2019 Jun 20;25(1):30. doi: 10.1186/s10020-019-0098-x.Pharmgenomics Pers Med. Not inducible. Epub 2008 Oct 6.Selvaraj C, Dinesh DC, Panwar U, Abhirami R, Boura E, Singh SK.J Biomol Struct Dyn.
CYP2C9 is subject to induction by rifampin, phenobarbital, and dexamethasone, indicating the involvement of pregnane X receptor, constitutive androstane receptor and glucocorticoid receptor in the regulation of CYP2C9. The substrates of CYP3A4 considerably overlap with those of P-glycoprotein (P-gp).
Cytochrome P450 2C9 (CYP2C9) is one of the most abundant CYP enzymes in the human liver. This site needs JavaScript to work properly.
A small number of drugs such as rifampin, phenytoin and ritonavir are identified as inducers of CYP3A4. The inhibition or induction of CYP3A4 by drugs often causes unfavorable and long-lasting drug-drug interactions and probably fatal toxicity, depending on many factors associated with the enzyme, drugs and the patients. Data from the site-directed mutagenesis studies have revealed that a number of residues (e.g.
Curr Drug Metab. Unable to load your collection due to an error
2020 Jan;108(1):102-108. doi: 10.1007/s10266-019-00457-z. CYP2C9 also plays a role in the metabolism of several endogenous compounds such as steroids, melatonin, retinoids and arachidonic acid. Tienilic acid, suprofen and silybin are mechanism-based inhibitors of CYP2C9. A number of compounds have been found to inhibit CYP2C9 and this may provide an explanation for some clinically important drug interactions. An herbal ingredient used in non-prescription therapeutic products for the short-term treatment of minor skin irritations, insomnia, depression, and anxiety. Please enable it to take advantage of the complete set of features! The ability of drugs to act as inducers, inhibitors, or substrates for CYP3A is predictive of whether concurrent administration of these compounds with a known CYP3A substrate might lead to altered drug disposition, efficacy or toxicity.
Shu-Feng Zhou, “ Drugs Behave as Substrates, Inhibitors and Inducers of Human Cytochrome P450 3A4”, Current Drug Metabolism (2008) 9: 310. https://doi.org/10.2174/138920008784220664
2020 Jun 22:1-12. doi: 10.1080/07391102.2020.1778535. Clipboard, Search History, and several other advanced features are temporarily unavailable. The study of interactions of newly synthesized compounds with CYP3A4 has been incorporated into drug development and detection of possible CYP3A4 inhibitors and inducers during the early stages of drug development is critical in preventing potential drug-drug interactions and side effects.
A number of ligand-based and homology models of CYP2C9 have been reported and this has provided insights into the binding of ligands to the active site of CYP2C9.
Many of these drugs are also mechanism-based inhibitors of CYP3A4, which involves formation of reactive metabolites, binding to CYP3A4 and irreversible enzyme inactivation. Division of Chinese Medicine,School of Health Sciences, WHO Collaborating Center for TraditionalMedicine, RMIT University, Victoria, Australia., Australia A small number of drugs such as rifampin, phenytoin and ritonavir are identified as inducers of CYP3A4.
2011;18(5):667-713. doi: 10.2174/092986711794480131.Hutzler JM, Balogh LM, Zientek M, Kumar V, Tracy TS.Drug Metab Dispos. It exhibits polymorphism and there are extensive and poor metabolisers. Name must be less than 100 characters Given the critical role of CYP2C9 in drug metabolism and the presence of polymorphisms, it is important to identify drug candidates as potential substrates, inducer or inhibitors of CYP2C9 in drug development and drug discovery scientists should develop drugs with minimal interactions with this enzyme. Some natural and herbal …
Further studies are warranted to explore the molecular determinants for ligand-CYP2C9 binding and the structure-activity relationships. Our results allowed us to elucidate the molecular mechanism of previously observed, but unexplained, drug interactions involving CsA, and to detect drugs that should interfere with CsA metabolism as inducers or inhibitors.
A recent study indicates that CYP3A4 undergoes dramatic conformational changes upon binding to ketoconazole or erythromycin with a differential but substantial ( > 80%) increase in the active site volume, providing a structural basis for ligand promiscuity of CYP3A4.
A number of important drugs have been identified as substrates, inducers and/or inhibitors of CYP3A4. Unable to load your delegates due to an error
2009 Dec;10(10):1075-126. doi: 10.2174/138920009790820129.Curr Drug Metab.