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

General Information of Drug (ID: DMXI8CD)

Drug Name

TRC-253 Drug Info

Synonyms

OUEHJEYKNYQVRC-UHFFFAOYSA-N; TRC253; SCHEMBL19128768; EX-A1808; 2110426-27-0; 5-(8-oxo-5-(6-(piperidin-4-yloxy)pyridin-3-yl)-6-thioxo-5,7-diazaspiro[3.4]octan-7-yl)-3-(trifluoromethyl)picolinonitrile

Indication

Disease Entry	ICD 11	Status	REF
Prostate cancer	2C82.0	Phase 1/2	[1]

Cross-matching ID

PubChem CID: 130229812
TTD Drug ID: DMXI8CD

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Patented Agent(s)

Discontinued Drug(s)

Investigative Drug(s)

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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	[3]
BAY 86-5044	DMRZLU4	Breast cancer	2C60-2C65	Phase 2	[4]
IONIS-AR-2.5Rx	DMF2DMS	Prostate cancer	2C82.0	Phase 1/2	[5]
ISIS-AR	DM8P3N5	Prostate cancer	2C82.0	Phase 1	[6]
EZN-4176	DMNPS59	Prostate cancer	2C82.0	Phase 1	[7]
EUGENOL	DM7US1H	Discovery agent	N.A.	Patented	[8]
RU-58841	DMMEAZ2	Acne vulgaris	ED80	Discontinued in Phase 1	[9]
flavone	DMEQH6J	Discovery agent	N.A.	Investigative	[10]
APIGENIN	DMI3491	Discovery agent	N.A.	Investigative	[10]
KAEMPFEROL	DMHEMUB	Discovery agent	N.A.	Investigative	[10]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Androgen receptor messenger RNA (AR mRNA)	TTKPW01	ANDR_HUMAN	Antagonist	[2]

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References

1	ClinicalTrials.gov (NCT02987829) Phase 1/2A Study of TRC253, an Androgen Receptor Antagonist, in Metastatic Castration-resistant Prostate Cancer Patients. U.S. National Institutes of Health.
2	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3	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).
4	Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. J Med Chem. 2000 Dec 28;43(26):5010-6.
5	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.
6	Clinical pipeline report, company report or official report of ISIS Pharmaceuticals.
7	2011 Pipeline of Santaris Pharma.
8	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.
9	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.
10	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.