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.
Chemical Biology and Drug Design
SEPTEMBER 20, 2023
Magnoflorine increased the systemic exposure and metabolic stability and suppressed the transport of luteolin. The pharmacokinetic study was performed on male Sprague–Dawley rats randomly grouped as the single administration of luteolin and the co-administration of luteolin and magnoflorine with six rats of each.
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.
Chemical Biology and Drug Design
JUNE 8, 2023
The co-administration of cryptotanshinone with ophiopogonin D induced pharmacokinetic interaction prolonging the systemic exposure and improving metabolic stability of cryptotanshinone. Abstract Cryptotanshinone and ophiopogonin D are sourced from herbs with similar indications. to 8.58 ± 0.71 μg/mL μg/mL and from 15.99 ± 1.81
Covalent Modifiers
AUGUST 4, 2024
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. These results provide a quantitative framework to guide appropriate method selection for human PK prediction with covalent drugs.
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.
DrugBank
OCTOBER 17, 2024
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.
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