General Information of Drug (ID: DMSHPW8)

Drug Name
Tolterodine Drug Info
Synonyms
Tolterodina; Tolterodinum; Detrol (TN); Detrusitol (TN); Kabi-2234; 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
Indication
Disease Entry ICD 11 Status REF
Overactive bladder GC50.0 Approved [1]
Priapism Investigative [2]
Therapeutic Class
Antispasmodics
Cross-matching ID
PubChem CID
443879
ChEBI ID
CHEBI:9622
CAS Number
CAS 124937-51-5
TTD Drug ID
DMSHPW8
INTEDE Drug ID
DR1616
ACDINA Drug ID
D00183

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Muscarinic acetylcholine receptor M3 (CHRM3) TTQ13Z5 ACM3_HUMAN Antagonist [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [4]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Approved [5]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Approved [4]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Approved [4]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.867 5.142 5.52 7.08
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 3.307 5.005 3.921 5.327
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 11.76 5.931 6.164 9.423
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Overactive bladder
ICD Disease Classification GC50.0
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Muscarinic acetylcholine receptor M3 (CHRM3) DTT CHRM3 4.61E-07 -0.59 -0.73
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 2.40E-01 -3.31E-02 -1.97E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 7.30E-01 -1.91E-02 -1.41E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 1.90E-01 -9.81E-03 -5.96E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.04E-02 6.29E-02 3.54E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2 Tolterodine FDA Label
3 Signal transduction underlying carbachol-induced contraction of human urinary bladder. J Pharmacol Exp Ther. 2004 Jun;309(3):1148-53.
4 Tolterodine, a new muscarinic receptor antagonist, is metabolized by cytochromes P450 2D6 and 3A in human liver microsomes. Drug Metab Dispos. 1998 Apr;26(4):289-93.
5 Effect of the CYP2D6*10 genotype on tolterodine pharmacokinetics. Drug Metab Dispos. 2010 Sep;38(9):1456-63.