Structure via PubChem · Public domain (PubChem)
pomaglumetad
Sign in to saveAlso known as LY-404039
Pomaglumetad (LY-404,039) is an amino acid analog drug that acts as a highly selective agonist for the metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3. Pharmacological research has focused on its potential antipsychotic and anxiolytic effects. Pomaglumetad is intended as a treatment for schizophrenia and other psychotic and anxiety disorders by modulating glutamatergic activity and reducing presynaptic release of glutamate at synapses in limbic and forebrain areas relevant to these disorders. Human studies investigating therapeutic use of pomaglumetad have focused on the pr
Chemical data
- Formula
- C7H9NO6S
- Molecular weight
- 235.22 g/mol
- IUPAC name
- (1R,4S,5S,6S)-4-amino-2,2-dioxo-2lambda6-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid
- SMILES
- C1[C@]([C@@H]2[C@H]([C@@H]2S1(=O)=O)C(=O)O)(C(=O)O)N
- InChIKey
- AVDUGNCTZRCAHH-MDASVERJSA-N
- XLogP
- -4.8
- Polar surface area
- 143 Ų
- H-bond donors
- 3
- H-bond acceptors
- 7
- Formal charge
- 0
via PubChem
Drug data · ChEMBL
- Max clinical phase
- Phase 1
- Molecule type
- Small molecule
via ChEMBL · EBI
Wikidata facts
- Subclass of
- chemical compound
- Mass
- 235.015
Show 4 more facts
- chemical formula
- C₇H₉NO₆S
- canonical SMILES
- C1C(C2C(C2S1(=O)=O)C(=O)O)(C(=O)O)N
- isomeric SMILES
- C1[C@]([C@@H]2[C@H]([C@@H]2S1(=O)=O)C(=O)O)(C(=O)O)N
- Commons category
- Pomaglumetad
Sources (2)
via Wikidata · CC0
~15 min read
Encyclopedic overview
14 sectionsContents
- Pharmacology
- Pharmacodynamics
- Novelty
- Animal studies
- Pomaglumetad methionil
- Synthesis and pharmacology
- Treatment for schizophrenia
- Dosage and usage
- Efficacy and clinical trials
- Tolerability and side effects
- Eli Lilly stops phase III development
- Denovo Biopharma licenses pomaglumetad methionil
- See also
- References
Pomaglumetad (LY-404,039) is an amino acid analog drug that acts as a highly selective agonist for the metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3. Pharmacological research has focused on its potential antipsychotic and anxiolytic effects. Pomaglumetad is intended as a treatment for schizophrenia and other psychotic and anxiety disorders by modulating glutamatergic activity and reducing presynaptic release of glutamate at synapses in limbic and forebrain areas relevant to these disorders. Human studies investigating therapeutic use of pomaglumetad have focused on the prodrug pomaglumetad methionil (LY-2140023), a methionine amide of pomaglumetad since pomaglumetad exhibits low oral absorption and bioavailability in humans.
Early human trials using this prodrug form of pomaglumetad gave encouraging results. However, pharmaceutical company Eli Lilly terminated further development of the compound in 2012 after it failed in phase III clinical trials. In September 2013, the results of a randomized, placebo-controlled clinical trial investigating the impact of adjunctive pomaglumetad methionil on prominent negative symptoms in schizophrenia was published and failed to demonstrate any benefit.
Excerpted from Wikipedia’s “pomaglumetad” article, available under the CC BY-SA 4.0 licence.