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Drug-Target Interaction

Drug

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PubChem ID:5029
Structure:
Synonyms:
117976-89-3
117976-90-6
1H-Benzimidazole,
1H-Benzimidazole, 2-(((4-(3-methoxypropoxy)-3-methyl-2-pyridinyl)methyl)sulfinyl)-
1H-Benzimidazole, 2-(((4-(3-methoxypropoxy)-3-methyl-2-pyridinyl)methyl)sulfinyl)-, sodium salt
2-(((4-(3-Methoxypropoxy)-3-methyl-2-pyridinyl)methyl)sulfinyl)-1H-benzimidazole
2-((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methylsulfinyl)-1H-benzimidazole
2-({[4-(3-methoxypropoxy)-3-methylpyridin-2-yl]methyl}sulfinyl)-1H-benzimidazole
2-[[4-(3-methoxypropoxy)-3-methylpyridin-2-yl]methylsulfinyl]-1H-benzimidazole
Aciphex
C063129
C07864
C18H21N3O3S
CHEBI:8768
Clofezone
CPD000469174
DB01129
dexrabeprazole
E 3810
E3810
HSDB 7321
Irsogladine Maleate
LS-172365
LY-307640
LY307640
MLS001401446
Pariet
Rabeprazole
rabeprazole sodium
Rabeprazole [BAN:INN]
Rabeprazole [INN:BAN]
Rebeprazole sodium
SAM001246619
SMR000469174
ATC-Codes:
Side-Effects:
Side-EffectFrequency
interstitial nephritis0.0010
supraventricular tachycardia0.0010
thrombocytopenia0.0010
thrombophlebitis0.0010
liver fatty0.0010
urinary incontinence0.0010
edema0.0010
ventricular tachycardia0.0010
duodenitis0.0010
diarrhea0.0010
drug eruptions0.0010
agitation0.0010
delirium0.0010
gastrointestinal hemorrhage0.0010
deafness0.0010
corneal opacity0.0010
confusion0.0010
pancytopenia0.0010
strabismus0.0010
menorrhagia0.0010
orchitis0.0010
leukopenia0.0010
jaundice0.0010
impotence0.0010
psoriasis0.0010
salivary gland enlargement0.0010
breast enlargement0.0010
pulmonary embolus0.0010
retinal degeneration0.0010
rhabdomyolysis0.0010
herpes zoster0.0010
hepatoma0.0010
hepatitis0.0010
hepatic encephalopathy0.0010
hematuria0.0010
coma0.0010
anaphylaxis0.0010
amnesia0.0010
angioedema0.0010
hemolytic anemia0.0010
blurry vision0.0010
interstitial pneumonia0.0010
hypoventilation0.0010
agranulocytosis0.0010
diplopia0.0010
dry skin0.0010
bradycardia0.0010
cholangitis0.0010
apnea0.0010
eye pain0.0010
acne0
paresthesia0
skin carcinoma0
retinopathy0
lung cancer0
seborrhea0
seizures0
ecg abnormal0
skin nodule0
stevens - johnson syndrome0
ulcerative stomatitis0
stomatitis0
allergic reaction0
urinary frequency0
lymphadenopathy0
pruritus0
breast neoplasm0
pain0
otitis media0
otitis externa0
neutropenia0
neuralgia0
nervousness0
tumor0
palpitations0
pancreatitis0
proctitis0
polyuria0
sleep disorder0
insomnia0
pneumonia0
periodontal abscess0
pelvic pain0
gynecomastia0
nausea0
neuropathy0
bone pain0
malaise0
sinus bradycardia0
chills0
dry mouth0
myalgia0
weight loss0
weight gain0
vomiting0
prostatic specific antigen increase0
iron deficiency anemia0
cataract0
chest pain substernal0
liver function tests abnormal0
vaginal hemorrhage0
ventricular extrasystoles0
neck rigidity0
migraine0
dementia0
mouth ulceration0
right upper quadrant pain0
voice alteration0
abnormal vision0
tooth disorder0
tinnitus0
photosensitivity0
tachycardia0
peripheral edema0
syncope0
swelling0
sweating0
tremor0
dry eyes0
urticaria0
vestibular disorders0
vertigo0
hypoxia0
vascular disorders0
rectal hemorrhage0
varicose vein0
vaginitis0
uterine hemorrhage0
suicide attempt0
ear pain0
dysphagia0
decreased libido0
cyst0
cystitis0
coronary artery disease0
constipation0
conjunctivitis0
ulcerative colitis0
colitis0
cholelithiasis0
dehydration0
tooth caries0
dysuria0
dyspnea0
dyspepsia0
dysmenorrhea0
somnolence0
dizziness0
abdominal pain0
diabetes mellitus0
fungal dermatitis0
contact dermatitis0
cholecystitis0
neck pain0
cerebral hemorrhage0
arthralgia0
arrhythmia0
anxiety0
anorexia0
angina pectoris0
hypochromic anemia0
anemia0
amblyopia0
alopecia0
albuminuria0
arthritis0
rheumatoid arthritis0
cellulitis0
carcinoma0
moniliasis0
bursitis0
bundle branch block0
blepharitis0
skin benign neoplasm0
asthma0
asthenia0
ascites0
abscess0
nail disorder0
lacrimation disorder0
polycystic kidney0
kidney calculus0
arthrosis0
hypothyroidism0
hypotension0
hyponatremia0
hypokalemia0
hyperthyroidism0
hypertension0
laryngitis0
leg cramps0
myocardial infarction0
metrorrhagia0
menstrual disorder0
melena0
melanoma0
breast pain0
mastitis0
lung disorder0
cirrhosis0
leukocytosis0
hyperlipidemia0
hyperglycemia0
hypercholesterolemia0
flatulence0
fever0
rash0
esophagitis0
esophageal stricture0
erythema multiforme0
eructation0
epistaxis0
toxic epidermal necrolysis0
embolism0
gastritis0
gastroenteritis0
hiccup0
herpes simplex0
herpes0
hernia0
hemorrhage0
headache0
gout0
glossitis0
glaucoma0
gingivitis0
ecchymosis0

Target

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Uniprot ID:CP1A1_HUMAN
Synonyms:
CYPIA1
Cytochrome P450 1A1
P450 form 6
P450-C
P450-P1
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

12623754
16359346
CYP2C19 genotype and the PPIs--focus on rabeprazole.. P W Y Lim; K L Goh; B C Y Wong (2005) Journal of gastroenterology and hepatology display abstract
Amongst all the proton pump inhibitors (PPI), the hepatic metabolism of rabeprazole is least dependent on the CYP4502C19 system. Rabeprazole is therefore the PPI least affected by CYP4502C19 genetic polymorphism. This unique feature of rabeprazole complements rabeprazole's fast onset of action, and may lead to profound and consistent inhibition of gastric acid secretion in the treatment of acid-related disorders.
16783561
Effects of clarithromycin and verapamil on rabeprazole pharmacokinetics between CYP2C19 genotypes.. Mikiko Shimizu; Tsukasa Uno; Norio Yasui-Furukori; Kazunobu Sugawara; Tomonori Tateishi (2006) European journal of clinical pharmacology display abstract
OBJECTIVE: Rabeprazole as a proton pump inhibitor (PPI) is mainly reduced to rabeprazole thioether via a nonenzymatic pathway, with minor CYP2C19 and CYP3A4 involvement. The aim of this study was to compare possible effects of clarithromycin and verapamil as inhibitors of CYP3A4 on the pharmacokinetics of rabeprazole among CYP2C19 genotypes. METHODS: A three-way randomized, double-blind, placebo-controlled crossover study was performed. Nineteen volunteers, of whom six were homozygous extensive metabolizers (EMs), eight were heterozygous EMs, and five were poor metabolizers (PMs) for CYP2C19, received three 6-day courses of either daily 800 mg clarithromycin, 240 mg verapamil, or placebo in a randomized fashion, with a single oral dose of 20 mg rabeprazole on day 6 in all cases. Plasma concentrations of rabeprazole and rabeprazole thioether were monitored up to 24 h after the dosing. RESULTS: In the control phase, the AUC(0-infinity) values for rabeprazole and rabeprazole thioether were 1,005+/-366 and 412+/-149 ng.h/ml in homozygous EMs, 1,108+/-340 and 491+/-245 ng.h/ml in heterozygous EMs, and 2,697+/-364 and 2,116+/-373 ng.h/ml in PMs, respectively. There were significant differences (p
16915367
Identification of the time-point which gives a plasma rabeprazole concentration that adequately reflects the area under the concentration-time curve.. Takenori Niioka; Tsukasa Uno; Norio Yasui-Furukori; Mikiko Shimizu; Kazunobu Sugawara; Tomonori Tateishi (2006) European journal of clinical pharmacology display abstract
OBJECTIVE: The purpose of this study is to evaluate whether a simple formula using limited blood samples can predict the area under the plasma rabeprazole concentration-time curve (AUC) in co-administration with CYP inhibitors. METHODS: A randomized double-blind placebo-controlled crossover study design in three phases was conducted at intervals of 2 weeks. Twenty-one healthy Japanese volunteers, including three CYP2C19 genotype groups, took a single oral 20-mg dose of rabeprazole after three 6-day pretreatments, i.e., clarithromycin 800 mg/day, fluvoxamine 50 mg/day, and placebo. Prediction formulas of the AUC were derived from pharmacokinetics data of 21 subjects in three phases using multiple linear regression analysis. Ten blood samples were collected over 24 h to calculate AUC. Plasma concentrations of rabeprazole was measured by an HPLC-assay (l.l.q.=1 ng/ml). RESULTS: The AUC was based on all the data sets (n=63). The linear regression using two points (C3 and C6) could predict AUC(0-infinity) precisely, irrespective of CYP2C19 genotypes and CYP inhibitors (AUC(0-infinity)=1.39xC3+7.17xC6+344.14, r (2)=0.825, p