Talaglumetad (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; developmental code name LY-544344) is a metabotropic glutamate mGlu2 and mGlu3 receptor agonist which was under development for the treatment of generalized anxiety disorder.
Pharmacology The drug is a prodrug of eglumetad (LY-354740), a potent and selective metabotropic glutamate mGlu2 and mGlu3 receptor agonist. Eglumetad showed modest oral bioavailability (~10%) and brain penetration in animal and human studies, so talaglumetad was developed to enhance its pharmacokinetic properties for clinical use. Through uptake by the peptide transporter 1 (PepT1), the drug increased systemic exposure to eglumetad in humans by approximately 13-fold relative to administration of eglumetad itself, with an approximate oral bioavailability of 85%. Eglumetad shows anxiolytic-like effects in animals and talaglumetad produced anxiolytic effects in humans. The drug did not produce the problematic side effects typical of benzodiazepines in clinical studies.
Development Talaglumetad was under development by Eli Lilly and Company. It appears to have been under development until at least 2005. The drug reached phase 2 clinical trials for treatment of generalized anxiety disorder. However, development of talaglumetad was discontinued due to findings of convulsions in preclinical rodent studies.
See also Eglumetad Pomaglumetad Pomaglumetad methionil
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