Firuglipel

Firuglipel
Clinical data
Other namesDS-8500; DS8500; DS-8500a; DS8500a
Routes of
administration		Oral
Drug classGPR119 agonist; Antihyperglycemic agent
ATC code
  • None
Identifiers
  • 4-[5-[(1R)-1-[4-(cyclopropanecarbonyl)phenoxy]propyl]-1,2,4-oxadiazol-3-yl]-2-fluoro-N-[(2R)-1-hydroxypropan-2-yl]benzamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC25H26FN3O5
Molar mass467.497 g·mol−1
3D model (JSmol)
  • CC[C@H](C1=NC(=NO1)C2=CC(=C(C=C2)C(=O)N[C@H](C)CO)F)OC3=CC=C(C=C3)C(=O)C4CC4
  • InChI=1S/C25H26FN3O5/c1-3-21(33-18-9-6-16(7-10-18)22(31)15-4-5-15)25-28-23(29-34-25)17-8-11-19(20(26)12-17)24(32)27-14(2)13-30/h6-12,14-15,21,30H,3-5,13H2,1-2H3,(H,27,32)/t14-,21-/m1/s1
  • Key:LRXRIKVDAVVQCP-SPLOXXLWSA-N

Firuglipel (INNTooltip International Nonproprietary Name; developmental code name DS-8500 or DS-8500a) is a GPR119 agonist with antihyperglycemic actions which was under development for the treatment of type 2 diabetes but was never marketed. It is taken orally. Through activation of the GPR119, the drug has been found to increase glucagon-like peptide 1 (GLP-1) secretion and glucose-stimulated insulin secretion and to lower glucose levels in the glucose tolerance test without altering fasting glucose levels in rodents. Firuglipel was under development by Daiichi Sankyo Company. It reached phase 2 clinical trials prior to the discontinuation of its development in 2021.

See also

References

  1. 1 2 3 4 5 "Firuglipel - Daiichi Sankyo Company". adisinsight.springer.com. Retrieved 28 October 2026.
  2. 1 2 3 Kato M, Furuie H, Kamiyama E, Shiosakai K, Yoshihara K, Taguchi T (June 2018). "Safety and Pharmacokinetics of DS-8500a, a Novel GPR119 Agonist, After Multiple Oral Doses in Healthy Japanese Males". Clinical Drug Investigation. 38 (6): 519–525. doi:10.1007/s40261-018-0633-5. PMID 29582248.
  3. ↑ Yamada Y, Terauchi Y, Watada H, Nakatsuka Y, Shiosakai K, Washio T, et al. (March 2018). "Efficacy and Safety of GPR119 Agonist DS-8500a in Japanese Patients with Type 2 Diabetes: a Randomized, Double-Blind, Placebo-Controlled, 12-Week Study". Advances in Therapy. 35 (3): 367–381. doi:10.1007/s12325-018-0668-2. PMC 5859088. PMID 29488152.
  4. 1 2 Terauchi Y, Yamada Y, Watada H, Nakatsuka Y, Shiosakai K, Washio T, et al. (November 2018). "Efficacy and safety of the G protein-coupled receptor 119 agonist DS-8500a in Japanese type 2 diabetes mellitus patients with inadequate glycemic control on sitagliptin: A phase 2 randomized placebo-controlled study". Journal of Diabetes Investigation. 9 (6): 1333–1341. doi:10.1111/jdi.12846. PMC 6215943. PMID 29607623.
  5. 1 2 3 Matsumoto K, Yoshitomi T, Shimada T (2018). "フィルグリペル（GPR119作動薬）創製における薬理学研究の役割" [The role of pharmacology to produce firuglipel (DS-8500a), an orally available GPR119 agonist for type 2 diabetes mellitus]. Nihon Yakurigaku Zasshi. 152 (3): 119–124. doi:10.1254/fpj.152.119. PMID 30185729.
  6. ↑ Matsumoto K, Yoshitomi T, Ishimoto Y, Tanaka N, Takahashi K, Watanabe A, et al. (December 2018). "DS-8500a, an Orally Available G Protein-Coupled Receptor 119 Agonist, Upregulates Glucagon-Like Peptide-1 and Enhances Glucose-Dependent Insulin Secretion and Improves Glucose Homeostasis in Type 2 Diabetic Rats". The Journal of Pharmacology and Experimental Therapeutics. 367 (3): 509–517. doi:10.1124/jpet.118.250019. PMID 30217957.
  7. ↑ Hryciw DH, Patten RK, Rodgers RJ, Proietto J, Hutchinson DS, McAinch AJ (March 2024). "GPR119 agonists for type 2 diabetes: past failures and future hopes for preclinical and early phase candidates". Expert Opinion on Investigational Drugs. 33 (3): 183–190. doi:10.1080/13543784.2024.2321271. PMID 38372052.