RST-01 Origins

RST-01 (Fluoro Ethyl Nor-Memantine) has its origin from its 18F analogue,  assessed in collaboration with the Hospital-University of Toulouse, France, as the first highly selective and functional NMDA receptor radiotracer.

Rationale

From the high selectivity of RST-01 to NMDA receptor, came the conclusion that non-radioactive RST-01could be an ideal candidate to treat CNS diseases in which balanced activation and blockade of NMDA receptor activity is involded. Building a strong network of academic partners (University of Columbia – New York, University of Montpellier, CNRS Toulouse, Ecole Normale Superieure Paris), ReST has been able to acquire evidence that the differentiated effects of FENMRST-01 on NMDA subtypes should enable a full recovery from traumatic stress, paving the way for a development as a secondary prophylactic for PTSD. 

 

Disabled by AD (Worldwide)

Suffering from long lasting PTSD (USA & EU)

Publications

Published patents

FENM – Scientific Documentation

Patents

    • 2013 – EP3003399 – novel chemical compounds derived from normemantine and use of same in the medical field​

    • 2017 – EP3723742 – use of fluoroethylnormemantine for the prevention and treatment of anxiety

    • 2020 – WO2021234324 – compound and composition for inducing neuroprotection​

    • 2021 – WO2023079187 – new synergistic combinations based on fenm and an acetylcholinesterase inhibitor

    • 2020 – EP3968977 – compositions and methods against stress-induced affective disorders and their associated symptoms

Publications

FENM as a Biomarker

    • Anne-Sophie Salabert et al.; Radiolabeling of [18F]-fluoroethylnormemantine and initial in vivo evaluation of this innovative PET tracer for imaging the PCP sites of NMDA receptors; Nuclear Medicine and Biology (2015)​

    • Anne-Sophie Salabert et al.; Evaluation of [18F]FNM biodistribution and dosimetry based on whole-body PET imaging of rats; Nuclear Medicine and Biology (2018)​

    • Marie Beaurain et al.; Pharmacological Characterization of [18F]-FNM and Evaluation of NMDA Receptors Activation in a Rat Brain Injury Model; Mol Imaging Biol. (2023)

FENM as a Drug candidate

    • Simon Couly et al.; Anti-amnesic and neuroprotective effects of Fluoroethylnormemantine in a pharmacological mouse model of Alzheimer’s disease; International Journal of Neuropsychopharmacology (2020)
    • Fluoroethylnormemantine, A novel derivative of memantine, facilitates extinction learning without sensorimotor deficits Briana K. Chen et al., International Journal of Neuropsychopharmacology (2021)
    • Fluoroethylnormemantine, a Novel NMDA Receptor Antagonist, for the Prevention and Treatment of Stress-Induced Maladaptive Behavior. Briana K.Chen et al., Biological Psychiatry (2021)
    • Freyssin A, Carles A, Guehairia S, Rubinstenn G, Maurice T. Fluoroethylnormemantine (FENM) shows synergistic protection in combination with a sigma-1 receptor agonist in a mouse model of Alzheimer’s disease. Neuropharmacology (2023)​