Parkinson’s disease: Servier and Oncodesign announce the selection of a preclinical candidate
Initiated in March 2019, this Research and Development partnership is focused on the identification of LRRK2 kinase inhibitors derived from Oncodesign’s proprietary Nanocyclix® platform and their potential to act as therapeutic agents against Parkinson’s disease, drawing on Servier and Oncodesign’s complementary expertise in the field of neurodegenerative disease and kinase inhibitors.
Oncodesign is paving the way for new kinases of therapeutic interest in several indications, including central nervous system (CNS) diseases.
Since the integration of Nanocyclix® into Oncodesign in 2010, we have significantly expanded the technology to a platform containing over 10,000 inhibitors based on over 50 different scaffolds and over 300 different linkers. These molecules have been extensively characterized in the human kinome and in eADME tests. As a pioneering company in precision medicine and artificial intelligence, Oncodesign has leveraged our vast Nanocyclix® knowledge base to increase the efficiency and speed of development of new therapeutic and diagnostic products. Nanocyclix® enjoys strong industry recognition with multiple past and present drug discovery partnerships: Ipsen, Sanofi, UCB, Guerbet, Cyclopharma, Bristol-Myers Squibb and Servier.
Collection of > 10 000 Macrocyclic Kinase Inhibitors
Nanocyclix prime properties
> 50 scaffolds , > 300 linkers
Attractive molecular properties with consistent SAR
Potent and selective type 1 inhibitors with low MW
Cellular potency as an intrinsic property
Annotated across the human kinome and in eADME
Potencial to cross BBB
Different shape based paradigm - unique value proposition
Address unexplored and intractable kinases
Not a screening library : these are all kinase inhibitors
Prone to radio-labelling for diagnostics design
The molecular weight of a Nanocyclix® kinase inhibitor, even after complete optimization, is generally around 350 to 450 daltons, significantly lower than a linear inhibitor with similar potency and selectivity. This generates a more drug-like profile that is still optimized using a rational and structure-based design and multi-parameter optimization (MPO) techniques from modern medicinal chemistry.
Nanocyclix® molecules can precisely target untreatable and unexplored kinases in various kinase families, including lipid kinases. Due to their small size and limited conformation space, the Nanocyclix® inhibitors easily cross cell membranes and even cross the blood-brain barrier. They can also be radiolabeled with 18F for diagnostic purposes. Kinome selectivity