Identification

Name
Eletriptan
Accession Number
DB00216  (APRD00945)
Type
Small Molecule
Groups
Approved, Investigational
Description

Eletriptan is a second generation triptan drug developed by Pfizer Inc for the treatment of migraine headaches. [Wikipedia]

Structure
Thumb
Synonyms
  • Eletriptanum
Product Ingredients
IngredientUNIICASInChI Key
Eletriptan hydrobromideM41W832TA3177834-92-3UTINOWOSWSPFLJ-FSRHSHDFSA-N
Eletriptan hydrobromide monohydrate4139X692FA273211-28-2BORDVONYOHPTGR-JQDLGSOUSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EletriptanTablet, film coated40 mg/1OralGreenstone, Llc2017-07-24Not applicableUs
EletriptanTablet, film coated20 mg/1OralGreenstone, Llc2017-07-24Not applicableUs
Gd-eletriptanTablet20 mgOralGenmed A Division Of Pfizer Canada Inc2012-10-11Not applicableCanada
Gd-eletriptanTablet40 mgOralGenmed A Division Of Pfizer Canada Inc2012-10-11Not applicableCanada
PMS-eletriptanTablet20 mgOralPharmascience Inc2014-11-26Not applicableCanada
PMS-eletriptanTablet40 mgOralPharmascience Inc2014-11-26Not applicableCanada
RelpaxTablet, film coated40 mg/1OralPhysicians Total Care, Inc.2007-11-19Not applicableUs
RelpaxTablet, film coated20 mg/1OralRoerig2002-12-26Not applicableUs00049 2330 45 nlmimage10 3c1c9e04
RelpaxTablet40 mgOralPfizer2004-10-13Not applicableCanada
RelpaxTablet, film coated40 mg/1OralRebel Distributors2002-12-26Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-eletriptanTablet20 mgOralApotex Corporation2013-09-12Not applicableCanada
Apo-eletriptanTablet40 mgOralApotex Corporation2013-09-12Not applicableCanada
Eletriptan hydrobromideTablet, film coated20 mg/1OralZydus Pharmaceuticals Usa, Inc.2017-07-12Not applicableUs
Eletriptan HydrobromideTablet, film coated20 mg/1OralMylan Pharmaceuticals2017-08-15Not applicableUs
Eletriptan HydrobromideTablet, film coated40 mg/1OralTeva2017-07-21Not applicableUs
Eletriptan hydrobromideTablet, film coated40 mg/1OralCadila Pharnmaceuticals2017-07-12Not applicableUs
Eletriptan HydrobromideTablet, film coated20 mg/1OralAmneal Pharmaceuticals2017-09-01Not applicableUs
Eletriptan hydrobromideTablet, film coated40 mg/1OralZydus Pharmaceuticals Usa, Inc.2017-07-12Not applicableUs
Eletriptan HydrobromideTablet, film coated40 mg/1OralMylan Pharmaceuticals2017-08-15Not applicableUs
Eletriptan HydrobromideTablet, film coated20 mg/1OralAjanta Pharma Limited2017-08-29Not applicableUs
Categories
UNII
22QOO9B8KI
CAS number
143322-58-1
Weight
Average: 382.519
Monoisotopic: 382.171498776
Chemical Formula
C22H26N2O2S
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[[email protected]@H]1CC1=CNC2=C1C=C(CCS(=O)(=O)C1=CC=CC=C1)C=C2

Pharmacology

Indication

For the acute treatment of migraine with or without aura in adults.

Structured Indications
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. Eletriptan has no significant affinity or pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors. Two theories have been proposed to explain the efficacy of 5-HT receptor agonists in migraine. One theory suggests that activation of 5-HT1 receptors located on intracranial blood vessels, including those on the arteriovenous anastomoses, leads to vasoconstriction, which is correlated with the relief of migraine headache. The other hypothesis suggests that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.

TargetActionsOrganism
A5-hydroxytryptamine receptor 1D
agonist
Human
A5-hydroxytryptamine receptor 1B
agonist
Human
A5-hydroxytryptamine receptor 1F
agonist
Human
U5-hydroxytryptamine receptor 1A
agonist
Human
U5-hydroxytryptamine receptor 1E
agonist
Human
U5-hydroxytryptamine receptor 2B
agonist
Human
U5-hydroxytryptamine receptor 7
agonist
Human
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.

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
Toxicity

Based on the pharmacology of the 5-HT1B/1D agonists, hypertension or other more serious cardiovascular symptoms could occur on overdose.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3---(T;T) / (C;T)T AlleleEffect Directly StudiedPatients with this genotype have an increased likelihood of responding to elitriptan when treating (condition: cluster headache).Details

Interactions

Drug Interactions
DrugInteractionDrug group
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe metabolism of Eletriptan can be decreased when combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.Experimental
AbirateroneThe serum concentration of Eletriptan can be increased when it is combined with Abiraterone.Approved
AcepromazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Aceprometazine.Approved
AcetophenazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Acetophenazine.Approved
AlmotriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Almotriptan.Approved, Investigational
AmiodaroneThe serum concentration of Eletriptan can be increased when it is combined with Amiodarone.Approved, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Amisulpride.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Amitriptyline.Approved
AmoxapineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Amoxapine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Amperozide.Experimental
AprepitantThe serum concentration of Eletriptan can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Eletriptan.Approved, Investigational
ArmodafinilThe metabolism of Eletriptan can be decreased when combined with Armodafinil.Approved, Investigational
ArtemetherThe metabolism of Eletriptan can be decreased when combined with Artemether.Approved
AsenapineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Asenapine.Approved
AtazanavirThe serum concentration of Eletriptan can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe serum concentration of Eletriptan can be increased when it is combined with Atomoxetine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Azaperone.Investigational, Vet Approved
BenmoxinThe metabolism of Eletriptan can be decreased when combined with Benmoxin.Withdrawn
BenperidolThe risk or severity of adverse effects can be increased when Eletriptan is combined with Benperidol.Investigational
BetaxololThe metabolism of Eletriptan can be decreased when combined with Betaxolol.Approved
BifeprunoxThe risk or severity of adverse effects can be increased when Eletriptan is combined with Bifeprunox.Investigational
BoceprevirThe serum concentration of Eletriptan can be increased when it is combined with Boceprevir.Approved, Withdrawn
BortezomibThe serum concentration of Eletriptan can be increased when it is combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Eletriptan can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe risk or severity of adverse effects can be increased when Eletriptan is combined with Brexpiprazole.Approved
BrofaromineThe serum concentration of Eletriptan can be increased when it is combined with Brofaromine.Experimental
BromocriptineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Bromocriptine.Approved, Investigational
BromperidolThe risk or severity of adverse effects can be increased when Eletriptan is combined with Bromperidol.Investigational
BupropionThe metabolism of Eletriptan can be decreased when combined with Bupropion.Approved
BuspironeThe risk or severity of adverse effects can be increased when Eletriptan is combined with Buspirone.Approved, Investigational
ButaperazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Butaperazine.Experimental
CabergolineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Cabergoline.Approved
CapecitabineThe metabolism of Eletriptan can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Eletriptan can be increased when combined with Carbamazepine.Approved, Investigational
CariprazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Cariprazine.Approved
CaroxazoneThe metabolism of Eletriptan can be decreased when combined with Caroxazone.Withdrawn
CelecoxibThe metabolism of Eletriptan can be decreased when combined with Celecoxib.Approved, Investigational
ChloramphenicolThe metabolism of Eletriptan can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChlorproethazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Chlorproethazine.Experimental
CholecalciferolThe metabolism of Eletriptan can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CinacalcetThe metabolism of Eletriptan can be decreased when combined with Cinacalcet.Approved
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Eletriptan.Approved
ClarithromycinThe serum concentration of Eletriptan can be increased when it is combined with Clarithromycin.Approved
ClemastineThe serum concentration of Eletriptan can be increased when it is combined with Clemastine.Approved
ClobazamThe metabolism of Eletriptan can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Clomipramine.Approved, Vet Approved
ClopenthixolThe risk or severity of adverse effects can be increased when Eletriptan is combined with Clopenthixol.Experimental
ClothiapineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Clothiapine.Experimental
ClotrimazoleThe serum concentration of Eletriptan can be increased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Eletriptan can be decreased when combined with Clozapine.Approved
CocaineThe metabolism of Eletriptan can be decreased when combined with Cocaine.Approved, Illicit
CrisaboroleThe metabolism of Eletriptan can be decreased when combined with Crisaborole.Approved
CrizotinibThe serum concentration of Eletriptan can be increased when it is combined with Crizotinib.Approved
CyamemazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Cyamemazine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Cyclobenzaprine.Approved
CyclosporineThe serum concentration of Eletriptan can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Eletriptan can be decreased when it is combined with Dabrafenib.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Eletriptan is combined with Dapiprazole.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Eletriptan.Investigational
DarifenacinThe metabolism of Eletriptan can be decreased when combined with Darifenacin.Approved, Investigational
DasatinibThe serum concentration of Eletriptan can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Eletriptan can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe serum concentration of Eletriptan can be increased when it is combined with Delavirdine.Approved
DesipramineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Desipramine.Approved
DesvenlafaxineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Desvenlafaxine.Approved
DextromethorphanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Dextromethorphan.Approved
DihydroergotamineThe serum concentration of Eletriptan can be increased when it is combined with Dihydroergotamine.Approved
DiltiazemThe serum concentration of Eletriptan can be increased when it is combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Eletriptan can be decreased when combined with Diphenhydramine.Approved
DixyrazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Dixyrazine.Experimental
DolasetronDolasetron may increase the serotonergic activities of Eletriptan.Approved
DosulepinThe metabolism of Eletriptan can be decreased when combined with Dosulepin.Approved
DoxepinThe risk or severity of adverse effects can be increased when Eletriptan is combined with Doxepin.Approved
DoxycyclineThe serum concentration of Eletriptan can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe serum concentration of Eletriptan can be increased when it is combined with Dronedarone.Approved
DroperidolThe risk or severity of adverse effects can be increased when Eletriptan is combined with Droperidol.Approved, Vet Approved
DroxidopaEletriptan may increase the hypertensive activities of Droxidopa.Approved, Investigational
DuloxetineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Duloxetine.Approved
EcopipamThe risk or severity of adverse effects can be increased when Eletriptan is combined with Ecopipam.Investigational
EfavirenzThe metabolism of Eletriptan can be decreased when combined with Efavirenz.Approved, Investigational
EliglustatThe metabolism of Eletriptan can be decreased when combined with Eliglustat.Approved
EnzalutamideThe serum concentration of Eletriptan can be decreased when it is combined with Enzalutamide.Approved
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Eletriptan is combined with Ergoloid mesylate.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Ergonovine.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Ergotamine.Approved
ErythromycinThe serum concentration of Eletriptan can be increased when it is combined with Erythromycin.Approved, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Eletriptan is combined with Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe metabolism of Eletriptan can be decreased when combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Eletriptan can be decreased when combined with Esomeprazole.Approved, Investigational
FencamfamineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Fencamfamine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Eletriptan is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FloxuridineThe metabolism of Eletriptan can be decreased when combined with Floxuridine.Approved
FluanisoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Fluanisone.Experimental
FluconazoleThe serum concentration of Eletriptan can be increased when it is combined with Fluconazole.Approved
FluorouracilThe metabolism of Eletriptan can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Eletriptan can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluspirileneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Fluspirilene.Approved, Investigational
FluvastatinThe metabolism of Eletriptan can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe serum concentration of Eletriptan can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe serum concentration of Eletriptan can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Eletriptan can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Eletriptan can be increased when combined with Fosphenytoin.Approved
FrovatriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Frovatriptan.Approved, Investigational
FurazolidoneThe metabolism of Eletriptan can be decreased when combined with Furazolidone.Approved, Investigational, Vet Approved
Fusidic AcidThe serum concentration of Eletriptan can be increased when it is combined with Fusidic Acid.Approved
GemfibrozilThe metabolism of Eletriptan can be decreased when combined with Gemfibrozil.Approved
GranisetronGranisetron may increase the serotonergic activities of Eletriptan.Approved, Investigational
HarmalineThe serum concentration of Eletriptan can be increased when it is combined with Harmaline.Experimental
HydracarbazineThe metabolism of Eletriptan can be decreased when combined with Hydracarbazine.Experimental
IdelalisibThe serum concentration of Eletriptan can be increased when it is combined with Idelalisib.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Iloperidone.Approved
ImatinibThe serum concentration of Eletriptan can be increased when it is combined with Imatinib.Approved
ImipramineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Imipramine.Approved
IndinavirThe serum concentration of Eletriptan can be increased when it is combined with Indinavir.Approved
IproclozideThe metabolism of Eletriptan can be decreased when combined with Iproclozide.Withdrawn
IproniazidThe metabolism of Eletriptan can be decreased when combined with Iproniazid.Withdrawn
IrbesartanThe metabolism of Eletriptan can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe serum concentration of Eletriptan can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsocarboxazidThe risk or severity of adverse effects can be increased when Eletriptan is combined with Isocarboxazid.Approved
IsoniazidThe metabolism of Eletriptan can be decreased when combined with Isoniazid.Approved
IsradipineThe serum concentration of Eletriptan can be increased when it is combined with Isradipine.Approved
ItraconazoleThe serum concentration of Eletriptan can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Eletriptan can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe serum concentration of Eletriptan can be increased when it is combined with Ketoconazole.Approved, Investigational
LeflunomideThe metabolism of Eletriptan can be decreased when combined with Leflunomide.Approved, Investigational
LevomilnacipranThe risk or severity of adverse effects can be increased when Eletriptan is combined with Levomilnacipran.Approved
LinezolidThe risk or severity of adverse effects can be increased when Eletriptan is combined with Linezolid.Approved, Investigational
LithiumThe risk or severity of adverse effects can be increased when Eletriptan is combined with Lithium.Approved
LobeglitazoneThe metabolism of Eletriptan can be decreased when combined with Lobeglitazone.Approved, Investigational
LopinavirThe serum concentration of Eletriptan can be increased when it is combined with Lopinavir.Approved
LorcaserinThe risk or severity of adverse effects can be increased when Eletriptan is combined with Lorcaserin.Approved
LovastatinThe serum concentration of Eletriptan can be increased when it is combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Loxapine.Approved
LuliconazoleThe serum concentration of Eletriptan can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Eletriptan can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Eletriptan can be decreased when combined with Lumefantrine.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Lurasidone.Approved
ManidipineThe metabolism of Eletriptan can be decreased when combined with Manidipine.Approved, Investigational
MaprotilineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Maprotiline.Approved
MebanazineThe metabolism of Eletriptan can be decreased when combined with Mebanazine.Withdrawn
MelperoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Melperone.Approved, Investigational
MesoridazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Mesoridazine.Approved, Investigational
MethadoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Methadone.Approved
MethotrimeprazineThe metabolism of Eletriptan can be decreased when combined with Methotrimeprazine.Approved
Methylene blueThe metabolism of Eletriptan can be decreased when combined with Methylene blue.Approved, Investigational
MethylergometrineMethylergometrine may increase the vasoconstricting activities of Eletriptan.Approved
MetoclopramideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Metoclopramide.Approved, Investigational
MidostaurinThe metabolism of Eletriptan can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Eletriptan can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Eletriptan is combined with Milnacipran.Approved
MinaprineThe metabolism of Eletriptan can be decreased when combined with Minaprine.Approved
MirabegronThe metabolism of Eletriptan can be decreased when combined with Mirabegron.Approved
MirtazapineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Mirtazapine.Approved
MitotaneThe serum concentration of Eletriptan can be decreased when it is combined with Mitotane.Approved
MoclobemideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Moclobemide.Approved
ModafinilThe metabolism of Eletriptan can be decreased when combined with Modafinil.Approved, Investigational
MolindoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Molindone.Approved
MoperoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Moperone.Experimental
MosapramineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Mosapramine.Experimental
NaratriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Naratriptan.Approved, Investigational
NefazodoneThe serum concentration of Eletriptan can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Eletriptan can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Eletriptan can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Eletriptan can be increased when it is combined with Nevirapine.Approved
NialamideThe metabolism of Eletriptan can be decreased when combined with Nialamide.Withdrawn
NicardipineThe metabolism of Eletriptan can be decreased when combined with Nicardipine.Approved
NilotinibThe serum concentration of Eletriptan can be increased when it is combined with Nilotinib.Approved, Investigational
NortriptylineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Nortriptyline.Approved
OctamoxinThe metabolism of Eletriptan can be decreased when combined with Octamoxin.Withdrawn
OlanzapineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Olanzapine.Approved, Investigational
OlaparibThe serum concentration of Eletriptan can be increased when it is combined with Olaparib.Approved
OndansetronOndansetron may increase the serotonergic activities of Eletriptan.Approved
OsanetantThe risk or severity of adverse effects can be increased when Eletriptan is combined with Osanetant.Investigational
OsimertinibThe serum concentration of Eletriptan can be increased when it is combined with Osimertinib.Approved
OxypertineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Oxypertine.Experimental
PalbociclibThe serum concentration of Eletriptan can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Paliperidone.Approved
PalonosetronPalonosetron may increase the serotonergic activities of Eletriptan.Approved, Investigational
PanobinostatThe serum concentration of Eletriptan can be increased when it is combined with Panobinostat.Approved, Investigational
PargylineThe metabolism of Eletriptan can be decreased when combined with Pargyline.Approved
ParoxetineThe metabolism of Eletriptan can be decreased when combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Eletriptan can be decreased when it is combined with Peginterferon alfa-2b.Approved
PenfluridolThe risk or severity of adverse effects can be increased when Eletriptan is combined with Penfluridol.Experimental
PentobarbitalThe metabolism of Eletriptan can be increased when combined with Pentobarbital.Approved, Vet Approved
PerazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Perazine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Eletriptan is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Perphenazine.Approved
PethidineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Pethidine.Approved
PhenelzineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Phenelzine.Approved
PheniprazineThe metabolism of Eletriptan can be decreased when combined with Pheniprazine.Withdrawn
PhenobarbitalThe metabolism of Eletriptan can be increased when combined with Phenobarbital.Approved
PhenoxypropazineThe metabolism of Eletriptan can be decreased when combined with Phenoxypropazine.Withdrawn
PhenytoinThe metabolism of Eletriptan can be increased when combined with Phenytoin.Approved, Vet Approved
PipamperoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Pipamperone.Approved, Investigational
PipotiazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Pipotiazine.Approved, Investigational
PirlindoleThe metabolism of Eletriptan can be decreased when combined with Pirlindole.Approved
PivhydrazineThe metabolism of Eletriptan can be decreased when combined with Pivhydrazine.Withdrawn
PosaconazoleThe serum concentration of Eletriptan can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Eletriptan can be increased when combined with Primidone.Approved, Vet Approved
ProcarbazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Procarbazine.Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Prochlorperazine.Approved, Vet Approved
PromazineThe metabolism of Eletriptan can be decreased when combined with Promazine.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Promethazine.Approved
PropericiazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Propericiazine.Approved
ProthipendylThe risk or severity of adverse effects can be increased when Eletriptan is combined with Prothipendyl.Investigational
ProtriptylineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Protriptyline.Approved
PyrimethamineThe metabolism of Eletriptan can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuetiapineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Quetiapine.Approved
QuinidineThe metabolism of Eletriptan can be decreased when combined with Quinidine.Approved
RacloprideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Raclopride.Investigational
RanolazineThe serum concentration of Eletriptan can be increased when it is combined with Ranolazine.Approved, Investigational
RasagilineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Rasagiline.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Remoxipride.Approved, Withdrawn
RifabutinThe metabolism of Eletriptan can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Eletriptan can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Eletriptan can be increased when combined with Rifapentine.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Risperidone.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Eletriptan is combined with Ritanserin.Investigational
RitonavirThe serum concentration of Eletriptan can be increased when it is combined with Ritonavir.Approved, Investigational
RizatriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Rizatriptan.Approved
RopiniroleThe metabolism of Eletriptan can be decreased when combined with Ropinirole.Approved, Investigational
SafrazineThe metabolism of Eletriptan can be decreased when combined with Safrazine.Withdrawn
SaquinavirThe serum concentration of Eletriptan can be increased when it is combined with Saquinavir.Approved, Investigational
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Eletriptan.Approved
SecobarbitalThe metabolism of Eletriptan can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Selegiline.Approved, Investigational, Vet Approved
SertindoleThe risk or severity of adverse effects can be increased when Eletriptan is combined with Sertindole.Approved, Investigational, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Sertraline.Approved
SildenafilThe serum concentration of Eletriptan can be increased when it is combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Eletriptan can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Eletriptan can be increased when it is combined with Simeprevir.Approved
St. John's WortThe serum concentration of Eletriptan can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Eletriptan can be increased when it is combined with Stiripentol.Approved
SulfadiazineThe metabolism of Eletriptan can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Eletriptan can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe serum concentration of Eletriptan can be increased when it is combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Sulpiride.Approved, Investigational
SultoprideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Sultopride.Experimental
SumatriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Sumatriptan.Approved, Investigational
TapentadolThe risk or severity of adverse effects can be increased when Eletriptan is combined with Tapentadol.Approved
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Eletriptan.Approved
TelaprevirThe serum concentration of Eletriptan can be increased when it is combined with Telaprevir.Approved, Withdrawn
TelithromycinThe serum concentration of Eletriptan can be increased when it is combined with Telithromycin.Approved
TerbinafineThe metabolism of Eletriptan can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Tetrahydropalmatine.Investigational
ThiopropazateThe risk or severity of adverse effects can be increased when Eletriptan is combined with Thiopropazate.Experimental
ThioproperazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Thioproperazine.Approved
ThioridazineThe metabolism of Eletriptan can be decreased when combined with Thioridazine.Approved, Withdrawn
ThiothixeneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Thiothixene.Approved
TiaprideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Tiapride.Approved, Investigational
TiclopidineThe serum concentration of Eletriptan can be increased when it is combined with Ticlopidine.Approved
TipranavirThe metabolism of Eletriptan can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Eletriptan can be decreased when it is combined with Tocilizumab.Approved
TolbutamideThe metabolism of Eletriptan can be decreased when combined with Tolbutamide.Approved
ToloxatoneThe metabolism of Eletriptan can be decreased when combined with Toloxatone.Approved
TopiramateThe metabolism of Eletriptan can be decreased when combined with Topiramate.Approved
TopiroxostatThe metabolism of Eletriptan can be decreased when combined with Topiroxostat.Approved, Investigational
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Eletriptan.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe metabolism of Eletriptan can be decreased when combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Tranylcypromine.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Trazodone.Approved, Investigational
TrifluperidolThe risk or severity of adverse effects can be increased when Eletriptan is combined with Trifluperidol.Experimental
TrimipramineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Trimipramine.Approved
TropisetronTropisetron may increase the serotonergic activities of Eletriptan.Approved, Investigational
Valproic AcidThe metabolism of Eletriptan can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Eletriptan can be decreased when combined with Valsartan.Approved, Investigational
VenlafaxineThe serum concentration of Eletriptan can be increased when it is combined with Venlafaxine.Approved
VeraliprideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Veralipride.Experimental
VerapamilThe serum concentration of Eletriptan can be increased when it is combined with Verapamil.Approved
VilazodoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Vilazodone.Approved
VoriconazoleThe serum concentration of Eletriptan can be increased when it is combined with Voriconazole.Approved, Investigational
VortioxetineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Vortioxetine.Approved
ZafirlukastThe metabolism of Eletriptan can be decreased when combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe serum concentration of Eletriptan can be increased when it is combined with Ziprasidone.Approved
ZolmitriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Zolmitriptan.Approved, Investigational
ZotepineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Zotepine.Approved, Investigational
ZucapsaicinThe metabolism of Eletriptan can be decreased when combined with Zucapsaicin.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Eletriptan is combined with Zuclopenthixol.Approved, Investigational
Food Interactions
  • Exposure to the product (area below curve) and maximum concentrations are increased when product is taken with a high-fat meal.

References

Synthesis Reference

Ronald Ogilvie, "Process for the preparation of eletriptan." U.S. Patent US20050059828, issued March 17, 2005.

US20050059828
General References
Not Available
External Links
Human Metabolome Database
HMDB14361
KEGG Drug
D01973
PubChem Compound
77993
PubChem Substance
46506380
ChemSpider
70379
BindingDB
50103594
ChEBI
50922
ChEMBL
CHEMBL1510
Therapeutic Targets Database
DAP000008
PharmGKB
PA134687947
IUPHAR
40
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Eletriptan
ATC Codes
N02CC06 — Eletriptan
AHFS Codes
  • 28:32.28 — Selective Serotonin Agonists
FDA label
Download (148 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentMigraine Disorders1
3CompletedTreatmentMigraine Disorders / Migraine With or Without Aura1
3CompletedTreatmentMigraine With or Without Aura4
4CompletedPreventionMigraines1
4CompletedTreatmentMigraines3
Not AvailableCompletedTreatmentHeadache Disorders / Migraine, Acute / Migrainous Headache1

Pharmacoeconomics

Manufacturers
  • Pfizer ireland pharmaceuticals
Packagers
Dosage forms
FormRouteStrength
Tablet, film coatedOral20 mg/1
TabletOral20 mg
TabletOral40 mg
Tablet, film coatedOral40 mg/1
Prices
Unit descriptionCostUnit
Relpax 6 20 mg tablet Box156.05USD box
Relpax 6 40 mg tablet Box156.05USD box
Relpax 20 mg tablet25.01USD tablet
Relpax 40 mg tablet25.01USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2352392No2006-01-242019-11-01Canada
CA2198599No2000-06-062015-05-17Canada
US5545644No1996-12-262016-12-26Us
US6110940No1997-08-292017-08-29Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityReadily soluble as hydrobromide formulationNot Available
logP3.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00118 mg/mLALOGPS
logP3.84ALOGPS
logP3.77ChemAxon
logS-5.5ALOGPS
pKa (Strongest Acidic)17.11ChemAxon
pKa (Strongest Basic)8.37ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area53.17 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity110.94 m3·mol-1ChemAxon
Polarizability42.99 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9872
Blood Brain Barrier+0.9774
Caco-2 permeable-0.628
P-glycoprotein substrateSubstrate0.6308
P-glycoprotein inhibitor INon-inhibitor0.8046
P-glycoprotein inhibitor IINon-inhibitor0.8383
Renal organic cation transporterInhibitor0.7
CYP450 2C9 substrateNon-substrate0.6591
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.643
CYP450 1A2 substrateNon-inhibitor0.7021
CYP450 2C9 inhibitorNon-inhibitor0.8103
CYP450 2D6 inhibitorNon-inhibitor0.7615
CYP450 2C19 inhibitorNon-inhibitor0.7519
CYP450 3A4 inhibitorNon-inhibitor0.6355
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6986
Ames testNon AMES toxic0.5945
CarcinogenicityNon-carcinogens0.8556
BiodegradationNot ready biodegradable0.9883
Rat acute toxicity2.5492 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6436
hERG inhibition (predictor II)Inhibitor0.7581
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

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 / Benzenesulfonyl group / Aralkylamine / Monocyclic benzene moiety / Substituted pyrrole / N-alkylpyrrolidine / Benzenoid / Pyrrole / Pyrrolidine / Sulfone
show 14 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
sulfone, indoles, N-alkylpyrrolidine (CHEBI:50922)

Targets

Kind
Protein
Organism
Human
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
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. 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. [PubMed:10193663]
  3. 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. [PubMed:15821444]
  4. 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. [PubMed:11513839]
  5. Strijbos PJ, Parsons AA, Fugelli A: Eletriptan Pfizer. Curr Opin Investig Drugs. 2002 Sep;3(9):1359-68. [PubMed:12498013]
  6. 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. [PubMed:11152011]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:10193663]
  2. 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. [PubMed:11050304]
  3. 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. [PubMed:11069595]
  4. 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. [PubMed:11513839]
  5. 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. [PubMed:12384251]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:10193663]
  2. 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. [PubMed:11834243]
  3. 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. [PubMed:15185063]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:11513839]
Kind
Protein
Organism
Human
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 alkaloids and psychoactive substances. Ligand binding causes a conformation change that trig...
Gene Name
HTR1E
Uniprot ID
P28566
Uniprot Name
5-hydroxytryptamine receptor 1E
Molecular Weight
41681.57 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Human
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 ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation...
Gene Name
HTR2B
Uniprot ID
P41595
Uniprot Name
5-hydroxytryptamine receptor 2B
Molecular Weight
54297.41 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Serotonin receptor 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. The activity of this receptor ...
Gene Name
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
Molecular Weight
53554.43 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. 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. [PubMed:19515014]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:19515014]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. 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. [PubMed:19515014]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:19515014]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:19515014]
Kind
Protein
Organism
Human
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
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Transporters

Kind
Protein
Organism
Human
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
  1. 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. [PubMed:12814962]

Drug created on June 13, 2005 07:24 / Updated on November 16, 2017 13:31