Talaglumetad
Pharmaceutical compound
From Wikipedia, the free encyclopedia
Talaglumetad (INN, USAN; 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.[2]
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| Other names | LY-544344; LY544344 |
| Drug class | Metabotropic glutamate mGlu2 and mGlu3 receptor agonist |
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| Bioavailability | 85%[1] |
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| Formula | C11H16N2O5 |
| Molar mass | 256.258 g·mol−1 |
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Pharmacology
The drug is a prodrug of eglumetad (LY-354740), a potent and selective metabotropic glutamate mGlu2 and mGlu3 receptor agonist.[3][4][1] 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.[4][1] 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%.[5][1] Eglumetad shows anxiolytic-like effects in animals and talaglumetad produced anxiolytic effects in humans.[4] The drug did not produce the problematic side effects typical of benzodiazepines in clinical studies.[4]
Development
Talaglumetad was under development by Eli Lilly and Company.[2] It appears to have been under development until at least 2005.[3] The drug reached phase 2 clinical trials for treatment of generalized anxiety disorder.[4] However, development of talaglumetad was discontinued due to findings of convulsions in preclinical rodent studies.[4]
