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Drug-Target Interaction

Drug

show drug details
PubChem ID:151165
Structure:
Synonyms:
170729-80-3
221350-96-5
3-(((2R,3S)-3-(p-Fluorophenyl)-2-(((alphaR)-alpha-methyl-3,5-bis(trifluoromethyl)benzyl)oxy)morpholino)methyl)-delta(sup 2)-1,2,4-triazolin-5-one
3H-1,2,4-Triazol-3-one,
3H-1,2,4-Triazol-3-one, 5-(((2R,3S)-2-((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)-4-morpholinyl)methyl)-1,2-dihydro-
3H-1,2,4-Triazol-3-one, 5-((2-(1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)-4-morpholinyl)methyl)-1,2-dihydro-, (2R-(2alpha(R*),3alpha))-
5-[[(2S,3R)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,2-dihydro-1,2,4-triazol-3-one
Aprepitant
Aprepitant [USAN]
DB00673
Emend
L 754030
LS-156477
MK 0869
MK 869
NCGC00181785-01
ATC-Codes:
Side-Effects:
Side-EffectFrequency
anaphylactic reactions0.0010
rash0.0010
hypersensitivity0.0010
pruritus0.0010
urticaria0.0010
anorexia0
breast disorders0
dysphagia0
polyps0
sensory disturbance0
somnolence0
infection0
dysarthria0
connective tissue disorders0
palpitations0
angioedema0
lower respiratory infection0
pelvic pain0
sinus tachycardia0
musculoskeletal pain0
stomatitis0
vascular disorders0
sgot increased0
small cell lung cancer0
mediastinal disorders0
hypothermia0
heart disease0
abdominal pain upper0
tachycardia0
dyspepsia0
wound dehiscence0
proteinuria0
thrombocytopenia0
heartburn0
cyst0
siadh0
neuropathy0
myalgia0
loss of consciousness0
arthralgia0
upper respiratory tract infection0
hallucinations0
increased sweating0
hypotension0
anxiety0
sepsis0
hiccup0
hemorrhage0
neutropenia0
wheezing0
dehydration0
abdominal pain0
enterocolitis0
hypoxia0
dyspnea0
white blood cell count increased0
insomnia0
headache0
paresthesia0
gastritis0
gastroesophageal reflux0
septic shock0
pain0
herpes simplex0
syncope0
tumor0
alopecia0
conjunctivitis0
bradycardia0
hyponatremia0
duodenal ulcer0
renal insufficiency0
anemia0
back pain0
increased salivation0
fever0
myocardial infarction0
acne0
confusion0
urinary tract infection0
stevens - johnson syndrome0
muscle weakness0
hypertension0
dry mouth0
hypokalemia0
deep vein thrombosis0
flushing0
dysuria0
pulmonary embolism0
seizures0
moniliasis0
tremor0
hematoma0
hot flashes0
peripheral neuropathy0
malaise0
weight loss0
eructation0
diabetes mellitus0
tinnitus0
pneumonia0
cough0
flatulence0
alkaline phosphatase increased0
hyperglycemia0
edema0
dizziness0
pharyngitis0
fatigue0
asthenia0
diarrhea0
constipation0

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:

015562136
12891225
Effects of aprepitant on cytochrome P450 3A4 activity using midazolam as a probe.. Anup K Majumdar; Jacqueline B McCrea; Deborah L Panebianco; Michael Hesney; James Dru; Marvin Constanzer; Michael R Goldberg; Gail Murphy; Keith M Gottesdiener; Christopher R Lines; Kevin J Petty; Robert A Blum (2003) Clinical pharmacology and therapeutics display abstract
BACKGROUND: Aprepitant is a neurokinin(1) receptor antagonist that enhances prevention of chemotherapy-induced nausea and vomiting when added to conventional therapy with a corticosteroid and a 5-hydroxytryptamine(3) (5-HT(3)) antagonist. Because aprepitant may be used with a variety of chemotherapeutic agents and ancillary support drugs, which may be substrates of cytochrome P450 (CYP) 3A4, assessment of the potential of this drug to inhibit CYP3A4 activity in vivo is important. The effect of aprepitant on in vivo CYP3A4 activity in humans with oral midazolam used as a sensitive probe of CYP3A4 activity was evaluated in this study. METHODS: In this open-label, randomized, single-period study, 16 healthy male subjects were enrolled. Subjects received one of two oral aprepitant regimens for 5 days (8 subjects per regimen): (1) 125 mg aprepitant on day 1 and then 80 mg/d on days 2 to 5 or (2) 40 mg aprepitant on day 1 and then 25 mg/d on days 2 to 5. All subjects also received a single oral dose of midazolam, 2 mg, at prestudy (3 to 7 days before aprepitant treatment) and on days 1 and 5 (1 hour after aprepitant administration). RESULTS: Coadministration of midazolam and 125/80 mg aprepitant increased the midazolam area under the plasma concentration-time curve by 2.3-fold on day 1 (P
15
15304427
15723220
15838656