Talaglumetad (, ; 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 mGlu
2 and mGlu
3 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
typical of
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
for treatment of generalized anxiety disorder.
However, development of talaglumetad was discontinued due to findings of
in preclinical rodent studies.
See also
