ASPET

FEBRUARY 26, 2024

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.

Metabolic Stability 100

Metabolic Stability Pharmacokinetics Pharmacogenetics Treatment 100

ASPET

MAY 22, 2024

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.

Pharmacokinetics 100

Pharmacokinetics Metabolic Stability Clinical Pharmacology Disease 100

Covalent Modifiers

AUGUST 4, 2024

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.

Pharmacokinetics 72

Pharmacokinetics Metabolic Stability Drugs 72

ASPET

OCTOBER 24, 2023

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.

Metabolic Stability 100

Metabolic Stability Pharmacokinetics Regulations Treatment 100

DrugBank

OCTOBER 17, 2024

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.

Drug Development 63

Drug Development Metabolic Stability Clinical Trials Drugs 63

Drug Target Review

JUNE 12, 2023

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.

Metabolic Stability 92

Metabolic Stability Clinical Trials Small Molecule Pharmacokinetics 92

Metabolite Tales Blog

DECEMBER 13, 2023

N -glucuronidation: the human element By Julia Shanu-Wilson In our last blog of the year, we look at why N -glucuronidation of drugs is important in human drug metabolism. Glucuronidation is the most common phase II reaction observed in the metabolism of drugs in humans.

Small Molecule 59

Small Molecule Metabolic Stability Treatment Pharmacokinetics 59