2008 Clinical Development Metabolic Stability 
Metabolite Tales Blog
APRIL 4, 2023
Deuteration at this position was found to block generation of a less selective primary amide metabolite in vivo and increase metabolic stability. Insights into drug metabolism by cytochromes P450 from modelling studies of CYP2D6-drug interactions. 2008 Mar;153 Suppl 1(Suppl 1):S82-9. Br J Pharmacol.
Metabolite Tales Blog
JULY 5, 2023
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. Still, of the 34 macrocycles currently in clinical trials, only 18% are de novo designed.
Metabolite Tales Blog
JULY 5, 2023
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. Still, of the 34 macrocycles currently in clinical trials, only 18% are de novo designed.
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