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

General Information of Drug (ID: DM9LNXS)

• Drug Name: ARI-3037MO Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Cardiovascular disease	BA00-BE2Z	Phase 2	[1]
Dyslipidemia	5C80-5C81	Phase 2	[2]
Hypertriglyceridemia	5C80.1	Phase 2	[1]

• Cross-matching ID: TTD Drug ID: DM9LNXS

Molecule-Related Drug Atlas

Drug(s) Targeting Hydroxycarboxylic acid receptor 3 (HCAR3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
NIA-114	DM3ADQW	Plaque psoriasis	EA90.0	Clinical trial	[4]
3-hydroxyoctanoic acid	DMS658R	Discovery agent	N.A.	Investigative	[5]
PMID17358052C5b	DMR9TYV	Discovery agent	N.A.	Investigative	[6]
D-tryptophan	DMKIML1	Discovery agent	N.A.	Investigative	[7]
D-kynurenine	DM0QZ6I	Discovery agent	N.A.	Investigative	[7]
5-methyl-5-(5-methylthiophen-3-yl)-4-oxo-4,5-dihydrofuran-2-carboxylic acid	DMO37W4	Discovery agent	N.A.	Investigative	[6]
4-(n-propyl)amino-3-nitrobenzoic acid	DMP43HI	Discovery agent	N.A.	Investigative	[8]
2-hydroxyoctanoic acid	DMMILJS	Discovery agent	N.A.	Investigative	[5]
PMID19524438C6o	DMK5JB8	Discovery agent	N.A.	Investigative	[9]
IBC 293	DM8J24A	Discovery agent	N.A.	Investigative	[10]

Drug(s) Targeting Nicotinic acid receptor (HCAR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Vitamin B3	DMQVRZH	Chronic renal failure	GB61.Z	Approved	[11]
SCH-900271	DMBJY1Z	Ischemic stroke	8B11.5Z	Phase 2	[12]
GSK-256073	DMMAIY2	Hyperlipidaemia	5C80	Phase 2	[13]
MK-1903	DMVJB09	Arteriosclerosis	BD40	Phase 2	[14]
MK-0354	DMWFTRJ	N. A.	N. A.	Phase 2	[15]
NIA-114	DM3ADQW	Plaque psoriasis	EA90.0	Clinical trial	[4]
INCB19602	DMRHZBD	Type-2 diabetes	5A11	Discontinued in Phase 2	[16]
cinnamic acid	DM340FH	Discovery agent	N.A.	Investigative	[17]
5-Benzyl-1H-pyrazole-3-carboxylic acid	DMJVGUZ	Discovery agent	N.A.	Investigative	[18]
Sazetidine-A	DM68JI5	Major depressive disorder	6A70.3	Investigative	[12]

Drug(s) Targeting Diacylglycerol O-acyltransferase 2 (DGAT2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Vitamin B3	DMQVRZH	Chronic renal failure	GB61.Z	Approved	[11]
PF-06865571	DMZE3GK	Non-alcoholic steatohepatitis	DB92.1	Phase 2	[19]
PF-06427878	DMGB32Z	Cardiovascular disease	BA00-BE2Z	Phase 1	[1]
PMID25470667-Compound-Figure4-1A	DMMVQW8	N. A.	N. A.	Patented	[20]
PMID25470667-Compound-roselipins	DMCF2G7	N. A.	N. A.	Patented	[20]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Diacylglycerol O-acyltransferase 2 (DGAT2)	TTRHEQ4	DGAT2_HUMAN	Inhibitor	[3]
Hydroxycarboxylic acid receptor 3 (HCAR3)	TT8WFXV	HCAR3_HUMAN	Agonist	[1]
Nicotinic acid receptor (HCAR2)	TTWNV8U	HCAR2_HUMAN	Agonist	[1]

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] ClinicalTrials.gov (NCT02250105) Trial of ARI-3037MO to Reduce Triglyceride Levels in Adults With Severe ( 00 mg/dl) Hypertriglyceridemia. U.S. National Institutes of Health.
• [3] 2011 Pipeline of Arisaph Pharmaceuticals.
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] Deorphanization of GPR109B as a receptor for the beta-oxidation intermediate 3-OH-octanoic acid and its role in the regulation of lipolysis. J Biol Chem. 2009 Aug 14;284(33):21928-33.
• [6] Analogues of acifran: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b. J Med Chem. 2007 Apr 5;50(7):1445-8.
• [7] Aromatic D-amino acids act as chemoattractant factors for human leukocytes through a G protein-coupled receptor, GPR109B. Proc Natl Acad Sci U S A. 2009 Mar 10;106(10):3930-4.
• [8] 3-Nitro-4-amino benzoic acids and 6-amino nicotinic acids are highly selective agonists of GPR109b. Bioorg Med Chem Lett. 2007 Dec 1;17(23):6619-22.
• [9] 5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4207-9.
• [10] 1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b. J Med Chem. 2006 Feb 23;49(4):1227-30.
• [11] Hakozaki T, Minwalla L, Zhuang J, Chhoa M, Matsubara A, Miyamoto K, Greatens A, Hillebrand GG, Bissett DL, Boissy RE: The effect of niacinamide on reducing cutaneous pigmentation and suppression of melanosome transfer. Br J Dermatol. 2002 Jul;147(1):20-31.
• [12] Discovery of SCH 900271, a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia. ACS Med Chem Lett. 2011 Nov 24;3(1):63-8.
• [13] GSK256073, a selective agonist of G-protein coupled receptor 109A (GPR109A) reduces serum glucose in subjects with type 2 diabetes mellitus. Diabetes Obes Metab. 2013 Nov;15(11):1013-21.
• [14] Niacin lipid efficacy is independent of both the niacin receptor GPR109A and free fatty acid suppression. Sci Transl Med. 2012 Aug 22;4(148):148ra115.
• [15] GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4472-4.
• [16] DOI: 10.1038/scibx.2010.313
• [17] Phenolic acids suppress adipocyte lipolysis via activation of the nicotinic acid receptor GPR109A (HM74a/PUMA-G). J Lipid Res. 2009 May;50(5):908-14.
• [18] Pyrazole derivatives as partial agonists for the nicotinic acid receptor. J Med Chem. 2003 Aug 28;46(18):3945-51.
• [19] Discovery of Ervogastat (PF-06865571): A Potent and Selective Inhibitor of Diacylglycerol Acyltransferase 2 for the Treatment of Non-alcoholic Steatohepatitis. J Med Chem. 2022 Nov 24;65(22):15000-15013.
• [20] Acyltransferase inhibitors: a patent review (2010-present).Expert Opin Ther Pat. 2015 Feb;25(2):145-58.