Yang SH, Lee MG (2008) Effects of CYP inducers and inhibitors on the ondansetron pharmacokinetics in rats: involvement of CYP2D subfamily and 3A1/2 for the ondansetron metabolism. J Pharm Pharmacol 60:853–861YANG SH,LEE MG.Effects of cytochrome P450(CYP)inducers and inhibitors on ondansetron...
表 1 实验所用探针底物,抑制剂,诱导剂 Table 1 Probe substrates, inhibitors and inducers used in this study CYP 酶 体外探针底物 名称 浓度/(μmol·L−1) 体外阳性抑制剂 名称 浓度/(μmol·L−1) 体外阳性诱导剂 名称 浓度/(μmol·L−1) 体内探针底物 名称 给药量/(mg·kg−1) CYP1A2...
Cytochrome P450 (CYP) enzymes are members of the hemoprotein superfamily, and are involved in the mono-oxygenation reactions of a wide range of endogenous and exogenous compounds in mammals and plants. Characterization of CYP genes in fish has been carried out intensively over the last 20 years....
In addition to drugs, humans are exposed to a large number of other chemical substances through diet, use of cosmetics, in workplaces, by environmental pollutants, etc., and many of these chemicals are in vitro inhibitors or inducers of CYP enzymes but compared to pharmaceutics often poorly cha...
This may enable the prediction of cytokine-mediated drug interactions with CYP substrates/inhibitors/inducers typically administered in intended patient populations, especially during later stages of drug development. The recently updated FDA guidance provides a risk-based approach to assess the need for ...
13 3 674 Archives of Toxicology (2020) 94:3671–3722 Table 1 Tyrosine (protein) kinase inhibitor anticancer drugs as CYP substrates, inhibitors, and inducers AnƟcancer Drug Abemaciclib (2017) TKI as a CYP substrate1 (vicƟm) Role of CYPs in TKI eliminaƟon M: 3A4 3 act....
To investigate the metabolic enzymes of the two compounds and the drug-drug interactions with enzyme inducers or inhibitors, a series of in vitro and in vivo experiments were conducted. In vitro studies using recombinant human cytochrome P450 enzyme demonstrated that cytochrome P450 3A4 (CYP3A4) ...
Cytochrome P450 Drug Interactions Table Use of this Table: • Definitions Substrates: drugs that are metabolized as substrates by the enzyme Inhibitors: drugs that prevent the enzyme from metabolizing the substrates Activators: drugs that increase the enzyme’s ability to metabolize the substrates ...
Drugs behave as substrates, inhibitors and inducers of human cytochrome P450 3A4. Curr Drug Metab 2008; 9: 310–22. 2 Guengerich FP. Cytochrome P450s and other enzymes in drug meta bolism and toxicity. AAPS J 2006; 8: 101–11. 3 Henderson CJ, Otto DM, Carrie D, Magnuson MA, ...
Enzyme phenotyping for the formation of ART-M (10β–hydroxyartemisinin) from artemisinin (ART; 1 µM) using human liver microsomes (HLM, 1 mg/mL) in the presence of (non)selective inhibitors of total P450 enzymes (1-ABT), CYP1A2 (α-naphthoflavone, NAPH), CYP2B6 (ticlopidine, TCL)...