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1576 n/a Ensembl ENSG00000160868 n/a UniProt P08684 n/a RefSeq (mRNA) NM_001202855 NM_001202856 NM_001202857 NM_017460 n/a RefSeq (protein) NP_001189784 NP_059488 n/a Location (UCSC) Chr 7: 99.76 – 99.78 Mb n/a PubMed search n/a Wikidata View/Edit Human Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1.14.13.97) is an important enzyme in the body, mainly found in the liver and in the intestine ...
Many substrates for CYP3A4 are drugs with a narrow therapeutic index, such as amiodarone [10] or carbamazepine. [11] Because these drugs are metabolized by CYP3A4, the mean plasma levels of these drugs may increase because of enzyme inhibition or decrease because of enzyme induction.
CYP4F3 (leukotriene-B4 ω-hydroxylase 2) CYP5A1 (thromboxane-A synthase) CYP8A1 (prostacyclin synthase) See the list of steroid metabolism modulators instead for steroid/sterol-specific CYP450s, including: CYP7A1 (cholesterol 7α-hydroxylase) CYP7B1 (25-hydroxycholesterol 7α-hydroxylase) CYP8B1 (sterol 12α-hydroxylase)
Peak plasma concentration is reached in 2.5 to 4.1 hours. In vitro protein binding is over 99%. Axitinib is primarily metabolized in the liver by CYP3A4/5. 30-60% of the drug is excreted in faeces, and about 23% in urine. [31] Regorafenib is a pyridine derivative, but also a urea derivative and has therefore been covered in that section.
Examples of drugs metabolized by CYP3A4 are statins (used to lower cholesterol levels), benzodiazepines (used to treat anxiety and insomnia), calcium channel blockers (used to treat high blood pressure), etc. By measuring 6β-hydroxycortisol levels in clinical trials, researchers can assess whether certain drugs affect the activity CYP3A4 which ...
Drug metabolism is the metabolic breakdown of drugs by living organisms, usually through specialized enzymatic systems. More generally, xenobiotic metabolism (from the Greek xenos "stranger" and biotic "related to living beings") is the set of metabolic pathways that modify the chemical structure of xenobiotics, which are compounds foreign to an organism's normal biochemistry, such as any drug ...
Zafirlukast is an inhibitor of the hepatic drug-metabolizing enzyme cytochrome P450 family 3 subfamily A member 4 (CYP3A4). [1] Zafirlukast may increase the concentration of drugs that are metabolized through CYP3A4, such as the anticoagulant medication warfarin and the antiepileptic drugs phenytoin and carbamazepine .
Nefazodone has a short elimination half-life of about 2 to 4 hours. [2] Its metabolite hydroxynefazodone similarly has an elimination half-life of about 1.5 to 4 hours, whereas the elimination half-lives of triazoledione and mCPP are longer at around 18 hours and 4 to 8 hours, respectively. [ 2 ]