General Information of Drug (ID: DM0JETC)

Drug Name
Genistein Drug Info
Synonyms
Bonistein; GEN; Genestein; Genisteol; Genisterin; Prunetol; Sophoricol; Differenol A; G 6649; G10000; IN1327; NPI 031L; STO514; TNP00151; GENISTEIN (ENDOCRINE DISRUPTER); Lactoferrin-genistein; PTI G4660 (Genistein); PTI-G4660; SIPI 807-1; C.I. 75610; SIPI-9764-I; ENDOCRINE DISRUPTOR (GENISTEIN) (SEE ALSO GENISTEIN (446-72-0)); 4 inverted exclamation marka,5,7-Trihydroxyisoflavone; ,5,7-Trihydroxyisoflavone; 4',5, 7-Trihydroxyisoflavone; 4',5,7-Trihydroxy isoflavone; 4',5,7-Trihydroxyisoflavone; 4,5,7-Trihydroxyiso-flavone; 4,6,7-Trihydroxyisoflavone; 5,7,4'-Trihydroxyisoflavone; 5,7-Dihydroxy-3-(4-hydroxyphenyl)-4-benzopyrone; 5,7-Dihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one; 5,7-dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one; 5,7-dihydroxy-3-(4-hydroxyphenyl)chromen-4-one
Indication
Disease Entry ICD 11 Status REF
Menopause symptom GA30.0 Phase 2/3 [1]
Prostate cancer 2C82.0 Phase 2 [2]
Cross-matching ID
PubChem CID
5280961
ChEBI ID
CHEBI:28088
CAS Number
CAS 446-72-0
TTD Drug ID
DM0JETC
VARIDT Drug ID
DR00641
INTEDE Drug ID
DR0768

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Estrogen receptor beta (ESR2) TTOM3J0 ESR2_HUMAN Modulator [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Phase 2 [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Phase 2 [5]
Sulfotransferase 2A1 (SULT2A1) DE0P6LK ST2A1_HUMAN Phase 2 [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 beta (ESR2) DTT ESR2 3.365 3.776 3.485 3.036
Breast cancer resistance protein (ABCG2) DTP BCRP 6.732 7.513 6.326 9.277
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 10.036 5.779 6.508 6.481
Sulfotransferase 2A1 (SULT2A1) DME SULT2A1 9.177 3.42 3.591 7.614
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 Menopause symptom
ICD Disease Classification GA30.0
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Estrogen receptor beta (ESR2) DTT ESR2 1.12E-20 -0.22 -0.7
Breast cancer resistance protein (ABCG2) DTP BCRP 1.46E-65 -1.41E+00 -1.41E+00
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 4.34E-02 -5.62E-03 -1.44E-02
Sulfotransferase 2A1 (SULT2A1) DME SULT2A1 8.40E-01 5.46E-03 3.67E-02
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 ClinicalTrials.gov (NCT00355953) Vascular and Skeletal Protective Effects of Genistein in Postmenopausal Women. U.S. National Institutes of Health.
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: 2826).
3 Company report (Axcentua)
4 Differential selectivity of efflux transporter inhibitors in Caco-2 and MDCK-MDR1 monolayers: a strategy to assess the interaction of a new chemical entity with P-gp, BCRP, and MRP2. J Pharm Sci. 2012 May;101(5):1888-97.
5 Differential mechanisms for the inhibition of human cytochrome P450 1A2 by apigenin and genistein. J Biochem Mol Toxicol. 2010 Jul-Aug;24(4):230-4.
6 Sulfation of environmental estrogens by cytosolic human sulfotransferases. Drug Metab Pharmacokinet. 2002;17(3):221-8.