Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTOD7B3)

• DTT Name: Retinoic acid receptor (RAR)
• Synonyms: Retinoic acid receptor
• Gene Name: RAR
• DTT Type: Successful target; [1]
• UniProt ID: NOUNIPROTAC
• TTD ID: T11822

Molecular Interaction Atlas (MIA) of This DTT

4 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Adapalene	DMX2358	Acne vulgaris	ED80	Approved	[2]
Isotretinoin	DM4QTBN	Acne vulgaris	ED80	Approved	[1]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[3]
Vitamin A	DMJ2AH4	Night blindness	9D45	Approved	[4]

5 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
13-cis-retinoic acid	DMTZ1A5	Glioma	2A00.0	Phase 3	[5]
Fenretinide	DMRD5SP	Macular degeneration	9B78.3	Phase 3	[6]
Peretinoin	DMESAZK	Hepatocellular carcinoma	2C12.02	Phase 3	[7]
Velac Gel	DMXHI89	Acne vulgaris	ED80	Phase 3	[8]
Amsilarotene	DMOB01U	Solid tumour/cancer	2A00-2F9Z	Phase 2	[9]

5 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LAS-41001	DMXZ4BK	Rosacea	ED90.0	Discontinued in Preregistration	[10]
IRX-4310	DMUYQH8	Psoriasis vulgaris	EA90	Discontinued in Phase 3	[11]
BMY-30123	DMMJDYI	Acne vulgaris	ED80	Discontinued in Phase 2	[12]
LG-1550	DM8W31H	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 2	[13]
MX-781	DMNZ356	Breast cancer	2C60-2C65	Terminated	[14]

References

• [1] Retinoid agonist isotretinoin ameliorates obstructive renal injury. J Urol. 2003 Oct;170(4 Pt 1):1398-402.
• [2] A review of adapalene in the treatment of acne vulgaris. J Adolesc Health. 2008 Nov;43(5):421-4.
• [3] Retinoids--which dermatological indications will benefit in the near future Skin Pharmacol Appl Skin Physiol. 2001 Sep-Oct;14(5):303-15.
• [4] Vitamins and cofactors: highlights of ESBOC 2009. Nat Chem Biol. 2009 Aug;5(8):530-3.
• [5] 13-cis retinoic acid exerts its specific activity on human sebocytes through selective intracellular isomerization to all-trans retinoic acid and binding to retinoid acid receptors. J Invest Dermatol. 2000 Aug;115(2):321-7.
• [6] National Cancer Institute Drug Dictionary (drug id 39582).
• [7] Peretinoin, an acyclic retinoid, improves the hepatic gene signature of chronic hepatitis C following curative therapy of hepatocellular carcinoma. BMC Cancer. 2013 Apr 15;13:191.
• [8] Chromosomal translocation t(15;17) in human acute promyelocytic leukemia fuses RAR alpha with a novel putative transcription factor, PML. Cell. 1991 Aug 23;66(4):663-74.
• [9] Initial clinical trial of oral TAC-101, a novel retinoic acid receptor-alpha selective retinoid, in patients with advanced cancer. J Clin Oncol. 2002 Aug 15;20(16):3522-32.
• [10] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027956)
• [11] An antagonist of retinoic acid receptors more effectively inhibits growth of human prostate cancer cells than normal prostate epithelium. Br J Cancer. 2004 Aug 2;91(3):580-8.
• [12] The pharmacology of a novel topical retinoid, BMY 30123: comparison with tretinoin. J Pharm Pharmacol. 1992 May;44(5):379-86.
• [13] US patent application no. 2005,0014,729, Method for the treatment or prevention of dermatological disorders with a cyclooxygenase-2 inhibitor alone and in combination with a dermatological treatment agent and compositions therewith.
• [14] The retinoid antagonist MX781 induces clusterin expression in prostate cancer cells via heat shock factor-1 and activator protein-1 transcription factors. Cancer Res. 2004 Aug 15;64(16):5905-12.