Drug intelligence / Profile preview

ly404039

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

LY404039 is a potent and selective small molecule agonist of group II metabotropic glutamate receptors (mGluR2 and mGluR3), with Ki values of approximately 149 nM for mGluR2 and 92 nM for mGluR3. It acts by modulating glutamatergic neurotransmission in the brain, reducing presynaptic release of glutamate in regions where these receptors are expressed. Preclinical studies have demonstrated antipsychotic and anxiolytic efficacy across multiple animal models without significant sedative or motor side effects. LY404039 is the active moiety of the prodrug pomaglumetad methionil (LY2140023), which was developed primarily as a potential treatment for schizophrenia and other psychiatric disorders[1][5][6][7].

Other names
pomaglumetad (active moiety)(1R,4S,5S,6S)-4-Amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide
02

Targets

GRM3 (mGluR3)GRM2 (mGluR2)

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