General Information of Drug (ID: DM3S8XC)

Drug Name
Dihydrotestosterone Drug Info
Synonyms
Androstanolone; STANOLONE; dihydrotestosterone; 521-18-6; Andractim; Androlone; Proteina; Anaboleen; Stanaprol; Anabolex; Protona; Neodrol; Cristerona MB; 4-Dihydrotestosterone; 17beta-Hydroxy-5alpha-androstan-3-one; 5alpha-Dihydrotestosterone; Androstanolonum; Androstanolona; DHT; 5-alpha-Dihydrotestosterone; Dihydrotestosteron; Testosterone, dihydro-; 4,5alpha-Dihydrotestosterone; 5alpha-Androstan-17beta-ol-3-one; Stanorone; Stanolon; 17beta-Hydroxyandrostan-3-one; 5alpha-DHT; LG 152; 17beta-Hydroxy-3-androstanone; [3H]dihydrotestosterone
Indication
Disease Entry ICD 11 Status REF
Prostate hyperplasia GA90 Phase 4 [1]
Cross-matching ID
PubChem CID
10635
ChEBI ID
CHEBI:16330
CAS Number
CAS 521-18-6
TTD Drug ID
DM3S8XC
VARIDT Drug ID
DR00733
INTEDE Drug ID
DR0114

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Androgen receptor (AR) TTS64P2 ANDR_HUMAN Modulator [2]
Androgen receptor messenger RNA (AR mRNA) TTKPW01 ANDR_HUMAN Agonist [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Phase 2 [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Phase 4 [5]
Aromatase (CYP19A1) DEQX145 CP19A_HUMAN Phase 4 [6]
Aldo-keto reductase 1C1 (AKR1C1) DE7P2FB AK1C1_HUMAN Phase 4 [7]
Steroid 17-alpha-monooxygenase (CYP17A1) DEX2KIA CP17A_HUMAN 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
Androgen receptor (AR) DTT AR 5.955 4.868 5.902 5.567
Androgen receptor messenger RNA (AR mRNA) DTT AR 5.955 4.868 5.902 5.567
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Steroid 17-alpha-monooxygenase (CYP17A1) DME CYP17A1 6.213 5.615 6.895 6.025
Aromatase (CYP19A1) DME CYP19A1 6.002 5.514 3.278 3.322
Aldo-keto reductase 1C1 (AKR1C1) DME AKR1C1 10.667 8.55 9.706 8.77
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 Prostate hyperplasia
ICD Disease Classification GA90
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Androgen receptor (AR) DTT AR 2.13E-01 -0.07 -0.11
P-glycoprotein 1 (ABCB1) DTP P-GP 2.80E-02 -1.36E-01 -1.05E+00
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 6.96E-03 -1.95E-01 -8.72E-01
Steroid 17-alpha-monooxygenase (CYP17A1) DME CYP17A1 2.51E-05 -2.92E-01 -2.29E+00
Aromatase (CYP19A1) DME CYP19A1 1.92E-04 -1.80E-01 -1.31E+00
Aldo-keto reductase 1C1 (AKR1C1) DME AKR1C1 2.85E-02 -3.00E-01 -7.48E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 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: 2856).
2 Inhibition of the dihydrotestosterone-activated androgen receptor by nuclear receptor corepressor. Mol Endocrinol. 2002 Jul;16(7):1492-501.
3 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. (Target id: 628).
4 P-glycoprotein increases the efflux of the androgen dihydrotestosterone and reduces androgen responsive gene activity in prostate tumor cells. Prostate. 2004 Apr 1;59(1):77-90.
5 UDP-glucuronosyltransferase 2B15 (UGT2B15) and UGT2B17 enzymes are major determinants of the androgen response in prostate cancer LNCaP cells. J Biol Chem. 2007 Nov 16;282(46):33466-74.
6 Identifying susceptibility genes for prostate cancer--a family-based association study of polymorphisms in CYP17, CYP19, CYP11A1, and LH-beta. Cancer Epidemiol Biomarkers Prev. 2005 Aug;14(8):2035-9.
7 Human 3-alpha hydroxysteroid dehydrogenase type 3 (3alpha-HSD3): the V54L mutation restricting the steroid alternative binding and enhancing the 20alpha-HSD activity. J Steroid Biochem Mol Biol. 2014 May;141:135-43.