DT-Web

DB00858 - Drostanolone


Identification
Name Drostanolone
Accession Number DB00858 (APRD00938)
Type small molecule
Description Drostanolone (also known as dromostanolone) is a potent synthetic androgenic anabolic steroid similar to testosterone. Drostanolone is indicated in postmenopausal women with recurrent breast cancer, in a combined hormone therapy.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 304.4669
Groups illicit
Monoisotopic Weight 304.240230268
Pharmacology
Indication For use in females, for palliation of androgenresponsive recurrent mammary cancer in women who are more than one year but less than five years postmenopausal.
Mechanism of action Dromostanolone is a synthetic androgenic anabolic steroid and is approximately 5 times as potent as natural methyltestosterone. Like testosterone and other androgenic hormones, dromostanolone binds to the androgen receptor. This causes downstream genetic transcriptional changes. This ultimately causes retention of nitrogen, potassium, and phosphorus; increases protein anabolism; and decreases amino acid catabolism. The antitumour activity of dromostanolone appears related to reduction or competitive inhibition of prolactin receptors or estrogen receptors or production.
Absorption Well absorbed following parenteral administration.
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Side effects include virilization (masculine traits in women), acne, fluid retention, and hypercalcemia.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


Androgen receptor
Name Androgen receptor
Gene Name AR
Pharmacological action yes
Actions agonist
References
  • Zakar T, Kaufmann G, Toth M: Assignment of anabolic-androgenic and antiandrogenic properties to some chlorine-substituted steroids on the basis of their binding characteristics to the androgen receptor of the rat seminal vesicle. Exp Clin Endocrinol. 1986 Jul;87(2):133-41. - Pubmed
  • Takahashi M, Tatsugi Y, Kohno T: Endocrinological and pathological effects of anabolic-androgenic steroid in male rats. Endocr J. 2004 Aug;51(4):425-34. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 1.1718

Enzymes


Cytochrome P450 19A1
Name Cytochrome P450 19A1
Gene Name CYP19A1
Actions inhibitor
References
  • Navarro-Martin L, Blazquez M, Piferrer F: Masculinization of the European sea bass (Dicentrarchus labrax) by treatment with an androgen or aromatase inhibitor involves different gene expression and has distinct lasting effects on maturation. Gen Comp Endocrinol. 2009 Jan 1;160(1):3-11. Epub 2008 Oct 18. - Pubmed
DTHybrid score 0.4325

Carriers


Predictions


Id Partner name Gene Name Score
4512 Cytochrome P450 3A4 CYP3A4 0.1014
136 Estrogen receptor ESR1 0.0813
869 Estrogen receptor beta ESR2 0.0632
614 Progesterone receptor PGR 0.063
381 Prolactin receptor PRLR 0.0477
1588 Multidrug resistance protein 1 ABCB1 0.0464
871 Glucocorticoid receptor NR3C1 0.0462
6017 Cholesterol side-chain cleavage enzyme, mitochondrial CYP11A1 0.0456
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.042
6016 Cytochrome P450 2C19 CYP2C19 0.0407
226 Gonadotropin-releasing hormone receptor GNRHR 0.0384
4757 Cytochrome P450 2C9 CYP2C9 0.0366
269 Adrenodoxin, mitochondrial FDX1 0.0348
4200 Cytochrome P450 1A2 CYP1A2 0.0347
587 Serum albumin ALB 0.0338
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0327
4924 Cytochrome P450 2C8 CYP2C8 0.0327
6030 Cytochrome P450 2B6 CYP2B6 0.031
1649 Small inducible cytokine A2 CCL2 0.0291
217 Estradiol 17-beta-dehydrogenase 1 HSD17B1 0.0286
380 Cytochrome P450 17A1 CYP17A1 0.0286
4118 Cytochrome P450 3A5 CYP3A5 0.0282
737 Mineralocorticoid receptor NR3C2 0.0267
6107 Cytochrome P450 3A7 CYP3A7 0.0261
232 Corticosteroid-binding globulin SERPINA6 0.0229
6142 Solute carrier family 22 member 8 SLC22A8 0.022
260 Cytochrome P450 51 ERG11 0.0214
761 Cytochrome P450 51 ERG11 0.0214
3163 Cytochrome P450 51 cyp51 0.0214
563 Thyroid peroxidase TPO 0.0207
4116 Dihydropteroate synthetase Not Available 0.0199
3941 Amine oxidase [flavin-containing] A MAOA 0.0193
6013 Cytochrome P450 2E1 CYP2E1 0.0191
148 Lutropin-choriogonadotropic hormone receptor LHCGR 0.0175
5718 Cytochrome P450 2A6 CYP2A6 0.0167
1898 Cytochrome P450 1B1 CYP1B1 0.0161
596 3-oxo-5-alpha-steroid 4-dehydrogenase 1 SRD5A1 0.0161
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0159
6024 Cytochrome P450 1A1 CYP1A1 0.0153
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0151
6145 Solute carrier family 22 member 1 SLC22A1 0.0148
3939 Amine oxidase [flavin-containing] B MAOB 0.0148
3810 Catechol O-methyltransferase COMT 0.0145
4119 Cytochrome P450 2D6 CYP2D6 0.0137
290 Prostaglandin G/H synthase 2 PTGS2 0.0133
6022 UDP-glucuronosyltransferase 1-1 UGT1A1 0.0131
6241 Nuclear receptor coactivator 2 NCOA2 0.013
469 Annexin A1 ANXA1 0.013
3923 Cholinesterase BCHE 0.0125
6044 Serum paraoxonase/lactonase 3 PON3 0.0118
6014 Cytochrome P450 2A13 CYP2A13 0.0081
3957 Adenosine deaminase ADA 0.0079
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0078
1680 Solute carrier family 2, facilitated glucose transporter member 1 SLC2A1 0.0078
6031 Cytochrome P450 3A43 CYP3A43 0.0076
373 Transthyretin TTR 0.0076
4120 NADPH--cytochrome P450 reductase POR 0.0074
6147 Solute carrier family 22 member 3 SLC22A3 0.0074
650 Aldo-keto reductase family 1 member C3 AKR1C3 0.0071
1656 CYP2B protein CYP2B 0.0068
20 Prostaglandin G/H synthase 1 PTGS1 0.0062
6141 Sodium/bile acid cotransporter SLC10A1 0.0062
6078 Neuronal acetylcholine receptor subunit beta-4 CHRNB4 0.006
6143 Solute carrier family 22 member 7 SLC22A7 0.0058
847 Mu-type opioid receptor OPRM1 0.0056
6079 Neuronal acetylcholine receptor subunit alpha-3 CHRNA3 0.0054
6220 Aryl hydrocarbon receptor AHR 0.0053
833 Organic cation/carnitine transporter 1 SLC22A4 0.005
3947 Xanthine dehydrogenase/oxidase XDH 0.005
1284 Nuclear receptor subfamily 1 group I member 2 NR1I2 0.0049
144 Hemoglobin subunit alpha HBA1 0.0049
3809 Estrogen-related receptor gamma ESRRG 0.0048
564 Cellular retinoic acid-binding protein 1 CRABP1 0.0047
776 Bile salt export pump ABCB11 0.0047
6020 Aldehyde oxidase AOX1 0.0047
629 Alpha-2B adrenergic receptor ADRA2B 0.0047
5934 Cytochrome P450 26A1 CYP26A1 0.0047
1010 Cytochrome P450 51A1 CYP51A1 0.0046
1729 Solute carrier family 22 member 6 SLC22A6 0.0046
6153 Solute carrier organic anion transporter family member 4A1 SLCO4A1 0.0045
1178 Adenosine A2a receptor ADORA2A 0.0045
6148 Multidrug resistance-associated protein 7 ABCC10 0.0043
780 Retinoic acid receptor RXR-gamma RXRG 0.0043
229 Retinoic acid receptor beta RARB 0.0043
634 Squalene monooxygenase SQLE 0.0043
7196 Squalene monooxygenase ERG1 0.0043
730 Retinoic acid receptor alpha RARA 0.0042
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.0042
6158 Solute carrier organic anion transporter family member 1C1 SLCO1C1 0.0041
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.004
462 Intermediate conductance calcium-activated potassium channel protein 4 KCNN4 0.004
459 Retinoic acid receptor RXR-alpha RXRA 0.004
6157 Solute carrier organic anion transporter family member 1B3 SLCO1B3 0.0039
88 Retinoic acid receptor RXR-beta RXRB 0.0039
162 Retinoic acid receptor gamma-1 RARG 0.0039
567 Receptor tyrosine-protein kinase erbB-2 ERBB2 0.0038
2782 Complement C1s subcomponent C1S 0.0037
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.0037
6085 Fatty acid-binding protein, intestinal FABP2 0.0036
3815 Complement C1q subcomponent subunit A C1QA 0.0034
3816 Complement C1q subcomponent subunit B C1QB 0.0034
3817 Complement C1q subcomponent subunit C C1QC 0.0034
1024 Solute carrier family 22 member 11 SLC22A11 0.0034
3818 Low affinity immunoglobulin gamma Fc region receptor III-A FCGR3A 0.0034
3819 Low affinity immunoglobulin gamma Fc region receptor II-a FCGR2A 0.0034
1102 Low affinity immunoglobulin gamma Fc region receptor III-B FCGR3B 0.0034
3821 Low affinity immunoglobulin gamma Fc region receptor II-c FCGR2C 0.0034
3814 Complement C1r subcomponent C1R 0.0034
3830 Calreticulin CALR 0.0034
3820 Low affinity immunoglobulin gamma Fc region receptor II-b FCGR2B 0.0034
474 Acetylcholinesterase ACHE 0.0033
784 High affinity immunoglobulin gamma Fc receptor I FCGR1A 0.0032
6035 Nuclear receptor ROR-beta RORB 0.0032
6034 Hydroxyindole O-methyltransferase ASMT 0.0032
6036 Eosinophil peroxidase EPX 0.0032
6144 Solute carrier family 22 member 2 SLC22A2 0.0031
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0029
844 Epidermal growth factor receptor EGFR 0.0028
765 Indoleamine 2,3-dioxygenase IDO1 0.0027
571 Melatonin receptor type 1A MTNR1A 0.0026
362 Melatonin receptor type 1B MTNR1B 0.0026
5923 Microtubule-associated protein tau MAPT 0.0024
5924 Microtubule-associated protein 4 MAP4 0.0024
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.0023
267 Plasminogen activator inhibitor 1 SERPINE1 0.0023
1852 Microtubule-associated protein 2 MAP2 0.0023
7 Nitric oxide synthase, inducible NOS2 0.0022
6931 Calcium-activated potassium channel subunit beta-1 KCNMB1 0.0022
6933 Calcium-activated potassium channel subunit beta-4 KCNMB4 0.0022
6932 Calcium-activated potassium channel subunit beta-3 KCNMB3 0.0022
6934 Small conductance calcium-activated potassium channel protein 1 KCNN1 0.0022
6935 Small conductance calcium-activated potassium channel protein 2 KCNN2 0.0022
6936 Small conductance calcium-activated potassium channel protein 3 KCNN3 0.0022
273 Apoptosis regulator Bcl-2 BCL2 0.0021
6221 Steroid hormone receptor ERR1 ESRRA 0.0021
6002 Prostaglandin E2 receptor EP4 subtype PTGER4 0.002
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.002
243 Ribosyldihydronicotinamide dehydrogenase [quinone] NQO2 0.0019
5463 Calcium-activated potassium channel subunit beta 2 KCNMB2 0.0019
29 Tubulin beta-1 chain TUBB1 0.0019
84 Nuclear receptor 0B1 NR0B1 0.0019
4131 Prostaglandin E2 receptor, EP3 subtype PTGER3 0.0018
1457 Long-chain-fatty-acid--CoA ligase 4 ACSL4 0.0018
406 Prostaglandin E2 receptor, EP2 subtype PTGER2 0.0018
6106 Cytochrome P450 2C18 CYP2C18 0.0018
6167 Organic solute transporter subunit beta OSTB 0.0018
6166 Organic solute transporter subunit alpha OSTA 0.0018
467 Delta-type opioid receptor OPRD1 0.0018
1192 Sulfotransferase 1A1 SULT1A1 0.0018
1757 Myeloperoxidase MPO 0.0017
6104 Dimethylaniline monooxygenase [N-oxide-forming] 1 FMO1 0.0017
465 Calmodulin CALM1 0.0017
6181 UDP-glucuronosyltransferase 1-8 UGT1A8 0.0016
6177 UDP-glucuronosyltransferase 1-10 UGT1A10 0.0016
73 Prostaglandin E2 receptor, EP1 subtype PTGER1 0.0016
1709 Canalicular multispecific organic anion transporter 2 ABCC3 0.0016
514 Potassium voltage-gated channel subfamily H member 6 KCNH6 0.0015
772 Potassium voltage-gated channel subfamily H member 7 KCNH7 0.0015
6160 Solute carrier organic anion transporter family member 3A1 SLCO3A1 0.0015
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0014
2222 Equilibrative nucleoside transporter 1 SLC29A1 0.0014
6152 Solute carrier organic anion transporter family member 2A1 SLCO2A1 0.0014
610 Calcium-activated potassium channel subunit alpha 1 KCNMA1 0.0014
468 Cytochrome P450 4A11 CYP4A11 0.0014
6136 Multidrug resistance-associated protein 5 ABCC5 0.0013
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0013
862 Multidrug resistance-associated protein 1 ABCC1 0.0013
4604 Liver carboxylesterase 1 CES1 0.0012
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0012
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0012
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0012
238 Peroxisome proliferator-activated receptor gamma PPARG 0.0012
2164 Multidrug resistance-associated protein 4 ABCC4 0.0011
291 Nitric-oxide synthase, endothelial NOS3 0.0011
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