Identification
- Summary
Eletriptan is a triptan used for the treatment of migraines.
- Brand Names
- Relpax
- Generic Name
- Eletriptan
- DrugBank Accession Number
- DB00216
- Background
Eletriptan is a second generation triptan drug developed by Pfizer Inc for the treatment of migraine headaches.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Eletriptan (DB00216)
- Weight
- Average: 382.519
Monoisotopic: 382.171498776 - Chemical Formula
- C22H26N2O2S
- Synonyms
- Eletriptán
- Eletriptan
- élétriptan
- Eletriptanum
- External IDs
- UK-116,044
- UK-116,044-04 FREE BASE
- UK-116044
- UK-116044-04 FREE BASE
Pharmacology
- Indication
For the acute treatment of migraine with or without aura in adults.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Migraine with aura •••••••••••• ••••• •••••• Treatment of Migraine without aura •••••••••••• ••••• •••••• - 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
Eletriptan is a selective 5-hydroxytryptamine 1B/1D receptor agonist. In the anesthetized dog, eletriptan has been shown to reduce carotid arterial blood flow, with only a small increase in arterial blood pressure at high doses. While the effect on blood flow was selective for the carotid arterial bed, decreases in coronary artery diameter were observed. Eletriptan has also been shown to inhibit trigeminal nerve activity in the rat.
- Mechanism of action
Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors, and little or no affinity for 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, 5-HT5A and 5-HT6 receptors. In contrast, eletriptan displays insignificant pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors. While the full mechanism of action of 5-HT receptor agonists in relieving migrains is not fully elucidated, it is proposed that the activation of 5-HT1 receptors located on intracranial blood vessels leads to vasoconstriction that correlates with the relief of migraine headaches. It is also proposed that the activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system leads to the inhibition of release of pro-inflammatory neuropeptides.
Target Actions Organism A5-hydroxytryptamine receptor 1D agonistHumans A5-hydroxytryptamine receptor 1B agonistHumans A5-hydroxytryptamine receptor 1F agonistHumans U5-hydroxytryptamine receptor 1A agonistHumans - Absorption
Well absorbed after oral administration with a mean absolute bioavailability of approximately 50%.
- Volume of distribution
- 138 L
- Protein binding
Plasma protein binding is moderate and approximately 85%.
- Metabolism
In vitro studies indicate that eletriptan is primarily metabolized by cytochrome P-450 enzyme CYP3A4. The N-demethylated metabolite of eletriptan is the only known active metabolite.
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- Route of elimination
Not Available
- Half-life
The terminal elimination half-life of eletriptan is approximately 4 hours.
- Clearance
- Renal cl=3.9 L/h
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Based on the pharmacology of the 5-HT1B/1D agonists, hypertension or other more serious cardiovascular symptoms could occur on overdose.
- 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);">
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3 --- (T;T) / (C;T) T Allele Effect Directly Studied Patients with this genotype have an increased likelihood of responding to elitriptan when treating (condition: cluster headache). Details
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 software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Eletriptan is combined with 1,2-Benzodiazepine. Abametapir The serum concentration of Eletriptan can be increased when it is combined with Abametapir. Abatacept The metabolism of Eletriptan can be increased when combined with Abatacept. Abiraterone The metabolism of Eletriptan can be decreased when combined with Abiraterone. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Eletriptan. - Food Interactions
- Take with or without food. High-fat meals increase exposure, but not to a clinically relevant 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 Eletriptan hydrobromide M41W832TA3 177834-92-3 UTINOWOSWSPFLJ-FSRHSHDFSA-N Eletriptan hydrobromide monohydrate 4139X692FA 273211-28-2 BORDVONYOHPTGR-JQDLGSOUSA-N - Product Images
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Eletriptan Tablet 40 mg Oral Pro Doc Limitee 2019-07-31 Not applicable Canada 
Eletriptan Tablet 40 mg Oral Sanis Health Inc 2021-07-22 Not applicable Canada Eletriptan Tablet 20 mg Oral Pro Doc Limitee 2019-07-31 Not applicable Canada Eletriptan Tablet 20 mg Oral Sanis Health Inc 2021-07-22 Not applicable Canada Relpax Tablet 20 mg Oral Bgp Pharma Ulc 2004-10-13 Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-eletriptan Tablet 20 mg Oral Apotex Corporation 2013-09-12 Not applicable Canada Apo-eletriptan Tablet 40 mg Oral Apotex Corporation 2013-09-12 Not applicable Canada Apo-eletriptan Tablets Tablet 40 mg Oral Apotex Corporation 2022-06-01 Not applicable Canada Apo-eletriptan Tablets Tablet 20 mg Oral Apotex Corporation 2022-06-01 Not applicable Canada Auro-eletriptan Tablet 40 mg Oral Auro Pharma Inc 2019-02-01 Not applicable Canada
Categories
- ATC Codes
- N02CC06 — Eletriptan
- Drug Categories
- Agents that produce hypertension
- Amines
- Analgesics
- Antidepressive Agents
- Antimigraine Preparations
- Biogenic Amines
- Biogenic Monoamines
- Central Nervous System Depressants
- Cytochrome P-450 CYP2A6 Inducers
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Substrates
- Heterocyclic Compounds, Fused-Ring
- Indoles
- Nervous System
- Neurotransmitter Agents
- P-glycoprotein substrates
- Selective Serotonin 5-HT1 Receptor Agonists
- Selective Serotonin Agonists
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin 1b Receptor Agonists
- Serotonin 1d Receptor Agonists
- Serotonin 5-HT1 Receptor Agonists
- Serotonin Agents
- Serotonin Modulators
- Serotonin Receptor Agonists
- Serotonin-1b and Serotonin-1d Receptor Agonist
- Triptans
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as 3-alkylindoles. These are compounds containing an indole moiety that carries an alkyl chain at the 3-position.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Indoles and derivatives
- Sub Class
- Indoles
- Direct Parent
- 3-alkylindoles
- Alternative Parents
- Benzenesulfonyl compounds / Aralkylamines / Substituted pyrroles / N-alkylpyrrolidines / Sulfones / Heteroaromatic compounds / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Organic oxides show 1 more
- Substituents
- 3-alkylindole / Amine / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Benzenesulfonyl group / Benzenoid / Heteroaromatic compound / Hydrocarbon derivative / Monocyclic benzene moiety show 14 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- sulfone, indoles, N-alkylpyrrolidine (CHEBI:50922)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 22QOO9B8KI
- CAS number
- 143322-58-1
- InChI Key
- PWVXXGRKLHYWKM-LJQANCHMSA-N
- InChI
- InChI=1S/C22H26N2O2S/c1-24-12-5-6-19(24)15-18-16-23-22-10-9-17(14-21(18)22)11-13-27(25,26)20-7-3-2-4-8-20/h2-4,7-10,14,16,19,23H,5-6,11-13,15H2,1H3/t19-/m1/s1
- IUPAC Name
- 5-[2-(benzenesulfonyl)ethyl]-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-1H-indole
- SMILES
- CN1CCC[C@@H]1CC1=CNC2=C1C=C(CCS(=O)(=O)C1=CC=CC=C1)C=C2
References
- Synthesis Reference
Ronald Ogilvie, "Process for the preparation of eletriptan." U.S. Patent US20050059828, issued March 17, 2005.
US20050059828- General References
- FDA Approved Drug Products: RELPAX (eletriptan hydrobromide) tablets [Link]
- External Links
- Human Metabolome Database
- HMDB0014361
- KEGG Drug
- D07887
- PubChem Compound
- 77993
- PubChem Substance
- 46506380
- ChemSpider
- 70379
- BindingDB
- 50103594
- 231049
- ChEBI
- 50922
- ChEMBL
- CHEMBL1510
- ZINC
- ZINC000003823475
- Therapeutic Targets Database
- DAP000008
- PharmGKB
- PA134687947
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Eletriptan
- FDA label
- Download (148 KB)
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 4 Completed Other Workplace Migraine Treatment 1 4 Completed Prevention Migraine 1 4 Completed Treatment Migraine 3 3 Completed Treatment Migraine 1 3 Completed Treatment Migraine Headache, With or Without Aura 4
Pharmacoeconomics
- Manufacturers
- Pfizer ireland pharmaceuticals
- Packagers
- Chunghwa Chemical Synthesis and Biotech Co. Ltd.
- Pfizer Inc.
- Physicians Total Care Inc.
- Rebel Distributors Corp.
- US Pharmaceutical Group
- Dosage Forms
Form Route Strength Tablet, film coated Oral 20 MG Tablet, film coated Oral 40 MG Tablet, film coated Oral 20 mg/1 Tablet Oral 80.000 mg Tablet Oral 40.000 mg Tablet Oral Tablet Oral 20 mg Tablet Oral 40 mg Tablet, film coated Oral 40 mg/1 Tablet, coated Oral 40 mg Tablet, film coated Oral Tablet, film coated Oral 80 mg - Prices
Unit description Cost Unit Relpax 6 20 mg tablet Box 156.05USD box Relpax 6 40 mg tablet Box 156.05USD box Relpax 20 mg tablet 25.01USD tablet Relpax 40 mg tablet 25.01USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2352392 No 2006-01-24 2019-11-01 Canada CA2198599 No 2000-06-06 2015-05-17 Canada US5545644 No 1996-08-13 2016-12-26 US 
US6110940 No 2000-08-29 2017-08-29 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Readily soluble as hydrobromide formulation Not Available logP 3.9 Not Available - Predicted Properties
Property Value Source Water Solubility 0.00118 mg/mL ALOGPS logP 3.84 ALOGPS logP 3.77 Chemaxon logS -5.5 ALOGPS pKa (Strongest Acidic) 16.56 Chemaxon pKa (Strongest Basic) 8.37 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 53.17 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 110.94 m3·mol-1 Chemaxon Polarizability 42.99 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9872 Blood Brain Barrier + 0.9774 Caco-2 permeable - 0.628 P-glycoprotein substrate Substrate 0.6308 P-glycoprotein inhibitor I Non-inhibitor 0.8046 P-glycoprotein inhibitor II Non-inhibitor 0.8383 Renal organic cation transporter Inhibitor 0.7 CYP450 2C9 substrate Non-substrate 0.6591 CYP450 2D6 substrate Non-substrate 0.9115 CYP450 3A4 substrate Substrate 0.643 CYP450 1A2 substrate Non-inhibitor 0.7021 CYP450 2C9 inhibitor Non-inhibitor 0.8103 CYP450 2D6 inhibitor Non-inhibitor 0.7615 CYP450 2C19 inhibitor Non-inhibitor 0.7519 CYP450 3A4 inhibitor Non-inhibitor 0.6355 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6986 Ames test Non AMES toxic 0.5945 Carcinogenicity Non-carcinogens 0.8556 Biodegradation Not ready biodegradable 0.9883 Rat acute toxicity 2.5492 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.6436 hERG inhibition (predictor II) Inhibitor 0.7581
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-001i-9110000000-bef75cdb82e945554b4a Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-001i-0009000000-fa579ac6613cd384caea Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-001i-0009000000-2842335345e50729f81f Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-001i-1049000000-d0631600b8fc7f389120 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-001i-0329000000-32fc70bc10331ef74e6c Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-003r-5923000000-82431fdde65c0d0e0a8a Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0aou-4915000000-6466713f4780366f34b1 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]- 204.5012312 predictedDarkChem Lite v0.1.0 [M-H]- 205.6329312 predictedDarkChem Lite v0.1.0 [M-H]- 185.27248 predictedDeepCCS 1.0 (2019) [M+H]+ 205.2502312 predictedDarkChem Lite v0.1.0 [M+H]+ 206.5549312 predictedDarkChem Lite v0.1.0 [M+H]+ 187.76917 predictedDeepCCS 1.0 (2019) [M+Na]+ 204.9878312 predictedDarkChem Lite v0.1.0 [M+Na]+ 195.0475 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
- Gene Name
- HTR1D
- Uniprot ID
- P28221
- Uniprot Name
- 5-hydroxytryptamine receptor 1D
- Molecular Weight
- 41906.38 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Napier C, Stewart M, Melrose H, Hopkins B, McHarg A, Wallis R: Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol. 1999 Mar 5;368(2-3):259-68. [Article]
- Wackenfors A, Jarvius M, Ingemansson R, Edvinsson L, Malmsjo M: Triptans induce vasoconstriction of human arteries and veins from the thoracic wall. J Cardiovasc Pharmacol. 2005 May;45(5):476-84. [Article]
- Johnson DE, Rollema H, Schmidt AW, McHarg AD: Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain. Eur J Pharmacol. 2001 Aug 17;425(3):203-10. [Article]
- Strijbos PJ, Parsons AA, Fugelli A: Eletriptan Pfizer. Curr Opin Investig Drugs. 2002 Sep;3(9):1359-68. [Article]
- Tfelt-Hansen P, De Vries P, Saxena PR: Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. Drugs. 2000 Dec;60(6):1259-87. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
- Gene Name
- HTR1B
- Uniprot ID
- P28222
- Uniprot Name
- 5-hydroxytryptamine receptor 1B
- Molecular Weight
- 43567.535 Da
References
- Napier C, Stewart M, Melrose H, Hopkins B, McHarg A, Wallis R: Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol. 1999 Mar 5;368(2-3):259-68. [Article]
- van den Broek RW, MaassenVanDenBrink A, de Vries R, Bogers AJ, Stegmann AP, Avezaat CJ, Saxena PR: Pharmacological analysis of contractile effects of eletriptan and sumatriptan on human isolated blood vessels. Eur J Pharmacol. 2000 Oct 27;407(1-2):165-73. [Article]
- Knyihar-Csillik E, Tajti J, Csillik AE, Chadaide Z, Mihaly A, Vecsei L: Effects of eletriptan on the peptidergic innervation of the cerebral dura mater and trigeminal ganglion, and on the expression of c-fos and c-jun in the trigeminal complex of the rat in an experimental migraine model. Eur J Neurosci. 2000 Nov;12(11):3991-4002. [Article]
- Johnson DE, Rollema H, Schmidt AW, McHarg AD: Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain. Eur J Pharmacol. 2001 Aug 17;425(3):203-10. [Article]
- Lambert GA, Boers PM, Hoskin KL, Donaldson C, Zagami AS: Suppression by eletriptan of the activation of trigeminovascular sensory neurons by glyceryl trinitrate. Brain Res. 2002 Oct 25;953(1-2):181-8. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that trig...
- Gene Name
- HTR1F
- Uniprot ID
- P30939
- Uniprot Name
- 5-hydroxytryptamine receptor 1F
- Molecular Weight
- 41708.505 Da
References
- Napier C, Stewart M, Melrose H, Hopkins B, McHarg A, Wallis R: Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol. 1999 Mar 5;368(2-3):259-68. [Article]
- Bhalla P, Sharma HS, Wurch T, Pauwels PJ, Saxena PR: Molecular cloning and expression of the porcine trigeminal ganglion cDNA encoding a 5-ht(1F) receptor. Eur J Pharmacol. 2002 Feb 1;436(1-2):23-33. [Article]
- Jahnichen S, Radtke OA, Pertz HH: Involvement of 5-HT1B receptors in triptan-induced contractile responses in guinea-pig isolated iliac artery. Naunyn Schmiedebergs Arch Pharmacol. 2004 Jul;370(1):54-63. Epub 2004 Jun 8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
- Gene Name
- HTR1A
- Uniprot ID
- P08908
- Uniprot Name
- 5-hydroxytryptamine receptor 1A
- Molecular Weight
- 46106.335 Da
References
- Johnson DE, Rollema H, Schmidt AW, McHarg AD: Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain. Eur J Pharmacol. 2001 Aug 17;425(3):203-10. [Article]
Enzymes
- 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
References
- Evans DC, O'Connor D, Lake BG, Evers R, Allen C, Hargreaves R: Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein. Drug Metab Dispos. 2003 Jul;31(7):861-9. [Article]
- Kim YK, Shin KH, Alderman J, Yu KS, Jang IJ, Lee S: Pharmacokinetics and tolerability of eletriptan hydrobromide in healthy Korean subjects. Drug Des Devel Ther. 2018 Feb 19;12:331-337. doi: 10.2147/DDDT.S149119. eCollection 2018. [Article]
- 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
- 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. [Article]
- Capi M, Curto M, Lionetto L, de Andres F, Gentile G, Negro A, Martelletti P: Eletriptan in the management of acute migraine: an update on the evidence for efficacy, safety, and consistent response. Ther Adv Neurol Disord. 2016 Sep;9(5):414-23. doi: 10.1177/1756285616650619. Epub 2016 Jun 3. [Article]
- 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
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- 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
- Pichard-Garcia L, Hyland R, Baulieu J, Fabre JM, Milton A, Maurel P: Human hepatocytes in primary culture predict lack of cytochrome P-450 3A4 induction by eletriptan in vivo. Drug Metab Dispos. 2000 Jan;28(1):51-7. [Article]
- Kind
- Protein
- Organism
- Humans
- 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 gas...
- Gene Name
- PTGS1
- Uniprot ID
- P23219
- Uniprot Name
- Prostaglandin G/H synthase 1
- Molecular Weight
- 68685.82 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
References
- 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. [Article]
- Evans DC, O'Connor D, Lake BG, Evers R, Allen C, Hargreaves R: Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein. Drug Metab Dispos. 2003 Jul;31(7):861-9. [Article]
- Eletriptan FDA label [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Evans DC, O'Connor D, Lake BG, Evers R, Allen C, Hargreaves R: Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein. Drug Metab Dispos. 2003 Jul;31(7):861-9. [Article]
- Tepper SJ: Safety and rational use of the triptans. Med Clin North Am. 2001 Jul;85(4):959-70. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55