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Complex challenges such as metabolicstability 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.
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].
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].
Deuteration at this position was found to block generation of a less selective primary amide metabolite in vivo and increase metabolicstability. 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.
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 metabolicstability. Huber, Maricel Torrent, Thomayant Prueksaritanont, Chunze Li, Donald E. Slaughter, Elizabeth Mahan, Carmen Fernandez-Metzler, Youwei Yan, Lawrence C.
Nature Reviews Drug Discovery , 7(7):608624, 2008. Cyclic Peptide Design, Chapter 2: Strategies to Enhance MetabolicStabilities. Advanced Drug Delivery Reviews , 64:417, 2012. Driggers EM, Hale SP, Lee J, Terrett NK. The exploration of macrocycles for drug discovery: An underexploited structural class. Springer, 2019.
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