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Drug-Target Interaction

Drug

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PubChem ID:151166
Structure:
Synonyms:
2-((2-Chloro-6-fluorophenyl)amino)-5-methylbenzeneacetic acid
2-((2-Chloro-6-fluorophenyl)amino)-5-methylphenyl)acetic acid
2-(2-((2-chloro-6-fluoro-phenyl)amino)-5-methyl-phenyl)acetic acid
2-[2-(2-chloro-6-fluoroanilino)-5-methylphenyl]acetic acid
2-[2-[(2-chloro-6-fluorophenyl)amino]-5-methylphenyl]acetic acid
220991-20-8
AC-1738
AC1L45SO
Benzeneacetic acid, 2-((2-chloro-6-fluorophenyl)amino)-5-methyl-
C473384
CHEBI:524824
CHEMBL404108
COX 189
COX-189
COX189
D03714
DB01283
HMS3264F19
I06-0368
Joicela
LS-185762
LS-187022
LS-187647
Lumiracoxib
Lumiracoxib (USAN/INN)
Lumiracoxib [USAN:INN]
NCGC00181795-01
Prexige
Prexige (Novartis)
STOCK6S-73581
UNII-V91T9204HU
ATC-Codes:

Target

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Uniprot ID:CP2C9_HUMAN
Synonyms:
(R)-limonene 6-monooxygenase
(S)-limonene 6-monooxygenase
(S)-limonene 7-monooxygenase
CYPIIC9
Cytochrome P450 2C9
P-450MP
P450 MP-4/MP-8
P450 PB-1
S-mephenytoin 4-hydroxylase
EC-Numbers:1.14.13.48
1.14.13.49
1.14.13.80
Organism:Homo sapiens
Human
PDB IDs:1OG2 1OG5 1R9O
Structure:
1R9O

Binding Affinities:

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

References:

14747429
Lumiracoxib: pharmacokinetic and pharmacodynamic profile when coadministered with fluconazole in healthy subjects.. Graham Scott; Linda Yih; Ching-Ming Yeh; Slavica Milosavljev; Aziz Laurent; Christiane Rordorf (2004) Journal of clinical pharmacology display abstract
This two-way crossover study evaluated the effect of fluconazole on the pharmacokinetics and selective COX-2 inhibition of lumiracoxib. Thirteen healthy subjects were randomized to fluconazole (day 1: 400 mg; days 2-4: 200 mg) or no drug. On day 4, all subjects received a single dose of lumiracoxib (400 mg). Lumiracoxib pharmacokinetics were assessed during the following 48 hours. Thromboxane B(2) (TxB(2)) inhibition was measured prior to lumiracoxib dosing and 2 hours afterwards. Fluconazole caused a small (18%) but not clinically relevant increase in lumiracoxib mean AUC(0- infinity ) but had no effect on lumiracoxib mean C(max). The geometric mean ratio (lumiracoxib plus fluconazole/lumiracoxib alone) for AUC(0- infinity ) was 1.19 (90% confidence interval [CI] = 1.12, 1.27) and for C(max) was 1.11 (90% CI = 0.98, 1.27). The decrease in TxB(2) from predose was not significantly different for lumiracoxib (11.8%) or lumiracoxib plus fluconazole (7.1%); no correlation between lumiracoxib concentration and TxB(2) decrease was seen. As fluconazole is a strong inhibitor of cytochrome P450 (CYP) 2C9, other CYP2C9 inhibitors are unlikely to affect lumiracoxib pharmacokinetics with clinical relevance, making dosage adjustment unnecessary.
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