Oxazaphosphorine metabolites

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August undefined, 2024

WebThe active metabolites of cyclophosphamide are highly protein bound and distributed to all tissues, are assumed to cross the placenta and are known to be present in breast milk. … WebJan 1, 2005 · Oxazaphosphorine metabolism and transport have a major impact on pharmacokinetic variability, pharmacokinetic-pharmacodynamic relationship, toxicity, resistance, and drug interactions since the drug-metabolizing enzymes and drug transporters involved are key determinants of the pharmacokinetics and …

Mesna Tablets 400 mg - Summary of Product Characteristics (SmPC) - …

WebThe P450 metabolites of CPA and IFA, CA (formed by the N-dechloroethylation pathway) and acrolein (formed by the 4-hydroxylation pathway), were determined in parallel using a single incubation tube [27]. Incubations were carried out for 30 min in a total volume of 100 mL, and included 50 mM potassium phosphate buffer, pH 7.4, 0.1 WebNov 25, 2001 · The metabolism of oxazaphosphorines can be divided into three stages: activation, toxification, and deactivation. The initial activation is based on hydroxylation of the ring at C-4 by mixed function oxidases in the liver (cytochrome P-450) to give 4-hydroxyoxazaphosphorines. new england regional oireachtas

Oxazaphosphorines: New therapeutic strategies for an …

WebMafosfamide (4-thioethane sulfonic acid salt of 4-hydroxy-cyclophosphamide, MAF) belongs to a new generation of the oxazaphosphorine agents. MAF is a cyclophosphamide analog which spontaneously degrades to 4-hydroxy-cyclophosphamide. The effects of WebOxazaphosphorine metabolism and transport have a major impact on pharmacokinetic variability, pharmacokinetic-pharmacodynamic relationship, toxicity, resistance, and drug … WebThe active metabolites of cyclophosphamide are highly protein bound and distributed to all tissues, are assumed to cross the placenta and are known to be present in breast milk. [40] It is specifically in the oxazaphosphorine group of medications. [41] new england regional job fair mass.gov

Metabolism and transport of oxazaphosphorines and the clinical ...

Oxazaphosphorines: new therapeutic strategies for an old class ... - Pub…

http://www.bccancer.bc.ca/drug-database-site/Drug%20Index/Mesna_monograph_1Nov07.pdf WebMesna is a synthetic compound that protects the bladder from the urotoxic metabolites of oxazaphosphorine derivatives (e.g., ifosfamide, cyclophosphamide) by chemically interacting with them and their metabolites as a ... by 48% of the oxazaphosphorine dose PO at hour 3 and 7 Intravenous: N/A2,3,10 20% of the oxazaphosphorine dose at hour 0, 4, ... interpol washington budgetWebMay 1, 2002 · CAA, a byproduct of oxazaphosphorine metabolism, displayed appreciable cytotoxic activity in cell culture (EC 50 ϳ 2.5 M, compared with EC 50 values of 3-5 M for the 4-hydroxy derivatives of CPA ... new england regional student program

"WebOXAZAPHOSPHORINE METABOLISM BY THE HUMAN CYTOCHROME P450s AND SOME COMMONLY EXPRESSED P450 POLYMORPHIC VARIANTS by Diane M. Calinski A dissertation submitted in partial fulfillment of the requirements for the degree of Doctor of Philosophy (Pharmacology) in the University of Michigan 2013 Doctoral Committee: … " - Oxazaphosphorine metabolites

Oxazaphosphorine metabolites

Metabolism and transport of oxazaphosphorines and the

WebJul 1, 2004 · Oxazaphosphorine metabolism is affected by a number of factors associated with the drugs (e.g., dosage, route of administration, chirality, and drug combination) and patients (e.g., age, gender ... WebThe concentrations of the parent oxazaphosphorine and its principal metabolites were measured simultaneously in the plasma and CSF of 25 children. Twenty-one patients received CP for the treatment of either acute lymphoblastic leukemia, non-Hodgkin's lymphoma, or medulloblastoma, and 4 children received IF for the treatment of …

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WebSep 28, 2024 · In vitro, toxic acrolein is formed during the formation of the cytotoxic metabolite phosphoreamidemustard (PAM), whereas in vivo proapoptotic hydroxypropanal (HPA) is formed. The CP metabolites formed in sequence 4-hydroxycyclophosphamide (OHCP) are the main cause of toxicity, aldophosphamide (ALDO) is the pharmacologically … WebThe formation and rapid urinary excretion of conjugates of the activated (4-hydroxylated) oxazaphosphorine metabolites with mesna has been suggested as the pharmacological basis for the selective detoxification, but separation and identification of such metabolites in vivo have been extremely difficult due to their high polarity and chemical ...

Webthe oxazaphosphorine metabolites. After oral or intravenous administration, mesna undergoes rapid oxidation in the plasma to dimesna. Only a small portion of the dose remains in the circulation as the physiologically active compound. Both mesna and dimesna are very hydrophilic and therefore remain in the intravascular compartment, WebCyclophosphamide is an oxazaphosphorine that contributes alkyl groups to DNA, forming covalent linkages. It depletes T and B cells and suppresses antibody production. It is metabolized to 4-hydroxycyclophosphamide and its tautomer aldophosphamide by liver … Yanfeng Wang, Weiyang He, in The Liver, 2024. Introduction of mitochondria …

Webwhich is caused by oxazaphosphorine metabolites such as 4-hydroxy-cyclophosphamide, 4-hydroxy-ifosfamide or acrolein, is sometimes the dose-limiting toxicity of these cytostatics (Brock et al. 1979, 1981). Mesna (sodium 2-mercaptoethane sulfonate, Fig. 1), which shows low toxicity, very limited tissue transfer and WebOXAZAPHOSPHORINE METABOLISM BY THE HUMAN CYTOCHROME P450s AND SOME COMMONLY EXPRESSED P450 POLYMORPHIC VARIANTS by Diane M. Calinski A …

WebApr 1, 2015 · (Total dose = 160% (w/w) of the oxazaphosphorine dose). This larger dose is recommended in children, in patients whose urothelium may be damaged from previous …

WebMar 1, 2024 · On the basis of the discovery that the proapoptotic aldehyde 3-hydroxypropanal is a cyclophosphamide metabolite, a novel mechanism of action of oxazaphosphorine cytostatics is presented and ... interpol warning on computerWebJan 1, 1989 · Abstract. The development of the oxazaphosphorine cytostatics cyclophosphamide, ifosfamide, and trofosfamide was based on the idea of applying the transport form/active form principle to the highly reactive nitrogen mustard group. A critical analysis and synopsis of the available results and knowledge will include examination of … interpol warningWebThe metabolism of oxazaphosphorines is auto-inducible, with the activation of the orphan nuclear receptor pregnane X receptor (PXR) being the major mechanism. Oxazaphosphorine metabolism is affected by a number of factors associated with the drugs (e.g., dosage, route of administration, chirality, and drug combination) and patients (e.g., age ... interpol weaponsWebApr 1, 2012 · 2.1. Cytochrome P450. Prototypical oxazaphosphorine cytostatics such as CPA and IFO are chemically and pharmacologically inactive transport forms of alkylating nitrogen mustards that are biotransformed to their active forms predominantly in the liver 47; 48.As one of the key mechanisms of action, hepatic metabolism of CPA, has been … interpol warrant interpol west coast lyricsWebJul 1, 2005 · Oxazaphosphorine metabolism is affected by a number of factors associated with the drugs (e.g., dosage, route of administration, chirality, and drug combination) and patients (e.g., age, gender ... interpol warned fraudsters january 2021WebOxazaphosphorine metabolism and transport have a major impact on pharmacokinetic variability, pharmacokinetic-pharmacodynamic relationship, toxicity, resistance, and drug … interpol washington address