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The Novel GlycoPEGylated FGF21 Analog Pegozafermin Activates Human FGF Receptors and Improves Metabolic and Liver Outcomes in Diabetic Monkeys and Healthy Human Volunteers [Drug Discovery and Translational Medicine]

ASPET

In cell-based assays, pegozafermin had a similar receptor engagement profile as native FGF21, with approximately 8-fold higher potency at FGF receptor 1 (FGFR1). Pharmacokinetic half-lives ranged from 55 to 100 hours over the clinically relevant dose range, consistent with the expected half-life extension by glycoPEGylation.

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Inside The Altascientist Issue 41: Immunomodulation Assessments for Clinical Trials–Sophisticated Bioanalytical Approaches to Support Complex Modalities

Alta Sciences

As the complexity of these therapeutics increases, so must the sophistication of the bioanalytical assays designed to either quantify them or measure their impact on the patient. This includes careful consideration of pharmacokinetic and pharmacodynamic endpoints , as well as regulatory and bioanalytical requirements.

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Leadeth me unto Truth and delivereth me from those who have already found it

Molecular Design

For example, we might examine the structure-activity relationship in a cell-based assay for consistency with the structure-activity relationship that we’ve observed in the enzyme inhibition assay. We have to make assumptions in these situations and we also need to check that these assumptions are reasonable.

Drugs 79