2024 Oxazaphosphorine metabolites

Oxazaphosphorine metabolites

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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 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 ...

OXAZAPHOSPHORINE METABOLISM BY THE HUMAN …

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: … 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 … package gas electric units

Investigations on the pharmacokinetics of trofosfamide and its ...

WebOXAZAPHOSPHORINE METABOLISM BY THE HUMAN CYTOCHROME P450s AND SOME COMMONLY EXPRESSED P450 POLYMORPHIC VARIANTS by Diane M. Calinski A … 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. WebThat the oxazaphosphorines continue to be the subject of intensive investigation over 30 years after their introduction into clinical practice is partly because of their antitumour activity. The 2 most commonly used oxazaphosphorines are cyclophosphamide and ifosfamide, although other bifunctional mustard analogues continue to be investigated. … package games for ps

The anti-tumour activity of ifosfamide on heterotransplanted

Cyclophosphamide - Wikipedia

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 … WebApr 1, 2015 · 1. Name of the medicinal product 2. Qualitative and quantitative composition 3. Pharmaceutical form 4. Clinical particulars 5. Pharmacological properties 6. … package getaway dealsWebThe 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 jerry lawler health update

"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 … " - Oxazaphosphorine metabolites

Oxazaphosphorine metabolites

Oxazaphosphorine bioactivation and detoxification The role of ...

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, WebJan 11, 2013 · The oxazaphosphorine cyclophosphamide (CPA) and ifosfamide (IFO) are two commonly used DNAalkylating agents in cancer chemotherapy. This review highlights …

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WebMay 6, 2010 · Importance of the field: The oxazaphosphorines (cyclophosphamide, ifosfamide and trofosfamide) are widely used in clinical practice for their antitumor and … WebMay 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 ...

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 WebApr 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 …

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, ... 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]

WebMay 1, 2010 · The metabolism of oxazaphosphorines involves cytochrome P450 biotransformations, leading to highly reactive metabolites such as acrolein and …

WebJan 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 … jerry lawler deathWebJul 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 ... package gensymb warning not definingWebJul 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 ... package geometry latexWebDec 20, 1999 · 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 … package gdb-multiarch is not availableWebApr 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 … package geometry中 assembly_top层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. … jerry lawler heart attack on rawWebwhich 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 package gensymb warning: not defining micro