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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 ...
[1] [17] [31] The weak CYP3A4 inhibitor ranitidine (150 mg) is predicted to increase overall exposure to daridorexant by 1.5-fold; the moderate CYP3A4 inhibitor diltiazem (240 mg) increased exposure to daridorexant by 2.4-fold; and the strong CYP3A4 inhibitor itraconazole, on the basis of physiologically-based pharmacokinetic modeling, would be ...
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.
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.
The drug is highly protein bound (>99%), and is metabolized in the liver by CYP3A4 and SULT2A1 to inactive metabolites. The drug is excreted in feces (~88%) and urine (~5%), and has a terminal half-life of 12 ± 5 hours.
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 ...
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. [1]