Article · Wikipedia archive · Last revised Jun 17, 2026

Setogepram

Setogepram is an experimental drug which acts as a mixed agonist-antagonist for certain free fatty acid receptors, being an agonist at FFAR1 (GPR40) but an antagonist at GPR84. It has antiinflammatory and anti-fibrotic effects and has reached Phase II human clinical trials for treatment of idiopathic pulmonary fibrosis.

Last revised
Jun 17, 2026
Read time
≈ 1 min
Length
260 w
Citations
5
Source
Wikipedia ↗
Setogepram
Clinical data
Other namesPBI-4050, Fezagepras
Identifiers
  • 2-(3-pentylphenyl)acetic acid
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC13H18O2
Molar mass206.285 g·mol−1
3D model (JSmol)
  • CCCCCC1=CC(=CC=C1)CC(=O)O
  • InChI=1S/C13H18O2/c1-2-3-4-6-11-7-5-8-12(9-11)10-13(14)15/h5,7-9H,2-4,6,10H2,1H3,(H,14,15)
  • Key:PEGQOIGYZLJMIB-UHFFFAOYSA-N

Setogepram (PBI-4050, Fezagepras) is an experimental drug which acts as a mixed agonist-antagonist for certain free fatty acid receptors, being an agonist at FFAR1 (GPR40) but an antagonist at GPR84. It has antiinflammatory and anti-fibrotic effects and has reached Phase II human clinical trials for treatment of idiopathic pulmonary fibrosis.12345

References

References

  1. Li Y, Chung S, Li Z, Overstreet JM, Gagnon L, Grouix B, et al. (May 2018). "Fatty acid receptor modulator PBI-4050 inhibits kidney fibrosis and improves glycemic control". JCI Insight. 3 (10). doi:10.1172/jci.insight.120365. PMC 6012516. PMID 29769449.
  2. Khalil N, Manganas H, Ryerson CJ, Shapera S, Cantin AM, Hernandez P, et al. (March 2019). "Phase 2 clinical trial of PBI-4050 in patients with idiopathic pulmonary fibrosis". The European Respiratory Journal. 53 (3). doi:10.1183/13993003.00663-2018. PMC 6422836. PMID 30578394.
  3. Nguyen QT, Nsaibia MJ, Sirois MG, Calderone A, Tardif JC, Fen Shi Y, et al. (January 2020). "PBI-4050 reduces pulmonary hypertension, lung fibrosis, and right ventricular dysfunction in heart failure". Cardiovascular Research. 116 (1): 171–182. doi:10.1093/cvr/cvz034. PMID 30753422.
  4. Chen LH, Zhang Q, Xie X, Nan FJ (December 2020). "Modulation of the G-Protein-Coupled Receptor 84 (GPR84) by Agonists and Antagonists". Journal of Medicinal Chemistry. 63 (24): 15399–15409. doi:10.1021/acs.jmedchem.0c01378. PMID 33267584.
  5. Gagnon L, Leduc M, Thibodeau JF, Zhang MZ, Grouix B, Sarra-Bournet F, et al. (May 2018). "A Newly Discovered Antifibrotic Pathway Regulated by Two Fatty Acid Receptors: GPR40 and GPR84". The American Journal of Pathology. 188 (5): 1132–1148. doi:10.1016/j.ajpath.2018.01.009. PMID 29454750.