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I1*

Neurosteroids for the Treatment of Epilepsy

Dr Eva Kudová, Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences; Dr Hana Chodounská, Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences; Prof. Pavel Mareš, Institute of Physiology, Czech Academy of Sciences; Dr Karel Valeš, Institute of Physiology, Czech Academy of Sciences

IOCBTech


Challenge

There are currently over 25 antiepileptic drugs available in the EU. However, despite the current clinical armamentarium, about one-third of epilepsy patients remain pharmacoresistant and do not achieve seizure freedom.


Technology

The product presented here are novel steroidal compounds with a unique mechanism of action at the NMDA receptor. As inhibitors of excessive tonic NMDA activity, they are significantly more potent than memantine, with low toxicity and no apparent psychomimetic effects at therapeutic doses. We have also evidence of their modulator activity at the GABA receptor. In vivo, our compounds show consistent efficacy in several well-established models of epilepsy. In vitro evidence points to their potential neuroprotective properties.


Commercial Opportunity

Epilepsy affects more than 50 million people worldwide. The market size for epilepsy was estimated to exceed 6 billion USD in 2018 (all countries, source – Global Data).


Development Status

Preclinical.


Patent Situation

Submission of patent application planned in March 2019.


Further Reading

Vyklicky et al.: Journal of Neuroscience 2016, 36(7):2161-2175.

Vyklicky et al.: Scientific Reports 2015,18(5):10935.

Kudova et al.: Journal of Medicinal Chemistry 2015,58:5950-5966.

Borovska et al.: British Journal of Pharmacology 2012, 166(3):1069-1083.


 

Neurosteroids for the Treatment of Epilepsy