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Firuglipel

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Firuglipel
Clinical data
Other namesDS-8500; DS8500; DS-8500a; DS8500a
Routes of
administration		Oral[1][2]
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.[1][3][2][4][5] It is taken orally.[1][2][5] 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.[6] Firuglipel was under development by Daiichi Sankyo Company.[1][5] It reached phase 2 clinical trials prior to the discontinuation of its development in 2021.[1][4][7]

See also

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References

[edit | edit source]
  1. ^ a b c d e "Firuglipel - Daiichi Sankyo Company". adisinsight.springer.com. Retrieved 28 October 2026.
  2. ^ a b c 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. ^ a b 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. ^ a b c 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.
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