Details of the Drug Combination

General Information of Drug Combination (ID: DCHDU6O)

Drug Combination Name
Mestranol Etonogestrel
Indication
Disease Entry Status REF
Contraception Phase 1 [1]
Component Drugs Mestranol   DMG3F94 Etonogestrel   DMKA8J4
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 Mestranol
Disease Entry ICD 11 Status REF
Contraception QA21 Approved [2]
Menorrhagia GA20.50 Approved [3]
Endometriosis GA10 Investigative [3]
Mestranol Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Estrogen receptor (ESR) TTZAYWL ESR1_HUMAN Agonist [6]
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Mestranol Interacts with 3 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [7]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Metabolism [8]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Metabolism [9]
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Mestranol Interacts with 49 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Serine/threonine-protein kinase Sgk1 (SGK1) OT301T1U SGK1_HUMAN Increases Expression [5]
Prostaglandin E synthase (PTGES) OTB7YQFU PTGES_HUMAN Increases Expression [5]
E3 ubiquitin-protein ligase SIAH2 (SIAH2) OTKED2XN SIAH2_HUMAN Increases Expression [5]
Carbonic anhydrase 12 (CA12) OT6WNFU8 CAH12_HUMAN Increases Expression [5]
Tyrosine-protein kinase JAK2 (JAK2) OTBIDOOR JAK2_HUMAN Increases Expression [5]
monooxygenase MICAL2 (MICAL2) OT04OQQJ MICA2_HUMAN Increases Expression [5]
Serine protease 23 (PRSS23) OT6DQAM1 PRS23_HUMAN Increases Expression [5]
Supervillin (SVIL) OTWQQ1WK SVIL_HUMAN Increases Expression [5]
Transcription factor AP-2-alpha (TFAP2A) OTMYT3NK AP2A_HUMAN Decreases Expression [5]
Progesterone receptor (PGR) OT0FZ3QE PRGR_HUMAN Increases Expression [5]
Proto-oncogene tyrosine-protein kinase receptor Ret (RET) OTLU040A RET_HUMAN Increases Expression [5]
Monoacylglycerol lipase ABHD2 (ABHD2) OTCRUOCS ABHD2_HUMAN Increases Expression [5]
Transcriptional activator Myb (MYB) OTJH64IV MYB_HUMAN Increases Expression [5]
Myb-related protein A (MYBL1) OTBJMC2P MYBA_HUMAN Increases Expression [5]
Tissue factor pathway inhibitor (TFPI) OTA0FX16 TFPI1_HUMAN Decreases Expression [5]
Delta-aminolevulinic acid dehydratase (ALAD) OTHM9GSH HEM2_HUMAN Decreases Expression [5]
Amphiregulin (AREG) OTJFOR67 AREG_HUMAN Increases Expression [5]
CD44 antigen (CD44) OT9TTJ41 CD44_HUMAN Increases Expression [5]
Ephrin-A1 (EFNA1) OTU2NUA2 EFNA1_HUMAN Decreases Expression [5]
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Increases Expression [5]
Stromal cell-derived factor 1 (CXCL12) OT2QX5LL SDF1_HUMAN Increases Expression [5]
Ephrin type-A receptor 4 (EPHA4) OT3AMK0C EPHA4_HUMAN Decreases Expression [5]
Single-stranded DNA-binding protein 2 (SSBP2) OTYG1G80 SSBP2_HUMAN Decreases Expression [5]
Large neutral amino acids transporter small subunit 1 (SLC7A5) OT2WPVXD LAT1_HUMAN Increases Expression [5]
DNA-binding protein inhibitor ID-3 (ID3) OTUULW5Z ID3_HUMAN Decreases Expression [5]
Urokinase plasminogen activator surface receptor (PLAUR) OTIRKKEQ UPAR_HUMAN Increases Expression [5]
Early growth response protein 3 (EGR3) OTGPJIRA EGR3_HUMAN Increases Expression [5]
Forkhead box protein C1 (FOXC1) OTOWZGYO FOXC1_HUMAN Increases Expression [5]
Four and a half LIM domains protein 2 (FHL2) OT0OAYWT FHL2_HUMAN Increases Expression [5]
Cyclin-G2 (CCNG2) OTII38K2 CCNG2_HUMAN Decreases Expression [5]
Kynureninase (KYNU) OTINL2RE KYNU_HUMAN Decreases Expression [5]
Na(+)/H(+) exchange regulatory cofactor NHE-RF3 (PDZK1) OTGFK4MH NHRF3_HUMAN Increases Expression [5]
Phosphatidylinositol 3-kinase regulatory subunit gamma (PIK3R3) OTXGJ8N1 P55G_HUMAN Decreases Expression [5]
Dual specificity tyrosine-phosphorylation-regulated kinase 2 (DYRK2) OTMDVWPS DYRK2_HUMAN Decreases Expression [5]
Transcription factor AP-2 gamma (TFAP2C) OTUDIW05 AP2C_HUMAN Increases Expression [5]
Serine/threonine-protein kinase Sgk3 (SGK3) OTQ6QO99 SGK3_HUMAN Increases Expression [5]
Inactive rhomboid protein 1 (RHBDF1) OTCQ7UDS RHDF1_HUMAN Decreases Expression [5]
Calmin (CLMN) OT7U5J3T CLMN_HUMAN Decreases Expression [5]
DNA endonuclease RBBP8 (RBBP8) OTRHJ3GI CTIP_HUMAN Increases Expression [5]
Noelin (OLFM1) OTOYPEWW NOE1_HUMAN Increases Expression [5]
Pleckstrin homology domain-containing family F member 2 (PLEKHF2) OTBGDG8C PKHF2_HUMAN Decreases Expression [5]
Spermine oxidase (SMOX) OT11E62Y SMOX_HUMAN Increases Expression [5]
Nicotinamide riboside kinase 1 (NMRK1) OT0STQLV NRK1_HUMAN Increases Expression [5]
Rap guanine nucleotide exchange factor-like 1 (RAPGEFL1) OTYKE9ZM RPGFL_HUMAN Increases Expression [5]
RNA 3'-terminal phosphate cyclase-like protein (RCL1) OT7O00YX RCL1_HUMAN Increases Expression [5]
Estrogen receptor (ESR1) OTKLU61J ESR1_HUMAN Increases Activity [10]
Coagulation factor VII (F7) OTGNJ97M FA7_HUMAN Increases Expression [11]
Protein GREB1 (GREB1) OTU6ZA26 GREB1_HUMAN Increases Expression [12]
Estrogen receptor beta (ESR2) OTXNR2WQ ESR2_HUMAN Affects Binding [13]
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⏷ Show the Full List of 49 DOT(s)
Indication(s) of Etonogestrel
Disease Entry ICD 11 Status REF
Contraception QA21 Approved [4]
Etonogestrel Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Progesterone receptor (PGR) TTUV8G9 PRGR_HUMAN Binder [14]
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Etonogestrel Interacts with 1 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [15]
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References

1 ClinicalTrials.gov (NCT01709318) A Dose-Finding Study to Evaluate Ovarian Function and Vaginal Bleeding in Next Generation Rings (P06109/MK-8175A/MK-8342B-012)
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: 7087).
3 Mestranol FDA Label
4 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: 7590).
5 Moving toward integrating gene expression profiling into high-throughput testing: a gene expression biomarker accurately predicts estrogen receptor alpha modulation in a microarray compendium. Toxicol Sci. 2016 May;151(1):88-103.
6 Short-term effects of environmentally relevant concentrations of EDC mixtures on Mytilus galloprovincialis digestive gland. Aquat Toxicol. 2008 May 30;87(4):272-9.
7 Prescribrt's digital referenve - Ethinyl estradiol/norethindrone; mestranol/norethindrone - Drug Summary
8 Loss of orally administered drugs in GI tract. Saudi Pharm J. 2012 Oct;20(4):331-44.
9 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
10 A binary screening assay for pro-oestrogens in food: metabolic activation using hepatic microsomes and detection with oestrogen sensitive recombinant yeast cells. Food Addit Contam. 2002 Dec;19(12):1138-47. doi: 10.1080/0265203021000014789.
11 Vascular complications of long-term oestrogen therapy. Front Horm Res. 1977;5:174-91. doi: 10.1159/000401993.
12 A Gene Expression Biomarker Identifies Chemical Modulators of Estrogen Receptor in an MCF-7 Microarray Compendium. Chem Res Toxicol. 2021 Feb 15;34(2):313-329. doi: 10.1021/acs.chemrestox.0c00243. Epub 2021 Jan 6.
13 Relationship between estrogen receptor-binding and estrogenic activities of environmental estrogens and suppression by flavonoids. Biosci Biotechnol Biochem. 2002 Jul;66(7):1479-87. doi: 10.1271/bbb.66.1479.
14 Pharmacological profile of progestins. Maturitas. 2008 Sep-Oct;61(1-2):151-7.
15 The role of CYP2C and CYP3A in the disposition of 3-keto-desogestrel after administration of desogestrel. Br J Clin Pharmacol. 2005 Jul;60(1):69-75.