General Information of Drug (ID: DMMG26Z)

Drug Name
Dolasetron Drug Info
Synonyms Dolasetronum; Dolasteron; Anzemet (TN); Dolasetron (INN); Dolasetron [INN:BAN]; Dolasetronum [INN-Latin]; 3-oxooctahydro-2h-2,6-methanoquinolizin-8-yl 1h-indole-3-carboxylate
Indication
Disease Entry ICD 11 Status REF
Nausea MD90 Approved [1]
Therapeutic Class
Antiemetics
Cross-matching ID
PubChem CID
3033818
ChEBI ID
CHEBI:94561
CAS Number
CAS 115956-12-2
TTD Drug ID
DMMG26Z
INTEDE Drug ID
DR0524
ACDINA Drug ID
D00209

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 3A receptor (HTR3A) TTPC4TU 5HT3A_HUMAN Antagonist [2]

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

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
5-HT 3A receptor (HTR3A) DTT HTR3A 5.693 5.728 5.986 6.087
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 Nausea
ICD Disease Classification MD90
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
5-HT 3A receptor (HTR3A) DTT HTR3A 6.60E-01 1.08E-02 0.04
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 8.20E-01 -1.63E-03 -1.13E-02
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 7.48E-04 3.43E-01 6.77E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 9.40E-01 -2.17E-02 -4.03E-02
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
2 Palonosetron plus dexamethasone versus granisetron plus dexamethasone for prevention of nausea and vomiting during chemotherapy: a double-blind, do... Lancet Oncol. 2009 Feb;10(2):115-24.
3 Characterization of the cytochrome P450 enzymes involved in the in vitro metabolism of dolasetron. Comparison with other indole-containing 5-HT3 antagonists. Drug Metab Dispos. 1996 May;24(5):602-9.
4 Reappraisal of the role of dolasetron in prevention and treatment of nausea and vomiting associated with surgery or chemotherapy. Cancer Manag Res. 2012;4:67-73.
5 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.