Drug Target Review
SEPTEMBER 20, 2023
Complex challenges such as metabolic stability or absorption, distribution, metabolism or excretion (ADME) properties could be better predicted, accurately filtering out poor candidates and streamlining discovery. To really benefit from AI, the pharmaceutical industry must be more open to data sharing.
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. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4].
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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. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4].
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
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. Huber, Maricel Torrent, Thomayant Prueksaritanont, Chunze Li, Donald E. Slaughter, Elizabeth Mahan, Carmen Fernandez-Metzler, Youwei Yan, Lawrence C.
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