Remove Drugs Remove Metabolic Stability Remove Pharmacokinetics
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Pharmacokinetics of panobinostat: Inter-species difference in metabolic stability [Metabolism, Transport, and Pharmacogenetics]

ASPET

The objective of this study was to examine the in vitro metabolic stability of panobinostat in different matrices and assess the influence of that metabolic stability on the in vivo pharmacokinetics and CNS delivery of panobinostat.

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

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Predicting the Intravenous Pharmacokinetics of Covalent Drugs in Animals and Humans

Covalent Modifiers

4c00776 30 covalent drugs were used to assess clearance (CL) prediction reliability in animals and humans. Improved quantitative performance was observed by combining metabolic stability data from LMs and liver S9 fractions, the latter supplemented with reduced glutathione for glutathione transferase activity.

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Pantothenate kinase activation restores brain coenzyme A in a mouse model of pantothenate kinase associated neurodegeneration [Drug Discovery and Translational Medicine]

ASPET

The metabolic stability, protein binding and membrane permeability of BBP-671 all suggest it has the physical properties required to cross the blood brain barrier. Significance Statement The blood brain barrier represents a major hurdle for drugs targeting brain metabolism.

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The Data-Driven Future of Drug Development

DrugBank

Data science has emerged as an innovative tool in the biopharmaceutical industry, leveraging the power of machine learning and artificial intelligence to drive innovation and efficiency across the entire drug development lifecycle.

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Game-changing pan-TEAD inhibitor for solid tumours

Drug Target Review

TEAD proteins are crucial for tumour progression and drug resistance, making them an attractive focus for therapeutic interventions. Leveraging AI-guided structure-based drug design, Insilico’s research and development team generated an impressive portfolio of over 6,000 molecules and identified three highly promising hit series.

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Metabolism of 2022 FDA approved small molecule drugs PART 2

Metabolite Tales Blog

Metabolism of 2022 FDA approved small molecule drugs part 2 Mixing it Up By Julia Shanu-Wilson In Part 1 of this topic we looked at metabolism of the small molecule drugs approved by the FDA in 2022 that were mediated by CYP3A4.