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

Molecular Design

MAY 11, 2019

While I would agree that efficiency metrics are integral to the philatelic aspects of modern drug discovery, I don’t believe that YL2018 actually presents a single convincing example of efficiency metrics being used for decision making in a specific drug design project. Increasing the extent of ionization may also compromise permeability.

Metabolic Stability 52

Metabolic Stability Pharmacokinetics Pharmaceuticals Drugs 52

Metabolite Tales Blog

DECEMBER 13, 2023

Conversely, and interestingly, UGTs present in the bladder can protect against accumulation of toxins since they are highly expressed on the surface of bladder tissue, particularly in females where it is postulated that the lower incidence of bladder cancer is related to increased UGT isoform activity. J Pharm Biomed Anal. Oncotarget.

Small Molecule 59

Small Molecule Metabolic Stability Treatment Pharmacokinetics 59

Metabolite Tales Blog

APRIL 4, 2023

In fact, CYP2C8, CYP1A2, CYP2B6, CYP2C9, and CYP2D6 all contribute to adagrasib’s metabolism at steady-state. A poster presentation at the 2022 ISSX meeting on metabolism of MRTX849 revealed three circulating metabolites, M11, M55a and M68, at > 10% following a single oral dose. Br J Pharmacol. Acta Pharm Sin B.

Small Molecule 52

Small Molecule FDA Approval FDA Drugs 52

Metabolite Tales Blog

MARCH 1, 2023

22 Figure 17 Conclusion We hope you find this vignette on the metabolism of five membered nitrogen containing heterocycles a useful resource. There is much to be learnt from the pathways described above but in general, the more nitrogens present in your ring, the less likely you are to see Phase I type oxidations of the ring itself.

Metabolic Stability 52

Metabolic Stability Pharmacokinetics Drugs Science 52