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Drug-Target Interaction

Drug

show drug details
PubChem ID:77993
Structure:
Synonyms:
143322-58-1
1H-Indole,
1H-Indole, 3-(((2R)-1-methyl-2-pyrrolidinyl)methyl)-5-(2-(phenylsulfonyl)ethyl)ethyl)-
3-(((R)-1-Methyl-2-pyrrolidinyl)methyl)-5-(2-(phenylsulfonyl)ethyl)indole
3-[[(2R)-1-methylpyrrolidin-2-yl]methyl]-5-(2-phenylsulfonylethyl)-1H-indole
3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole
CHEBI:50922
DB00216
Eletriptan
Eletriptan [INN:BAN]
LS-186998
LS-187637
NCGC00181130-01
Relpax
UK 116044
UK-116044
UK-116044-04
ATC-Codes:
Side-Effects:
Side-EffectFrequency
chills1.0
pharyngitis1.0
back pain1.0
palpitation1.0
sweating1.0
vertigo1.0
pain0.20090908
asthenia0.057272732
nausea0.056666672
dizziness0.05333333
somnolence0.050909087
headache0.034999996
paresthesia0.03125
dry mouth0.030000001
flushing0.02
cramps0.015
dyspepsia0.015
dysphagia0.011749999
esophagitis0.01
glossitis0.01
liver function tests abnormal0.01
gastritis0.01
flatulence0.01
migraine0.01
peripheral edema0.01
photophobia0.01
tremor0.01
lacrimation disorder0.01
infection0.01
impotence0.01
abnormal vision0.01
voice alteration0.01
hypertension0.01
hyperesthesia0.01
nervousness0.01
peripheral vascular disorder0.01
tinnitus0.01
agitation0.01
eructation0.01
bone pain0.01
malaise0.01
ataxia0.01
asthma0.01
increased salivation0.01
arthritis0.01
arthralgia0.01
rhinitis0.01
anxiety0.01
anorexia0.01
urinary frequency0.01
insomnia0.01
tachycardia0.01
polyuria0.01
myalgia0.01
eye pain0.01
ear pain0.01
confusion0.01
conjunctivitis0.01
constipation0.01
dyspnea0.01
diarrhea0.01
arthrosis0.0055
edema0.0055
pruritus0.0055
rash0.0040
urticaria0.0010
thyroiditis0.0010
sinusitis0.0010
stomatitis0.0010
tenosynovitis0.0010
dementia0.0010
syncope0.0010
thrombophlebitis0.0010
tooth disorder0.0010
abnormal gait0.0010
kidney pain0.0010
paralysis0.0010
lymphadenopathy0.0010
neuropathy0.0010
lab test abnormal0.0010
bradycardia0.0010
dry eyes0.0010
allergic reaction0.0010
ischaemic colitis0.0010
dry skin0.0010
alkaline phosphatase increased0.0010
thyroid adenoma0.0010
weight loss0.0010
weight gain0.0010
vomiting0.0010
vaginitis0.0010
sleep disorder0.0010
abscess0.0010
cerebrovascular disorder0.0010
choking0.0010
cough0.0010
exfoliative dermatitis0.0010
diplopia0.0010
eczema0.0010
epistaxis0.0010
fever0.0010
gingivitis0.0010
goiter0.0010
moniliasis0.0010
bronchitis0.0010
alopecia0.0010
amnesia0.0010
anemia0.0010
angina pectoris0.0010
aphasia0.0010
arrhythmia0.0010
rheumatoid arthritis0.0010
atrial fibrillation0.0010
av block0.0010
bone neoplasm0.0010
halitosis0.0010
shock0.0010
breast pain0.0010
menorrhagia0.0010
menstrual disorder0.0010
myopathy0.0010
neurosis0.0010
otitis media0.0010
ptosis0.0010
psoriasis0.0010
purpura0.0010
seizure0.0010
leukopenia0.0010
laryngitis0.0010
hallucinations0.0010
hematemesis0.0010
hemiplegia0.0010
hemorrhage0.0010
hernia0.0010
hiccup0.0010
bilirubinemia0.0010
hyperglycemia0.0010
hypotension0.0010
hypothermia0.0010
flu syndrome0.0010
weakness0
stupor0
manic0
thinking abnormal0
depersonalization0
emotional lability0
apathy0
viral infection0
muscle atrophy0
burning sensation0
myocardial ischemia0
fatigue0
ventricular fibrillation0
ventricular tachycardia0
numbness0
myocardial infarction0
euphoria0

Target

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Uniprot ID:CP3A4_HUMAN
Synonyms:
Albendazole monooxygenase
Albendazole sulfoxidase
CYPIIIA3
CYPIIIA4
Cytochrome P450 3A3
Cytochrome P450 3A4
HLp
NF-25
Nifedipine oxidase
P450-PCN1
Quinine 3-monooxygenase
Taurochenodeoxycholate 6-alpha-hydroxylase
EC-Numbers:1.14.13.32
1.14.13.67
1.14.13.97
Organism:Homo sapiens
Human
PDB IDs:1TQN 1W0E 1W0F 1W0G 2J0D 2V0M
Structure:
2V0M

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----
----
----
----

References:

014511273
10611140
11480267
12814962
Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein.. David C Evans; Desmond O'Connor; Brian G Lake; Raymond Evers; Christopher Allen; Richard Hargreaves (2003) Drug metabolism and disposition: the biological fate of chemicals display abstract
"Reaction phenotyping" studies were performed with eletriptan (ETT) to determine its propensity to interact with coadministered medications. Its ability to serve as a substrate for human P-glycoprotein (P-gp) was also investigated since a central mechanism of action has been proposed for this "triptan" class of drug. In studies with a characterized bank of human liver microsome preparations, a good correlation (r2 = 0.932) was obtained between formation of N-desmethyl eletriptan (DETT) and CYP3A4-catalyzed testosterone 6 beta-hydroxylation. DETT was selected to be monitored in our studies since it represents a significant ETT metabolite in humans, circulating at concentrations 10 to 20% of those observed for parent drug. ETT was metabolized to DETT by recombinant CYP2D6 (rCYP2D6) and rCYP3A4, and to a lesser extent by rCYP2C9 and rCYP2C19. The metabolism of ETT to DETT in human liver microsomes was markedly inhibited by troleandomycin, erythromycin, miconazole, and an inhibitory antibody to CYP3A4, but not by inhibitors of other major P450 enzymes. ETT had little inhibitory effect on any of the P450 enzymes investigated. ETT was determined to be a good substrate for human P-gp in vitro. In bidirectional transport studies across LLC-MDR1 and LLC-Mdr1a cell monolayers, ETT had a BA/AB transport ratio in the range 9 to 11. This finding had significance in vivo since brain exposure to ETT was reduced 40-fold in Mdr1a+/+ relative to Mdr1a-/- mice. ETT metabolism to DETT is therefore catalyzed primarily by CYP3A4, and plasma concentrations are expected to be increased when coadministered with inhibitors of CYP3A4 and P-gp activity.