Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTQ916P)

• DTT Name: Fibroblast growth factor-21 (FGF21)
• Synonyms: UNQ3115/PRO10196; Fibroblast growth factor 21; FGF-21
• Gene Name: FGF21
• DTT Type: Clinical trial target; [1]
• BioChemical Class: Growth factor
• UniProt ID: FGF21_HUMAN
• TTD ID: T42928
• Sequence:
  MDSDETGFEHSGLWVSVLAGLLLGACQAHPIPDSSPLLQFGGQVRQRYLYTDDAQQTEAH
  LEIREDGTVGGAADQSPESLLQLKALKPGVIQILGVKTSRFLCQRPDGALYGSLHFDPEA
  CSFRELLLEDGYNVYQSEAHGLPLHLPGNKSPHRDPAPRGPARFLPLPGLPPALPEPPGI
  LAPQPPDVGSSDPLSMVGPSQGRSPSYAS
• Function: Activity requires the presence of KLB. Stimulates glucose uptake in differentiated adipocytes via the induction of glucose transporter SLC2A1/GLUT1 expression (but not SLC2A4/GLUT4 expression).
• KEGG Pathway:
  MAPK signaling pathway (hsa04010)
  Ras signaling pathway (hsa04014)
  Rap1 signaling pathway (hsa04015)
  PI3K-Akt signaling pathway (hsa04151)
  Regulation of actin cytoskeleton (hsa04810)
  Pathways in cancer (hsa05200)
  Melanoma (hsa05218)
• Reactome Pathway:
  Glucose transport (R-HSA-70153)
  Facilitative Na+-independent glucose transporters (R-HSA-428790)

Molecular Interaction Atlas (MIA) of This DTT

3 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pegozafermin	DM5D7VG	Hypertriglyceridemia	5C80.1	Phase 3	[2]
BMS-986036	DMIZKEC	Type-2 diabetes	5A11	Phase 2	[1]
PF-05231023	DMQYBSH	Type-2 diabetes	5A11	Phase 1	[3]

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
FGF-21	DMB35UN	Type-2 diabetes	5A11	Discontinued in Phase 1/2	[4]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Type 2 diabetes	5A11	Liver tissue	9.68E-01	0.05	0.22

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] Safety, pharmacokinetics, and pharmacodynamics of pegozafermin in patients with non-alcoholic steatohepatitis: a randomised, double-blind, placebo-controlled, phase 1b/2a multiple-ascending-dose study. Lancet Gastroenterol Hepatol. 2023 Feb;8(2):120-132.
• [3] Mechanistic investigation of the preclinical pharmacokinetics and interspecies scaling of PF-05231023, a fibroblast growth factor 21-antibody protein conjugate. Drug Metab Dispos. 2015 Jun;43(6):803-11.
• [4] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028644)