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Topic: CYP3A4

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	CYP3A4 - Wikipedia, the free encyclopedia
		CYP3A4 is involved in the oxidation of the largest range of substrates of all the CYPs.
		CYP3A4 is also, correspondingly, present in the largest quantity of all the CYPs in the liver.
		CYP3A4 is induced by a wide variety of ligands.
	en.wikipedia.org /wiki/CYP3A4 (478 words)

	A Simultaneous Assessment of CYP3A4 Metabolism and Induction in the DPX-2 Cell Line (Site not responding. Last check: 2007-10-30)
		CYP3A4 is a critical member of the CYP3A subfamily of cytochrome P450 enzymes and is involved in the metabolism of more than half of all currently used drugs.
		CYP3A4 is a highly inducible enzyme with modulators that belong to a chemically diverse group of compounds consisting of drugs, steroids, and various nutraceuticals including herbal preparations.
		CYP3A4 is involved in a significant number of drug-drug interactions leading to adverse drug reactions and toxicity stemming from alterations in activity and expression.
	www.aapsj.org /view.asp?art=aapsj070102 (3937 words)

	AEGiS-FDA: DESYREL (trazodone hydrochloride) and CYP3A4 Inhibitors - ketoconazole, ritonavir, and indinavir
		AEGiS-FDA: DESYREL (trazodone hydrochloride) and CYP3A4 Inhibitors - ketoconazole, ritonavir, and indinavir
		DESYREL (trazodone hydrochloride) and CYP3A4 Inhibitors - ketoconazole, ritonavir, and indinavir
		It is likely that CYP3A4 inhibitors may lead to substantial increases in trazodone plasma concentrations with the potential for adverse effects.
	www.aegis.com /news/fda/2004/FD040503.html (631 words)

	[No title]
		Since liver CYP3A4 activity appears to be rate limiting in the elimination of many drugs, knowledge that a NCE is metabolized by CYP3A4 may therefore imply that significant interpatient differences in elimination kinetics will be observed.
		However, it is not possible to extrapolate these observations made in vitro to the situations in vivo, in part because the concentration of drug attained at or within the liver cell during therapy is rarely known with certainty.
		CYP3A4 activity is estimated by the percentage of administered radiolabel exhaled in a single breath collection obtained just 20 minutes after injection of the test dose of erythromycin.
	www.metsol.com /ermbt_background.htm (782 words)

	Pharmacy Update, May-Jun 2003 (Site not responding. Last check: 2007-10-30)
		Aprepitant is a substrate, a moderate inhibitor, and an inducer of the microsomal cytochrome P450 CYP3A4 isoform; i.e., it may affect, and conversely, its pharmacokinetics may be affected by other drugs that are metabolized by CYP3A4.
		Therefore, concomitant administration of aprepitant with strong CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, ketoconazole, nefazodone, nelfinavir, troleandomycin, ritonavir, voriconazole) should be approached with caution.
		CYP3A4 is expressed on gastrointestinal epithelial cells as well as intrahepatically.
	www.cc.nih.gov /phar/updates/mayjune03/page6.html (710 words)

	Genomics\|HuGENet\|Reviews\|Breast, prostate cancer & CYP3A4\|PubMed ID: 15496535 (Site not responding. Last check: 2007-10-30)
		The CYP3A4 gene is expressed in the liver, gut, colon, prostate, and breast.
		CYP3A4 activity varies widely in humans, and more than 78 DNA sequence polymorphisms are known.
		CYP3A4 is associated with oxidative deactivation of testosterone and is responsible for regulation of testosterone’s metabolism to 2ß-, 6ß-, and 15ß-hydroxytestosterone, less biologically active forms of testosterone.
	www.cdc.gov /genomics/hugenet/reviews/CYP3A4.htm (4183 words)

	Using the Erythromycin Breath Test as a biomarker for CYP3A4 activity.
		CYP3A4 (cytochrome P450) is the major metabolic pathway taken by drugs in the human body.
		2) Is the NME an inhibitor or inducer of CYP3A4?
		Because CYP3A4 appears to have at least two distinct substrate binding sites, it is now recommended that two structurally different probes should be used in in vitro and in vivo inhibition studies.
	www.metsol.com /ermbt_biomarkerselection.htm (2647 words)

	RedOrbit - Health - Possible Involvement of Pregnane X Receptor-Enhanced CYP24 Expression in Drug-Induced Osteomalacia
		The relative induction potency of rifampicin, hyperforin, carbamazepine, and phenobarbital was identical for CYP3A4 and CYP24 genes: i.e., rifampicin > phenobarbital > hyperforin > carbamazepine.
		Radiolabeled CYP3A4 ER6 oligonucleotide (50,000 cpm) was incubated in the presence of PXR and RXRα proteins prepared by in vitro translation using a transcription-translation coupled system (lane 1).
		CYP3A4 induction by drugs: correlation between a pregnane X receptor reporter gene assay and CYP3A4 expression in human hepatocytes.
	www.redorbit.com /news/display?id=123028 (7842 words)

	[No title]
		May be harmful due to reduction in cerebral blood flow; may precipitate angina, myocardial infarction, or aggravate intermittent claudication; therefore, not considered a drug of choice in the elderly.
		Concomitant use with medications considered to be "potent" CYP3A4 inhibitors has been associated with acute ergot toxicity; use caution with medications considered "less potent" inhibitors of CYP3A4 enzymes.
		CYP3A4 enzyme inhibitors: Blood levels of ergot alkaloids may be increased leading to increased adverse effects.
	www.musc.edu /pharmacyservices/Drugs/E/Ergotamine.doc (292 words)

	CYP3A4 and VDR gene polymorphisms and the risk of prostate cancer in men with benign prostate hyperplasia
		CYP3A4 and VDR gene polymorphisms and the risk of prostate cancer in men with benign prostate hyperplasia
		The vitamin D receptor (VDR) and CYP3A4 have been shown to be involved in the regulation of cell proliferation and differentiation in prostate cells.
		The association between CYP3A4 and VDR TaqI SNPs and the risk of developing PRCa have been investigated in this study by determining the variant genotype frequencies of both SNPs in 400 patients with BPH who have been followed clinically for a median of 11 years.
	www.nature.com /bjc/journal/v88/n6/abs/6600825a.html (342 words)

	The Body: Clinically Significant Drug Interactions Associated With Highly Active Antiretroviral Therapy
		Efavirenz is a potent inducer of CYP3A4 in vivo.
		As a result of CYP3A4 inhibition, medication levels of agents also metabolized by the same izoenzyme have the potential to be markedly increased by the PI, potentially leading to an increased incidence of adverse effects.
		The most potent inhibitor of CYP3A4 is ritonavir, whereas the least potent is saquinavir; CYP3A4 inhibition associated with indinavir, nelfinavir, and amprenavir, and atazanavir tends to be intermediate.
	www.thebody.com /hepp/jan04/interactions.html?m35o (4284 words)

	Erowid.org: Erowid Reference 6371 : Involvement of CYP3A4, CYP2C8, and CYP2D6 in the metabolism of (R)- and ...
		Involvement of CYP3A4, CYP2C8, and CYP2D6 in the metabolism of (R)- and (S)-methadone in vitro
		Based on studies with isoform-selective chemical inhibitors and expressed enzymes, CYP3A4 was the predominant enzyme involved in the metabolism of (R)-methadone.
		In recombinant CYP3A4, the metabolic clearance of (R)-methadone was about 4-fold higher than that of (S)-methadone.
	www.erowid.org /references/refs_view.php?ID=6371 (307 words)

	Australian Adverse Drug Reactions Bulletin, Volume 19, Number 3, August 2000
		CYP3A4 is the most abundant cytochrome P450 enzyme in the liver and gut wall.
		Since CYP3A4 is the only major route of metabolism for indinavir, this study provides strong evidence that St John's wort induces CYP3A4.
		Simvastatin is a known substrate for CYP3A4 and nefazodone is both a substrate and an inhibitor of this isoenzyme.
	www.tga.gov.au /docs/html/aadrbltn/aadr0008.htm (1319 words)

	PharmGKB: CYP3A4 (Site not responding. Last check: 2007-10-30)
		Submitted by: Mary Relling, PharmD involving CYP3A, CYP3A4, CYP3A5, NR1I2,, midazolam, nifedipine, rifampin and troleandomycin.
		Submitted by: Mary Relling, PharmD involving ABCB1, CYP3A4, CYP3A5, GSTP1, UGT1A1, VDR, etoposide, and ALL (acute lymphoblastic leukemia).
		Submitted by: Mary Relling, PharmD involving CYP3A4, CYP3A5, NQO1, mercaptopurine, methotrexate, topoisomerase ii inhibitors,, Leukemia, Lymphocytic, Acute and therapy-related acute myeloid leukemia (t-ML).
	www.pharmgkb.org /do/serve?objId=PA130 (440 words)

	CYP3A4 - Cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 4 - Cancer GeneticsWeb
		CYP3A4; Cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 4
		Re: Modification of clinical presentation of prostate tumors by a novel genetic variant in CYP3A4.
		Modification of clinical presentation of prostate tumors by a novel genetic variant in CYP3A4.
	www.cancerindex.org /geneweb/CYP3A4.htm (260 words)

	Catalytic Characteristics of CYP3A4: Requirement for a Phenolic Function in ortho Hydroxylation of Estradiol and ...
		CYP3A4 is the major human cytochrome P-450 in a superfamily of heme-thiolate proteins that catalyze the oxidation of numerous lipophilic compounds.
		In this investigation, we report that CYP3A4 requires a phenolic function for ortho hydroxylation of estradiol and mono-O-demethylated methoxychlor and that CYP3A4 aromatic hydroxylation in general may be dependent on the presence of a free phenolic group.
		Thus, the disparities in aromatic hydroxylation rates between compounds containing phenolic hydroxyls and those with methoxyls cannot be explained by differences in their binding affinities.
	pubs.acs.org /cgi-bin/abstract.cgi/bichaw/1997/36/i08/abs/bi962129k.html (414 words)

	Expression of the Human CYP3A4 Gene in the Small Intestine of Transgenic Mice: In Vitro Metabolism and Pharmacokinetics ...
		CYP3A4 is the most abundant P450 isozyme present in human liver and small intestine, and contributes to the biotransformations
		CYP3A4 is a major P450 enzyme expressed in the liver and gastrointestinal tract and plays an important role in the metabolism
		Sata F, Sapone A, Elizondo G, Stocker P, Miller VP, Zheng W, Raunio H, Crespi CL and Gonzalez FJ (2000) CYP3A4 allelic variants with amino acid substitutions in exons 7 and 12: evidence for an allelic variant with altered catalytic activity.
	dmd.aspetjournals.org /cgi/content/full/31/5/548 (6570 words)

	Pharmacy Update, November/December 2001 (Site not responding. Last check: 2007-10-30)
		The CAR and PXR orphan nuclear receptors are primarily affected by drugs and, similar to CYP3A4 and P-gp, there appears to be considerable overlap of drugs affecting these receptors (48).
		This overlap obscures the specific contribution of inhibition of CYP3A4 and modulation of P-gp function to gastrointestinal site interactions.One exception is the P-gp substrate digoxin, a metabolite of the CYP3A4 substrate digitoxin, but not itself a substrate of this isoenzyme.
		However, not all drugs listed as CYP3A4 substrates or inhibitors have been evaluated with regard to their role as substrates or inhibitors of P-gp.
	www.cc.nih.gov /phar/updates/novdec01/page6-novdec01.html (919 words)

	Troglitazone Induces CYP3A4 Activity Leading to Falsely Abnormal Dexamethasone Suppression Test -- Dimaraki and Jaffe ...
		Dexamethasone is primarily metabolized by hepatic CYP3A4 (9),
		the activity of CYP3A4 (4, 12, 13, 14, 15).
		quantify the activity of CYP3A4 (23, 24, 25, 26, 27, 28).
	jcem.endojournals.org /cgi/content/full/88/7/3113 (2902 words)

	CYP3A4-V Polymorphism Detection by PCR-Restriction Fragment Length Polymorphism Analysis and Its Allelic Frequency ...
		the 5' regulatory region of the CYP3A4 gene (7)(8).
		CYP3A4 allelic variants with amino acid substitutions in exons 7 and 12: evidence for an allelic variant with altered catalytic activity.
		Characterization of an allelic variant in the nifedipine-specific element of CYP3A4: ethnic distribution and implications for prostate cancer risk.
	www.clinchem.org /cgi/content/full/46/11/1834 (1847 words)

	3rd International Workshop on Clinical Pharmacology of HIV Therapy - Dr. Gerber
		Nevirapine induces CYP3A4 and CYP2B6, and the antimycobacterial rifabutin induces CYP3A4.
		The CYP3A4 inducer efavirenz significantly lowered methadone concentrations in people on maintenance therapy and withdrawal symptoms were common [8].
		Methadone is not mainly metabolized by CYP3A4 because:
	www.drugabuse.gov /MeetSum/CPHTWorkshop/Gerber.html (1050 words)

	Drug Metabolism/Toxicology Models: chemical toxicity, heavy metal toxicity, CYP3A4 gene regulation, Cyp1a2-mediated ... (Site not responding. Last check: 2007-10-30)
		Injections of CYP3A4 inducers, such as dexamethasone, clotrimazole, phenobarbital, etc., resulted in a time-dependent induction of luciferase expression, primarily in liver, which peaked at 6 hours post injection.
		Injections of CYP3A4 inducers such as dexamethasone, clotrimazole, phenobarbital, etc., resulted in a time-dependent induction of luciferase expression, primarily in liver, that peaked at 12 hours post injection.
		The CYP3A4-luc RAT LPTA® animal model is useful in studying the kinetics of the CYP3A4 gene regulation by xenobiotics and CYP3A4-mediated drug-drug interactions in rats.
	www.xenogen.com /wt/page/animal_metabolism (1143 words)

	Cytochrome P450 CPY3A4 , monospecific, antibodies from Research Diagnostics Inc
		Antiserum was developed in rabbits using a 21 amino acid peptide corresponding to human CYP3A4 residues 253 to 273 as immunogen.
		Anti-human CYP3A4 IgG is provided as a powder after lyophylization from 100 mM potassium phosphate buffer (pH 7.4), 250 mM KCl, and 2.5 µM thimerosal (added as a preservative).
		Anti-human CYP3A4 peptide IgG reacts exclusively with its corresponding 51.5 kDa antigen and does not cross-react with either CYP3A5 or CYP3A7 in human liver microsomes.
	www.researchd.com /cyp450/cyp3a4m.htm (454 words)

	CYP3A4 and CYP3A5 Genotypes, Haplotypes, and Risk of Prostate Cancer -- Plummer et al. 12 (9): 928 -- Cancer ...
		CYP3A4 and CYP3A5 Genotypes, Haplotypes, and Risk of Prostate Cancer -- Plummer et al.
		and activity of the CYP3A4 enzyme (10, 11, 12, 13).
		The genotype and haplotype frequencies of the CYP3A4 and CYP3A5
	cebp.aacrjournals.org /cgi/content/full/12/9/928 (3404 words)

	Measurement of hepatic and intestinal CYP3A4 and PGP activity by combined po + iv [14C]erythromycin breath and urine ...
		Measurement of hepatic and intestinal CYP3A4 and PGP activity by combined po + iv [14C]erythromycin breath and urine test -- Lemahieu et al.
		is a probe for both CYP3A4 and PGP (1, 20).
		CYP3A4 and PGP activity and may be a reliable tool for dose
	ajpgi.physiology.org /cgi/content/full/285/3/G470 (5506 words)

	Texas Medicaid Vendor Drug Program, Cilostazol (Pletal®)
		Cilostazol is extensively metabolized by the CYP3A4 isoenzyme and, to a lesser extent, CYP2C19.
		Cilostazol is metabolized primarily by CYP3A4 isoenzymes and to a lesser extent, CYP2C19.
		Cilostazol is metabolized primarily by CYP3A4 and to a lesser extent, CYP2C19.
	www.hhsc.state.tx.us /HCF/vdp/Criteria/cilostaz.html (878 words)

	The Effect of an Individual's Cytochrome CYP3A4 Activity on Docetaxel Clearance -- Hirth et al. 6 (4): 1255 -- Clinical ...
		CYP3A4 activity, the ERMBT may be clinically useful in tailoring
		CYP3A4 (3, 4) and is therefore ideally suited for drugs given i.v.,
		CL in this study was hepatic CYP3A4 activity as measured by ERMBT.
	clincancerres.aacrjournals.org /cgi/content/full/6/4/1255 (3067 words)

	CYP3A4, CYP3A5, and CYP3A43 Genotypes and Haplotypes in the Etiology and Severity of Prostate Cancer -- Zeigler-Johnson ...
		CYP3A4, CYP3A5, and CYP3A43 Genotypes and Haplotypes in the Etiology and Severity of Prostate Cancer -- Zeigler-Johnson et al.
		CYP3A4, CYP3A5, and CYP3A43 Genotypes and Haplotypes in the Etiology and Severity of Prostate Cancer
		The CYP3A genes reside on chromosome 7q21 in a multigene cluster.
	cancerres.aacrjournals.org /cgi/content/full/64/22/8461 (4440 words)

	The Human Orphan Nuclear Receptor PXR Is Activated by Compounds That Regulate CYP3A4 Gene Expression and Cause Drug ...
		The cytochrome P-450 monooxygenase 3A4 (CYP3A4) is responsible for the oxidative metabolism of a wide variety of xenobiotics
		Expression of the CYP3A4 gene is markedly induced both in vivo and in primary hepatocytes in response to treatment with a
		CYP3A4 gene expression is induced in response to a remarkable array of xenobiotics including synthetic steroids (15-18), macrolide
	www.jci.org /cgi/content/full/102/5/1016 (5550 words)

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