ELETRIPTAN MESYLATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C22H26N2O2S.CH4O3S
Molecular Weight	478.625
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CS(O)(=O)=O.CN1CCC[C@@H]1CC2=CNC3=C2C=C(CCS(=O)(=O)C4=CC=CC=C4)C=C3

InChI

InChIKey=ONTTXXMBZRRMPL-FSRHSHDFSA-N

InChI=1S/C22H26N2O2S.CH4O3S/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;1-5(2,3)4/h2-4,7-10,14,16,19,23H,5-6,11-13,15H2,1H3;1H3,(H,2,3,4)/t19-;/m1./s1

HIDE SMILES / InChI

Molecular Formula	CH4O3S
Molecular Weight	96.106
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C22H26N2O2S
Molecular Weight	382.519
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdf
Curator's Comment: Description was created using several sources including: https://www.ncbi.nlm.nih.gov/pubmed/10193663 | http://www.migraines.org/treatment/pro_rlpx.htm

Eletriptan (eletriptan hydrobromide, trade name Relpax) is a selective 5-hydroxytryptamine (5-HT1B/1D) serotonin receptor agonist (triptan) indicated for the acute treatment of migraine with or without aura in adults. Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, and has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors. The therapeutic activity of eletriptan for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release. Eletriptan (Relpax) has been approved for use in the acute treatment of migraine in 51 countries and has been introduced in 17 countries including Mexico, Italy, France and Japan.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
5-hydroxytryptamine receptor 1D 17 Target ID: P28221 Gene ID: 3352.0 Gene Symbol: HTR1D Target Organism: Homo sapiens (Human) Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdf	Agonist 2637	0.92 nM [Kd]
5-hydroxytryptamine receptor 1B 21 Target ID: P28222 Gene ID: 3351.0 Gene Symbol: HTR1B Target Organism: Homo sapiens (Human) Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdf	Agonist 2637	3.14 nM [Kd]
5-hydroxytryptamine receptor 1F 8 Target ID: P30939 Gene ID: 3355.0 Gene Symbol: HTR1F Target Organism: Homo sapiens (Human) Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/11834243	Agonist 2637

Conditions

Condition	Modality	Targets	Highest Phase	Product
Migraine 103 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdf	Primary		Approved 8307	RELPAX Approved Use RELPAX is indicated for the acute treatment of migraine with or without aura in adults. RELPAX is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. Safety and effectiveness of RELPAX Tablets have not been established for cluster headache, which is present in an older, predominantly male population. Launch Date 1.04086077E12

C_max

Value	Dose	Analyte	Population
183.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
200.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
46.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
94.72 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

AUC

Value	Dose	Analyte	Population
1278 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
1282 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
291.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
575.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

T_1/2

Value	Dose	Analyte	Population
4.75 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
4.58 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
4.92 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
4.63 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29497279	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	ELETRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
15% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021016s021s023s024s027lbl.pdf			ELETRIPTAN plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	Disc. AE: Nausea, Dizziness... AEs leading to discontinuation/dose reduction: Nausea (0.4%) Dizziness (0.4%) Asthenia (0.3%) Chest pain (0.3%) Headache (0.2%) Vomiting (0.2%) Hypertonia (0.2%) Paresthesia (0.2%) Somnolence (0.2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102

AEs

AE	Significance	Dose	Population
Headache	0.2% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Hypertonia	0.2% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Paresthesia	0.2% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Somnolence	0.2% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Vomiting	0.2% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Asthenia	0.3% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Chest pain	0.3% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Dizziness	0.4% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102
Nausea	0.4% Disc. AE	80 mg 1 times / day single, oral (typical) Recommended Dose: 80 mg, 1 times / day Route: oral Route: single Dose: 80 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102	unhealthy, 41.9 n = 312 Health Status: unhealthy Condition: migraine Age Group: 41.9 Sex: M+F Population Size: 312 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_Medr_P3.pdf Page: Study 102

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1670 inhibitor 1532 inducer 753	inhibitor 1695 inducer 372	substrate 1168 inhibitor 1789 inducer 97

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2C19 1410 CYP1A2 1463 CYP2B6 770 CYP2E1 846	CYP1A 22 P-gp 1491	CYP2A6 79 CYP1A2 671 CYP2C19 283 CYP2E1 121

Drug as perpetrator

Target	Modality	Activity
CYP2A6 702	inducer 1515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	likely
CYP2B6 946	inhibitor 3185 Sources: https://dmd.aspetjournals.org/content/31/7/861.long Page: 7,8	little
CYP2C19 1484	inhibitor 3185 Sources: https://dmd.aspetjournals.org/content/31/7/861.long Page: 7,8	little
CYP1A2 1620	inducer 1515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP1A2 1620	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	no
CYP2C19 1484	inducer 1515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP2C9 1747	inducer 1515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP2C9 1747	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	no
CYP2D6 1826	inducer 1515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP2E1 929	inducer 1515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=78 Page: 78.0	no
CYP2E1 929	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	no
CYP3A4 1857	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	no
CYP2D6 1826	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	yes [IC50 41 uM]
CYP3A4 1857	inducer 1515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=77 Page: 77.0	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
P-gp 1491	substrate 3264 Sources: https://dmd.aspetjournals.org/content/31/7/861.long Page: 9.0	inconclusive
CYP3A4 1670	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=9 Page: 9.0	major	yes (co-administration study) Comment: when administered with ketoconazole, Cmax and AUC increased by 2.7-fold and 5.9-fold, respectively; when administered with verapamil, Cmax and AUC increased by 2.2-fold and 2.7-fold, respectively; when administered with fluconazole, Cmax and AUC increased by 1.4-fold and 2-fold, respectively; Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=9 Page: 9.0
CYP1A 22	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=9 Page: 9.0	minor
CYP2D6 1168	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax_BioPharmr.pdf#page=9 Page: 9.0	minor

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:50922	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:50922
ChemicalBook	CB1404591	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB1404591
MolPort	MolPort-005-940-717	https://www.molport.com/shop/molecule-link/MolPort-005-940-717
ZINC	ZINC000003823475	http://zinc15.docking.org/substances/ZINC000003823475
eMolecules	30512783	https://www.emolecules.com/cgi-bin/more?vid=30512783

PubMed

Title	Date	PubMed
Comparative aspects of triptans in treating migraine.	2001	12739316
Eletriptan: pharmacological differences and clinical results.	2001	12463280
Safety and rational use of the triptans.	2001 Jul	11480267
Establishing a standard of speed for assessing the efficacy of the serotonin(1B/1D) agonists (triptans).	2001 Jul	11448293
Craniovascular selectivity of eletriptan and sumatriptan in human isolated blood vessels.	2001 Jul 10	11445657
[New potent serotonin receptor agonist. Helps migraine patients even when other triptans fail].	2001 Jul 5	11481924
Pharmacology and efficacy of eletriptan for the treatment of migraine attacks.	2001 Jun	11452689
[Eletriptan shortly before drug approval. Fewer problems in migraine therapy].	2001 May 28	11434261
Eletriptan.	2001 Oct	11772292
Advances in pharmacological treatment of migraine.	2001 Oct	11772289
Efficacy, tolerability and safety of oral eletriptan and ergotamine plus caffeine (Cafergot) in the acute treatment of migraine: a multicentre, randomised, double-blind, placebo-controlled comparison.	2002	11844898
Efficacy, safety and tolerability of oral eletriptan in the acute treatment of migraine: results of a phase III, multicentre, placebo-controlled study across three attacks.	2002 Feb	11993610
[Migraine has to be treated. Otherwise a stroke threatens].	2002 Feb 14	11887744
[New triptanes in control of migraine attacks. More rapid onset of action--more efficient reduction of pain].	2002 Jan 24	11862794
Agonist-directed trafficking explaining the difference between response pattern of naratriptan and sumatriptan in rabbit common carotid artery.	2002 May	12010764
Triptans (serotonin, 5-HT1B/1D agonists) in migraine: detailed results and methods of a meta-analysis of 53 trials.	2002 Oct	12383060
New medications show promise for migraine sufferers.	2002 Oct	12382492
Eletriptan Pfizer.	2002 Sep	12498013
Gateways to Clinical Trials.	2002 Sep	12428432
Current perspectives on effective migraine treatments: are small clinical differences important for patients?	2003	15071619
Newer formulations of the triptans: advances in migraine management.	2003	14524731
Pharmacological approaches to migraine.	2003	12830928
[Strong and sustained-acting triptan. Therewith migraine does not return soon].	2003 Aug 7	14524078
[Treatment of migraine: an update].	2003 Jan	15095723
[Pharmacological, pharmacokinetic and clinical profile of eletriptan (Relpax), a new triptan for migraine].	2003 Jul	12843576
Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein.	2003 Jul	12814962
Eletriptan for the treatment of migraine in patients with previous poor response or tolerance to oral sumatriptan.	2003 Jul	12807526
Safety profile of the triptans.	2003 Mar	12904112
Musing on Mathew et al.	2003 Sep	14562838
Encapsulated sumatriptan is not bioequivalent to commercial sumatriptan.	2003 Sep	14562837
Unilateral time-delayed encapsulation does not make for a fair race.	2003 Sep	12940818
Meta-analysis of oral triptans.	2004 Aug	15265060
The 40-mg dose of eletriptan: comparative efficacy and tolerability versus sumatriptan 100 mg.	2004 Feb	14748774
[Recent progress in therapy for migraine headache].	2004 Feb 10	15007953
Neuronal expression and regulation of CGRP promoter activity following viral gene transfer into cultured trigeminal ganglia neurons.	2004 Jan 30	14715155
Effect of high-dose intravenous eletriptan on coronary artery diameter.	2004 Jul	15196292
Involvement of 5-HT1B receptors in triptan-induced contractile responses in guinea-pig isolated iliac artery.	2004 Jul	15185063
Nitrergic and glutamatergic neuronal mechanisms at the trigeminovascular first-order synapse.	2004 Jul	15165837
Gateways to clinical trials.	2004 Jul-Aug	15349141
Triptans and CNS side-effects: pharmacokinetic and metabolic mechanisms.	2004 Jun	15154851
Gateways to clinical trials.	2004 Mar	15071612
Eletriptan for the acute treatment of migraine: results of bridging a Japanese study to Western clinical trials.	2004 Mar	15025836
[A case of the usefulness of MR angiography and diffusion weighted image to evaluate migraine].	2004 Oct	15529793
[Meta-analysis of triptan treatment in migraine].	2004 Sep	15552863
[Triptans in migraine: from clinical view].	2004 Sep	15552862
[Triptans in migraine: a comparative review of pharmacology, pharmacokinetics].	2004 Sep	15552861
Gateways to clinical trials.	2004 Sep	15538546
TRIPSTAR: prioritizing oral triptan treatment attributes in migraine management.	2004 Sep	15285768

Patents

Sample Use Guides

In Vivo Use Guide

The maximum recommended single dose of Relpax (eletriptan hydrobromide) is 40 mg. If after the initial dose, headache improves but then returns, a repeat dose may be beneficial. If a second dose is required, it should be taken at least 2 hours after the initial dose. If the initial dose is ineffective, controlled clinical trials have not shown a benefit of a second dose to treat the same attack. The maximum daily dose should not exceed 80 mg.

Route of Administration: Oral

In Vitro Use Guide

The 5-hydroxytryptamine (5-HT) receptor mediation of the contraction in guinea-pig iliac arteries moderately precontracted by prostaglandin F2alpha (PGF2alpha) was characterized in vitro using eletriptan. Eletriptan contracted guinea-pig iliac arteries and the concentration-response curve for eletriptan was biphasic (first phase: 0.01-3 uM, pD2 approximately 6.6; second phase: greater or equal 10 uM).

Substance Class	Chemical Created by `admin` on `Sun Dec 18 08:46:56 UTC 2022` Edited by `admin` on `Sun Dec 18 08:46:56 UTC 2022`
Record UNII	607KP935Y1
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ELETRIPTAN MESYLATE

Common Name

English

1H-INDOLE, 3-(((2R)-1-METHYL-2-PYRROLIDINYL)METHYL)-5-(2-(PHENYLSULFONYL)ETHYL)-, METHANESULFONATE (1:1)

Systematic Name

English

Code System Code Type Description

CAS

1261286-61-6

Created by admin on Sun Dec 18 08:46:57 UTC 2022 , Edited by admin on Sun Dec 18 08:46:57 UTC 2022

PRIMARY

FDA UNII

607KP935Y1

Created by admin on Sun Dec 18 08:46:57 UTC 2022 , Edited by admin on Sun Dec 18 08:46:57 UTC 2022

PRIMARY

PUBCHEM

49857984

Created by admin on Sun Dec 18 08:46:57 UTC 2022 , Edited by admin on Sun Dec 18 08:46:57 UTC 2022

PRIMARY

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ACTIVE MOIETY

Details

SMILES

InChI

DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdfCurator's Comment: Description was created using several sources including: https://www.ncbi.nlm.nih.gov/pubmed/10193663 | http://www.migraines.org/treatment/pro_rlpx.htm

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Cmax

AUC

T1/2

Funbound

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Sourcing

PubMed

Patents

Sample Use Guides

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21016_relpax_lbl.pdf
Curator's Comment: Description was created using several sources including: https://www.ncbi.nlm.nih.gov/pubmed/10193663 | http://www.migraines.org/treatment/pro_rlpx.htm

C_max

T_1/2

F_unbound

Drug as perpetrator