General Information of Drug (ID: DM67VKL)

Drug Name
Prasterone Drug Info
Synonyms
Dehydroepiandrosterone; DHEA; 53-43-0; PRASTERONE; Dehydroisoandrosterone; Androstenolone; trans-Dehydroandrosterone; Psicosterone; Diandrone; Diandron; 3beta-hydroxyandrost-5-en-17-one; 17-Hormoforin; Prestara; 17-Chetovis; Andrestenol; 5-Dehydroepiandrosterone; Intrarosa; Siscelar plus; 5,6-Didehydroisoandrosterone; Dehydro-epi-androsterone; Prasteronum; 5,6-Dehydroisoandrosterone; Prasterona; Epiandrosterone, 5-dehydro-; Caswell No 051F; 5,6-Dehydroisoandrostorone
Indication
Disease Entry ICD 11 Status REF
Chronic obstructive pulmonary disease CA22 Approved [1]
Cardiovascular disease BA00-BE2Z Phase 4 [2]
Cross-matching ID
PubChem CID
5881
ChEBI ID
CHEBI:28689
CAS Number
CAS 53-43-0
TTD Drug ID
DM67VKL
VARIDT Drug ID
DR01193
INTEDE Drug ID
DR0431

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Androgen receptor (AR) TTS64P2 ANDR_HUMAN Antagonist [3]
Glucose-6-phosphate dehydrogenase (G6PD) TTKN8W0 G6PD_HUMAN Inhibitor [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Multidrug resistance-associated protein 8 (ABCC11) DTWN7FC ABCCB_HUMAN Approved [5]
Multidrug resistance-associated protein 4 (ABCC4) DTCSGPB MRP4_HUMAN Approved [6]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Approved [7]
Organic anion transporter 3 (SLC22A8) DTVP67E S22A8_HUMAN Approved [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [9]
Aromatase (CYP19A1) DEQX145 CP19A_HUMAN Approved [10]
Beta-HSD adrenal and gonadal type (HSD3B2) DEN0GVQ 3BHS2_HUMAN Approved [11]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Approved [12]
Sulfotransferase 2A1 (SULT2A1) DE0P6LK ST2A1_HUMAN Approved [13]
Estradiol 17-beta-dehydrogenase 2 (HSD17B2) DEBMFZ8 DHB2_HUMAN Approved [14]
Estradiol 17-beta-dehydrogenase 1 (HSD17B1) DEZS5YK DHB1_HUMAN Approved [14]
Dihydrotestosterone oxidoreductase (HSD3B1) DERDQWN 3BHS1_HUMAN Approved [11]
Peroxisomal multifunctional enzyme 2 (HSD17B4) DEJHG19 DHB4_HUMAN Approved [14]
Sulfotransferase 2B1 (SULT2B1) DEZBN53 ST2B1_HUMAN Approved [15]
Cytochrome P450 7B1 (CYP7B1) DE36TMY CP7B1_HUMAN Approved [16]

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
Glucose-6-phosphate dehydrogenase (G6PD) DTT G6PD 3.868 3.733 5.853 5.498
Organic anion transporter 3 (SLC22A8) DTP OAT3 2.722 2.07 8.103 3.597
Breast cancer resistance protein (ABCG2) DTP BCRP 6.732 7.513 6.326 9.277
Multidrug resistance-associated protein 4 (ABCC4) DTP MRP4 4.797 7.054 6.875 5.42
Estradiol 17-beta-dehydrogenase 1 (HSD17B1) DME HSD17B1 2.459 3.935 2.263 2.848
Sulfotransferase 2B1 (SULT2B1) DME SULT2B1 5.781 4.921 5.413 6.345
Dihydrotestosterone oxidoreductase (HSD3B1) DME HSD3B1 3.926 3.018 3.755 5.684
Aromatase (CYP19A1) DME CYP19A1 6.002 5.514 3.278 3.322
Beta-HSD adrenal and gonadal type (HSD3B2) DME HSD3B2 5.158 5.244 4.053 3.036
Peroxisomal multifunctional enzyme 2 (HSD17B4) DME HSD17B4 9.491 7.489 7.983 8.154
Estradiol 17-beta-dehydrogenase 2 (HSD17B2) DME HSD17B2 9.546 8.31 4.358 10.177
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
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 Chronic obstructive pulmonary disease
ICD Disease Classification CA22
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Androgen receptor (AR) DTT AR 2.13E-01 -0.07 -0.11
Multidrug resistance-associated protein 8 (ABCC11) DTP MRP8 8.53E-01 -1.36E-02 -1.47E-01
Organic anion transporter 3 (SLC22A8) DTP OAT3 4.32E-04 -2.82E-01 -1.59E+00
Breast cancer resistance protein (ABCG2) DTP BCRP 1.91E-02 2.50E-01 1.01E+00
Multidrug resistance-associated protein 4 (ABCC4) DTP MRP4 4.07E-01 2.22E-01 6.78E-01
Estradiol 17-beta-dehydrogenase 1 (HSD17B1) DME HSD17B1 6.19E-01 -3.50E-02 -1.64E-01
Sulfotransferase 2B1 (SULT2B1) DME SULT2B1 6.20E-04 -3.23E-01 -1.55E+00
Dihydrotestosterone oxidoreductase (HSD3B1) DME HSD3B1 5.08E-01 -9.14E-03 -6.31E-02
Aromatase (CYP19A1) DME CYP19A1 1.92E-04 -1.80E-01 -1.31E+00
Beta-HSD adrenal and gonadal type (HSD3B2) DME HSD3B2 5.77E-03 -2.35E-01 -1.08E+00
Peroxisomal multifunctional enzyme 2 (HSD17B4) DME HSD17B4 8.37E-03 -1.16E-01 -7.40E-01
Estradiol 17-beta-dehydrogenase 2 (HSD17B2) DME HSD17B2 1.04E-04 -2.41E-01 -1.69E+00
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 7.93E-02 -8.20E-02 -8.93E-01
Cytochrome P450 7B1 (CYP7B1) DME CYP7B1 7.78E-02 6.64E-02 8.61E-01
Sulfotransferase 2A1 (SULT2A1) DME SULT2A1 6.05E-02 -4.22E-02 -5.22E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Direct agonist/antagonist functions of dehydroepiandrosterone. Endocrinology. 2005 Nov;146(11):4568-76.
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: 2370).
3 Dehydroepiandrosterone, glucose-6-phosphate dehydrogenase, and longevity. Ageing Res Rev. 2004 Apr;3(2):171-87.
4 Glucose utilization and activity of glucose-6-phosphate dehydrogenase, isocitrate dehydrogenase and malate dehydrogenase in rat erythrocytes after treatment with tuberculostatic agents. Vopr Med Khim. 1986 Sep-Oct;32(5):32-5.
5 Human multidrug resistance protein 8 (MRP8/ABCC11), an apical efflux pump for steroid sulfates, is an axonal protein of the CNS and peripheral nervous system. Neuroscience. 2006;137(4):1247-57.
6 Steroid and bile acid conjugates are substrates of human multidrug-resistance protein (MRP) 4 (ATP-binding cassette C4). Biochem J. 2003 Apr 15;371(Pt 2):361-7.
7 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
8 Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. Mol Pharmacol. 2001 May;59(5):1277-86.
9 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
10 Urinary and serum octopamine in patients with portal-systemic encephalopathy. Lancet. 1975 Nov 15;2(7942):943-6.
11 Selective inhibition of human 3beta-hydroxysteroid dehydrogenase type 1 as a potential treatment for breast cancer. J Steroid Biochem Mol Biol. 2011 May;125(1-2):57-65.
12 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
13 Sulfation of environmental estrogens by cytosolic human sulfotransferases. Drug Metab Pharmacokinet. 2002;17(3):221-8.
14 Steroid signalling in the ovarian surface epithelium. Trends Endocrinol Metab. 2005 Sep;16(7):327-33.
15 Expression and characterization of the human 3 beta-hydroxysteroid sulfotransferases (SULT2B1a and SULT2B1b). J Steroid Biochem Mol Biol. 2001 Jun;77(4-5):261-9.
16 CYP7B1-mediated metabolism of dehydroepiandrosterone and 5alpha-androstane-3beta,17beta-diol--potential role(s) for estrogen signaling. FEBS J. 2008 Apr;275(8):1778-89.