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LX6171

Indications
Cognitive Disorders (i.e., Alzheimer’s disease, Vascular Dementia, Schizophrenia,
Fragile X)

Overview
LX6171 is an orally-delivered small molecule intended to improve cognitive functions such as learning and memory by inhibiting a membrane protein of the central nervous system. 

Principal Target
LX6171 targets a membrane protein that is expressed in the central nervous system.  The target is found at synaptic vesicles and presynaptic membranes of glutamatergic neurons, which are ubiquitous in the central nervous system and critical to learning and memory, and neurotransmission.  From research conducted in the Genome5000 project, Lexicon scientists discovered that mice lacking this protein perform better in

Detail

The LX6171 target is expressed in regions of the brain that are known to be important in learning and memory.


Preclinical Data
In preclinical studies, animals treated with LX6171 performed better than untreated animals in tests of learning and memory, with no adverse effects observed in treated animals.

Clinical Status
In Phase 1 clinical trials, all dosages of LX6171 were well tolerated and achieved good systemic exposure, supporting once daily administration.  There were no apparent effects on ECG, vital signs, blood chemistry, hematology, or urinalysis.  The most common adverse events were mild, GI-related, and associated with the vehicle used to deliver the compound. 

Lexicon initiated Phase 2 studies of LX6171 in November 2007.  The initial stage of the trial will assess the bioavailability of a new oral-suspension formulation in healthy elderly participants.  The second stage of the Phase 2 trial will evaluate safety, tolerability and cognitive effects in elderly participants with age-associated memory impairment.



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