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

General Information of Drug (ID: DMC0YOE)

• Drug Name: AGN193109 Drug Info
• Synonyms: AGN 193109; AGN-93109

Indication

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

• Cross-matching ID:
  PubChem CID: 177238
  CAS Number: CAS 171746-21-7
  TTD Drug ID: DMC0YOE

Molecule-Related Drug Atlas

Drug(s) Targeting Retinoic acid receptor beta (RARB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Alitretinoin	DMME8LH	Kaposi sarcoma	2B57	Approved	[3]
Tamibarotene	DM3G74J	T-cell leukaemia	2A90	Phase 3	[4]
PMID27336223-Compound-10	DMYUP6G	N. A.	N. A.	Patented	[5]
PMID27336223-Compound-8	DM460D1	N. A.	N. A.	Patented	[5]
PMID27336223-Compound-7	DM9QM6I	N. A.	N. A.	Patented	[5]
CD666	DMC8X9Y	Discovery agent	N.A.	Investigative	[6]
AC55649	DM4JNY9	Discovery agent	N.A.	Investigative	[7]
BMS641	DMRT7G3	Discovery agent	N.A.	Investigative	[8]
AC261066	DMSKE1I	Discovery agent	N.A.	Investigative	[7]
TTNPB	DMSABD0	Discovery agent	N.A.	Investigative	[9]

Drug(s) Targeting Retinoic acid receptor gamma (RARG)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[10]
Alitretinoin	DMME8LH	Kaposi sarcoma	2B57	Approved	[3]
Trifarotene	DMOL793	Acne vulgaris	ED80	Approved	[11]
Tazarotene	DM8SMD1	Acne vulgaris	ED80	Approved	[12]
Palovarotene	DMAD2OZ	Fibrodysplasia ossificans progressiva	FB31.1	Approved	[13]
PMID27336223-Compound-13	DMSZLYD	N. A.	N. A.	Patented	[5]
PMID27336223-Compound-12	DMT4P7K	N. A.	N. A.	Patented	[5]
PMID27336223-Compound-14	DMC41MA	N. A.	N. A.	Patented	[5]
PMID27336223-Compound-11	DMBN6KU	N. A.	N. A.	Patented	[5]
PMID27336223-Compound-15	DMIYCFE	N. A.	N. A.	Patented	[5]

Drug(s) Targeting Retinoic acid receptor alpha (RARA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tamibarotene	DM3G74J	T-cell leukaemia	2A90	Phase 3	[4]
IRX-5183	DMCED9U	Solid tumour/cancer	2A00-2F9Z	Phase 1	[14]
SY-1425	DMH8UF0	Acute myeloid leukaemia	2A60	Phase 1	[15]
PMID27336223-Compound-4	DMJFSOM	N. A.	N. A.	Patented	[5]
PMID27336223-Compound-5	DM6E50A	N. A.	N. A.	Patented	[5]
LG100268	DM41RK2	Acquired immune deficiency syndrome	1C62.3	Discontinued in Phase 1	[16]
CD666	DMC8X9Y	Discovery agent	N.A.	Investigative	[6]
AGN193836	DMEB93D	Discovery agent	N.A.	Investigative	[17]
BMS614	DMZWNO9	Discovery agent	N.A.	Investigative	[18]
Ro-40-0655	DM8PYAN	Colorectal cancer	2B91.Z	Investigative	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Retinoic acid receptor alpha (RARA)	TTW38KT	RARA_HUMAN	Antagonist	[2]
Retinoic acid receptor beta (RARB)	TTISP28	RARB_HUMAN	Antagonist	[2]
Retinoic acid receptor gamma (RARG)	TT1Q3IE	RARG_HUMAN	Antagonist	[2]

References

• [1] 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. (Ligand id: 2640).
• [2] Therapeutic applications for ligands of retinoid receptors. Curr Pharm Des. 2000 Jan;6(1):25-58.
• [3] Retinoic acid receptors and retinoid X receptors: interactions with endogenous retinoic acids. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):30-4.
• [4] Tamibarotene: a candidate retinoid drug for Alzheimer's disease. Biol Pharm Bull. 2012;35(8):1206-12.
• [5] Therapeutic use of selective synthetic ligands for retinoic acid receptors: a patent review.Expert Opin Ther Pat. 2016 Aug;26(8):957-71.
• [6] Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor gamma. Biochem Biophys Res Commun. 1992 Jul 31;186(2):977-83.
• [7] Discovery of a potent, orally available, and isoform-selective retinoic acid beta2 receptor agonist. J Med Chem. 2005 Dec 1;48(24):7517-9.
• [8] Rational design of RAR-selective ligands revealed by RARbeta crystal stucture. EMBO Rep. 2004 Sep;5(9):877-82.
• [9] 9-cis-retinoic acid analogues with bulky hydrophobic rings: new RXR-selective agonists. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6117-22.
• [10] Targacept active conformation search: a new method for predicting the conformation of a ligand bound to its protein target. J Med Chem. 2004 Dec 30;47(27):6831-9.
• [11] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [12] Recent developments in receptor-selective retinoids. Curr Pharm Des. 2000 Jun;6(9):919-31.
• [13] Randomised controlled trial for emphysema with a selective agonist of the gamma-type retinoic acid receptor. Eur Respir J. 2012 Aug;40(2):306-12.
• [14] Retinoic acid receptor alpha and retinoid X receptor specific agonists reduce renal injury in established chronic glomerulonephritis of the rat. J Mol Med (Berl). 2004 Feb;82(2):116-25.
• [15] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [16] Placental steroidogenesis in rats is independent of signaling pathways induced by retinoic acids. Gen Comp Endocrinol. 2009 Sep 15;163(3):285-91.
• [17] Synthesis and biological activity of retinoic acid receptor-alpha specific amides. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3145-8.
• [18] Co-regulator recruitment and the mechanism of retinoic acid receptor synergy. Nature. 2002 Jan 10;415(6868):187-92.
• [19] Tamibarotene. Drugs Today (Barc). 2007 Aug;43(8):563-8.