Metabolite Tales Blog

JULY 5, 2023

Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders. However, more de novo designed molecules in this “beyond the Rule of 5 chemical space” have emerged, with the first in this class, plerixafor , approved in oncology in 2008.

Drugs 52

Drugs Metabolic Stability FDA Approval Treatment 52

Metabolite Tales Blog

JULY 5, 2023

Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders. 2] However, more de novo designed molecules in this “beyond the Rule of 5 chemical space” have emerged, with the first in this class, plerixafor , approved in oncology in 2008.

Metabolic Stability 52

Metabolic Stability Drugs FDA Approval Treatment 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

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. Christopher D. Cox, Paul J. Coleman, Michael J. Breslin, David B. Whitman, Robert M. Garbaccio, Mark E. Fraley, Carolyn A. Buser, Eileen S. Kuo, Nancy E.

Drugs 52

Drugs Small Molecule Metabolic Stability FDA Approval 52