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

General Information of Drug (ID: DMY85QW)

Drug Name
Bazedoxifene Drug Info
Synonyms Brilence; Conbriza; Viviant; Bazedoxifene acetate; TSE-424; WAY-140424; WAY-TES 424
Indication
Disease Entry ICD 11 Status REF
Hot flushes GA30 Approved [1]
Osteopetrosis LD24.10 Approved [2]
Cross-matching ID
PubChem CID
154257
ChEBI ID
CHEBI:135947
CAS Number
CAS 198481-32-2
TTD Drug ID
DMY85QW
INTEDE Drug ID
DR0177

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Estrogen receptor (ESR) TTZAYWL ESR1_HUMAN Modulator [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Phase 4 [4]
UDP-glucuronosyltransferase 1A10 (UGT1A10) DEL5N6Y UD110_HUMAN Phase 4 [5]
Beta-glucuronidase (uidA) DEWTCUK Q9AHJ8_LACGS Phase 4 [6]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Estrogen receptor (ESR) DTT ESR1 3.728 3.17 4.897 4.505
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 Hot flushes
ICD Disease Classification GA30
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 7.69E-01 1.91E-02 5.45E-02
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Bazedoxifene FDA Label
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7355).
3 Bazedoxifene, a selective estrogen receptor modulator: effects on the endometrium, ovaries, and breast from a randomized controlled trial in osteoporotic postmenopausal women. Menopause. 2009 Nov-Dec;16(6):1109-15.
4 UGT1A1*28 polymorphism influences glucuronidation of bazedoxifene. Pharmazie. 2015 Feb;70(2):94-6.
5 In vitro metabolism, permeability, and efflux of bazedoxifene in humans. Drug Metab Dispos. 2010 Sep;38(9):1471-9.
6 Long-term administration of conjugated estrogen and bazedoxifene decreased murine fecal beta-glucuronidase activity without impacting overall microbiome community. Sci Rep. 2018 May 25;8(1):8166.