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Oncodesign opens up a path to new kinases of therapeutic interest

Nanocyclix® is a proprietary medicinal chemistry technology based on the macrocyclization of small Lead-like molecules, which supports Oncodesign’s drug design and biomarker discovery programs.

Given Oncodesign’s expertise in designing, synthesizing and optimizing this type of macrocyclic small molecules, Nanocyclix can be applied to numerous therapeutic targets and kinases in particular. Nanocyclix® technology brings multiple benefits:

  • Low molecular-weight compounds
  • Nanomolar affinities, leading to high efficacy (LE=0.4-0.6),
  • Attractive selectivity profiles, even with extremely close targets,
  • Conformational rigidity favorable for complexation through shape recognition, with thermodynamic entropy and enthalpy parameters, which is unique for this class of molecules.

Oncodesign’s kinase inhibitor library currently features over 8,000 macrocycles. These type I kinase inhibitors profiled on the human kinome are powerful, highly selective and demonstrate good cellular penetration. They also possess a favorable developability, physical chemistry and eADMET profile, with a highly predictive SAR.

Several leads are currently being optimized, both for known kinases and for unexplored kinases. They are set to become future targeted therapies in precision medicine. Probe-based drug discovery helps to identify first-in-class opportunities arising from barely explored or unexplored kinases, and screening our molecular diversity for kinases of interest opens up the path to next-generation inhibitors that are potentially best in class.

Contact us today for further information about our partnerships and our internal projects.