Pomaglumetad methionil

Last updated

Pomaglumetad methionil
LY2140023 structure.png
Clinical data
Other namesLY-2140023; LY2140023; LY-2812223; LY2812223; Pomaglumetad prodrug; LY-404039 prodrug; DB-103; DB103
Routes of
administration 		Oral [1] [2]
Drug class Metabotropic glutamate mGlu2 and mGlu3 receptor agonist
ATC code
  • None
Pharmacokinetic data
Bioavailability 49% [2]
Protein binding Minimal [2]
Elimination half-life 1.5–2.4 hours [2]
Pomaglumetad: 2–6.2 hours [2]
Identifiers
  • (1R,4S,5S,6S)-4-[[(2S)-2-amino-4-methylsulfanylbutanoyl]amino]-2,2-dioxo-2λ6-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C12H18N2O7S2
Molar mass 366.40 g·mol−1
3D model (JSmol)
  • CSCC[C@@H](C(=O)N[C@]1(CS(=O)(=O)[C@@H]2[C@H]1[C@H]2C(=O)O)C(=O)O)N
  • InChI=1S/C12H18N2O7S2/c1-22-3-2-5(13)9(15)14-12(11(18)19)4-23(20,21)8-6(7(8)12)10(16)17/h5-8H,2-4,13H2,1H3,(H,14,15)(H,16,17)(H,18,19)/t5-,6+,7+,8-,12-/m0/s1
  • Key:VOYCNOJFAJAILW-CAMHOICYSA-N

Pomaglumetad methionil (INN Tooltip International Nonproprietary Name, USAN Tooltip United States Adopted Name; developmental code names LY-2140023 and LY-2812223) is a metabotropic glutamate mGlu2 and mGlu3 receptor agonist which is or was under development for the treatment of schizophrenia, substance-related disorders, and post-traumatic stress disorder (PTSD). [1] [2] It is taken orally. [1] [2]

Contents

Pharmacology

The drug is an inactive prodrug of pomaglumetad (LY-404039), which acts as a highly selective metabotropic glutamate mGlu2 and mGlu3 receptor agonist. [2] Whereas the oral bioavailability of pomaglumetad was found to be low in humans, pomaglumetad methionil has an estimated oral bioavailability of approximately 49%. [2] The drug is transported by the peptide transporter 1 (PepT1), resulting in it being rapidly and efficiently absorbed, and is then hydrolyzed into pomaglumetad. [2] The elimination half-life of pomaglumetad methionil is 1.5 to 2.4 hours, whereas the half-life of pomaglumetad is 2 to 6.2 hours. [2]

Development

Pomaglumetad methionil was under development by Eli Lilly and Company, Denovo Biopharma, and other institutions. [1] [3] As of January 2025, no recent development has been reported for treatment of schizophrenia or substance-related disorders, whereas development has been discontinued for PTSD. [1] [3] The highest developmental stage that pomaglumetad methionil has reached is phase 2 clinical trials. [1] [3]

See also

References

  1. 1 2 3 4 5 6 "Pomaglumetad methionil - Denovo Biopharma/Eli Lilly and Company". AdisInsight. 28 January 2025. Retrieved 1 October 2025.
  2. 1 2 3 4 5 6 7 8 9 10 11 Kinon BJ, Gómez JC (March 2013). "Clinical development of pomaglumetad methionil: a non-dopaminergic treatment for schizophrenia". Neuropharmacology. 66: 82–86. doi:10.1016/j.neuropharm.2012.06.002. PMID   22722029.
  3. 1 2 3 "Delving into the Latest Updates on Pomaglumetad methionil with Synapse". Synapse. 23 September 2025. Retrieved 1 October 2025.



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