General Information of Drug (ID: DMDXRP1)

Drug Name
ETHISTERONE Drug Info
Synonyms
17-Hydroxypregn-4-en-20-yn-3-one; Syngestrotabs; Aethisteron; Progestolets; Pregneninolone; Progestoral; Gestoral; Ethinone; Colutoid; Trosinone; Prolutol; Progestab; Produxan; Nalutoral; Prodroxan; Prodoxan; Nugestoral; Pregnin; Prone; Lucorteum Oral; Lutidon Oral; Progestin P; Proluton C; Primolut C; Ora-Lutin; Ethinyltestosterone; Anhydroxyprogesterone; 17.alpha.-Ethynyltestosterone; Anhydrohydroxyprogesterone; Ethynyltestosterone; Testosterone, 17-ethynyl-; NSC-9565; 17-Ethinyltestosterone; 17.alpha.-Pregn-4-en-20-yn-3-one, 17-hydroxy-
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
5284557
ChEBI ID
CHEBI:34749
CAS Number
CAS 434-03-7
TTD Drug ID
DMDXRP1

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Drug(s) Targeting Tyrosinase (TYR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [3]
Monobenzone DMVJS2K Vitiligo ED63.0 Approved [3]
Multi-epitope peptide melanoma vaccine DMZPEHY Melanoma 2C30 Phase 3 [4]
Melanoma vaccine DMQEC6Z Melanoma 2C30 Phase 3 [5]
Polynoma-1 DM3QDA6 Melanoma 2C30 Phase 2 [6]
MKC-1106-MT DMXKOW6 Melanoma 2C30 Phase 2 [7]
Multi-epitope tyrosinase/gp100 vaccine DMN68ZL Melanoma 2C30 Phase 2 [8]
PMID29130358-Compound-Figure11(3) DMSME2B N. A. N. A. Patented [9]
Benzothiazole analog 1 DMHXFCQ Albinism EC23.2 Patented [10]
Monoamine derivative 2 DMAZ6DI Albinism EC23.2 Patented [10]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [11]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [12]
Spironolactone DM2AQ5N Chronic heart failure BD1Z Approved [2]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [13]
Quercetin DM3NC4M Obesity 5B81 Approved [14]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [15]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [16]
Estrone DM5T6US Acne vulgaris ED80 Approved [11]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [17]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [18]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Myb-related protein A (MYBL1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [11]
Spironolactone DM2AQ5N Chronic heart failure BD1Z Approved [2]
Quercetin DM3NC4M Obesity 5B81 Approved [14]
Panobinostat DM58WKG Chronic graft versus host disease Approved [19]
Estrone DM5T6US Acne vulgaris ED80 Approved [11]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [20]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [21]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [22]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [23]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [2]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Protein GREB1 (GREB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [24]
Spironolactone DM2AQ5N Chronic heart failure BD1Z Approved [2]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [25]
Testosterone DM7HUNW Hot flushes GA30 Approved [26]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [27]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [28]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [29]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [2]
Nandrolone DMFWKG1 Osteoporosis FB83.0 Approved [30]
Mestranol DMG3F94 Contraception QA21 Approved [2]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Tyrosinase (TYR) TTULVH8 TYRO_HUMAN Inhibitor [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Myb-related protein A (MYBL1) OTBJMC2P MYBA_HUMAN Gene/Protein Processing [2]
Protein GREB1 (GREB1) OTU6ZA26 GREB1_HUMAN Gene/Protein Processing [2]
Serine/threonine-protein kinase Sgk1 (SGK1) OT301T1U SGK1_HUMAN Gene/Protein Processing [2]

References

1 TOMOCOMD-CARDD descriptors-based virtual screening of tyrosinase inhibitors: evaluation of different classification model combinations using bond-b... Bioorg Med Chem. 2007 Feb 1;15(3):1483-503.
2 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.
3 Identification of an Alkylhydroquinone from Rhus succedanea as an Inhibitor of Tyrosinase and Melanogenesis. J Agric Food Chem. 2009 Mar 25;57(6):2200-5.
4 Safety and immunogenicity of vaccination with MART-1 (26-35, 27L), gp100 (209-217, 210M), and tyrosinase (368-376, 370D) in-adjuvant with PF-3512676 and GM-CSF in metastatic melanoma. Correction in: volume 35 on page 650.
5 National Cancer Institute Drug Dictionary (drug id 685201).
6 An immuno-oncology company developing a novel polyvalent antigen therapy for the treatment of melanoma. Polynoma. 2015.
7 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
8 ClinicalTrials.gov (NCT00003362) Vaccine Therapy Plus Immune Adjuvants in Treating Patients With Advanced Melanoma. U.S. National Institutes of Health.
9 Gelatinase inhibitors: a patent review (2011-2017).Expert Opin Ther Pat. 2018 Jan;28(1):31-46.
10 Tyrosinase inhibitors: a patent review (2011-2015).Expert Opin Ther Pat. 2016;26(3):347-62.
11 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.
12 A novel, integrated in vitro carcinogenicity test to identify genotoxic and non-genotoxic carcinogens using human lymphoblastoid cells. Arch Toxicol. 2018 Feb;92(2):935-951. doi: 10.1007/s00204-017-2102-y. Epub 2017 Nov 6.
13 Utilization of CDKN1A/p21 gene for class discrimination of DNA damage-induced clastogenicity. Toxicology. 2014 Jan 6;315:8-16. doi: 10.1016/j.tox.2013.10.009. Epub 2013 Nov 6.
14 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
15 Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
16 Transcriptome-based functional classifiers for direct immunotoxicity. Arch Toxicol. 2014 Mar;88(3):673-89.
17 Gene expression profile of multiple myeloma cell line treated by arsenic trioxide. J Huazhong Univ Sci Technolog Med Sci. 2007 Dec;27(6):646-9. doi: 10.1007/s11596-007-0606-z.
18 THC exposure of human iPSC neurons impacts genes associated with neuropsychiatric disorders. Transl Psychiatry. 2018 Apr 25;8(1):89. doi: 10.1038/s41398-018-0137-3.
19 Development and validation of the TGx-HDACi transcriptomic biomarker to detect histone deacetylase inhibitors in human TK6 cells. Arch Toxicol. 2021 May;95(5):1631-1645. doi: 10.1007/s00204-021-03014-2. Epub 2021 Mar 26.
20 Changes in gene expression profiles of multiple myeloma cells induced by arsenic trioxide (ATO): possible mechanisms to explain ATO resistance in vivo. Br J Haematol. 2005 Mar;128(5):636-44.
21 Single-cell Transcriptome Mapping Identifies Common and Cell-type Specific Genes Affected by Acute Delta9-tetrahydrocannabinol in Humans. Sci Rep. 2020 Feb 26;10(1):3450. doi: 10.1038/s41598-020-59827-1.
22 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
23 The neuroprotective action of the mood stabilizing drugs lithium chloride and sodium valproate is mediated through the up-regulation of the homeodomain protein Six1. Toxicol Appl Pharmacol. 2009 Feb 15;235(1):124-34.
24 Arsenite and cadmium promote the development of mammary tumors. Carcinogenesis. 2020 Jul 14;41(7):1005-1014. doi: 10.1093/carcin/bgz176.
25 Arsenic induces functional re-expression of estrogen receptor by demethylation of DNA in estrogen receptor-negative human breast cancer. PLoS One. 2012;7(4):e35957. doi: 10.1371/journal.pone.0035957. Epub 2012 Apr 27.
26 The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.
27 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
28 Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
29 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
30 Evaluation of an imaging-based in vitro screening platform for estrogenic activity with OECD reference chemicals. Toxicol In Vitro. 2022 Jun;81:105348. doi: 10.1016/j.tiv.2022.105348. Epub 2022 Mar 18.