General Information of Drug (ID: DMN8R2U)

Drug Name
APD668 Drug Info
Synonyms
832714-46-2; APD-668; CHEMBL1775179; Isopropyl 4-((1-(2-fluoro-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)oxy)piperidine-1-carboxylate; isopropyl 4-(1-(2-fluoro-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate; 1-Piperidinecarboxylic acid,4-[[1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]-, 1-methylethyl ester; SCHEMBL389323; AOB6271; XTRUQJBVQBUKSQ-UHFFFAOYSA-N; MolPort-039-331-631; EX-A1795; BCP10207; BDBM50343442; ZINC68266967
Indication
Disease Entry ICD 11 Status REF
Type-2 diabetes 5A11 Discontinued in Phase 1 [1]
Cross-matching ID
PubChem CID
11705608
TTD Drug ID
DMN8R2U

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
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]
GSK1292263 DMDMXKQ Gastric adenocarcinoma 2B72 Phase 2 [6]
BMS-903452 DM7JW0B Type-2 diabetes 5A11 Phase 1 [7]
APD-597 DM36FOG Type-2 diabetes 5A11 Phase 1 [8]
DA-1241 DMPJA64 Type 2 diabetes 5A11 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]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Glucose-dependent insulinotropic receptor (GPR119) TT7QNVC GP119_HUMAN Agonist [2]

References

1 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023882)
2 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.
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 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.
7 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.
8 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.
9 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.
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.