Friday, 14 December 2018

Animal proof of concept in Parkinson´s disease models obtained


KUALA LUMPUR, Dec 11 (Bernama) -- CereSpir Inc. and The National Neuroscience Institute (NNI) Singapore have obtained animal proof of concept for CereSpir’s clinical stage compound itanapraced in Parkinson’s disease models.
Its lead compound, itanapraced (CSP-1103), is a small molecule with good oral bioavailability, a long plasma half-life and substantial penetration into the brain, a statement said.
Itanapraced blocks LRRK2 expression and LRRK2-mediated neurotoxicity. Itanapraced also ready to advance to Phase 2 in Parkinson’s disease patients with and without genetic mutation.
Parkinson’s disease is a common, progressive neurodegenerative disorder associated with loss of midbrain dopaminergic neurons which produce the essential neurotransmitter, dopamine.  
LRRK2 gain of function mutants are responsible for the majority of cases of familial Parkinson’s disease.  
Additionally, LRRK2 kinase activity is aberrantly increased in vulnerable dopamine neurons by oxidative mechanisms involving α-synuclein and mitochondrial impairment, suggesting LRRK2 inhibition will be useful for the majority of Parkinson’s disease patients.
Itanapraced was previously tested with positive results in patients with mild cognitive impairment (MCI), was shown to block the expression of LRRK2 and prevent neurotoxicity resulting in the preservation of healthy dopaminergic neurons.  
CereSpir  is a privately held, science-driven pharmaceutical company with an innovative approach to treating neurodegenerative disorders. More details at www.cerespir.com
-- BERNAMA

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