Talaglumetad
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| Other names | LY-544344; LY544344 |
| Drug class | Metabotropic glutamate mGlu2 and mGlu3 receptor agonist |
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| Pharmacokinetic data | |
| Bioavailability | 85%[1] |
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| Chemical and physical data | |
| Formula | C11H16N2O5 |
| Molar mass | 256.258 g·mol−1 |
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Talaglumetad (INN Tooltip International Nonproprietary Name, USAN Tooltip 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.[2]
Pharmacology
[edit ]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
[edit ]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]
See also
[edit ]References
[edit ]- ^ a b c d Vig BS, Huttunen KM, Laine K, Rautio J (October 2013). "Amino acids as promoieties in prodrug design and development". Advanced Drug Delivery Reviews. 65 (10): 1370–1385. doi:10.1016/j.addr.201210001. PMID 23099277.
- ^ a b "Talaglumetad". AdisInsight. 31 March 2009. Retrieved 1 October 2025.
- ^ a b Danysz W (September 2005). "LY-544344. Eli Lilly". IDrugs. 8 (9): 755–762. PMID 16118698.
- ^ a b c d e f Spooren W, Lesage A, Lavreysen H, Gasparini F, Steckler T (2010). "Metabotropic glutamate receptors: their therapeutic potential in anxiety". Behavioral Neurobiology of Anxiety and Its Treatment. Curr Top Behav Neurosci. Vol. 2. pp. 391–413. doi:10.1007/7854_2010_36. ISBN 978-3-642-02911-0. PMID 21309118.
- ^ Vig B, Rautio J (August 2011). "Amino acid prodrugs for oral delivery: challenges and opportunities". Therapeutic Delivery. 2 (8): 959–962. doi:10.4155/tde.11.75. PMID 22826863.
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