现在已经明确CsA在人体内主要由CYP450酶系中的CYP3A酶代谢,而P-gP则在CsA的吸收和分布中发挥重要作用。在肾移植受者中,携带CYP3A4 *1B(C392T,rs2740574),CYP3A5*3(A6986G,rs776746)突变体基因型患者代谢CsA的速率减慢,因此需降低用药剂量才能达到目标血药浓度。研究表明多个SNPs位点(C1236T,rs1128503;C3435...
The article reports that the manufacturer of trazodone hydrochloride, indicated for the symptomatic relief of depressive illness, has advised health care professionals of important safety information concerning drug ...
BACKGROUND: The integrase inhibitor elvitegravir (EVG) has been co-formulated with the CYP3A4 inhibitor cobicistat (COBI), emtricitabine (FTC), and tenofovir disoproxil fumarate (TDF) in a single tablet given once daily. We compared the efficacy ...
The plasma concentration of midazolam at 4 hours was also estimated as another phenotyping index for CYP3A4 activity. The simultaneous assay of all these analytes in a single matrix (plasma) will increase the feasibility of CYP phenotyping...
1. The importance of CYP3A enzymes in drug metabolism and toxicology has yielded a wealth of information on the structure, function and regulation of this subfamily and recent research emphasis has been placed on the human forms, namely CYP3A4, CYP3A...
CONCLUSION: Berberine has no influence on the activities of CYP3A4, CYP1A2 and CYP2C19 below 2 000 microg x L(-1), but can inhibit the activity of CYP2E1 and CYP2D6 in concentration-dependent.doi:10.5840/thought199065313Jaime Cas...
Endoxifen is the key active metabolite of tamoxifen, a widely used breast cancer drug. Orally administered tamoxifen, is extensively metabolized by cytochrome P450 (CYP) enzymes, namely CYP3A4 and CYP2D6, into active metab...
The compound inhibited CYP3A4 activity with an IC50 value of 45 μM, whereas the activity of CYP 1A2, 2C9 and 2D6 was not inhibited. In the Caco-2 model, P57 ex...
The CYP3A4 and 17OH-hydroxylase and 17,20 lyase activities of CYP17A1 are reduced but CYP19A1, CYP21A2 remain unaffected. We have performed detailed enzymatic and biochemical characterization of the A287P variant of POR to st...
Six cytochrome P450 (CYP) isoforms have been shown to hydroxylate vitamin D. Four of these, CYP27A1, CYP2R1, CYP3A4 and CYP2J3, are candidates for the enzyme vitamin D 25-hydroxylase that is inv...