Identification
- Summary
Tapentadol is an opioid used to manage severe pain that has not responded to non-opioid medications, and for which opioid analgesic therapy is appropriate.
- Brand Names
- Nucynta
- Generic Name
- Tapentadol
- DrugBank Accession Number
- DB06204
- Background
Opioid analgesic for treatment of moderate to severe pain. FDA approved on Nov 20, 2008.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Tapentadol (DB06204)
- Weight
- Average: 221.3385
Monoisotopic: 221.177964363 - Chemical Formula
- C14H23NO
- Synonyms
- Tapentadol
- External IDs
- BN 200
- BN-200
- CG-5503
- CG5503
- CG5503 IR
- R331333
Pharmacology
- Indication
The immediate-release formulation of tapentadol is indicated for the relief of moderate to severe acute pain. The long-acting formulation serves as a continuous, around-the-clock analgesic that is indicated for the relief of moderate to severe chronic pain or neuropathic pain associated with diabetic peripheral neuropathy.
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Tapentadol is a centrally-acting synthetic analgesic that is 18 times less potent than morphine in binding mu-opioid receptors. It also increases norepinephrine concentrations in the brains of rats via inhibition of norepinephrine reuptake. Selective mu-opioid antagonists like naloxone can block analgesia from tapentadol. It also has not effect on the QT interval.
- Mechanism of action
Tapendadol causes large increases in levels of extracellular norepinephrine (NE) due to a dual mechanism of action involving mu opioid receptor (MOR) agonism as well as noradrenaline reuptake inhibition.
Target Actions Organism AMu-type opioid receptor agonistHumans ASodium-dependent noradrenaline transporter inhibitorHumans UKappa-type opioid receptor Not Available Humans UDelta-type opioid receptor Not Available Humans U5-hydroxytryptamine receptor 3A Not Available Humans USodium-dependent serotonin transporter inhibitorHumans - Absorption
Bioavailability, immediate release (IR), 86 mg: 32%; Bioavailability, extended release (ER), 86 mg: 32%; Cmax, IR: 64.2 ng/mL; Cmax, ER: 22.5 ng/mL; T max, IR: 1.5 hours; T max, ER: 5.0 hours; Tapentadol accumulates following multiple repeat doses.
- Volume of distribution
Following IV administration, volume of distribution is 540 ± 98 L.
- Protein binding
~20%
- Metabolism
97% of the dose is metabolized mostly via conjugation with glucuronic acid to produce glucuronides. Tapentadol is also metabolized into N-desmethyl tapentadol (13%) by CYP2C9 and CYP 2C19. CYP2D6 is involved in the formation of the metabolite, hydroxy tapentadol (2%). All metabolites are inactive.
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- Route of elimination
Tapentadol and its metabolites are excreted almost exclusively (99%) via the kidneys. Approximately 70% (55% O-glucuronide and 15% sulfate of tapentadol) is excreted in conjugated form. A total of 3% of drug was excreted in urine as unchanged drug.
- Half-life
Elimination half-life, IV: 4 hours.
- Clearance
Total clearance = 1530 ± 177 ml/min.
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Oral, rabbit: LD50 = 3200 mg/kg; Oral, mouse: LD50 = 300 mg/kg; Oral, rat: LD50: 980 mg/kg; The most common reasons for discontinuation due to adverse events were dizziness, nausea, vomiting, somnolence, and headache.
- 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.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine Tapentadol may increase the central nervous system depressant (CNS depressant) activities of 1,2-Benzodiazepine. Acenocoumarol The risk or severity of adverse effects can be increased when Tapentadol is combined with Acenocoumarol. Acetazolamide Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Acetazolamide. Acetophenazine Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Acetophenazine. Aclidinium The risk or severity of adverse effects can be increased when Aclidinium is combined with Tapentadol. Agomelatine Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Agomelatine. Alfentanil Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Alfentanil. Alimemazine Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Alimemazine. Alloin The therapeutic efficacy of Alloin can be decreased when used in combination with Tapentadol. Almotriptan Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Almotriptan. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- Take with or without food. Food increases absorption, but not to a clinically significant extent.
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.- Product Ingredients
Ingredient UNII CAS InChI Key Tapentadol hydrochloride 71204KII53 175591-09-0 ZELFLGGRLLOERW-YECZQDJWSA-N - International/Other Brands
- Palexia (Grünenthal Ltd) / TAPAL (MSN Labs )
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Nucynta Tablet, film coated 100 mg/1 Oral Stat Rx USA 2009-06-01 Not applicable US 
Nucynta Tablet, film coated 50 mg/1 Oral Lake Erie Medical DBA Quality Care Products LLC 2018-04-20 2019-12-31 US Nucynta Tablet, film coated 75 mg/1 Oral Lake Erie Medical DBA Quality Care Products LLC 2011-07-13 2019-10-11 US Nucynta Tablet, film coated 75 mg/1 Oral Janssen Pharmaceuticals, Inc. 2009-06-01 2020-03-31 US Nucynta Tablet, film coated 75 mg/1 Oral Collegium Pharmaceutical, Inc. 2019-04-01 Not applicable US Nucynta Tablet, film coated 100 mg/1 Oral bryant ranch prepack 2009-06-01 2014-06-01 US Nucynta Tablet, film coated 75 mg/1 Oral Depo Nf Sub, Llc 2017-06-16 Not applicable US Nucynta Solution 20 mg/1mL Oral Janssen Pharmaceuticals, Inc. 2012-10-15 2012-10-15 US Nucynta Tablet, film coated 50 mg/1 Oral Physicians Total Care, Inc. 2010-03-19 Not applicable US Nucynta Tablet, film coated 50 mg/1 Oral Stat Rx USA 2009-06-01 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-tapentadol Tablet, multilayer, extended release 100 mg Oral Apotex Corporation Not applicable Not applicable Canada 
Apo-tapentadol Tablet, multilayer, extended release 75 mg Oral Apotex Corporation Not applicable Not applicable Canada Apo-tapentadol Tablet, multilayer, extended release 50 mg Oral Apotex Corporation Not applicable Not applicable Canada
Categories
- ATC Codes
- N02AX06 — Tapentadol
- Drug Categories
- Adrenergic Agents
- Adrenergic Uptake Inhibitors
- Analgesics
- Antidepressive Agents
- Benzene Derivatives
- Central Nervous System Agents
- Central Nervous System Depressants
- Combined Inhibitors of Serotonin/Norepinephrine Reuptake
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 Substrates
- Membrane Transport Modulators
- Narcotics
- Nervous System
- Neurotransmitter Agents
- Neurotransmitter Uptake Inhibitors
- Opiate Agonists
- Opioid Agonist
- Opioids
- Peripheral Nervous System Agents
- Phenols
- Sensory System Agents
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin Agents
- Serotonin Modulators
- UGT1A9 Substrates
- UGT2B7 substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenylpropanes. These are organic compounds containing a phenylpropane moiety.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Phenylpropanes
- Direct Parent
- Phenylpropanes
- Alternative Parents
- Aralkylamines / 1-hydroxy-4-unsubstituted benzenoids / 1-hydroxy-2-unsubstituted benzenoids / Trialkylamines / Organopnictogen compounds / Organooxygen compounds / Hydrocarbon derivatives
- Substituents
- 1-hydroxy-2-unsubstituted benzenoid / 1-hydroxy-4-unsubstituted benzenoid / Amine / Aralkylamine / Aromatic homomonocyclic compound / Hydrocarbon derivative / Organic nitrogen compound / Organic oxygen compound / Organonitrogen compound / Organooxygen compound
- Molecular Framework
- Aromatic homomonocyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- H8A007M585
- CAS number
- 175591-23-8
- InChI Key
- KWTWDQCKEHXFFR-SMDDNHRTSA-N
- InChI
- InChI=1S/C14H23NO/c1-5-14(11(2)10-15(3)4)12-7-6-8-13(16)9-12/h6-9,11,14,16H,5,10H2,1-4H3/t11-,14+/m0/s1
- IUPAC Name
- 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol
- SMILES
- CC[C@H]([C@@H](C)CN(C)C)C1=CC(O)=CC=C1
References
- Synthesis Reference
Giuseppe Motta, Domenico Vergani, Giorgio Bertolini, "PROCESS FOR THE PREPARATION OF TAPENTADOL AND INTERMEDIATES THEREOF." U.S. Patent US20120232306, issued September 13, 2012.
US20120232306- General References
- Tzschentke TM, Christoph T, Kogel B, Schiene K, Hennies HH, Englberger W, Haurand M, Jahnel U, Cremers TI, Friderichs E, De Vry J: (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. J Pharmacol Exp Ther. 2007 Oct;323(1):265-76. Epub 2007 Jul 26. [Article]
- Gohler K, Brett M, Smit JW, Rengelshausen J, Terlinden R: Comparative pharmacokinetics and bioavailability of tapentadol following oral administration of immediate- and prolonged-release formulations. Int J Clin Pharmacol Ther. 2013 Apr;51(4):338-48. doi: 10.5414/CP201722. [Article]
- Xu XS, Smit JW, Lin R, Stuyckens K, Terlinden R, Nandy P: Population pharmacokinetics of tapentadol immediate release (IR) in healthy subjects and patients with moderate or severe pain. Clin Pharmacokinet. 2010 Oct;49(10):671-82. doi: 10.2165/11535390-000000000-00000. [Article]
- External Links
- KEGG Drug
- D06007
- PubChem Compound
- 9838022
- PubChem Substance
- 175427057
- ChemSpider
- 8013742
- BindingDB
- 50386381
- 787390
- ChEBI
- 135935
- ChEMBL
- CHEMBL1201776
- ZINC
- ZINC000000020783
- PharmGKB
- PA166179720
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Tapentadol
- FDA label
- Download (666 KB)
- MSDS
- Download (481 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Prevention Osteoarthritis of the Knee 1 4 Completed Supportive Care Effects of 2 Mu-opiates on Gastrointestinal Transit 1 4 Completed Treatment Acute Pain / Analgesics, Antipyretics, and Antirheumatics Causing Adverse Effects in Therapeutic Use / Opioids Use / Pain Uterus / Postoperative pain / Visceral Pain 1 4 Completed Treatment Back Pain Lower Back / Neuropathic Pain 1 4 Completed Treatment Back pain / Back Pain Lower Back / Neuropathic Pain 1 4 Terminated Not Available Peripheral neuropathy 1 4 Withdrawn Treatment Chronic Back Pain / Chronic Lower Back Pain (CLBP) / Osteoarthritis Pain In The Hip or Knee / Pain 1 3 Completed Treatment Acute Pain 1 3 Completed Treatment Acute Pain / Bunionectomy / Pain / Postoperative pain 1 3 Completed Treatment Articular inflammation / Joint Dysfunction / Osteoarthritis (OA) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, coated Oral 50 mg Solution Oral 20 mg/1mL Tablet, film coated Oral 100 mg/1 Tablet, film coated Oral 50 mg/1 Tablet, film coated Oral 75 mg/1 Tablet, extended release Oral 100 mg Tablet, extended release Oral 150 mg Tablet, extended release Oral 200 mg Tablet, extended release Oral 250 mg Tablet, extended release Oral 50 mg Tablet, film coated, extended release Oral 100 mg/1 Tablet, film coated, extended release Oral 150 mg/1 Tablet, film coated, extended release Oral 200 mg/1 Tablet, film coated, extended release Oral 250 mg/1 Tablet, film coated, extended release Oral 50 mg/1 Tablet, film coated Oral 100 mg Tablet Oral 100 mg Tablet, film coated Oral 150 mg Tablet Oral 150 mg Tablet Oral 200 mg Tablet Oral 250 mg Tablet Oral 50 mg Tablet, multilayer, extended release Oral 100 mg Tablet, multilayer, extended release Oral 50 mg Tablet, multilayer, extended release Oral 75 mg Tablet, film coated Oral 50 mg Tablet, film coated Oral 75 mg Solution Oral 20 MG/ML Solution Oral 4 MG/ML Tablet, extended release Oral 25 MG Tablet, film coated Oral Solution Oral Tablet, extended release Oral Solution Oral 2 g - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8309060 No 2012-11-13 2023-11-20 US US8114383 No 2012-02-14 2024-10-10 US US6071970 No 2000-06-06 2017-06-06 US US7994364 No 2011-08-09 2025-06-27 US USRE39593 No 2007-04-24 2022-08-05 US US8075872 No 2011-12-13 2023-11-20 US US8536130 No 2013-09-17 2028-09-22 US US8420056 No 2013-04-16 2023-11-20 US US11007156 No 2021-05-18 2022-10-22 US US11344512 No 2008-04-21 2028-04-21 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 2.87 FDA label pKa 9.34 - 10.45 FDA label - Predicted Properties
Property Value Source Water Solubility 0.78 mg/mL ALOGPS logP 3.47 ALOGPS logP 2.96 Chemaxon logS -2.4 ALOGPS pKa (Strongest Acidic) 10.28 Chemaxon pKa (Strongest Basic) 9.6 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 23.47 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 69.56 m3·mol-1 Chemaxon Polarizability 26.58 Å3 Chemaxon Number of Rings 1 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
Property Value Probability Human Intestinal Absorption + 0.9937 Blood Brain Barrier + 0.9232 Caco-2 permeable + 0.7912 P-glycoprotein substrate Substrate 0.559 P-glycoprotein inhibitor I Non-inhibitor 0.9304 P-glycoprotein inhibitor II Non-inhibitor 0.9408 Renal organic cation transporter Non-inhibitor 0.6918 CYP450 2C9 substrate Non-substrate 0.8085 CYP450 2D6 substrate Non-substrate 0.5219 CYP450 3A4 substrate Substrate 0.5509 CYP450 1A2 substrate Inhibitor 0.6665 CYP450 2C9 inhibitor Non-inhibitor 0.8856 CYP450 2D6 inhibitor Non-inhibitor 0.5538 CYP450 2C19 inhibitor Non-inhibitor 0.921 CYP450 3A4 inhibitor Non-inhibitor 0.8389 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8875 Ames test Non AMES toxic 0.6862 Carcinogenicity Non-carcinogens 0.5177 Biodegradation Not ready biodegradable 0.9421 Rat acute toxicity 2.6035 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.7187 hERG inhibition (predictor II) Inhibitor 0.6155
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...
- Gene Name
- OPRM1
- Uniprot ID
- P35372
- Uniprot Name
- Mu-type opioid receptor
- Molecular Weight
- 44778.855 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Norepinephrine:sodium symporter activity
- Specific Function
- Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
- Gene Name
- SLC6A2
- Uniprot ID
- P23975
- Uniprot Name
- Sodium-dependent noradrenaline transporter
- Molecular Weight
- 69331.42 Da
References
- Tzschentke TM, Christoph T, Kogel B, Schiene K, Hennies HH, Englberger W, Haurand M, Jahnel U, Cremers TI, Friderichs E, De Vry J: (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. J Pharmacol Exp Ther. 2007 Oct;323(1):265-76. Epub 2007 Jul 26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Opioid receptor activity
- Specific Function
- G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
- Gene Name
- OPRK1
- Uniprot ID
- P41145
- Uniprot Name
- Kappa-type opioid receptor
- Molecular Weight
- 42644.665 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Opioid receptor activity
- Specific Function
- G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine n...
- Gene Name
- OPRD1
- Uniprot ID
- P41143
- Uniprot Name
- Delta-type opioid receptor
- Molecular Weight
- 40368.235 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gate...
- Gene Name
- HTR3A
- Uniprot ID
- P46098
- Uniprot Name
- 5-hydroxytryptamine receptor 3A
- Molecular Weight
- 55279.835 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Serotonin:sodium symporter activity
- Specific Function
- Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into t...
- Gene Name
- SLC6A4
- Uniprot ID
- P31645
- Uniprot Name
- Sodium-dependent serotonin transporter
- Molecular Weight
- 70324.165 Da
References
- Raffa RB, Buschmann H, Christoph T, Eichenbaum G, Englberger W, Flores CM, Hertrampf T, Kogel B, Schiene K, Strassburger W, Terlinden R, Tzschentke TM: Mechanistic and functional differentiation of tapentadol and tramadol. Expert Opin Pharmacother. 2012 Jul;13(10):1437-49. doi: 10.1517/14656566.2012.696097. Epub 2012 Jun 15. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Retinoic acid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks trans...
- Gene Name
- UGT1A9
- Uniprot ID
- O60656
- Uniprot Name
- UDP-glucuronosyltransferase 1-9
- Molecular Weight
- 59940.495 Da
References
- Kneip C, Terlinden R, Beier H, Chen G: Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett. 2008 Jan;2(1):67-75. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Glucuronosyltransferase activity
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
- Gene Name
- UGT2B7
- Uniprot ID
- P16662
- Uniprot Name
- UDP-glucuronosyltransferase 2B7
- Molecular Weight
- 60694.12 Da
References
- Kneip C, Terlinden R, Beier H, Chen G: Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett. 2008 Jan;2(1):67-75. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- Kneip C, Terlinden R, Beier H, Chen G: Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett. 2008 Jan;2(1):67-75. [Article]
Drug created at March 19, 2008 16:17 / Updated at June 03, 2023 08:16