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Evaluation of Systemic and Brain Pharmacokinetic Parameters for Repurposing Metformin Using Intravenous Bolus Administration [Drug Discovery and Translational Medicine]

ASPET

Yet, the absence of established systemic and brain pharmacokinetic (PK) parameters at relevant pre-clinical doses presents a significant knowledge gap. In vitro assays examined brain tissue binding and metabolic stability. It further emphasizes the importance of selecting pharmacologically relevant pre-clinical doses.

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Metabolism of macrocyclic drugs

Metabolite Tales Blog

Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. It was hypothesized that as glecaprevir is largely metabolized by the liver, the production of toxic or immunogenic metabolites was a possible source of injury [7].

Drugs 52
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Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. It was hypothesized that as glecaprevir is largely metabolized by the liver, the production of toxic or immunogenic metabolites was a possible source of injury [7].