ASPET

FEBRUARY 26, 2024

Panobinostat is a potent pan-HDAC inhibitor that has been tested in multiple studies for the treatment of brain tumors. There have been contrasting views surrounding its efficacy for the treatment of tumors in the CNS following systemic administration when examined in different models or species.

Metabolic Stability 100

Metabolic Stability Pharmacokinetics Pharmacogenetics Treatment 100

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. BBP-671 treatment elevated brain coenzyme A concentrations, and improved movement and body weight in a PKAN mouse model.

Metabolic Stability 100

Metabolic Stability Pharmacokinetics Regulations Treatment 100

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.

Drug Development 63

Drug Development Metabolic Stability Clinical Trials Drugs 63

Drug Target Review

JUNE 12, 2023

With 13 preclinical candidates and three AI-designed drugs currently undergoing clinical trials, Insilico is spearheading a revolution in cancer treatment and beyond. Can you provide a summary of the key findings and implications of the preclinical studies on ISM6331 for the treatment of advanced solid tumours?

Metabolic Stability 92

Metabolic Stability Clinical Trials Small Molecule Pharmacokinetics 92

Metabolite Tales Blog

DECEMBER 13, 2023

The pyrazole in a drug compound developed by LEO as an oral IL-17A protein-protein interaction modulator for the treatment of psoriasis and other inflammatory disorders is susceptible to N -glucuronidation. 22(5):803-11; [link] [10] Glucuronidation and UGT isozymes in bladder: new targets for the treatment of uroepithelial carcinomas?

Small Molecule 59

Small Molecule Metabolic Stability Treatment Pharmacokinetics 59

Metabolite Tales Blog

MARCH 1, 2023

9 The evidence here is that treatment with P450 inhibitors removed the toxic effects seen in the compounds of interest. 2010, 75, 9, 3141–3143 [link] 22 Clin Pharmacokinet. 44, 797–814 [link] Take a look at our other blogs The post Metabolism of five membered nitrogen containing heterocycles appeared first on Hypha Discovery.

Metabolic Stability 52

Metabolic Stability Pharmacokinetics Drugs Science 52

Metabolite Tales Blog

APRIL 4, 2023

3 Metabolism differences at steady state Adagrasib, Mirati’s irreversible KRASG12C inhibitor for treatment of non-small cell lung cancer is mainly metabolised by CYP3A4. Interestingly however, since adagrasib (MRTX849) inhibits CYP3A4 following multiple dosing, its metabolism is subsequently taken over by other CYPs.

Small Molecule 52

Small Molecule FDA Approval FDA Drugs 52