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Compound class:
Peptide
Comment: Pegozafermin (BIO89-100; originally from 89bio, now Roche) is a human FGF-21 analogue. It is O-glycosylated and PEGylated to extend circulating half-life, and has amino acid substitution R175>A to increase receptor potency [1,3]. It was designed to mimic the effects of FGF-21/FGFR signalling for clinical benefit in metabolic disorders (insulin resistance, hypertriglyceridemia, fatty liver disease, inflammation-driven fibrotic liver scarring, and obesity) [3].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| References |
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1. Bailey NN, Peterson SJ, Parikh MA, Jackson KA, Frishman WH. (2025)
Pegozafermin Is a Potential Master Therapeutic Regulator in Metabolic Disorders: A Review. Cardiol Rev, 33 (5): 402-406. [PMID:37889055] |
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2. Loomba R, Lawitz EJ, Frias JP, Ortiz-Lasanta G, Johansson L, Franey BB, Morrow L, Rosenstock M, Hartsfield CL, Chen CY et al.. (2023)
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, 8 (2): 120-132. [PMID:36521501] |
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3. Rosenstock M, Tseng L, Pierce A, Offman E, Chen CY, Charlton RW, Margalit M, Mansbach H. (2023)
The Novel GlycoPEGylated FGF21 Analog Pegozafermin Activates Human FGF Receptors and Improves Metabolic and Liver Outcomes in Diabetic Monkeys and Healthy Human Volunteers. J Pharmacol Exp Ther, 387 (2): 204-213. [PMID:37562970] |