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Drug-Target Interaction

Drug

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PubChem ID:3397
Structure:
Synonyms:
"pubertal flutamide study (pubertal studies of vinclozolin; methoxychlor; ethinyl estradiol)"
.alpha.,.alpha.,.alpha.-Trifluoro-2-methyl-4'-nitro-m-propionotoluidide
13311-84-7
1A Brand of Flutamide
2-Methyl-N-(4-nitro-3-[trifluoromethyl]phenyl)propanamide
2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide
2-Methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propionamide
337962-98-8
37209-54-4
4'-Nitro-3'-(trifluoromethyl)isobutyranilide
4'-Nitro-3'-trifluoromethylisobutyramilide
4'-Nitro-3'-trifluoromethylisobutyranilide
4-Nitro-3-(trifluoromethyl)isobutyranilide
AB00052188
AC-10517
AC1L1FUE
AKOS001025465
alpha,alpha,alpha-Trifluoro-2-methyl-4'-nitro-m-propionotoluidide
Alphapharm Brand of Flutamide
Apimid
Apo Flutamide
Apo-Flutamide
ApoFlutamide
Apogepha Brand of Flutamide
Apotex Brand of Flutamide
Azupharma Brand of Flutamide
BPBio1_000087
BRD-K28307902-001-05-0
BRN 2157663
BSPBio_000079
BSPBio_003122
C07653
C11H11F3N2O3
CAS-13311-84-7
CCG-39105
CCRIS 7246
Cebatrol
Cebatrol, veterinary
cell pharm Brand of Flutamide
CHEBI:5132
CHEMBL806
Chephasaar Brand of Flutamide
Chimax
Chiron Brand of Flutamide
Ciclum Brand of Flutamide
CPD000058187
Cytamid
D005485
D00586
DB00499
DivK1c_000459
Drogenil
EINECS 236-341-9
esparma Brand of Flutamide
Essex Brand of Flutamide
EU-0100557
Euflex
Eulexin
Eulexin (TN)
Eulexin, Flutamin, Drogenil,Flutamide
Eulexine
F 9397
F0663
F9397_SIGMA
Fluken
Flulem
Flumid
Fluta 1A Pharma
Fluta cell
Fluta GRY
Fluta-cell
Fluta-GRY
Flutacell
FlutaGRY
Flutamida
Flutamida [INN-Spanish]
Flutamide
Flutamide (JAN/USP/INN)
Flutamide (JP16/USP/INN)
Flutamide (pubertal study)
Flutamide USP25
Flutamide [USAN:BAN:INN]
Flutamide-Supplied by Selleck Chemicals
Flutamidum
Flutamidum [INN-Latin]
Flutamin
Flutandrona
Flutaplex
Flutexin
FTA
Fugerel
Grisetin
Gry Brand of Flutamide
Ham's F-12 medium
Hexal Brand of Flutamide
HMS1568D21
HMS1921O16
HMS2090I18
HMS2092O14
HMS2095D21
HMS2230P19
HMS3259I03
HMS3261P15
HMS501G21
I01-2470
IDI1_000459
Inibsa Brand of Flutamide
Ipsen Brand of Flutamide
Juta Brand of Flutamide
KBio1_000459
KBio2_001690
KBio2_004258
KBio2_006826
KBio3_002342
KBioGR_001377
KBioSS_001690
Kendrick Brand of Flutamide
Lemery Brand of Flutamide
Lopac-F-9397
Lopac0_000557
LS-2105
m-Propionotoluidide, .alpha.,.alpha.,.alpha.-trifluoro-2-methyl-4'-nitro-
m-Propionotoluidide, 2-methyl-4'-nitro-.alpha.,.alpha.,.alpha.-trifluoro-
m-Propionotoluidide, 2-methyl-4'-nitro-alpha,alpha,alpha-triflouro-
m-Propionotoluidide, alpha,alpha,alpha-trifluoro-2-methyl-4'-nitro-
m-Propionotoluidide, alpha,alpha,alpha-trifluoro-2-methyl-4'-nitro- (8CI)
m-propionotoluidide,alpha,alpha,alpha-trifluoro-2-methyl-4'-nitro
METHOXYCHLOR;
MLS000069634
MLS001065596
NCGC00015452-01
NCGC00015452-02
NCGC00015452-03
NCGC00015452-04
NCGC00015452-05
NCGC00015452-06
NCGC00015452-07
NCGC00015452-08
NCGC00015452-09
NCGC00015452-10
NCGC00015452-11
NCGC00015452-12
NCGC00015452-13
NCGC00015452-14
NCGC00015452-15
NCGC00015452-16
NCGC00091460-01
NCGC00091460-02
NCGC00091460-03
NCGC00091460-04
NCGC00091460-05
NCGC00091460-06
NCGC00091460-07
NCGC00091460-08
NCGC00091460-09
NFBA
Niftholide
Niftolid
Niftolide
NINDS_000459
NK-601
Novo Flutamide
Novo-Flutamide
NovoFlutamide
Novopharm Brand of Flutamide
NSC 215876
NSC147834
NSC215876
Odyne
Oncosal
Pharmascience Brand of Flutamide
PMS Flutamide
PMS-Flutamide
Prasfarma Brand of Flutamide
Prestwick0_000180
Prestwick1_000180
Prestwick2_000180
Prestwick3_000180
Prestwick_228
Propanamide, 2-methyl-N-(4-nitro-3-(trifluoromethyl)phenyl)-
Propanamide, 2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]-
Prostacur
Prostandril
Prostica
Prostogenat
PUBERTAL FLUTAMIDE STUDY (PUBERTAL STUDIES OF VINCLOZOLIN
PUBERTAL FLUTAMIDE STUDY (PUBERTAL STUDIES OF VINCLOZOLIN; METHOXYCHLOR; ETHINYL ESTRADIOL)
Q Pharm Brand of Flutamide
Q-Pharm Brand of Flutamide
S1908_Selleck
SAM002264612
SBB006930
Sch 13521
SCH-13521
SCH13521
Schering Brand of Flutamide
Schering Plough Brand of Flutamide
Schering-Plough Brand of Flutamide
SMR000058187
SPBio_000982
SPBio_002000
SPECTRUM1500995
Spectrum2_001201
Spectrum3_001421
Spectrum4_000829
Spectrum5_001450
Spectrum_001210
ST058409
TAD Brand of Flutamide
Tedec Meiji Brand of Flutamide
Testotard
UNII-76W6J0943E
ZINC03812944
ATC-Codes:
Side-Effects:
Side-EffectFrequency
hot flashes0.59666663
loss of libido0.34333333
impotence0.31666666
nausea0.10666668
vomiting0.10666668
gynecomastia0.09666667
diarrhea0.093333334
proctitis0
nervousness0
methemoglobinemia0
anemia0
thrombocytopenia0
ulcer0
erythema0
hepatic necrosis0
sgot increased0
rectal hemorrhage0
photosensitivity0
laboratory test abnormal0
leukopenia0
jaundice0
hemolytic anemia0
macrocytic anemia0
anorexia0
anxiety0
confusion0
cystitis0
somnolence0
edema0
rash0
hematuria0
hepatic encephalopathy0
hepatitis0
hypertension0
breast neoplasm0

Target

show target details
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:

11160641
Human CYP1B1 and anticancer agent metabolism: mechanism for tumor-specific drug inactivation?. B Rochat; J M Morsman; G I Murray; W D Figg; H L McLeod (2001) The Journal of pharmacology and experimental therapeutics display abstract
The cytochrome P450 1B1 (CYP1B1) is involved in the metabolism of procarcinogens and xenobiotics. Human CYP1B1 protein has been detected in a variety of tumors but is not detected in adjacent normal tissues or in liver. This suggests that CYP1B1 could biotransform anticancer agents specifically in the target cells. The interaction between CYP1B1 and 12 commonly used anticancer drugs was screened using an ethoxyresorufin deethylase assay. Four agents were competitive inhibitors of CYP1B1 activity: flutamide (K(i) = 1.0 microM), paclitaxel (K(i) = 31.6 microM), mitoxantrone (K(i) = 11.6 microM), and docetaxel (K(i) = 28.0 microM). Doxorubicin (K(i) = 2.6 microM) and daunomycin (K(i) = 2.1 microM) were mixed inhibitors, while tamoxifen was a noncompetitive inhibitor (K(i) = 5.0 microM). Vinblastine, vincristine, 5-fluorouracil, etoposide, and cyclophosphamide did not inhibit CYP1B1 activity. In vitro incubations with flutamide and CYP1B1 produced a metabolite consistent with 2-hydroxyflutamide. Comparison of kinetic parameters (K(m), K(i), V(max)) for flutamide 2-hydroxylation by CYP1B1, CYP1A1, and CYP1A2 indicate that CYP1B1 could play a major role for flutamide biotransformation in tumors. The results obtained indicate that several anticancer agents inhibit CYP1B1 activity. Drug inactivation by CYP1B1 may represent a novel mechanism of resistance, influencing the clinical outcome of chemotherapy.