General Information of DTT (ID: TT7QNVC)

DTT Name Glucose-dependent insulinotropic receptor (GPR119) DTT Info
Gene Name GPR119

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Discontinued Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
1 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Guanfacine extended release DMB1CZ8 Attention deficit hyperactivity disorder 6A05.Z Approved [1]
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6 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
DS-8500 DMUXIRM Diabetic complication 5A2Y Phase 2 [2]
GSK1292263 DMDMXKQ Gastric adenocarcinoma 2B72 Phase 2 [3]
SAR-260093 DMBJU2G Type-2 diabetes 5A11 Phase 2 [4]
APD-597 DM36FOG Type-2 diabetes 5A11 Phase 1 [5]
BMS-903452 DM7JW0B Type-2 diabetes 5A11 Phase 1 [6]
DA-1241 DMPJA64 Type 2 diabetes 5A11 Phase 1 [7]
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⏷ Show the Full List of 6 Clinical Trial Drug(s)
2 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
APD668 DMN8R2U Type-2 diabetes 5A11 Discontinued in Phase 1 [8]
PSN821 DMGEWUS Type-2 diabetes 5A11 Terminated [9]
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33 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(R)-N-oleoyltyrosinol DMIHR14 Discovery agent N.A. Investigative [10]
(S)-N-oleoyltyrosinol DMNOWZ2 Discovery agent N.A. Investigative [10]
1-oleoyl glycerol DM5KU8S Discovery agent N.A. Investigative [11]
1-palmitoyl-lysophosphatidylcholine DM9ZK0M Discovery agent N.A. Investigative [12]
1-stearoyl-lysophosphatidylcholine DM7K0B3 Discovery agent N.A. Investigative [12]
2-oleoyl glycerol DM5PXQU Discovery agent N.A. Investigative [11]
AR-7947 DM34P90 Non-insulin dependent diabetes 5A11 Investigative [1]
AR231453 DMN8W46 Discovery agent N.A. Investigative [13]
AS-1907417 DM0MAIW Non-insulin dependent diabetes 5A11 Investigative [1]
AS1269574 DM170G5 Discovery agent N.A. Investigative [14]
LC34AD3 DMGWSCI Non-insulin dependent diabetes 5A11 Investigative [1]
lysophosphatidylethanolamine DMI4FKH Discovery agent N.A. Investigative [12]
lysophosphatidylinositol DMETM3R Discovery agent N.A. Investigative [12]
MBX-3254 DM89WA1 Non-insulin dependent diabetes 5A11 Investigative [1]
N-oleoylethanolamide DMJQ4L7 Discovery agent N.A. Investigative [15]
oleoyl-lysophosphatidylcholine DMB5KQ4 Discovery agent N.A. Investigative [12]
PMID21273063C1 DMEFUZW Discovery agent N.A. Investigative [16]
PMID21273063C36 DMFYJ6O Discovery agent N.A. Investigative [16]
PMID21273063C58 DMDCUYB Discovery agent N.A. Investigative [16]
PMID21310611C3 DMTOM3E Discovery agent N.A. Investigative [17]
PMID21444206C23 DM9YVPU Discovery agent N.A. Investigative [18]
PMID21444206C3a DMN50B9 Discovery agent N.A. Investigative [18]
PMID21444206C3j DMM1YBE Discovery agent N.A. Investigative [18]
PMID21444206C8g DMR21YD Discovery agent N.A. Investigative [18]
PMID21536438C20f DMHWX2O Discovery agent N.A. Investigative [19]
PMID21536438C36j DM06V1Q Discovery agent N.A. Investigative [19]
PMID21939274C1 DMEUQFG Discovery agent N.A. Investigative [20]
PMID21939274C2 DMRCAEI Discovery agent N.A. Investigative [20]
PMID22545772C42 DMVZQ6U Discovery agent N.A. Investigative [21]
PSN375963 DM2U9SR Discovery agent N.A. Investigative [22]
PSN632408 DMJIB8N Discovery agent N.A. Investigative [22]
RO-5212651 DMP0GA6 Non-insulin dependent diabetes 5A11 Investigative [1]
SEA DMSB4WO Discovery agent N.A. Investigative [1]
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⏷ Show the Full List of 33 Investigative Drug(s)
Molecule Interaction Atlas

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. (Target id: 126).
2 Addressing Unmet Medical Needs in Type 2 Diabetes: A Narrative Review of Drugs under Development. Curr Diabetes Rev. 2015 March; 11(1): 17-31.
3 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.
4 GPR119 agonists for the treatment of type 2 diabetes. Expert Opin Ther Pat. 2009 Oct;19(10):1339-59.
5 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.
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 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.
8 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.
9 Clinical pipeline report, company report or official report of Astellas Pharma (2011).
10 N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119. Mol Endocrinol. 2010 Jan;24(1):161-70.
11 2-Oleoyl glycerol is a GPR119 agonist and signals GLP-1 release in humans. J Clin Endocrinol Metab. 2011 Sep;96(9):E1409-17.
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.
13 A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release. Endocrinology. 2007 Jun;148(6):2601-9.
14 Identification of a novel GPR119 agonist, AS1269574, with in vitro and in vivo glucose-stimulated insulin secretion. Biochem Biophys Res Commun. 2010 Sep 24;400(3):437-41.
15 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.
16 Design of potent and selective GPR119 agonists for type II diabetes. Bioorg Med Chem Lett. 2011 May 1;21(9):2665-9.
17 Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1306-9.
18 Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control. Bioorg Med Chem Lett. 2011 May 15;21(10):3134-41.
19 Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3290-6.
20 Oxidative metabolism of a quinoxaline derivative by xanthine oxidase in rodent plasma. Chem Res Toxicol. 2011 Dec 19;24(12):2207-16.
21 Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation. J Med Chem. 2012 Jun 14;55(11):5361-79.
22 Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. Cell Metab. 2006 Mar;3(3):167-75.