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

General Information of Drug (ID: DMDMXKQ)

• Drug Name: GSK1292263 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Gastric adenocarcinoma	2B72	Phase 2	[1]
Type-2 diabetes	5A11	Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 24996872
  CAS Number: CAS 1032823-75-8
  TTD Drug ID: DMDMXKQ

Molecule-Related Drug Atlas

Drug(s) Targeting Glucose-dependent insulinotropic receptor (GPR119)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Guanfacine extended release	DMB1CZ8	Attention deficit hyperactivity disorder	6A05.Z	Approved	[3]
DS-8500	DMUXIRM	Diabetic complication	5A2Y	Phase 2	[4]
SAR-260093	DMBJU2G	Type-2 diabetes	5A11	Phase 2	[5]
BMS-903452	DM7JW0B	Type-2 diabetes	5A11	Phase 1	[6]
APD-597	DM36FOG	Type-2 diabetes	5A11	Phase 1	[7]
DA-1241	DMPJA64	Type 2 diabetes	5A11	Phase 1	[8]
APD668	DMN8R2U	Type-2 diabetes	5A11	Discontinued in Phase 1	[9]
PSN821	DMGEWUS	Type-2 diabetes	5A11	Terminated	[10]
N-oleoylethanolamide	DMJQ4L7	Discovery agent	N.A.	Investigative	[11]
lysophosphatidylinositol	DMETM3R	Discovery agent	N.A.	Investigative	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Glucose-dependent insulinotropic receptor (GPR119)	TT7QNVC	GP119_HUMAN	Modulator	[2]

References

• [1] ClinicalTrials.gov (NCT01218204) A Study to Investigate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Administering Multiple Oral Doses of GSK1292263 Alone and With Atorvastatin.U.S. National Institutes of Health.
• [2] Gut hormone pharmacology of a novel GPR119 agonist (GSK1292263), metformin, and sitagliptin in type 2 diabetes mellitus: results from two randomized studies.PLoS One.2014 Apr 3;9(4):e92494.
• [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: 126).
• [4] Addressing Unmet Medical Needs in Type 2 Diabetes: A Narrative Review of Drugs under Development. Curr Diabetes Rev. 2015 March; 11(1): 17-31.
• [5] GPR119 agonists for the treatment of type 2 diabetes. Expert Opin Ther Pat. 2009 Oct;19(10):1339-59.
• [6] Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119. J MedChem. 2014 Sep 25;57(18):7499-508.
• [7] Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1750-5.
• [8] ClinicalTrials.gov (NCT03646721) A Study to Evaluate the Safety, Tolerability, PK and PD of DA-1241 in Healthy Male Subjects and Subjects With T2DM. U.S. National Institutes of Health.
• [9] Announces Initiation of Phase 1 Clinical Trial of Arena Type 2 Diabetes Drug Candidate in Collaboration With Ortho-McNeil. Arena Pharmaceuticals, Inc. FEBRUARY 07, 2006.
• [10] Clinical pipeline report, company report or official report of Astellas Pharma (2011).
• [11] Screening beta-arrestin recruitment for the identification of natural ligands for orphan G-protein-coupled receptors. J Biomol Screen. 2013 Jun;18(5):599-609.
• [12] Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor. Biochem Biophys Res Commun. 2005 Jan 28;326(4):744-51.