Harmsen, S.; Meijerman, I.; Beijnen, J. H.; Schellens, J. H. M. published the artcile< Nuclear receptor mediated induction of cytochrome P450 3A4 by anticancer drugs: a key role for the pregnane X receptor>, Name: 2-(Bis(2-chloroethyl)amino)-1,3,2-oxazaphosphinane 2-oxide hydrate, the main research area is pregnane X receptor cytochrome P450 3A4 colon adenocarcinoma anticancer.
Induction of cytochrome P 450 (CYP) 3A4, an enzyme that is involved in the biotransformation of more than 50% of all drugs, by xenobiotics is an important cause of pharmacokinetic drug-drug interactions in oncol. In addition to rifampicin and hyperforin, the anticancer drug paclitaxel has also been shown to be an inducer of CYP3A4 via activation of the pregnane X receptor (PXR). We therefore screened 18 widely used anticancer drugs for their ability to activate PXR-mediated CYP3A4 induction. A CYP3A4 reporter gene assay was employed to identify PXR agonists among the eighteen anticancer drugs. Subsequently CYP3A4 mRNA and protein expression following treatment with these PXR agonists was assessed. Finally, the effect of pre-treatment with these agents on the 1′-hydroxylation of midazolam (a specific CYP3A4 probe) was determined Paclitaxel, erlotinib, tamoxifen, ifosfamide, flutamide and docetaxel are able to activate PXR, while only strong PXR activation leads to significant induction of CYP3A4 activity. The identified PXR agonists may have the propensity to cause clin. relevant drug-drug interactions as a result of CYP3A4 induction.
Cancer Chemotherapy and Pharmacology published new progress about Antitumor agents. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Name: 2-(Bis(2-chloroethyl)amino)-1,3,2-oxazaphosphinane 2-oxide hydrate.
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