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Indications
Cognitive disorders such as Alzheimer's disease, vascular dementia, and schizophrenia.
Stage of Development
Phase 2
Clinical Data
Lexicon initiated Phase 2a 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 2a trial will evaluate safety, tolerability and cognitive effects in elderly volunteers with age-associated memory impairment.
In Phase 1 clinical trials, all dosages of LX6171 were well tolerated and achieved good systemic exposure. There were no serious adverse events and no effects on electrocardiogram, vital signs, blood chemistry, hematology, or urinalysis. The most common adverse events were gastrointestinal (GI)-related and associated with the vehicle used to deliver the compound. In order to avoid vehicle associated GI effects, we have replaced the vehicle used in Phase 1 with a new oral suspension and have also developed a solid oral formulation for future studies.
Overview
LX6171 is an orally-delivered small molecule under development as a potential treatment for cognitive disorders which acts by inhibiting SLC6A7, a high-affinity L-proline transporter located exclusively within the central nervous system.
Key Target
LX6171 targets SLC6A7, a high-affinity L-proline transporter that is expressed at nerve junctions or synapses in the central nervous system. Specifically, the target is found at synaptic vesicles and presynaptic membranes of glutamatergic neurons, which are critical to learning, memory, and neurotransmission. From research conducted in the Genome5000TM program, Lexicon scientists observed that mice lacking this protein perform better in tests of learning and memory compared to normal mice.
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Highlighted areas of the brain are important in learning and memory. |
Preclinical Data
In preclinical studies, mice treated with LX6171 performed better than untreated animals in tests of learning and memory.
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The LX6171 drug target is expressed in regions of the brain that are known to be important in learning and memory. |
Related Publications
Brown PM, Yu XQ, Savelieva KV, Childers M, Frazier KS, Walke DW, Wilson, A, Heydorn WE, Lanthorn TH (2008). LX6171: A Novel Potential Treatment for Cognitive Disorders. 2008 Annual Meeting of the American Academy of Neurology.
Poster  (825 KB)
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