DT-Web

DB00378 - Dydrogesterone


Identification
Name Dydrogesterone
Accession Number DB00378 (APRD00941)
Type small molecule
Description A synthetic progestational hormone with no androgenic or estrogenic properties. Unlike many other progestational compounds, dydrogesterone produces no increase in temperature and does not inhibit ovulation. [PubChem]
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 312.4458
Groups approved
Monoisotopic Weight 312.20893014
Pharmacology
Indication Used to treat irregular duration of cycles and irregular occurrence and duration of periods caused by progesterone deficiency. Also used to prevent natural abortion in patients who have a history of habitual abortions.
Mechanism of action Dydrogesterone is a progestogen that works by regulating the healthy growth and normal shedding of the womb lining by acting on progesterone receptors in the uterus.
Absorption Rapidly absorbed in the gastrointestinal tract with a bioavailability of 28%.
Protein binding Not Available
Biotransformation Metabolism is complete to a 20-dihydrodydrogesterone (DHD) metabolite.
Route of elimination Not Available
Toxicity No serious or unexpected toxicity has been observed with dydrogesterone. In acute toxicity studies, the LD50 doses in rats exceeded 4,640mg/kg for the oral route.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


Progesterone receptor
Name Progesterone receptor
Gene Name PGR
Pharmacological action yes
Actions agonist
References
  • Blois SM, Joachim R, Kandil J, Margni R, Tometten M, Klapp BF, Arck PC: Depletion of CD8+ cells abolishes the pregnancy protective effect of progesterone substitution with dydrogesterone in mice by altering the Th1/Th2 cytokine profile. J Immunol. 2004 May 15;172(10):5893-9. - Pubmed
  • Tamaya T, Tsurusaki T, Ide N, Yamada T, Murakami T, Wada K, Fujimoto Z, Okada H: Nuclear translocation of progesterone receptor--progestogen complex in vitro. Nippon Sanka Fujinka Gakkai Zasshi. 1983 Jan;35(1):77-82. - Pubmed
  • Raghupathy R, Al Mutawa E, Makhseed M, Azizieh F, Szekeres-Bartho J: Modulation of cytokine production by dydrogesterone in lymphocytes from women with recurrent miscarriage. BJOG. 2005 Aug;112(8):1096-101. - Pubmed
  • Okada H: [Metabolism, structure and biological activity of sex steroids] Nippon Naibunpi Gakkai Zasshi. 1993 Feb 20;69(2):67-79. - Pubmed
  • Tamaya T, Furuta N, Ohono Y, Ide N, Tsurusaki T, Okada H: Chromatin transcription by progesterone-receptor complex in rabbit uterus. Endocrinol Jpn. 1979 Feb;26(1):117-22. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 0.5685

Predictions


Id Partner name Gene Name Score
136 Estrogen receptor ESR1 0.1298
2202 Steryl-sulfatase STS 0.0552
146 Androgen receptor AR 0.0486
4512 Cytochrome P450 3A4 CYP3A4 0.0474
871 Glucocorticoid receptor NR3C1 0.0359
737 Mineralocorticoid receptor NR3C2 0.0293
1588 Multidrug resistance protein 1 ABCB1 0.0218
6241 Nuclear receptor coactivator 2 NCOA2 0.0206
756 Sex hormone-binding globulin SHBG 0.0195
6107 Cytochrome P450 3A7 CYP3A7 0.0173
596 3-oxo-5-alpha-steroid 4-dehydrogenase 1 SRD5A1 0.0172
66 3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type II HSD3B2 0.0167
4118 Cytochrome P450 3A5 CYP3A5 0.0163
3811 Cytochrome P450 19A1 CYP19A1 0.0159
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0151
1649 Small inducible cytokine A2 CCL2 0.0127
226 Gonadotropin-releasing hormone receptor GNRHR 0.0103
3923 Cholinesterase BCHE 0.0094
290 Prostaglandin G/H synthase 2 PTGS2 0.0091
723 Cytosolic phospholipase A2 PLA2G4A 0.0091
232 Corticosteroid-binding globulin SERPINA6 0.0088
862 Multidrug resistance-associated protein 1 ABCC1 0.0082
4924 Cytochrome P450 2C8 CYP2C8 0.008
4757 Cytochrome P450 2C9 CYP2C9 0.0073
6016 Cytochrome P450 2C19 CYP2C19 0.0062
4119 Cytochrome P450 2D6 CYP2D6 0.0057
587 Serum albumin ALB 0.0051
380 Cytochrome P450 17A1 CYP17A1 0.0036
6141 Sodium/bile acid cotransporter SLC10A1 0.003
6147 Solute carrier family 22 member 3 SLC22A3 0.0025
1898 Cytochrome P450 1B1 CYP1B1 0.0025
776 Bile salt export pump ABCB11 0.0025
6144 Solute carrier family 22 member 2 SLC22A2 0.0021
6145 Solute carrier family 22 member 1 SLC22A1 0.0021
5718 Cytochrome P450 2A6 CYP2A6 0.002
6024 Cytochrome P450 1A1 CYP1A1 0.002
4200 Cytochrome P450 1A2 CYP1A2 0.0016
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