Oxazaphosphorine metabolites
WebOxazaphosphorine metabolism and transport have a major impact on pharmacokinetic variability, pharmacokinetic-pharmacodynamic relationship, toxicity, resistance, and drug … 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 metabolites
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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 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, 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 … WebOxazaphosphorine metabolism and transport have a major impact on pharmacokinetic variability, pharmacokinetic-pharmacodynamic relationship, toxicity, resistance, and drug …
WebJan 11, 2013 · The oxazaphosphorine cyclophosphamide (CPA) and ifosfamide (IFO) are two commonly used DNAalkylating agents in cancer chemotherapy. This review highlights … 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 ...
WebMay 1, 2004 · Cyclophosphamide (CPA) and ifosfamide (IFA) are oxazaphosphorine anticancer prodrugs metabolized by two alternative cytochrome P450 (P450) pathways, drug activation by 4-hydroxylation and drug inactivation by N -dechloroethylation, which generates the neurotoxic and nephrotoxic byproduct chloroacetaldehyde.
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 ... induction first biologyWebMay 6, 2010 · Importance of the field: The oxazaphosphorines (cyclophosphamide, ifosfamide and trofosfamide) are widely used in clinical practice for their antitumor and … induction finite decending chainhttp://www.bccancer.bc.ca/drug-database-site/Drug%20Index/Mesna_monograph_1Nov07.pdf logan hagan welding supply statesboro gaWebMay 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 ... induction finite seriesWebJan 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 … induction fish kettleWebThat 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. … logan guthrie posingWebApr 1, 2015 · 1. Name of the medicinal product 2. Qualitative and quantitative composition 3. Pharmaceutical form 4. Clinical particulars 5. Pharmacological properties 6. … logan hair and spa by mlife