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

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

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. 2018, 26, 965-972 [link] 4a Pharmaceutics, 2022, 14, 1001 [link] 5 Phys. 2018, 61, 5, 2041–205 [link] 9 ACS Chem. 11 Figure 11 Pyrazoles – more stable to oxidative cleavage? 1980, 8, 34-38 [link] 4 J.

Metabolic Stability 52

Metabolic Stability Pharmacokinetics Drugs Science 52

Metabolite Tales Blog

MAY 12, 2023

This was surprising given that replacement of a phenyl with a pyrimidine and fluorination of aryl or heteroaryl rings are techniques often used to increase metabolic stability. Journal of Medicinal Chemistry 2018 61 (23), 10700-10708, [link] [13] Chemical Aspects of Human and Environmental Overload with Fluorine. Elizabeth A.

Drugs 52

Drugs Small Molecule Metabolic Stability FDA Approval 52