Identification

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Name
Triclabendazole
Accession Number
DB12245
Type
Small Molecule
Groups
Approved, Investigational
Description

Triclabendazole, manufactured by Novartis pharmaceuticals, is an antihelminthic drug that was approved by the FDA in February 2019 for the treatment of fascioliasis in humans.Label,4 Fascioliasis is a parasitic infection often caused by the helminth, Fasciola hepatica, which is also known as “the common liver fluke” or “the sheep liver fluke” or by Fasciola gigantica, another helminth. These parasites can infect humans following ingestion of larvae in contaminated water or food.

Triclabendazole was previously used in the treatment of fascioliasis in livestock, but is now approved for human use. This drug is currently the only FDA-approved drug for individuals with fascioliasis, which affects 2.4 million people worldwide.2,4

Structure
Thumb
Synonyms
  • Triclabendazole
External IDs
EGA230B / NVP-EGA230
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EgatenTablet250 mg/1OralNovartis Pharmaceuticals Corporation2019-02-13Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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International/Other Brands
Fasinex
Categories
UNII
4784C8E03O
CAS number
68786-66-3
Weight
Average: 359.65
Monoisotopic: 357.9501172
Chemical Formula
C14H9Cl3N2OS
InChI Key
NQPDXQQQCQDHHW-UHFFFAOYSA-N
InChI
InChI=1S/C14H9Cl3N2OS/c1-21-14-18-9-5-8(16)12(6-10(9)19-14)20-11-4-2-3-7(15)13(11)17/h2-6H,1H3,(H,18,19)
IUPAC Name
6-chloro-5-(2,3-dichlorophenoxy)-2-(methylsulfanyl)-1H-1,3-benzodiazole
SMILES
CSC1=NC2=C(N1)C=C(Cl)C(OC1=CC=CC(Cl)=C1Cl)=C2

Pharmacology

Indication

This drug is indicated for the treatment of fascioliasis in patients aged 6 years old and above.Label,4

Associated Conditions
Pharmacodynamics

Triclabendazole and its metabolites are active against both the immature and mature worms of Fasciola hepatica and Fasciola gigantica helminths.Label

Effect on QT interval

This drug may prolong the cardiac QT interval. Monitor ECG in patients with a history of QT prolongation or who are taking medications known to prolong the QT interval.Label

Mechanism of action

Triclabendazole is an anthelmintic agent against Fasciola species.Label

The mechanism of action against Fasciola species is not fully understood at this time. In vitro studies and animal studies suggest that triclabendazole and its active metabolites (sulfoxide and sulfone) are absorbed by the outer body covering of the immature and mature worms, causing a reduction in the resting membrane potential, the inhibition of tubulin function as well as protein and enzyme synthesis necessary for survival. These metabolic disturbances lead to an inhibition of motility, disruption of the worm outer surface, in addition to the inhibition of spermatogenesis and egg/embryonic cells.Label

A note on resistance

In vitro studies, in vivo studies, as well as case reports suggest a possibility for the development of resistance to triclabendazole. The mechanism of resistance may be multifactorial and include changes in drug uptake/efflux mechanisms, target molecules, and changes in drug metabolism. The clinical significance of triclabendazole resistance in humans is not yet elucidated.Label

TargetActionsOrganism
UExcretory Secretory (ES) proteins
inhibitor
Fasciola hepatica
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

After a single oral dose of 10 mg/kg triclabendazole with a 560-kcal meal to patients diagnosed with fascioliasis, mean peak plasma concentrations (Cmax) for triclabendazole, the sulfoxide, and sulfone metabolites were 1.16, 38.6, and 2.29 μmol/L, respectively. The area under the curve (AUC) for triclabendazole, the sulfoxide and sulfone metabolites were 5.72, 386, and 30.5 μmol∙h/L, respectively.Label

After the oral administration of a single dose of triclabendazole at 10 mg/kg with a 560 calorie meal to patients with fascioliasis, the median Tmax for the parent compound as well as the active sulfoxide metabolite was 3 to 4 hours.Label

Effect of Food Cmax and AUC of triclabendazole and sulfoxide metabolite increased about 2-3 times when triclabendazole was administered as a single dose at 10 mg/kg with a meal containing approximately 560 calories. Additionally, the sulfoxide metabolite Tmax increased from 2 hours in fasting subjects to 4 hours in fed subjects Label.

Volume of distribution

The apparent volume of distribution (Vd) of the sulfoxide metabolite in fed patients is about 1 L/kg.Label

Protein binding

Protein-binding of triclabendazole, sulfoxide metabolite and sulfone metabolite in human plasma was 96.7%, 98.4% and 98.8% respectively.Label

Metabolism

Based on in vitro studies, triclabendazole is mainly metabolized by CYP1A2 enzyme (approximately 64%) into its active sulfoxide metabolite and to a lesser extent by CYP2C9, CYP2C19, CYP2D6, CYP3A, and FMO (flavin containing monooxygenase). This sulfoxide metabolite is further metabolized mainly by CYP2C9 to the active sulfone metabolite, and to a smaller extent by CYP1A1, CYP1A2, CYP1B1, CYP2C19, CYP2D6, and CYP3A4, in vitro.Label

Route of elimination

No data regarding excretion is available in humans. In animals, triclabendazole is primarily excreted by the biliary tract in the feces (90%), together with the sulfoxide and sulfone metabolite. Less than 10% of an oral dose is found excreted in the urine.Label

Half life

The plasma elimination half-life (t1/2) of triclabendazole, the sulfoxide and sulfone metabolites in human is about 8, 14, and 11 hours, respectively.Label

Clearance
Not Available
Toxicity

Oral LD50 (rat): >8 gm/kg; Oral LD50 (mouse): >8 gm/kgMSDS

A note on the use in pregnancy

There are no available data on triclabendazole use in pregnant women to calculate a drug associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. Reproductive studies in animals (rat and rabbits) have not demonstrated an increased risk of increased fetal abnormalities with exposure to triclabendazole during the organogenesis period at doses which were about 0.3 to 1.6 times the maximum recommended human dose (MRHD) of 20 mg/kg.Label

Carcinogenesis/Mutagenesis

No genotoxic risk was noted for triclabendazole tested in 6 genotoxicity in vitro and in vivo assays.Label

Impairment of Fertility

No drug-related effects on reproductive performance, mating ratios or indices of fertility have been observed in a 2-generation reproductive and developmental toxicity study in rats.Label

A note on use in breastfeeding

There are no human findings on the presence of triclabendazole in milk, the effects on a nursing infant, or the effects on maternal milk production. The results of animal studies indicate that triclabendazole is found in goat milk when given as a single dose to a lactating female goat. When a drug is found to be present in animal milk, the likelihood that it will be found in human milk is high. Excercise caution if this drug is administered during nursing.Label

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Triclabendazole.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Triclabendazole.
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidineThe metabolism of Triclabendazole can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Triclabendazole.
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Triclabendazole.
5-methoxy-N,N-dimethyltryptamineThe metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Triclabendazole.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Triclabendazole.
8-azaguanineThe metabolism of 8-azaguanine can be decreased when combined with Triclabendazole.
8-chlorotheophyllineThe metabolism of 8-chlorotheophylline can be decreased when combined with Triclabendazole.
9-aminocamptothecinThe metabolism of 9-aminocamptothecin can be decreased when combined with Triclabendazole.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
Not Available

References

General References
  1. El-Tantawy WH, Salem HF, Mohammed Safwat NA: Effect of Fascioliasis on the pharmacokinetic parameters of triclabendazole in human subjects. Pharm World Sci. 2007 Jun;29(3):190-8. doi: 10.1007/s11096-006-9069-8. Epub 2007 Jan 30. [PubMed:17265093]
  2. Manouchehri Naeini K, Mohammad Nasiri F, Rokni MB, Kheiri S: Seroprevalence of Human Fascioliasis in Chaharmahal and Bakhtiyari Province, Southwestern Iran. Iran J Public Health. 2016 Jun;45(6):774-80. [PubMed:27648421]
  3. FDA Approves EGATEN (Triclabendazole) for Fascioliasis in Patients 6 Years of Age or Older [Link]
  4. Novartis receives FDA approval for Egaten® for the treatment of fascioliasis, a neglected tropical disease [Link]
External Links
KEGG Drug
D07364
PubChem Compound
50248
PubChem Substance
347828523
ChemSpider
45565
BindingDB
58491
ChEBI
94759
ChEMBL
CHEMBL1086440
Wikipedia
Triclabendazole
ATC Codes
P02BX04 — Triclabendazole
FDA label
Download (251 KB)
MSDS
Download (26.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
Not AvailableAvailableNot AvailableParasitic Diseases1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
TabletOral250 mg/1
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)189-191https://www.trc-canada.com/product-detail/?T773825
boiling point (°C)496http://sitem.herts.ac.uk/aeru/vsdb/Reports/1773.htm
water solubility1.0 mg/dLhttp://sitem.herts.ac.uk/aeru/vsdb/Reports/1773.htm
logP3.48http://helminto.inta.gob.ar/Fasciola/Alvarezetal.pdf
Predicted Properties
PropertyValueSource
Water Solubility0.000508 mg/mLALOGPS
logP5.5ALOGPS
logP5.88ChemAxon
logS-5.8ALOGPS
pKa (Strongest Acidic)10.46ChemAxon
pKa (Strongest Basic)4.54ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area37.91 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity87.86 m3·mol-1ChemAxon
Polarizability34.02 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-0002-0900000000-3fbd7829350b3af433e8
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-0002-0900000000-2fb79bfda8b99fe8585c
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-0002-0900000000-94c576ac00ee61093edc
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-0002-0900000000-d7b2f78bf0528ede0828
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-0002-0900000000-4e1a783d7691ad4bd8e6
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0a4i-0009000000-7f1cc56aaa6613e8fe57
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0a4i-0009000000-e6fec3ad89cc5d90283b
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0005-0936000000-920cfafffb0d59c0929a
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0002-0900000000-7c1864f299cbfbfaf0d4
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0002-1900000000-e79f0dad86cbb7cb4483
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0002-3900000000-79b4e72d8d6c11ae38cd
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-066r-9000000000-6ef46d3a6eaad77f377a
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-066r-9000000000-0143c04bcc788d3bacc1
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-066r-9000000000-ec03c59296086f67e89a
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0bt9-0019000000-8d8f52e04ea79bdcc664
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00dl-0396000000-bbdca10dffc2975f73b5
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00di-0390000000-19e15a4b196227bf4cd1
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-0009000000-1c6e57328ce0ce9875db
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-0009000000-4896d8b28bca85f865c8
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-0129000000-99f89b706bfbaa778d24
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00di-0393000000-56e5e0ba815538352227
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00di-0590000000-51b2132cbb0d623d35c7
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00di-0980000000-0003c9f1f8098a4b4b9e
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00fv-1920000000-b0c52a3ccb495f6bb434
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-004i-7900000000-e5becb861f440781a6ce
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-01t9-9400000000-01804ca8c80b2ce0ff18
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0bt9-0129000000-a88a1c1b435436e95170
MS/MS Spectrum - , positiveLC-MS/MSsplash10-006t-2698000000-e388e49687f3b4b05aed

Taxonomy

Description
This compound belongs to the class of organic compounds known as diarylethers. These are organic compounds containing the dialkyl ether functional group, with the formula ROR', where R and R' are aryl groups.
Kingdom
Organic compounds
Super Class
Organic oxygen compounds
Class
Organooxygen compounds
Sub Class
Ethers
Direct Parent
Diarylethers
Alternative Parents
Benzimidazoles / Phenoxy compounds / Phenol ethers / Dichlorobenzenes / Alkylarylthioethers / Aryl chlorides / Imidazoles / Heteroaromatic compounds / Sulfenyl compounds / Azacyclic compounds
show 4 more
Substituents
Diaryl ether / Benzimidazole / Phenoxy compound / Aryl thioether / Phenol ether / 1,2-dichlorobenzene / Alkylarylthioether / Chlorobenzene / Halobenzene / Aryl chloride
show 18 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein group
Organism
Fasciola hepatica
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
This is a possible target of this drug, but has not been confirmed.
General Function
Not Available
Specific Function
Protein domain specific binding

Components:
References
  1. Faridi A, Farahnak A, Golmohammadi T, Eshraghian M, Sharifi Y, Molaei Rad M: Triclabendazole (Anthelmintic Drug) Effects on the Excretory- Secretory Proteome of Fasciola hepatica in Two Dimension Electrophoresis Gel. Iran J Parasitol. 2014 Apr-Jun;9(2):202-8. [PubMed:25848386]
  2. FDA label, Egaten [File]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Giri P, Gupta L, Naidu S, Joshi V, Patel N, Giri S, Srinivas NR: In Vitro Drug-Drug Interaction Potential of Sulfoxide and/or Sulfone Metabolites of Albendazole, Triclabendazole , Aldicarb, Methiocarb, Montelukast and Ziprasidone. Drug Metab Lett. 2018;12(2):101-116. doi: 10.2174/1872312812666180816164626. [PubMed:30117405]
  2. Egaten FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Giri P, Gupta L, Naidu S, Joshi V, Patel N, Giri S, Srinivas NR: In Vitro Drug-Drug Interaction Potential of Sulfoxide and/or Sulfone Metabolites of Albendazole, Triclabendazole , Aldicarb, Methiocarb, Montelukast and Ziprasidone. Drug Metab Lett. 2018;12(2):101-116. doi: 10.2174/1872312812666180816164626. [PubMed:30117405]
  2. Egaten FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Giri P, Gupta L, Naidu S, Joshi V, Patel N, Giri S, Srinivas NR: In Vitro Drug-Drug Interaction Potential of Sulfoxide and/or Sulfone Metabolites of Albendazole, Triclabendazole , Aldicarb, Methiocarb, Montelukast and Ziprasidone. Drug Metab Lett. 2018;12(2):101-116. doi: 10.2174/1872312812666180816164626. [PubMed:30117405]
  2. Egaten FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d 24-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 un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. Egaten FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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 un...
Gene Name
CYP1B1
Uniprot ID
Q16678
Uniprot Name
Cytochrome P450 1B1
Molecular Weight
60845.33 Da
References
  1. Egaten FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Giri P, Gupta L, Naidu S, Joshi V, Patel N, Giri S, Srinivas NR: In Vitro Drug-Drug Interaction Potential of Sulfoxide and/or Sulfone Metabolites of Albendazole, Triclabendazole , Aldicarb, Methiocarb, Montelukast and Ziprasidone. Drug Metab Lett. 2018;12(2):101-116. doi: 10.2174/1872312812666180816164626. [PubMed:30117405]
  2. Egaten FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Egaten FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. Egaten FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
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 un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Giri P, Gupta L, Naidu S, Joshi V, Patel N, Giri S, Srinivas NR: In Vitro Drug-Drug Interaction Potential of Sulfoxide and/or Sulfone Metabolites of Albendazole, Triclabendazole , Aldicarb, Methiocarb, Montelukast and Ziprasidone. Drug Metab Lett. 2018;12(2):101-116. doi: 10.2174/1872312812666180816164626. [PubMed:30117405]
  2. Egaten FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
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 un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Egaten FDA label [File]

Drug created on October 20, 2016 15:42 / Updated on November 02, 2019 02:55