Remove Disease Remove Metabolic Stability Remove Pharmacokinetics
article thumbnail

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. The findings highlight metformin's rapid brain entry, minimal binding, and metabolic stability.

article thumbnail

The Data-Driven Future of Drug Development

DrugBank

Computational chemistry and molecular modeling techniques can predict potential drug candidates' binding affinity and pharmacokinetic properties, enabling the selection of the most promising compounds for further development. These complex molecules require precise engineering to ensure optimal efficacy and safety.

Insiders

Sign Up for our Newsletter

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

article thumbnail

Game-changing pan-TEAD inhibitor for solid tumours

Drug Target Review

What are the preclinical characteristics of ISM6331, including its efficacy, safety profile, and drug metabolism and pharmacokinetics (DMPK) properties? The system optimised the molecules that were most likely to succeed in terms of potency, metabolic stability, synthetic accessibility, and more.

article thumbnail

N-glucuronidation: the human element

Metabolite Tales Blog

To curb glucuronidation at that position a gem-dimethyl group was incorporated which not only boosted metabolic stability, but also resulted in increased potency of the final lead compound. 8(2):3640-3648; [link] [11] Pharmacokinetics of the Multi-kinase Inhibitor Pexidartinib: Mass Balance and Dose Proportionality. Oncotarget.