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Drug-Target Interaction

Drug

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PubChem ID:443879
Structure:
Synonyms:
(+)-(R)-2-(alpha-(2-(Diisopropylamino)ethyl)benzyl)-p-cresol
(+)-Tolterodine
124937-51-5
2-[(1R)-3-(diisopropylamino)-1-phenylpropyl]-4-methylphenol
2-[(1R)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-methylphenol
2-[3-[Bis(1-methylethyl)amino]-1-phenylpropyl]-4-methylphenol
2-{(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl}-4-methylphenol
AC-3472
AC1L9FDR
BIDD:GT0318
CHEBI:9622
CHEMBL1382
Detrol
FT-0082150
FT-0082998
HMS2230E24
Jsp001637
Kabi-2234
KS-1121
LS-187278
MLS001195620
MLS001304745
MolPort-005-934-224
NCGC00159519-02
SMR000596518
Tolterodina
Tolterodine
Tolterodinum
ATC-Codes:

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:

009531513
010583027
10583027
Ketoconazole inhibits the metabolism of tolterodine in subjects with deficient CYP2D6 activity.. N Brynne; C Forslund; B HallÚn; L L Gustafsson; L Bertilsson (1999) British journal of clinical pharmacology display abstract
AIMS: To investigate the pharmacokinetics and safety of tolterodine and tolterodine metabolites after single-and multiple-dose administration in the absence and presence of ketoconazole, an inhibitor of cytochrome P450 (CYP) 3A4, in healthy volunteers with deficient CYP2D6 activity, i.e. poor metabolisers of debrisoquine. METHODS: Eight healthy volunteers received single oral doses (2 mg) of tolterodine l-tartrate. Following a wash-out period of about 3 months, six of the subjects participated in a multiple-dose (1 mg twice daily) phase of the study. Ketoconazole 200 mg was given once daily for 4-4.5 days during both the single and multiple dose tolterodine administration phases. Blood samples were drawn and the pharmacokinetics of tolterodine and its metabolites were determined. RESULTS: A decrease (P