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Identification
NameVoriconazole
Accession NumberDB00582  (APRD00543)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Voriconazole (Vfend®, Pfizer) is a triazole antifungal medication used to treat serious fungal infections. It is used to treat invasive fungal infections that are generally seen in patients who are immunocompromised. These include invasive candidiasis, invasive aspergillosis, and emerging fungal infections.

Structure
Thumb
Synonyms
(AlphaR,betas)-alpha-(2,4-difluorophenyl)-5-fluoro-beta-methyl-alpha(1H-1,2,4-triazol-1-ylmethyl)-4-pyrimidineethanol
(R-(R*,s*))-alpha-(2,4-difluorophenyl)-5-fluoro-beta-methyl-alpha-(1H-1,2,4-triazol-1-ylmethyl)-4-pyrimidineethanol
VCZ
Vfend
Voriconazol
Voriconazolum
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ach-voriconazoletablet50 mgoralAccord Healthcare IncNot applicableNot applicableCanada
Auro-voriconazoletablet200 mgoralAuro Pharma IncNot applicableNot applicableCanada
Auro-voriconazoletablet50 mgoralAuro Pharma IncNot applicableNot applicableCanada
Mylan-voriconazoletablet200 mgoralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Mylan-voriconazoletablet50 mgoralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Sandoz Voriconazoletablet50 mgoralSandoz Canada Incorporated2014-04-02Not applicableCanada
Sandoz Voriconazoletablet200 mgoralSandoz Canada Incorporated2014-04-02Not applicableCanada
Teva-voriconazoletablet200 mgoralTeva Canada Limited2014-03-31Not applicableCanada
Teva-voriconazoletablet50 mgoralTeva Canada Limited2014-03-31Not applicableCanada
Vfendpowder, for suspension40 mg/mLoralRoerig2003-03-282016-04-23Us
Vfendinjection, powder, lyophilized, for solution10 mg/mLintravenousRoerig2002-05-242016-04-23Us
Vfendtablet, film coated50 mg/1oralCardinal Health2002-05-242016-04-05Us
Vfendpowder for suspension3 goralPfizer Canada Inc2008-07-17Not applicableCanada
Vfendtablet, film coated200 mg/1oralCardinal Health2002-05-242016-04-05Us
Vfendinjection, powder, lyophilized, for solution10 mg/mLintravenousRoerig2012-10-242016-04-23Us
Vfendtablet200 mgoralPfizer Canada Inc2004-11-12Not applicableCanada
Vfendtablet, film coated200 mg/1oralRoerig2003-03-282016-04-23Us
Vfendtablet50 mgoralPfizer Canada Inc2004-11-12Not applicableCanada
Vfendtablet, film coated50 mg/1oralRoerig2003-03-282016-04-23Us
Vfend for Injectionpowder for solution200 mgintravenousPfizer Canada Inc2004-11-12Not applicableCanada
Voriconazolepowder, for suspension40 mg/mLoralGreenstone LLC2013-12-162016-04-05Us
Voriconazoletablet, film coated200 mg/1oralGreenstone LLC2002-05-012016-04-05Us
Voriconazoletablet, film coated50 mg/1oralGreenstone LLC2002-05-012016-04-05Us
Voriconazole for Injectionpowder for solution200 mgintravenousSandoz Canada Incorporated2014-04-30Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-voriconazoletablet50 mgoralApotex Inc2014-04-14Not applicableCanada
Apo-voriconazoletablet200 mgoralApotex Inc2014-04-14Not applicableCanada
Voriconazoletablet, film coated200 mg/1oralGlenmark Pharmaceuticals Inc., Usa2015-09-042016-04-05Us
Voriconazoletablet, film coated200 mg/1oralMajor Pharmaceuticals2015-03-252016-04-05Us
Voriconazoletablet, film coated50 mg/1oralTeva Pharmaceuticals USA Inc2012-06-012016-04-23Us
Voriconazoletablet, film coated50 mg/1oralGlenmark Pharmaceuticals Inc., Usa2015-09-042016-04-05Us
Voriconazoletablet, film coated200 mg/1oralSandoz Inc2011-12-122016-04-05Us
Voriconazoletablet, film coated50 mg/1oralAmerican Health Packaging2014-01-072016-04-05Us
Voriconazoletablet, film coated50 mg/1oralSandoz Inc2011-12-122016-04-05Us
Voriconazoletablet, film coated200 mg/1oralAmerican Health Packaging2012-05-012016-04-05Us
Voriconazoleinjection, powder, lyophilized, for solution10 mg/mLintravenousSandoz Inc2012-05-302016-04-05Us
Voriconazoletablet, film coated200 mg/1oralAv Kare, Inc.2016-02-252016-04-05Us
Voriconazoletablet, film coated200 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2011-12-122016-04-05Us
Voriconazolepowder, for suspension40 mg/mLoralMylan Pharmaceuticals Inc.2013-09-252016-04-23Us
Voriconazoletablet, film coated200 mg/1oralAurobindo Pharma Limited2016-01-222016-04-05Us
Voriconazoletablet, film coated200 mg/1oralCardinal Health2012-09-212016-04-05Us
Voriconazoletablet, film coated200 mg/1oralMylan Pharmaceuticals Inc.2011-02-152016-04-23Us
Voriconazoletablet, film coated200 mg/1oralMylan Institutional Inc.2011-08-082016-04-05Us
Voriconazoletablet, film coated50 mg/1oralMylan Pharmaceuticals Inc.2011-02-152016-04-23Us
Voriconazoletablet, film coated50 mg/1oralAurobindo Pharma Limited2016-01-222016-04-05Us
Voriconazoletablet, film coated50 mg/1oralMylan Institutional Inc.2011-08-082016-04-05Us
Voriconazoletablet, film coated200 mg/1oralTeva Pharmaceuticals USA Inc2012-06-012016-04-23Us
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIJFU09I87TR
CAS number137234-62-9
WeightAverage: 349.3105
Monoisotopic: 349.11504471
Chemical FormulaC16H14F3N5O
InChI KeyInChIKey=BCEHBSKCWLPMDN-MGPLVRAMSA-N
InChI
InChI=1S/C16H14F3N5O/c1-10(15-14(19)5-20-7-22-15)16(25,6-24-9-21-8-23-24)12-3-2-11(17)4-13(12)18/h2-5,7-10,25H,6H2,1H3/t10-,16+/m0/s1
IUPAC Name
(2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol
SMILES
C[C@@H](C1=NC=NC=C1F)[C@](O)(CN1C=NC=N1)C1=C(F)C=C(F)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpropylamines. These are compounds containing a phenylpropylamine moiety, which consists of a phenyl group substituted at the third carbon by an propan-1-amine.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylpropylamines
Direct ParentPhenylpropylamines
Alternative Parents
Substituents
  • Phenylpropylamine
  • Phenylpropane
  • Halopyrimidine
  • Halobenzene
  • Fluorobenzene
  • Pyrimidine
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • 1,2,4-triazole
  • Tertiary alcohol
  • Azole
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Aromatic alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Alcohol
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp.
PharmacodynamicsVoriconazole is a triazole antifungal agent indicated for use in the treatment of fungal infections including invasive aspergillosis, esophageal candidiasis, and serious fungal infections caused by Scedosporium apiospermum (asexual form of Pseudallescheria boydii) and Fusarium spp. including Fusarium solani. Fungal plasma membranes are similar to mammalian plasma membranes, differing in having the nonpolar sterol ergosterol, rather than cholesterol, as the principal sterol. Membrane sterols such as ergosterol provide structure, modulation of membrane fluidity, and possibly control of some physiologic events. Voriconazole effects the formation of the fungal plasma membrane by indirectly inhibiting the biosynthesis of ergosterol. This results in plasma membrane permeability changes and inhibition of growth.
Mechanism of actionVoriconazole binds and inhibits ergosterol synthesis by inhibiting CYP450-dependent 14-alpha sterol demethylase. The inhibition of 14-alpha sterol demethylase results in a depletion of ergosterol in fungal cell membrane.
Related Articles
AbsorptionThe oral bioavailability is estimated to be 96% (CV 13%).
Volume of distribution
  • 4.6 L/kg
Protein binding58%
Metabolism

Hepatic. The major metabolite of voriconazole is the N-oxide, which accounts for 72% of the circulating radiolabelled metabolites in plasma. Since this metabolite has minimal antifungal activity, it does not contribute to the overall efficacy of voriconazole.

SubstrateEnzymesProduct
Voriconazole
UK-121,265 (Voriconazole N-oxide)Details
Voriconazole
4-HydroxyvoriconazoleDetails
4-Hydroxyvoriconazole
Not Available
4-Hydroxyvoriconazole 4-O-glucuronideDetails
UK-121,265 (Voriconazole N-oxide)
Not Available
UK-51,060Details
UK-51,060
Not Available
UK-215,364Details
UK-215,364
Not Available
Voriconazole O-glucuronide derivative (1)Details
Route of eliminationVoriconazole is eliminated via hepatic metabolism with less than 2% of the dose excreted unchanged in the urine.
Half lifeNot Available
ClearanceNot Available
ToxicityThe minimum lethal oral dose in mice and rats was 300 mg/kg (equivalent to 4 and 7 times the recommended maintenance dose (RMD), based on body surface area). At this dose, clinical signs observed in both mice and rats included salivation, mydriasis, titubation (loss of balance while moving), depressed behavior, prostration, partially closed eyes, and dyspnea. Other signs in mice were convulsions, corneal opacification and swollen abdomen.
Affected organisms
  • Yeast and other fungi
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9958
Blood Brain Barrier+0.9047
Caco-2 permeable+0.7219
P-glycoprotein substrateSubstrate0.591
P-glycoprotein inhibitor INon-inhibitor0.6113
P-glycoprotein inhibitor IINon-inhibitor0.8195
Renal organic cation transporterNon-inhibitor0.5354
CYP450 2C9 substrateNon-substrate0.727
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.5792
CYP450 1A2 substrateNon-inhibitor0.7491
CYP450 2C9 inhibitorInhibitor0.5203
CYP450 2D6 inhibitorNon-inhibitor0.8315
CYP450 2C19 inhibitorInhibitor0.5784
CYP450 3A4 inhibitorNon-inhibitor0.7011
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6649
Ames testNon AMES toxic0.7019
CarcinogenicityNon-carcinogens0.776
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.3469 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8791
hERG inhibition (predictor II)Non-inhibitor0.6282
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
Packagers
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for solutionintravenous10 mg/mL
Powder for suspensionoral3 g
Powder, for suspensionoral40 mg/mL
Tabletoral200 mg
Tabletoral50 mg
Tablet, film coatedoral200 mg/1
Tablet, film coatedoral50 mg/1
Powder for solutionintravenous200 mg
Prices
Unit descriptionCostUnit
Vfend 40 mg/ml Suspension 75ml Bottle870.72USD bottle
Vfend iv 200 mg vial143.5USD vial
Vfend 200 mg tablet49.74USD tablet
Vfend 50 mg tablet12.43USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2035314 No2000-01-182011-01-30Canada
CA2295035 No2005-04-192018-06-02Canada
US5116844 No1992-08-112009-08-11Us
US5567817 No1996-05-242016-05-24Us
US6632803 No1998-06-022018-06-02Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point127-130 °CNot Available
water solubilityLowNot Available
logP1Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0978 mg/mLALOGPS
logP1.65ALOGPS
logP1.82ChemAxon
logS-3.5ALOGPS
pKa (Strongest Acidic)12.71ChemAxon
pKa (Strongest Basic)2.27ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area76.72 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity95.28 m3·mol-1ChemAxon
Polarizability30.54 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Venkataraman Sundaram, Venkata Bhaskara Rao Uppala, Surya Prabhakar Akundi, Venkateswarlu Muvva, Vijayawardhan Chitta, Alekhya Donthula, Manoj Ramesh Kharkar, Surya Narayana Devarakonda, Subba Reddy Peddireddy, “Process For Preparing Voriconazole.” U.S. Patent US20080194820, issued August 14, 2008.

US20080194820
General References
  1. Herbrecht R, Denning DW, Patterson TF, Bennett JE, Greene RE, Oestmann JW, Kern WV, Marr KA, Ribaud P, Lortholary O, Sylvester R, Rubin RH, Wingard JR, Stark P, Durand C, Caillot D, Thiel E, Chandrasekar PH, Hodges MR, Schlamm HT, Troke PF, de Pauw B: Voriconazole versus amphotericin B for primary therapy of invasive aspergillosis. N Engl J Med. 2002 Aug 8;347(6):408-15. [PubMed:12167683 ]
  2. Patterson TF, Boucher HW, Herbrecht R, Denning DW, Lortholary O, Ribaud P, Rubin RH, Wingard JR, DePauw B, Schlamm HT, Troke P, Bennett JE: Strategy of following voriconazole versus amphotericin B therapy with other licensed antifungal therapy for primary treatment of invasive aspergillosis: impact of other therapies on outcome. Clin Infect Dis. 2005 Nov 15;41(10):1448-52. Epub 2005 Oct 13. [PubMed:16231256 ]
  3. Kullberg BJ, Sobel JD, Ruhnke M, Pappas PG, Viscoli C, Rex JH, Cleary JD, Rubinstein E, Church LW, Brown JM, Schlamm HT, Oborska IT, Hilton F, Hodges MR: Voriconazole versus a regimen of amphotericin B followed by fluconazole for candidaemia in non-neutropenic patients: a randomised non-inferiority trial. Lancet. 2005 Oct 22-28;366(9495):1435-42. [PubMed:16243088 ]
  4. Ally R, Schurmann D, Kreisel W, Carosi G, Aguirrebengoa K, Dupont B, Hodges M, Troke P, Romero AJ: A randomized, double-blind, double-dummy, multicenter trial of voriconazole and fluconazole in the treatment of esophageal candidiasis in immunocompromised patients. Clin Infect Dis. 2001 Nov 1;33(9):1447-54. Epub 2001 Sep 26. [PubMed:11577374 ]
  5. Walsh TJ, Pappas P, Winston DJ, Lazarus HM, Petersen F, Raffalli J, Yanovich S, Stiff P, Greenberg R, Donowitz G, Schuster M, Reboli A, Wingard J, Arndt C, Reinhardt J, Hadley S, Finberg R, Laverdiere M, Perfect J, Garber G, Fioritoni G, Anaissie E, Lee J: Voriconazole compared with liposomal amphotericin B for empirical antifungal therapy in patients with neutropenia and persistent fever. N Engl J Med. 2002 Jan 24;346(4):225-34. [PubMed:11807146 ]
External Links
ATC CodesJ02AC03
AHFS Codes
  • 08:14.08
PDB EntriesNot Available
FDA labelDownload (321 KB)
MSDSDownload (57.2 KB)
Interactions
Drug Interactions
Drug
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Voriconazole.
ado-trastuzumab emtansineThe serum concentration of the active metabolites of ado-trastuzumab emtansine can be increased when ado-trastuzumab emtansine is used in combination with Voriconazole.
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Voriconazole.
AlmotriptanThe serum concentration of Almotriptan can be increased when it is combined with Voriconazole.
AlosetronThe serum concentration of Alosetron can be increased when it is combined with Voriconazole.
AmlodipineThe risk or severity of adverse effects can be increased when Voriconazole is combined with Amlodipine.
AmobarbitalThe serum concentration of Voriconazole can be decreased when it is combined with Amobarbital.
Amphotericin BThe therapeutic efficacy of Amphotericin B can be decreased when used in combination with Voriconazole.
AmrinoneThe risk or severity of adverse effects can be increased when Voriconazole is combined with Amrinone.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Voriconazole.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Voriconazole.
AstemizoleThe serum concentration of Astemizole can be increased when it is combined with Voriconazole.
AtazanavirThe serum concentration of Voriconazole can be decreased when it is combined with Atazanavir.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Voriconazole.
AvanafilThe serum concentration of Avanafil can be increased when it is combined with Voriconazole.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Voriconazole.
BarnidipineThe serum concentration of Barnidipine can be increased when it is combined with Voriconazole.
BedaquilineThe serum concentration of Bedaquiline can be increased when it is combined with Voriconazole.
BepridilThe risk or severity of adverse effects can be increased when Voriconazole is combined with Bepridil.
BoceprevirThe serum concentration of Voriconazole can be increased when it is combined with Boceprevir.
BortezomibThe serum concentration of Bortezomib can be increased when it is combined with Voriconazole.
BosentanThe serum concentration of Bosentan can be increased when it is combined with Voriconazole.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Voriconazole.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Voriconazole.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Voriconazole.
BrinzolamideThe serum concentration of Brinzolamide can be increased when it is combined with Voriconazole.
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Voriconazole.
BuspironeThe metabolism of Buspirone can be decreased when combined with Voriconazole.
BusulfanThe serum concentration of Busulfan can be increased when it is combined with Voriconazole.
ButabarbitalThe serum concentration of Voriconazole can be decreased when it is combined with Butabarbital.
ButethalThe serum concentration of Voriconazole can be decreased when it is combined with Butethal.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Voriconazole.
CabozantinibThe serum concentration of Cabozantinib can be increased when it is combined with Voriconazole.
CarbamazepineThe serum concentration of Voriconazole can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Voriconazole.
CeritinibThe serum concentration of Ceritinib can be increased when it is combined with Voriconazole.
ChloramphenicolThe serum concentration of Voriconazole can be increased when it is combined with Chloramphenicol.
ChlorotrianiseneThe metabolism of Chlorotrianisene can be decreased when combined with Voriconazole.
ChlorpropamideThe serum concentration of Chlorpropamide can be increased when it is combined with Voriconazole.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Voriconazole.
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Voriconazole.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Voriconazole.
ClopidogrelThe serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Voriconazole resulting in a loss in efficacy.
CobicistatThe serum concentration of Cobicistat can be increased when it is combined with Voriconazole.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Voriconazole.
ConivaptanThe metabolism of Conivaptan can be decreased when combined with Voriconazole.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Voriconazole.
CyclosporineThe metabolism of Cyclosporine can be decreased when combined with Voriconazole.
DabrafenibThe serum concentration of Voriconazole can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Daclatasvir can be increased when it is combined with Voriconazole.
DapoxetineThe serum concentration of Dapoxetine can be increased when it is combined with Voriconazole.
DarunavirThe serum concentration of Voriconazole can be decreased when it is combined with Darunavir.
DasatinibVoriconazole may increase the QTc-prolonging activities of Dasatinib.
DiclofenacThe serum concentration of Diclofenac can be increased when it is combined with Voriconazole.
DicoumarolThe serum concentration of Dicoumarol can be increased when it is combined with Voriconazole.
DidanosineDidanosine can cause a decrease in the absorption of Voriconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
DienogestThe serum concentration of Dienogest can be increased when it is combined with Voriconazole.
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Voriconazole.
DocetaxelThe metabolism of Docetaxel can be decreased when combined with Voriconazole.
DofetilideThe metabolism of Dofetilide can be decreased when combined with Voriconazole.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Voriconazole.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Voriconazole.
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Voriconazole.
DronedaroneThe serum concentration of Dronedarone can be increased when it is combined with Voriconazole.
DrospirenoneThe serum concentration of Drospirenone can be increased when it is combined with Voriconazole.
DutasterideThe serum concentration of Dutasteride can be increased when it is combined with Voriconazole.
EfavirenzThe serum concentration of Voriconazole can be decreased when it is combined with Efavirenz.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Voriconazole.
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Voriconazole.
ElvitegravirThe serum concentration of Elvitegravir can be increased when it is combined with Voriconazole.
EnzalutamideThe serum concentration of Enzalutamide can be increased when it is combined with Voriconazole.
EplerenoneThe serum concentration of Eplerenone can be increased when it is combined with Voriconazole.
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Voriconazole.
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Voriconazole.
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Voriconazole.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Voriconazole.
EsomeprazoleThe serum concentration of Esomeprazole can be increased when it is combined with Voriconazole.
EstazolamThe serum concentration of Estazolam can be increased when it is combined with Voriconazole.
EtizolamThe serum concentration of Etizolam can be increased when it is combined with Voriconazole.
EtonogestrelThe serum concentration of Etonogestrel can be increased when it is combined with Voriconazole.
EtravirineThe serum concentration of Etravirine can be increased when it is combined with Voriconazole.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Voriconazole.
FelodipineThe risk or severity of adverse effects can be increased when Voriconazole is combined with Felodipine.
FentanylThe serum concentration of Fentanyl can be increased when it is combined with Voriconazole.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Voriconazole.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Voriconazole.
FloxuridineThe metabolism of Voriconazole can be decreased when combined with Floxuridine.
FluconazoleThe serum concentration of Voriconazole can be increased when it is combined with Fluconazole.
FludrocortisoneThe serum concentration of Fludrocortisone can be increased when it is combined with Voriconazole.
FlunarizineThe risk or severity of adverse effects can be increased when Voriconazole is combined with Flunarizine.
FlunisolideThe serum concentration of Flunisolide can be increased when it is combined with Voriconazole.
Fluticasone PropionateThe serum concentration of Fluticasone Propionate can be increased when it is combined with Voriconazole.
FluvoxamineThe metabolism of Voriconazole can be decreased when combined with Fluvoxamine.
FosamprenavirThe serum concentration of the active metabolites of Fosamprenavir can be increased when Fosamprenavir is used in combination with Voriconazole.
FosphenytoinThe serum concentration of Voriconazole can be decreased when it is combined with Fosphenytoin.
GabapentinThe risk or severity of adverse effects can be increased when Voriconazole is combined with Gabapentin.
GliclazideThe serum concentration of Gliclazide can be increased when it is combined with Voriconazole.
GlimepirideThe serum concentration of Glimepiride can be increased when it is combined with Voriconazole.
GlipizideThe serum concentration of Glipizide can be increased when it is combined with Voriconazole.
GlyburideThe serum concentration of Glyburide can be increased when it is combined with Voriconazole.
GoserelinVoriconazole may increase the QTc-prolonging activities of Goserelin.
GuanfacineThe serum concentration of Guanfacine can be increased when it is combined with Voriconazole.
HalofantrineThe serum concentration of Halofantrine can be increased when it is combined with Voriconazole.
HeptabarbitalThe serum concentration of Voriconazole can be decreased when it is combined with Heptabarbital.
HexobarbitalThe serum concentration of Voriconazole can be decreased when it is combined with Hexobarbital.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Voriconazole.
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Voriconazole.
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Voriconazole.
IdelalisibThe serum concentration of Idelalisib can be increased when it is combined with Voriconazole.
IfosfamideThe serum concentration of the active metabolites of Ifosfamide can be reduced when Ifosfamide is used in combination with Voriconazole resulting in a loss in efficacy.
IloperidoneThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Voriconazole.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Voriconazole.
ImidafenacinThe serum concentration of Imidafenacin can be increased when it is combined with Voriconazole.
IrinotecanThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Voriconazole.
IsavuconazoniumThe serum concentration of the active metabolites of Isavuconazonium can be increased when Isavuconazonium is used in combination with Voriconazole.
IsradipineThe risk or severity of adverse effects can be increased when Voriconazole is combined with Isradipine.
IvabradineThe serum concentration of Ivabradine can be increased when it is combined with Voriconazole.
IvacaftorThe serum concentration of Ivacaftor can be increased when it is combined with Voriconazole.
IxabepiloneThe serum concentration of Ixabepilone can be increased when it is combined with Voriconazole.
LacosamideThe serum concentration of Lacosamide can be increased when it is combined with Voriconazole.
LamotrigineThe risk or severity of adverse effects can be increased when Voriconazole is combined with Lamotrigine.
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Voriconazole.
LapatinibThe serum concentration of Lapatinib can be increased when it is combined with Voriconazole.
LercanidipineThe serum concentration of Lercanidipine can be increased when it is combined with Voriconazole.
LeuprolideVoriconazole may increase the QTc-prolonging activities of Leuprolide.
LevobupivacaineThe serum concentration of Levobupivacaine can be increased when it is combined with Voriconazole.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Voriconazole.
LevonorgestrelThe serum concentration of Levonorgestrel can be increased when it is combined with Voriconazole.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Voriconazole.
LopinavirThe serum concentration of Voriconazole can be decreased when it is combined with Lopinavir.
LosartanThe metabolism of Losartan can be decreased when combined with Voriconazole.
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Voriconazole.
LuliconazoleThe serum concentration of Voriconazole can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Voriconazole can be decreased when it is combined with Lumacaftor.
LurasidoneThe serum concentration of Lurasidone can be increased when it is combined with Voriconazole.
MACITENTANThe serum concentration of MACITENTAN can be increased when it is combined with Voriconazole.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Voriconazole is combined with Magnesium Sulfate.
MaravirocThe serum concentration of Maraviroc can be increased when it is combined with Voriconazole.
Medroxyprogesterone AcetateThe serum concentration of Medroxyprogesterone Acetate can be increased when it is combined with Voriconazole.
MeloxicamThe serum concentration of Meloxicam can be increased when it is combined with Voriconazole.
MethadoneThe serum concentration of Methadone can be increased when it is combined with Voriconazole.
MethohexitalThe serum concentration of Voriconazole can be decreased when it is combined with Methohexital.
MethylergometrineThe serum concentration of Methylergometrine can be increased when it is combined with Voriconazole.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Voriconazole.
MifepristoneThe serum concentration of Mifepristone can be increased when it is combined with Voriconazole.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Voriconazole.
NelfinavirThe serum concentration of Nelfinavir can be increased when it is combined with Voriconazole.
NevirapineThe serum concentration of Voriconazole can be decreased when it is combined with Nevirapine.
NicardipineThe risk or severity of adverse effects can be increased when Voriconazole is combined with Nicardipine.
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Voriconazole.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Voriconazole.
NisoldipineThe serum concentration of Nisoldipine can be increased when it is combined with Voriconazole.
NitrendipineThe risk or severity of adverse effects can be increased when Voriconazole is combined with Nitrendipine.
NorethisteroneThe serum concentration of Norethindrone can be increased when it is combined with Voriconazole.
OlaparibThe serum concentration of Olaparib can be increased when it is combined with Voriconazole.
OmeprazoleThe serum concentration of Omeprazole can be increased when it is combined with Voriconazole.
OspemifeneThe serum concentration of Ospemifene can be increased when it is combined with Voriconazole.
OxybutyninThe serum concentration of Oxybutynin can be increased when it is combined with Voriconazole.
OxycodoneThe risk or severity of adverse effects can be increased when Voriconazole is combined with Oxycodone.
PalbociclibThe serum concentration of Palbociclib can be increased when it is combined with Voriconazole.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Voriconazole.
PantoprazoleThe serum concentration of Pantoprazole can be increased when it is combined with Voriconazole.
ParecoxibThe serum concentration of Parecoxib can be increased when it is combined with Voriconazole.
ParicalcitolThe serum concentration of Paricalcitol can be increased when it is combined with Voriconazole.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Voriconazole.
PentobarbitalThe serum concentration of Voriconazole can be decreased when it is combined with Pentobarbital.
PerhexilineThe risk or severity of adverse effects can be increased when Voriconazole is combined with Perhexiline.
PhenobarbitalThe serum concentration of Voriconazole can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Voriconazole.
PimecrolimusThe metabolism of Pimecrolimus can be decreased when combined with Voriconazole.
PimozideVoriconazole may increase the arrhythmogenic activities of Pimozide.
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Voriconazole.
PorfimerVoriconazole may increase the photosensitizing activities of Porfimer.
PranlukastThe serum concentration of Pranlukast can be increased when it is combined with Voriconazole.
PrasugrelThe serum concentration of the active metabolites of Prasugrel can be reduced when Prasugrel is used in combination with Voriconazole resulting in a loss in efficacy.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Voriconazole.
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Voriconazole.
PrenylamineThe risk or severity of adverse effects can be increased when Voriconazole is combined with Prenylamine.
PrimidoneThe serum concentration of Voriconazole can be decreased when it is combined with Primidone.
PropafenoneThe serum concentration of Propafenone can be increased when it is combined with Voriconazole.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Voriconazole.
QuinidineThe metabolism of Quinidine can be decreased when combined with Voriconazole.
RabeprazoleThe serum concentration of Rabeprazole can be increased when it is combined with Voriconazole.
RamelteonThe serum concentration of Ramelteon can be increased when it is combined with Voriconazole.
RanolazineThe metabolism of Ranolazine can be decreased when combined with Voriconazole.
RegorafenibThe serum concentration of Regorafenib can be increased when it is combined with Voriconazole.
RepaglinideThe serum concentration of Repaglinide can be increased when it is combined with Voriconazole.
RetapamulinThe serum concentration of Retapamulin can be increased when it is combined with Voriconazole.
RifabutinThe serum concentration of Rifabutin can be increased when it is combined with Voriconazole.
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Voriconazole.
RifapentineThe serum concentration of Rifapentine can be increased when it is combined with Voriconazole.
RilpivirineThe serum concentration of Rilpivirine can be increased when it is combined with Voriconazole.
RisedronateThe risk or severity of adverse effects can be increased when Voriconazole is combined with Risedronate.
RitonavirThe serum concentration of Voriconazole can be decreased when it is combined with Ritonavir.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Voriconazole.
RuxolitinibThe serum concentration of Ruxolitinib can be increased when it is combined with Voriconazole.
SalmeterolThe serum concentration of Salmeterol can be increased when it is combined with Voriconazole.
SaxagliptinThe serum concentration of Saxagliptin can be increased when it is combined with Voriconazole.
SecobarbitalThe serum concentration of Voriconazole can be decreased when it is combined with Secobarbital.
SildenafilThe metabolism of Sildenafil can be decreased when combined with Voriconazole.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Voriconazole.
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Voriconazole.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Voriconazole.
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Voriconazole.
SolifenacinThe metabolism of Solifenacin can be decreased when combined with Voriconazole.
SonidegibThe serum concentration of Sonidegib can be increased when it is combined with Voriconazole.
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Voriconazole.
St. John's WortThe serum concentration of Voriconazole can be decreased when it is combined with St. John's Wort.
SucralfateSucralfate can cause a decrease in the absorption of Voriconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
SulfisoxazoleThe metabolism of Voriconazole can be decreased when combined with Sulfisoxazole.
SunitinibThe metabolism of Sunitinib can be decreased when combined with Voriconazole.
SuvorexantThe serum concentration of Suvorexant can be increased when it is combined with Voriconazole.
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Voriconazole.
TadalafilThe serum concentration of Tadalafil can be increased when it is combined with Voriconazole.
TamsulosinThe serum concentration of Tamsulosin can be increased when it is combined with Voriconazole.
TasimelteonThe serum concentration of Tasimelteon can be increased when it is combined with Voriconazole.
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Voriconazole.
TerfenadineThe serum concentration of Terfenadine can be increased when it is combined with Voriconazole.
TicagrelorThe serum concentration of the active metabolites of Ticagrelor can be reduced when Ticagrelor is used in combination with Voriconazole resulting in a loss in efficacy.
TofacitinibThe serum concentration of Tofacitinib can be increased when it is combined with Voriconazole.
TolazamideThe serum concentration of Tolazamide can be increased when it is combined with Voriconazole.
TolterodineThe serum concentration of Tolterodine can be increased when it is combined with Voriconazole.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Voriconazole.
ToremifeneThe risk or severity of adverse effects can be increased when Voriconazole is combined with Toremifene.
TrabectedinThe serum concentration of Trabectedin can be increased when it is combined with Voriconazole.
TramadolThe serum concentration of Tramadol can be increased when it is combined with Voriconazole.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Voriconazole.
VardenafilThe serum concentration of Vardenafil can be increased when it is combined with Voriconazole.
VemurafenibThe serum concentration of Vemurafenib can be increased when it is combined with Voriconazole.
VenlafaxineThe risk or severity of adverse effects can be increased when Voriconazole is combined with Venlafaxine.
VerapamilThe risk or severity of adverse effects can be increased when Voriconazole is combined with Verapamil.
VerteporfinVoriconazole may increase the photosensitizing activities of Verteporfin.
VilazodoneThe serum concentration of Vilazodone can be increased when it is combined with Voriconazole.
VinblastineThe risk or severity of adverse effects can be increased when Voriconazole is combined with Vinblastine.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Voriconazole.
VindesineThe risk or severity of adverse effects can be increased when Voriconazole is combined with Vindesine.
VinorelbineThe risk or severity of adverse effects can be increased when Voriconazole is combined with Vinorelbine.
VorapaxarThe serum concentration of Vorapaxar can be increased when it is combined with Voriconazole.
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Voriconazole.
ZolpidemThe serum concentration of Zolpidem can be increased when it is combined with Voriconazole.
ZopicloneThe serum concentration of Zopiclone can be increased when it is combined with Voriconazole.
ZuclopenthixolThe serum concentration of Zuclopenthixol can be increased when it is combined with Voriconazole.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Yeast
Pharmacological action
yes
Actions
antagonistinhibitor
General Function:
Sterol 14-demethylase activity
Specific Function:
Catalyzes C14-demethylation of lanosterol which is critical for ergosterol biosynthesis. It transforms lanosterol into 4,4'-dimethyl cholesta-8,14,24-triene-3-beta-ol.
Gene Name:
ERG11
Uniprot ID:
P10613
Molecular Weight:
60674.965 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Morales IJ, Vohra PK, Puri V, Kottom TJ, Limper AH, Thomas CF Jr: Characterization of a lanosterol 14 alpha-demethylase from Pneumocystis carinii. Am J Respir Cell Mol Biol. 2003 Aug;29(2):232-8. Epub 2003 Feb 26. [PubMed:12606318 ]
  4. Sanguinetti M, Posteraro B, Fiori B, Ranno S, Torelli R, Fadda G: Mechanisms of azole resistance in clinical isolates of Candida glabrata collected during a hospital survey of antifungal resistance. Antimicrob Agents Chemother. 2005 Feb;49(2):668-79. [PubMed:15673750 ]
  5. Li X, Brown N, Chau AS, Lopez-Ribot JL, Ruesga MT, Quindos G, Mendrick CA, Hare RS, Loebenberg D, DiDomenico B, McNicholas PM: Changes in susceptibility to posaconazole in clinical isolates of Candida albicans. J Antimicrob Chemother. 2004 Jan;53(1):74-80. Epub 2003 Dec 4. [PubMed:14657086 ]
  6. Thompson GR 3rd, Lewis JS 2nd: Pharmacology and clinical use of voriconazole. Expert Opin Drug Metab Toxicol. 2010 Jan;6(1):83-94. doi: 10.1517/17425250903463878. [PubMed:19947892 ]
  7. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  8. Xu Y, Sheng C, Wang W, Che X, Cao Y, Dong G, Wang S, Ji H, Miao Z, Yao J, Zhang W: Structure-based rational design, synthesis and antifungal activity of oxime-containing azole derivatives. Bioorg Med Chem Lett. 2010 May 1;20(9):2942-5. doi: 10.1016/j.bmcl.2010.03.014. Epub 2010 Mar 7. [PubMed:20362444 ]
  9. Xu J, Cao Y, Zhang J, Yu S, Zou Y, Chai X, Wu Q, Zhang D, Jiang Y, Sun Q: Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives. Eur J Med Chem. 2011 Jul;46(7):3142-8. doi: 10.1016/j.ejmech.2011.02.042. Epub 2011 Feb 24. [PubMed:21420761 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Nadp binding
Specific Function:
This protein is involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. Form I catalyzes the N-oxygenation of secondary and tertiary amines.
Gene Name:
FMO1
Uniprot ID:
Q01740
Molecular Weight:
60310.285 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Trimethylamine monooxygenase activity
Specific Function:
Involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. It N-oxygenates primary aliphatic alkylamines as well as secondary and tertiary amines. Plays an important role in the metabolism of trimethylamine (TMA), via the production of TMA N-oxide (TMAO). Is also able to perform S-oxidation when acting on sulfide compounds (PubMed:9224773).
Gene Name:
FMO3
Uniprot ID:
P31513
Molecular Weight:
60032.975 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
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Drug created on June 13, 2005 07:24 / Updated on May 05, 2016 02:28