Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMBPN7T)

Drug Name
RUPATADINE Drug Info
Synonyms
Rupatadine trihydrochloride; UNII-G61C8NZY2T; G61C8NZY2T; 156611-76-6; Rupatadine HCl; Rupatadine hydrochloride; UR 12592; AC1L320L; DTXSID90166109; BQFOTHHRVVHLEW-UHFFFAOYSA-N; 8-Chloro-6,11-dihydro-11-(1-((5-methyl-3-pyridinyl)methyl)-4-piperidinylidene)-5H-benzo(5,6)cyclohepta(1,2-b)pyridine trihydrochloride; 5H-Benzo(5,6)cyclohepta(1,2-b)pyridine, 8-chloro-6,11-dihydro-11-(1-((5-methyl-3-pyridinyl)methyl)-4-piperidinylidene)-, trihydrochloride
Cross-matching ID
PubChem CID
133017
ChEBI ID
CHEBI:135673
CAS Number
CAS 158876-82-5
TTD Drug ID
DMBPN7T
INTEDE Drug ID
DR1451

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histamine H1 receptor (H1R) TTTIBOJ HRH1_HUMAN Inhibitor [1]
Platelet-activating factor receptor (PTAFR) TTQL5VC PTAFR_HUMAN Inhibitor [1]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Phase 4 [2]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Phase 4 [3]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Phase 4 [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
Histamine H1 receptor (H1R) DTT HRH1 5.972 5.7 5.816 6.002
Platelet-activating factor receptor (PTAFR) DTT PTAFR 6.345 5.947 6.084 6.253
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
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

Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Histamine H1 receptor (H1R) DTT HRH1 6.86E-09 0.3 0.55
Platelet-activating factor receptor (PTAFR) DTT PTAFR 3.75E-05 0.25 0.35
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 3.85E-05 8.08E-01 6.07E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 2.25E-03 -4.98E-01 -6.49E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 6.90E-01 2.35E-02 7.88E-02
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
2 Rupatadine: pharmacological profile and its use in the treatment of allergic disorders. Expert Opin Pharmacother. 2006 Oct;7(14):1989-2001.
3 Product Monograph of Xtandi Rupatadine (as rupatadine fumarate).
4 CYP3A5*3 and MDR1 C3435T are influencing factors of inter-subject variability in rupatadine pharmacokinetics in healthy Chinese volunteers. Eur J Drug Metab Pharmacokinet. 2016 Apr;41(2):117-24.