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Drug-Target Interaction

Drug

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PubChem ID:47576
Structure:
Synonyms:
(+-)-cis-1-acetyl-4-(p-((2-(2,4-dichlorophenyl)-2-(imidazol-1- ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)piperazine
(+-)-cis-1-Acetyl-4-(p-((2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)piperazine
(-)-Ketoconazole
(2S,4R)-ketoconazole
1-acetyl-4-(4-{[(2S,4R)-2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-
1-ACETYL-4-(4-{[(2S,4R)-2-(2,4-DICHLOROPHENYL)-2-(1H-IMIDAZOL-1-YLMETHYL)-1,3-DIOXOLAN-4-YL]METHOXY}PHENYL)PIPERAZINE
1-[4-[4-[[(2S,4R)-2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]ethanone
65277-42-1
AIDS-112209
AIDS112209
BRN 4303081
CAS-65277-42-1
CHEBI:47518
CORT-001
CPD-4503
D00351
DB01026
DRG-0073
EINECS 265-667-4
Extina
Fungarest
Fungoral
Ketocanazole
Ketoconazol
Ketoconazol [INN-Spanish]
KETOCONAZOLE
Ketoconazole (JAN/USP)
Ketoconazole [USAN:BAN:INN:JAN]
Ketoconazolum
Ketoconazolum [INN-Latin]
Ketoderm
Ketoisdin
Ketozole
KW-1414
Lopac-K-1003
NCGC00015577-01
NCGC00016907-01
NCGC00161836-01
NCGC00161836-02
Nizoral
Nizoral (TN)
Nizoral a-D
NSC 317629
Orifungal M
Panfungol
Piperazine, (-)-1-acetyl-4-[4-[[(2S,4R)-2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-
piperazine, 1-acetyl-4-(4-((2-(2,4-dichlorophenyl)-2-(1H- imidazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)-, cis-
Piperazine, 1-acetyl-4-(4-((2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)-, cis-
R 41400
R-41400
Sebazole
Xolegel
Xolegel (TN)
ATC-Codes:
Side-Effects:
Side-EffectFrequency
abdominal pain0
nausea0
pain0
papilledema0
paresthesia0
pruritus0
swelling0
thrombocytopenia0
erythema0
urticaria0
vomiting0
chills0
photophobia0
pyogenic granuloma0
dry skin0
scalp seborrhea0
eye swelling0
acne0
leukopenia0
keratoconjunctivitis sicca0
alopecia0
anaphylaxis0
hemolytic anemia0
arrhythmia0
dermatitis0
contact dermatitis0
diarrhea0
dizziness0
somnolence0
rash0
fever0
gynecomastia0
headache0
hypersensitivity0
hypertriglyceridemia0
impetigo0
impotence0
allergic reaction0

Target

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Uniprot ID:CP3A7_HUMAN
Synonyms:
CYPIIIA7
Cytochrome P450 3A7
P450-HFLA
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

8690825
Inhibition of terfenadine metabolism in vitro by azole antifungal agents and by selective serotonin reuptake inhibitor antidepressants: relation to pharmacokinetic interactions in vivo.. L L von Moltke; D J Greenblatt; S X Duan; J S Harmatz; C E Wright; R I Shader (1996) Journal of clinical psychopharmacology display abstract
Biotransformation of the H-1 antagonist terfenadine to its desalkyl and hydroxy metabolites was studied in vitro using microsomal preparations of human liver. These metabolic reactions are presumed to be mediated by Cytochrome P450-3A isoforms. The azole antifungal agent ketoconazole was a highly potent inhibitor of both reactions, having mean inhibition constants (Ki) of 0.037 and 0.34 microM for desalkyl- and hydroxy-terfenadine formation, respectively. Itraconazole also was a potent inhibitor, with Ki values of 0.28 and 2.05 microM, respectively. Fluconazole, on the other hand, was a weak inhibitor. Six selective serotonin reuptake inhibitor antidepressants tested in this system were at least 20 times less potent inhibitors of terfenadine metabolism than was ketoconazole. An in vitro-in vivo scaling model used in vitro Ki values, typical clinically relevant plasma concentrations of inhibitors, and presumed liver:plasma partition ratios to predict the degree of terfenadine clearance impairment during coadministration of terfenadine with these inhibitors in humans. The model predicted a large and potentially hazardous impairment of terfenadine clearance by ketoconazole and, to a slightly lesser extent, by itraconazole. However, fluconazole and the six selective serotonin reuptake inhibitors (SSRIs) at usual clinical doses were not predicted to impair terfenadine clearance to a degree that would be of clinical importance. Caution is nonetheless warranted with the coadministration of SSRIs and terfenadine when high doses of SSRIs (particularly fluoxetine) are administered. Also, some individuals may be unusually susceptible to metabolic inhibition for a variety of reasons.