Page last updated: 2024-11-13

ly 2140023

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

LY 2140023: prodrug of LY-404039 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID74405857
MeSH IDM0528766

Synonyms (2)

Synonym
ly-2140023
ly 2140023

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"Ten phase 1 studies of LY2140023 monohydrate (LY2140023), an mGlu2/3 receptor agonist, in healthy male and female subjects were pooled to evaluate the adverse event profile."( Adverse events in healthy subjects exposed to single and multiple doses of LY2140023 monohydrate: pooled results from 10 phase 1 studies.
Ayan-Oshodi, M; Kinon, BJ; Kryzhanovskaya, L; Lowe, SL; Walker, DJ; Wondmagegnehu, ET, 2012
)
0.38
"5%) in the SOC group discontinued due to adverse events (physician and subject decision combined, P = ."( A long-term, phase 2, multicenter, randomized, open-label, comparative safety study of pomaglumetad methionil (LY2140023 monohydrate) versus atypical antipsychotic standard of care in patients with schizophrenia.
Adams, DH; Baygani, S; Kinon, BJ; Kollack-Walker, S; Millen, BA; Velona, I; Walling, DP, 2013
)
0.39
"These data provide further evidence that the potential antipsychotic LY2140023 monohydrate, with a glutamatergic mechanism of action, may have a unique tolerability profile characterized by a low association with some adverse events such as extrapyramidal symptoms and weight gain that may characterize currently available dopaminergic antipsychotics."( A long-term, phase 2, multicenter, randomized, open-label, comparative safety study of pomaglumetad methionil (LY2140023 monohydrate) versus atypical antipsychotic standard of care in patients with schizophrenia.
Adams, DH; Baygani, S; Kinon, BJ; Kollack-Walker, S; Millen, BA; Velona, I; Walling, DP, 2013
)
0.39

Pharmacokinetics

ExcerptReferenceRelevance
"Obtaining pharmacokinetic data from the intravenous route for drugs intended for oral administration has traditionally been expensive and time consuming because of the toxicology requirements and challenges in intravenous formulations."( Approaches to intravenous clinical pharmacokinetics: Recent developments with isotopic microtracers.
Lappin, G, 2016
)
0.43

Bioavailability

ExcerptReferenceRelevance
" Such studies are necessary, however, particularly when regulator agencies request absolute bioavailability data."( Approaches to intravenous clinical pharmacokinetics: Recent developments with isotopic microtracers.
Lappin, G, 2016
)
0.43

Dosage Studied

ExcerptRelevanceReference
"Effects on neurotransmitter/metabolite concentrations were assessed in male rats following single oral doses of LY2140023 monohydrate (microdiasylates from the prefrontal cortex), single intraperitoneal injection of LY404039 [cerebrospinal fluid (CSF)], or LY2140023 monohydrate dosed once daily for 7 days (CSF)."( Effects of a novel mGlu₂/₃ receptor agonist prodrug, LY2140023 monohydrate, on central monoamine turnover as determined in human and rat cerebrospinal fluid.
Ackermann, B; Anderson, S; Ayan-Oshodi, M; Dean, R; Eckstein, J; Ho, M; Jackson, K; Lowe, S; McKinzie, D; Natanegara, F; Perry, K; Svensson, K; Yuen, E, 2012
)
0.38
"Rat studies: Acute dosing with LY2140023 monohydrate resulted in significant dose-dependent increases in extracellular concentrations of dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA), but not 5-hydroxyindoleacetic acid (5-HIAA), in the prefrontal cortex."( Effects of a novel mGlu₂/₃ receptor agonist prodrug, LY2140023 monohydrate, on central monoamine turnover as determined in human and rat cerebrospinal fluid.
Ackermann, B; Anderson, S; Ayan-Oshodi, M; Dean, R; Eckstein, J; Ho, M; Jackson, K; Lowe, S; McKinzie, D; Natanegara, F; Perry, K; Svensson, K; Yuen, E, 2012
)
0.38
"LY2140023 monohydrate and/or LY404039 dosing potently affected dopamine turnover and also significantly affected serotonin turnover in the human and rat central nervous systems."( Effects of a novel mGlu₂/₃ receptor agonist prodrug, LY2140023 monohydrate, on central monoamine turnover as determined in human and rat cerebrospinal fluid.
Ackermann, B; Anderson, S; Ayan-Oshodi, M; Dean, R; Eckstein, J; Ho, M; Jackson, K; Lowe, S; McKinzie, D; Natanegara, F; Perry, K; Svensson, K; Yuen, E, 2012
)
0.38
" dosing in healthy subjects."( Relative contributions of presystemic and systemic peptidases to oral exposure of a novel metabotropic glutamate 2/3 receptor agonist (LY404039) after oral administration of prodrug pomaglumetad methionil (LY2140023).
Annes, WF; Ayan-Oshodi, MA; Cornelissen, K; Hall, SD; Knadler, MP; Long, A; Mitchell, MI; Witcher, JW; Zhang, W, 2015
)
0.42
" A method has emerged whereby the drug administered intravenously is isotopically labeled and dosed at a maximum of 100 µg concomitantly with an oral administration given at a therapeutically relevant level."( Approaches to intravenous clinical pharmacokinetics: Recent developments with isotopic microtracers.
Lappin, G, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (23)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (8.70)29.6817
2010's21 (91.30)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials12 (52.17%)5.53%
Reviews3 (13.04%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (34.78%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]