Deutetrabenazine
Identification
- Summary
Deutetrabenazine is a vesicular monoamine transporter 2 inhibitor used for the symptomatic treatment of tardive dyskinesia and chorea associated with Huntington's disease.
- Brand Names
- Austedo
- Generic Name
- Deutetrabenazine
- DrugBank Accession Number
- DB12161
- Background
Deutetrabenazine is a novel, highly selective vesicular monoamine transporter 2 (VMAT2) inhibitor indicated for the management of chorea associated with Huntington’s disease. It is a hexahydro-dimethoxybenzoquinolizine derivative and a deuterated Tetrabenazine 5. The presence of deuterium in deutetrabenazine increases the half-lives of the active metabolite and prolongs their pharmacological activity by attenuating CYP2D6 metabolism of the compound 5. This allows less frequent dosing and a lower daily dose with improvement in tolerability 2. Decreased plasma fluctuations of deutetrabenazine due to attenuated metabolism may explain a lower incidence of adverse reactions associated with deutetrabenazine 1. Deutetrabenazine is a racemic mixture containing RR-Deutetrabenazine and SS-Deutetrabenazine Label.
Huntington's disease (HD) is a hereditary, progressive neurodegenerative disorder characterized by motor dysfunction, cognitive decline, and neuropsychiatric disturbances 2 that interfere with daily functioning and significantly reduce the quality of life. The most prominent physical symptom of HD that may increase the risk of injury is chorea, which is an involuntary, sudden movement that can affect any muscle and flow randomly across body regions 5. Psychomotor symptoms of HD, such as chorea, are related to hyperactive dopaminergic neurotransmission 6. Deutetrabenazine depletes the levels of presynaptic dopamine by blocking VMAT2, which is responsible for the uptake of dopamine into synaptic vesicles in monoaminergic neurons and exocytotic release 6. As with other agents for the treatment of neurodegenerative diseases, deutetrabenazine is a drug to alleviate the motor symptoms of HD and is not proposed to halt the progression of the disease 7. In clinical trials of patients with HD, 12 weeks of treatment of deutetrabenazine resulted in overall improvement in mean total maximal chorea scores and motor signs than placebo 5. It was approved by FDA in April 2017 and is marketed under the trade name Austedo as oral tablets.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 323.466
Monoisotopic: 323.236754209 - Chemical Formula
- C19H27NO3
- Synonyms
- D6 tetrabenazine
- D6-tetrabenazine
- Deutetrabenazine
- Tetrabenazine D6
- Tetrabenazine-D6
- External IDs
- SD-809
Pharmacology
- Indication
Deutetrabenazine is indicated in adults patients for the treatment of tardive dyskinesia and for chorea associated with Huntington's disease.8
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Chorea •••••••••••• ••••• •••••• Management of Tardive dyskinesia (td) •••••••••••• ••••• •••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
In clinical trials, there was an evidence of clinical effectiveness of deutetrabenazine in improving the symptoms of involuntary movements in patient with tardive dyskinesia by reducing the mean Abnormal Involuntary Movement Scale (AIMS) score 3,4. In a randomized, double-blind, placebo-controlled crossover study in healthy male and female subjects, single dose administration of 24 mg deutetrabenazine results in an approximately 4.5 msec mean increase in QTc Label. Effects at higher exposures to deutetrabenazine or its metabolites have not been evaluated Label. Deutetrabenazine and its metabolites were shown to bind to melanin-containing tissues including eyes, skin and fur in pigmented rats. After a single oral dose of radiolabeled deutetrabenazine, radioactivity was still detected in eye and fur at 35 days following dosing Label.
- Mechanism of action
The precise mechanism of action of deutetrabenazine in mediating its anti-chorea effects is not fully elucidated. Deutetrabenazine reversibly depletes the levels of monoamines, such as dopamine, serotonin, norepinephrine, and histamine, from nerve terminals via its active metabolites. The major circulating metabolites are α-dihydrotetrabenazine [HTBZ] and β-HTBZ that act as reversible inhibitors of VMAT2. Inhibition of VMAT2 results in decreased uptake of monoamines into synaptic terminal and depletion of monoamine stores from nerve terminals Label.
Deutetrabenazine contains the molecule deuterium, which is a naturally-occurring, nontoxic hydrogen isotope but with an increased mass relative to hydrogen 5. Placed at key positions, deuterium forms a stronger hydrogen bond with carbon that requires more energy for cleavage, thus attenuating CYP2D6-mediated metabolism without having any effect on the therapeutic target 5.
Target Actions Organism ASynaptic vesicular amine transporter inhibitorHumans - Absorption
The extent of absorption is 80% with oral deutetrabenazine. As deutetrabenazine is extensively metabolized to its main active metabolites following administration, linear dose dependence of peak plasma concentrations (Cmax) and AUC was observed for the metabolites after single or multiple doses of deutetrabenazine (6 mg to 24 mg and 7.5 mg twice daily to 22.5 mg twice daily) Label. Cmax of deuterated α-HTBZ and β-HTBZ are reached within 3-4 hours post-dosing Label. Food may increase the Cmax of α-HTBZ or β-HTBZ by approximately 50%, but is unlikely to have an effect on the AUC Label.
- Volume of distribution
The median volume of distribution (Vc/F) of the α-HTBZ, and the β-HTBZ metabolites of deutetrabenazine are approximately 500 L and 730 L, respectively Label. Human PET-scans of tetrabenazine indicate rapid distribution to the brain, with the highest binding in the striatum and lowest binding in the cortex Label. Similar distribution pattern is expected for deutetrabenazine.
- Protein binding
At doses ranging from 50 to 200 ng/mL in vitro, tetrabenazine protein binding ranged from 82% to 85%, α-HTBZ binding ranged from 60% to 68%, and β-HTBZ binding ranged from 59% to 63% Label. Similar protein binding pattern is expected for deutetrabenazine and its metabolites.
- Metabolism
Deutetrabenazine undergoes extensive hepatic biotransformation mediated by carbonyl reductase to form its major active metabolites, α-HTBZ and β-HTBZ. These metabolites may subsequently metabolized to form several minor metabolites, with major contribution of CYP2D6 and minor contributions of CYP1A2 and CYP3A4/5 Label.
- Route of elimination
Deutetrabenazine is mainly excreted in the urine as metabolites. In healthy subjects, about 75% to 86% of the deutetrabenazine dose was excreted in the urine, and fecal recovery accounted for 8% to 11% of the dose Label. Sulfate and glucuronide conjugates of the α-HTBZ and β-HTBZ, as well as products of oxidative metabolism, accounted for the majority of metabolites in the urine Label. α-HTBZ and β-HTBZ metabolites accounted for less than 10% of the administered dose in the urine Label.
- Half-life
The half-life of total (α+β)-HTBZ from deutetrabenazine is approximately 9 to 10 hours Label.
- Clearance
In patients with Huntington's disease, the median clearance values (CL/F) of the α-HTBZ, and the β-HTBZ metabolites of deutetrabenazine are approximately 47 L/hour and 70 L/hour, respectively Label.
- Adverse Effects
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- Toxicity
Adverse reactions associated with overdosage include acute dystonia, oculogyric crisis, nausea and vomiting, sweating, sedation, hypotension, confusion, diarrhea, hallucinations, rubor, and tremor Label. In case of an overdose, general supportive and symptomatic measures are recommended while monitoring cardiac rhythm and vital signs. In managing overdosage, the possibility of multiple drug involvement should always be considered Label.
No carcinogenicity studies were performed with deutetrabenazine. In p53+/– transgenic mice, there were no detectable tumors following oral administration of deutetrabenazine at doses of 0, 5, 15, and 30 mg/kg/day for 26 weeks Label. Findings from in vitro assays and in vivo mice micronucleus assay suggest that deutetrabenazine and its metabolites are unlikely to be mutagenic Label. The effects of deutetrabenazine on fertility have not been evaluated. Oral administration of tetrabenazine had no effects on mating and reproductive systems of male and female rats Label.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Deutetrabenazine which could result in a higher serum level. Abametapir The serum concentration of Deutetrabenazine can be increased when it is combined with Abametapir. Abatacept The metabolism of Deutetrabenazine can be increased when combined with Abatacept. Abiraterone The metabolism of Deutetrabenazine can be decreased when combined with Abiraterone. Acalabrutinib The metabolism of Deutetrabenazine can be decreased when combined with Acalabrutinib. - Food Interactions
- Avoid alcohol. Additive sedative effects may occur from co-administration of deutetrabenazine with alcohol.
- Take with food. Taking deutetrabenazine with food increases its Cmax.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Austedo Kit; Tablet 6 mg/1 Oral Teva Neuroscience, Inc. 2020-02-01 2023-02-28 US Austedo Tablet, coated 6 mg/1 Oral Teva Neuroscience, Inc. 2017-04-12 Not applicable US Austedo Tablet, coated 12 mg/1 Oral Teva Neuroscience, Inc. 2017-04-12 Not applicable US Austedo Tablet, coated 9 mg/1 Oral Teva Neuroscience, Inc. 2017-04-12 Not applicable US Austedo XR Tablet, film coated, extended release 12 mg/1 Oral Teva Neuroscience, Inc. 2023-02-21 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Austedo Deutetrabenazine (6 mg/1) + Deutetrabenazine (9 mg/1) + Deutetrabenazine (12 mg/1) Kit; Tablet, coated Oral Teva Neuroscience, Inc. 2021-05-06 2023-02-28 US Austedo Deutetrabenazine (6 mg/1) + Deutetrabenazine (9 mg/1) Kit; Tablet Oral Teva Neuroscience, Inc. 2020-02-01 Not applicable US Austedo Deutetrabenazine (6 mg/1) + Deutetrabenazine (9 mg/1) + Deutetrabenazine (12 mg/1) Kit; Tablet, coated Oral Teva Neuroscience, Inc. 2021-05-06 2024-02-29 US Austedo Deutetrabenazine (6 mg/1) + Deutetrabenazine (9 mg/1) + Deutetrabenazine (12 mg/1) Kit; Tablet, coated Oral Teva Neuroscience, Inc. 2021-05-06 2023-02-28 US Austedo Deutetrabenazine (6 mg/1) + Deutetrabenazine (9 mg/1) + Deutetrabenazine (12 mg/1) Kit; Tablet, coated Oral Teva Neuroscience, Inc. 2021-05-06 2024-02-29 US
Categories
- ATC Codes
- N07XX16 — Deutetrabenazine
- Drug Categories
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 Substrates
- Drugs that are Mainly Renally Excreted
- Heterocyclic Compounds, Fused-Ring
- Highest Risk QTc-Prolonging Agents
- Nervous System
- QTc Prolonging Agents
- Quinolizines
- Vesicular Monoamine Transporter 2 Inhibitor
- Vesicular Monoamine Transporter 2 Inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as tetrahydroisoquinolines. These are tetrahydrogenated isoquinoline derivatives.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Tetrahydroisoquinolines
- Sub Class
- Not Available
- Direct Parent
- Tetrahydroisoquinolines
- Alternative Parents
- Anisoles / Piperidinones / Aralkylamines / Alkyl aryl ethers / Trialkylamines / Cyclic ketones / Azacyclic compounds / Organic oxides / Hydrocarbon derivatives
- Substituents
- Alkyl aryl ether / Amine / Anisole / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Carbonyl group / Cyclic ketone / Ether
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- P341G6W9NB
- CAS number
- 1392826-25-3
- InChI Key
- MKJIEFSOBYUXJB-WEZHFFAMSA-N
- InChI
- InChI=1S/C19H27NO3/c1-12(2)7-14-11-20-6-5-13-8-18(22-3)19(23-4)9-15(13)16(20)10-17(14)21/h8-9,12,14,16H,5-7,10-11H2,1-4H3/t14-,16-/m0/s1/i3D3,4D3
- IUPAC Name
- (3S,11bS)-9,10-di(2H3)methoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H,11bH-pyrido[2,1-a]isoquinolin-2-one
- SMILES
- [2H]C([2H])([2H])OC1=CC2=C(C=C1OC([2H])([2H])[2H])[C@@H]1CC(=O)[C@@H](CC(C)C)CN1CC2
References
- General References
- Paton DM: Deutetrabenazine: Treatment of hyperkinetic aspects of Huntington's disease, tardive dyskinesia and Tourette syndrome. Drugs Today (Barc). 2017 Feb;53(2):89-102. doi: 10.1358/dot.2017.53.2.2589164. [Article]
- Rodrigues FB, Duarte GS, Costa J, Ferreira JJ, Wild EJ: Tetrabenazine Versus Deutetrabenazine for Huntington's Disease: Twins or Distant Cousins? Mov Disord Clin Pract. 2017 Jul-Aug;4(4):582-585. doi: 10.1002/mdc3.12483. Epub 2017 Mar 29. [Article]
- Anderson KE, Stamler D, Davis MD, Factor SA, Hauser RA, Isojarvi J, Jarskog LF, Jimenez-Shahed J, Kumar R, McEvoy JP, Ochudlo S, Ondo WG, Fernandez HH: Deutetrabenazine for treatment of involuntary movements in patients with tardive dyskinesia (AIM-TD): a double-blind, randomised, placebo-controlled, phase 3 trial. Lancet Psychiatry. 2017 Aug;4(8):595-604. doi: 10.1016/S2215-0366(17)30236-5. Epub 2017 Jun 28. [Article]
- Fernandez HH, Factor SA, Hauser RA, Jimenez-Shahed J, Ondo WG, Jarskog LF, Meltzer HY, Woods SW, Bega D, LeDoux MS, Shprecher DR, Davis C, Davis MD, Stamler D, Anderson KE: Randomized controlled trial of deutetrabenazine for tardive dyskinesia: The ARM-TD study. Neurology. 2017 May 23;88(21):2003-2010. doi: 10.1212/WNL.0000000000003960. Epub 2017 Apr 26. [Article]
- Frank S, Testa CM, Stamler D, Kayson E, Davis C, Edmondson MC, Kinel S, Leavitt B, Oakes D, O'Neill C, Vaughan C, Goldstein J, Herzog M, Snively V, Whaley J, Wong C, Suter G, Jankovic J, Jimenez-Shahed J, Hunter C, Claassen DO, Roman OC, Sung V, Smith J, Janicki S, Clouse R, Saint-Hilaire M, Hohler A, Turpin D, James RC, Rodriguez R, Rizer K, Anderson KE, Heller H, Carlson A, Criswell S, Racette BA, Revilla FJ, Nucifora F Jr, Margolis RL, Ong M, Mendis T, Mendis N, Singer C, Quesada M, Paulsen JS, Brashers-Krug T, Miller A, Kerr J, Dubinsky RM, Gray C, Factor SA, Sperin E, Molho E, Eglow M, Evans S, Kumar R, Reeves C, Samii A, Chouinard S, Beland M, Scott BL, Hickey PT, Esmail S, Fung WL, Gibbons C, Qi L, Colcher A, Hackmyer C, McGarry A, Klos K, Gudesblatt M, Fafard L, Graffitti L, Schneider DP, Dhall R, Wojcieszek JM, LaFaver K, Duker A, Neefus E, Wilson-Perez H, Shprecher D, Wall P, Blindauer KA, Wheeler L, Boyd JT, Houston E, Farbman ES, Agarwal P, Eberly SW, Watts A, Tariot PN, Feigin A, Evans S, Beck C, Orme C, Edicola J, Christopher E: Effect of Deutetrabenazine on Chorea Among Patients With Huntington Disease: A Randomized Clinical Trial. JAMA. 2016 Jul 5;316(1):40-50. doi: 10.1001/jama.2016.8655. [Article]
- Wimalasena K: Vesicular monoamine transporters: structure-function, pharmacology, and medicinal chemistry. Med Res Rev. 2011 Jul;31(4):483-519. doi: 10.1002/med.20187. Epub 2010 Feb 4. [Article]
- 39. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 489-490). Edinburgh: Elsevier/Churchill Livingstone. [ISBN:978-0-7020-3471-8]
- FDA Approved Drug Products: Austedo (deutetrabenazine) tablets for oral use [Link]
- External Links
- PubChem Compound
- 73442840
- PubChem Substance
- 347828453
- ChemSpider
- 32700662
- 1876905
- Wikipedia
- Deutetrabenazine
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 3 Completed Treatment Cerebral Palsy, Dyskinetic / Coronavirus Disease 2019 (COVID‑19) 1 3 Completed Treatment Chorea 1 3 Completed Treatment Gilles de la Tourette's Syndrome 1 3 Completed Treatment Huntington's Disease (HD) 1 3 Completed Treatment Tardive Dyskinesia (TD) 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Kit; tablet Oral Kit; tablet Oral 6 mg/1 Kit; tablet, coated Oral Tablet, coated Oral 12 mg/1 Tablet, coated Oral 6 mg/1 Tablet, coated Oral 9 mg/1 Kit; tablet, film coated, extended release Oral Tablet, film coated, extended release Oral 12 mg/1 Tablet, film coated, extended release Oral 24 mg/1 Tablet, film coated, extended release Oral 6 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8524733 Yes 2013-09-03 2031-09-27 US US9296739 Yes 2016-03-29 2034-03-18 US US9233959 Yes 2016-01-12 2034-03-18 US US9550780 Yes 2017-01-24 2034-03-18 US US9814708 Yes 2017-11-14 2034-03-18 US US10959996 Yes 2021-03-30 2036-09-07 US US11179386 Yes 2021-11-23 2038-09-15 US US11357772 Yes 2016-09-07 2036-09-07 US US11446291 Yes 2016-09-07 2036-09-07 US US11564917 Yes 2016-09-07 2036-09-07 US US11311488 No 2021-06-10 2041-06-10 US US11648244 Yes 2016-09-07 2036-09-07 US US11666566 Yes 2014-03-18 2034-03-18 US US11813232 Yes 2018-09-15 2038-09-15 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.361 mg/mL ALOGPS logP 3.23 ALOGPS logP 3.4 Chemaxon logS -2.9 ALOGPS pKa (Strongest Acidic) 18.26 Chemaxon pKa (Strongest Basic) 7.33 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 38.77 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 91.31 m3·mol-1 Chemaxon Polarizability 36.83 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-014i-0009000000-ba78836c58b00ab4e6c4 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-014i-0009000000-f189fc658abb8f999018 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-014i-0049000000-e25754af93da67965901 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-014i-0139000000-13d752e602ef6e4c3252 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-01p9-2390000000-c94ee9cdbabd19c82d12 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0w29-0390000000-12b1bea577b46f85cc04 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 189.45454 predictedDeepCCS 1.0 (2019) [M+H]+ 191.34996 predictedDeepCCS 1.0 (2019) [M+Na]+ 197.1279 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Monoamine transmembrane transporter activity
- Specific Function
- Involved in the ATP-dependent vesicular transport of biogenic amine neurotransmitters. Pumps cytosolic monoamines including dopamine, norepinephrine, serotonin, and histamine into synaptic vesicles...
- Gene Name
- SLC18A2
- Uniprot ID
- Q05940
- Uniprot Name
- Synaptic vesicular amine transporter
- Molecular Weight
- 55712.075 Da
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Prostaglandin-e2 9-reductase activity
- Specific Function
- NADPH-dependent reductase with broad substrate specificity. Catalyzes the reduction of a wide variety of carbonyl compounds including quinones, prostaglandins, menadione, plus various xenobiotics. ...
- Gene Name
- CBR1
- Uniprot ID
- P16152
- Uniprot Name
- Carbonyl reductase [NADPH] 1
- Molecular Weight
- 30374.73 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Nadph binding
- Specific Function
- Has low NADPH-dependent oxidoreductase activity towards 4-benzoylpyridine and menadione (in vitro).
- Gene Name
- CBR3
- Uniprot ID
- O75828
- Uniprot Name
- Carbonyl reductase [NADPH] 3
- Molecular Weight
- 30849.97 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- Curator comments
- The FDA label states that CYP1A2 has a minor contribution to the metabolism of this drug.
- 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
- Deutetrabenazine FDA label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- 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
Drug created at October 20, 2016 21:30 / Updated at July 18, 2023 22:57