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

General Information of Drug (ID: DM276Y8)

• Drug Name: ARV-471 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Phase 1/2	[1]

• Cross-matching ID:
  PubChem CID: 134562533
  TTD Drug ID: DM276Y8

Molecule-Related Drug Atlas

Drug(s) Targeting Androgen receptor (AR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[3]
Flutamide	DMK0O7U	Prostate cancer	2C82.0	Approved	[4]
Darolutamide	DMV7YFT	Prostate cancer	2C82.0	Approved	[5]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[6]
Flufenamic Acid	DMC8VNH	Dysmenorrhea	GA34.3	Approved	[7]
Bicalutamide	DMZMSPF	Prostate cancer	2C82.0	Approved	[8]
Fludrocortisone	DMUDIR8	Addison disease	5A74.0	Approved	[9]
ARN-509	DMT81LZ	Acute myeloid leukaemia	2A60	Approved	[10]
Nilutamide	DMFN07X	Prostate cancer	2C82.0	Approved	[11]
Nandrolone	DMFWKG1	Osteoporosis	FB83.0	Approved	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Androgen receptor (AR)	TTS64P2	ANDR_HUMAN	Degrader	[2]

References

• [1] ClinicalTrials.gov (NCT04072952) A Phase 1/2 Trial of ARV-471 Alone and in Combination With Palbociclib (IBRANCE) in Patients With ER+/HER2- Locally Advanced or Metastatic Breast Cancer (mBC). U.S. National Institutes of Health.
• [2] Targeting estrogen receptor alpha for degradation with PROTACs: A promising approach to overcome endocrine resistance. Eur J Med Chem. 2020 Nov 15;206:112689.
• [3] Dehydroepiandrosterone, glucose-6-phosphate dehydrogenase, and longevity. Ageing Res Rev. 2004 Apr;3(2):171-87.
• [4] Androgen receptor as a target in androgen-independent prostate cancer. Urology. 2002 Sep;60(3 Suppl 1):132-8; discussion 138-9.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [6] Molecular mechanism of androgen action. Trends Endocrinol Metab. 1998 Oct 1;9(8):317-24.
• [7] Ouellet M, Percival MD: Effect of inhibitor time-dependency on selectivity towards cyclooxygenase isoforms. Biochem J. 1995 Feb 15;306 ( Pt 1):247-51.
• [8] Androgen receptor overexpression induces tamoxifen resistance in human breast cancer cells. Breast Cancer Res Treat. 2010 May;121(1):1-11.
• [9] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [10] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [11] CX3CR1 is expressed by prostate epithelial cells and androgens regulate the levels of CX3CL1/fractalkine in the bone marrow: potential role in prostate cancer bone tropism. Cancer Res. 2008 Mar 15;68(6):1715-22.
• [12] Expression of androgen receptor on fibroblast and hepatocyte of rats after deep second-degree burn caused by scalding. Sichuan Da Xue Xue Bao Yi Xue Ban. 2005 May;36(3):362-4.