetic action of thiotepa is believed to occur through the release of ethylenimine radicals which, like irradiation, disrupt the bonds of DNA. The DNA damage caused by thiotepa results in cell death. 2. It is supplied as a non-pyrogenic, sterile lyophilized powder for intravenous, intracavitary or intravesical ... mechanism of action. In vivo and vitro studies show alkylation of DNA by Thiotepa and Tepa can follow two pathways, but it remains unclear which pathway represents the precise mechanism of action. N,N′,N″-triethylenethiophosphoramide (Thiotepa) and its oxo analogue (Tepa) as the major metabolite are trifunctional alkylating agents with a broad spectrum of antitumor activity. ♦Thiotepa (thy-oh-tep'-ah) Triethylene, Thio-Tepa, TESPA, TSPA Pregnancy Category D Mechanism of Action An alkylating agent that alters DNA replication, RNA transcription, and nucleic acid formation, resulting in cell death. 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. 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. MECHANISM OF ACTION: Thiotepa, a derivative of nitrogen mustard, acts as a polyfunctional alkylating agent. Limited available data with thiotepa use in pregnant women are insufficient to inform a drug-associated risk of major birth defects and miscarriage. Ethylenimine groups attaches with N7 position of guanine base pair of DNA; This will induce the cross linkages between the ds-DNA. 2.
Patients treated with thiotepa are at a slightly increased risk of developing a secondary malignancy. It has generally been replaced by cyclophosphamide … This will further interferes with the … Mechanism of Action: Description: Thiotepa is an ethyleneimine alkylating agent which interferes with DNA replication and transcription of RNA, resulting in the disruption of nucleic acid function. Thiotepa for Injection, USP DESCRIPTION Thiotepa for injection is an ethylenimine-type compound. Thiotepa is a cytotoxic agent of the polyfunctional type, related chemically and pharmacologically to the nitrogen mustard. What is the mechanism of action? The radiomimetic action of thiotepa is believed to occur through the release of ethylenimine radicals which, like irradiation, disrupt the bonds of DNA. It is also immunosupressive. Upon administration, thiotepa is converted into highly reactive ethylenimine groups, which covalently bind to nucleophilic groups in DNA and demonstrate a preference for the N7 position of guanine bases. In vivo and vitro studies show alkylation of DNA by Thiotepa and Tepa can follow two pathways, but it remains unclear which pathway represents the precise mechanism of action. Following systemic absorption of busulfan, carbonium ions are formed, resulting in DNA alkylation and DNA breaks and inhibition of DNA replication and RNA transcription. Thiotepa belongs to a class of drugs called alkylating agents. Alkylating agents produce their anti-cancer effects by causing a chemical reaction that damages the DNA in a cell.
Zhang J(1), Stevens MF, Bradshaw TD. How is thiotepa … Mechanism of Action. The aziridine ring opens after protonation of the ring nitrogen.
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