Details of the Drug Combination

General Information of Drug Combination (ID: DCT2TOA)

Drug Combination Name
Estradiol Valerate Oestradiol valerate and dienogest
Indication
Disease Entry Status REF
Discovery agent Approved [1]
Component Drugs Estradiol Valerate   DM8MC6O Oestradiol valerate and dienogest   DMZK0FQ
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Estradiol Valerate
Disease Entry ICD 11 Status REF
Hormone replacement therapy 8E01 Approved [1]
Estradiol Valerate Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Estrogen receptor (ESR) TTZAYWL ESR1_HUMAN Modulator [3]
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Estradiol Valerate Interacts with 8 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [4]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Metabolism [5]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Metabolism [6]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [7]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Metabolism [7]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Metabolism [8]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Metabolism [4]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Metabolism [8]
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⏷ Show the Full List of 8 DME(s)
Indication(s) of Oestradiol valerate and dienogest
Disease Entry ICD 11 Status REF
Contraception QA21 Approved [1]
Endometriosis GA10 Approved [2]
Oestradiol valerate and dienogest Interacts with 1 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [9]
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Oestradiol valerate and dienogest Interacts with 8 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Aromatase (CYP19A1) OTZ6XF74 CP19A_HUMAN Decreases Expression [10]
Nuclear factor NF-kappa-B p105 subunit (NFKB1) OTNRRD8I NFKB1_HUMAN Affects Localization [10]
Prostaglandin G/H synthase 2 (PTGS2) OT75U9M4 PGH2_HUMAN Decreases Expression [10]
17-beta-hydroxysteroid dehydrogenase type 2 (HSD17B2) OT3K7HY5 DHB2_HUMAN Decreases Expression [11]
Aldo-keto reductase family 1 member C2 (AKR1C2) OTQ2XMO3 AK1C2_HUMAN Decreases Expression [11]
Aldo-keto reductase family 1 member C1 (AKR1C1) OTQKR4CM AK1C1_HUMAN Decreases Expression [11]
Follitropin subunit beta (FSHB) OTGLS283 FSHB_HUMAN Decreases Expression [12]
Lutropin subunit beta (LHB) OT5GBOVJ LSHB_HUMAN Decreases Expression [12]
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⏷ Show the Full List of 8 DOT(s)

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
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: 7654).
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
4 A potential role for the estrogen-metabolizing cytochrome P450 enzymes in human breast carcinogenesis. Breast Cancer Res Treat. 2003 Dec;82(3):191-7.
5 Inhibition of the human liver microsomal and human cytochrome P450 1A2 and 3A4 metabolism of estradiol by deployment-related and other chemicals. Drug Metab Dispos. 2006 Sep;34(9):1606-14.
6 Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
7 Drug Interactions Flockhart Table
8 Role of cytochrome P450 in estradiol metabolism in vitro. Acta Pharmacol Sin. 2001 Feb;22(2):148-54.
9 Progestogens in menopausal hormone therapy. Prz Menopauzalny. 2015 Jun;14(2):134-43.
10 Dienogest inhibits aromatase and cyclooxygenase-2 expression and prostaglandin E?production in human endometriotic stromal cells in spheroid culture. Fertil Steril. 2012 Feb;97(2):477-82.
11 Progestin effects on expression of AKR1C1-AKR1C3, SRD5A1 and PGR in the Z-12 endometriotic epithelial cell line. Chem Biol Interact. 2013 Feb 25;202(1-3):218-25.
12 Twenty-one day administration of dienogest reversibly suppresses gonadotropins and testosterone in normal men. J Clin Endocrinol Metab. 2002 May;87(5):2107-13. doi: 10.1210/jcem.87.5.8514.