Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMVZW92)

• Drug Name: Epierenone Drug Info
• Synonyms: epierenone; CHEMBL237122; SCHEMBL13806060

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 44433505
  TTD Drug ID: DMVZW92

Molecule-Related Drug Atlas

Drug(s) Targeting Glucocorticoid receptor messenger RNA (GCR mRNA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Vamorolone	DM047HI	Duchenne muscular dystrophy	8C70.1	Approved	[2]
CORT125281	DMHBOUX	Prostate cancer	2C82.0	Phase 2	[3]
ISIS-GCCR	DMICMNU	Diabetic complication	5A2Y	Phase 2	[4]
ORIC-101	DMR12S0	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
AZD9567	DMAXHC0	Rheumatoid arthritis	FA20	Phase 1	[2]
A-348441	DM25CBW	Type-2 diabetes	5A11	Phase 1	[5]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[6]
(11-BETA)-11,21-DIHYDROXY-PREGN-4-ENE-3,20-DIONE	DMTPQ84	Discovery agent	N.A.	Investigative	[7]
deoxycorticosterone	DMW6YLS	Discovery agent	N.A.	Investigative	[7]
LGD-5552	DM67KWM	Discovery agent	N.A.	Investigative	[8]

Drug(s) Targeting Androgen receptor messenger RNA (AR mRNA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dihydrotestosterone	DM3S8XC	Prostate hyperplasia	GA90	Phase 4	[9]
BAY 86-5044	DMRZLU4	Breast cancer	2C60-2C65	Phase 2	[10]
TRC-253	DMXI8CD	Prostate cancer	2C82.0	Phase 1/2	[3]
IONIS-AR-2.5Rx	DMF2DMS	Prostate cancer	2C82.0	Phase 1/2	[11]
ISIS-AR	DM8P3N5	Prostate cancer	2C82.0	Phase 1	[12]
EZN-4176	DMNPS59	Prostate cancer	2C82.0	Phase 1	[13]
EUGENOL	DM7US1H	Discovery agent	N.A.	Patented	[14]
RU-58841	DMMEAZ2	Acne vulgaris	ED80	Discontinued in Phase 1	[15]
flavone	DMEQH6J	Discovery agent	N.A.	Investigative	[16]
APIGENIN	DMI3491	Discovery agent	N.A.	Investigative	[16]

Drug(s) Targeting Mineralocorticoid receptor (MR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aldosterone	DM9S2JW	Hypertension	BA00-BA04	Approved	[17]
Eplerenone	DMF0NQR	Heart failure	BD10-BD13	Approved	[18]
Fludrocortisone	DMUDIR8	Addison disease	5A74.0	Approved	[19]
Desoxycorticosterone Acetate	DMS0AFE	Discovery agent	N.A.	Approved	[18]
Desoxycorticosterone Pivalate	DMSA4B3	Addison disease	5A74.0	Approved	[20]
Drospirenone	DM1A9W3	Acne vulgaris	ED80	Approved	[21]
Spironolactone	DM2AQ5N	Chronic heart failure	BD1Z	Approved	[18]
Finerenone	DMM4FJ3	Chronic kidney disease	GB61	Approved	[22]
ZK-91587	DMJ94L0	Cardiovascular disease	BA00-BE2Z	Phase 2	[23]
Nerenone	DMBJ3GL	Diabetic nephropathy	GB61.Z	Phase 2	[24]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Androgen receptor messenger RNA (AR mRNA)	TTKPW01	ANDR_HUMAN	Inhibitor	[1]
Glucocorticoid receptor messenger RNA (GCR mRNA)	TTOZRK6	GCR_HUMAN	Inhibitor	[1]
Mineralocorticoid receptor (MR)	TT26PHO	MCR_HUMAN	Inhibitor	[1]

References

• [1] (S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mine... J Med Chem. 2007 Dec 27;50(26):6443-5.
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [4] Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2011).
• [5] Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists. Bioorg Med Chem Lett. 2006 Dec 1;16(23):6086-90.
• [6] Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
• [7] Functional probing of the human glucocorticoid receptor steroid-interacting surface by site-directed mutagenesis. Gln-642 plays an important role in steroid recognition and binding. J Biol Chem. 2000Jun 23;275(25):19041-9.
• [8] Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19244-9.
• [9] 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. (Target id: 628).
• [10] Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. J Med Chem. 2000 Dec 28;43(26):5010-6.
• [11] Perspectives on the current and emerging chemical androgen receptor antagonists for the treatment of prostate cancer. Expert Opin Pharmacother. 2019 Feb;20(2):163-172.
• [12] Clinical pipeline report, company report or official report of ISIS Pharmaceuticals.
• [13] 2011 Pipeline of Santaris Pharma.
• [14] Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2111-4.
• [15] Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen recepto... J Med Chem. 2008 Nov 13;51(21):7010-4.
• [16] Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4706-10.
• [17] Stimulation of testosterone production in rat Leydig cells by aldosterone is mineralocorticoid receptor mediated. Mol Cell Endocrinol. 2005 Nov 24;243(1-2):35-42.
• [18] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [19] Mineralocorticoid receptor-mediated inhibition of the hypothalamic-pituitary-adrenal axis in aged humans. J Gerontol A Biol Sci Med Sci. 2003 Oct;58(10):B900-5.
• [20] Characterization of rat brain aldosterone receptors reveals high affinity for corticosterone. Endocrinology. 1983 Dec;113(6):2043-51.
• [21] Biochemical mechanisms of New Molecular Entities (NMEs) approved by United States FDA during 2001-2004: mechanisms leading to optimal efficacy and ... Curr Top Med Chem. 2006;6(5):461-78.
• [22] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [23] ZK91587: a novel synthetic antimineralocorticoid displays high affinity for corticosterone (type I) receptors in the rat hippocampus. Life Sci. 1988;43(19):1537-43.
• [24] 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. (Target id: 626).