ArticleMetabolites2012
Metabolic and Pharmacokinetic Differentiation of STX209 and Racemic Baclofen in Humans.
Article in Metabolites, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
12 citing papers in PubMed, 31 citations in OpenAlex.
- Differential GABA dynamics across brain functional networks in autism.Communications biology · 2026Trial
- Retinal GABAergic Alterations in Adults with Autism Spectrum Disorder.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2024Trial
- Exploratory evidence for differences in GABAergic regulation of auditory processing in autism spectrum disorder.Translational psychiatry · 2023Trial
- Sex-related differences in the efficacy of Baclofen enantiomers on self-administered alcohol in a binge drinking pattern and dopamine release in the core of the nucleus accumbens.Frontiers in pharmacology · 2023Article
- The GABAB receptor agonist STX209 reverses the autism‑like behaviour in an animal model of autism induced by prenatal exposure to valproic acid.Molecular medicine reports · 2022Article
- Development and Optimization of Microballoons Assisted Floating Tablets of Baclofen.AAPS PharmSciTech · 2021Article
- Simultaneous Quantitation of S(+)- and R(-)-Baclofen and Its Metabolite in Human Plasma and Cerebrospinal Fluid using LC-APCI-MS/MS: An Application for Clinical Studies.Molecules (Basel, Switzerland) · 2020Article
- Paradoxical effect of baclofen on social behavior in the fragile X syndrome mouse model.Brain and behavior · 2018Article
- Pharmacokinetic Studies of Baclofen Are Not Sufficient to Establish an Optimized Dosage for Management of Alcohol Disorder.Frontiers in psychiatry · 2018Review
- Arbaclofen in fragile X syndrome: results of phase 3 trials.Journal of neurodevelopmental disorders · 2017Article
- Rearrangements leading to fragmentations of hydrocinnamate and analogous nitrogen-containing anions upon collision-induced dissociation.Journal of the American Society for Mass Spectrometry · 2014Article
- Clinical potential, safety, and tolerability of arbaclofen in the treatment of autism spectrum disorder.Drug, healthcare and patient safety · 2014Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
STX209 is an exploratory drug comprising the single, active R-enantiomer of baclofen which is in later stage clinical trials for the treatment of fragile x syndrome (FXS) and autism spectrum disorders (ASD). New clinical data in this article on the metabolism and pharmacokinetics of the R- and S-enantiomers of baclofen presents scientific evidence for stereoselective metabolism of only S-baclofen to an abundant oxidative deamination metabolite that is sterically resolved as the S-enantiomeric configuration. This metabolite undergoes some further metabolism by glucuronide conjugation. Consequences of this metabolic difference are a lower Cmax and lower early plasma exposure of S-baclofen compared to R-baclofen and marginally lower urinary excretion of S-baclofen after racemic baclofen administration. These differences introduce compound-related exposure variances in humans in which subjects dosed with racemic baclofen are exposed to a prominent metabolite of baclofen whilst subjects dosed with STX209 are not. For potential clinical use, our findings suggest that STX209 has the advantage of being a biologically defined and active enantiomer.
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.