Trial reportEuropean journal of drug metabolism and pharmacokinetics2018
Safety, Tolerability and Pharmacokinetics of Oral BI 425809, a Glycine Transporter 1 Inhibitor, in Healthy Male Volunteers: A Partially Randomised, Single-Blind, Placebo-Controlled, First-in-Human Study.
Trial report in European journal of drug metabolism and pharmacokinetics, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT02068690 (Safety, Tolerability, and Pharmacokinetics of Single Rising Oral Doses of BI 425809 in Healthy Male Subjects), which is not on this map. Cited by 25 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.
Safety, Tolerability, and Pharmacokinetics of Single Rising Oral Doses of BI 425809 in Healthy Male Subjects (Partially Randomised, Single-blind, Placebo-controlled) and Investigation of Relative Bioavailability and Food Effect of BI 425809 (Open-label, Randomised, Three-way Crossover)
Who cites it
25 citing papers in PubMed, 36 citations in OpenAlex.
- Assessing the Effect of Food on the Pharmacokinetics of Iclepertin in Healthy Volunteers: A Phase I, Open-Label, Randomised, Cross-over Trial.European journal of drug metabolism and pharmacokinetics · 2025Trial
- Efficacy and safety of the novel GlyT1 inhibitor BI 425809 in Alzheimer's dementia: a randomized controlled trial.Alzheimer's research & therapy · 2023Trial
- Quantitative electroencephalography parameters as neurophysiological biomarkers of schizophrenia-related deficits: A Phase II substudy of patients treated with iclepertin (BI 425809).Translational psychiatry · 2022Trial
- Multiple Rising Doses of Oral BI 425809, a GlyT1 Inhibitor, in Young and Elderly Healthy Volunteers: A Randomised, Double-Blind, Phase I Study Investigating Safety and Pharmacokinetics.Clinical drug investigation · 2018Trial
- GlyT1 (SLC6A9) inhibition in neurological and psychiatric disorders.Naunyn-Schmiedeberg's archives of pharmacology · 2026Review
- The Effect of Iclepertin on Hematological Parameters: An Overview of Nonclinical Studies and Clinical Trials in Healthy Volunteers and Patients with Cognitive Impairment Associated with Schizophrenia.Journal of clinical pharmacology · 2026Review
- New Pharmacological Treatment Approaches for Schizophrenia: Navigating the Post-iclepertin Landscape.CNS drugs · 2026Review
- Pharmacokinetic/pharmacodynamic analysis to characterize the effect of long-term GlyT1 inhibitor iclepertin exposure on hemoglobin levels.Frontiers in pharmacology · 2026Article
- The Effect of Multiple Oral Doses of a Glycine Transporter 1 Inhibitor, Iclepertin (BI 425809), on the Steady-state Pharmacokinetics of a Combined Oral Contraceptive Containing Ethinylestradiol and Levonorgestrel: a Phase I Clinical Trial in Healthy Females.Clinical drug investigation · 2025Article
- Evaluation of the Drug-Drug Interaction Potential of the GlyT1 Inhibitor Iclepertin (BI 425809): A Physiologically Based Pharmacokinetic (PBPK) Modeling Approach.CPT: pharmacometrics & systems pharmacology · 2025Article
- Modulation of the human GlyT1 by clinical drugs and cholesterol.Nature communications · 2025Article
- The excitatory-inhibitory balance as a target for the development of novel drugs to treat schizophrenia.Biochemical pharmacology · 2024Review
- Treatment of Cognitive Impairment Associated with Schizophrenia Spectrum Disorders: New Evidence, Challenges, and Future Perspectives.Brain sciences · 2024Review
- Antibiotics treatment promotes vasculogenesis in the brain of glioma-bearing mice.Cell death & disease · 2024Article
- Pharmacological Treatment of Cognitive Impairment Associated With Schizophrenia: State of the Art and Future Perspectives.Schizophrenia bulletin open · 2024Article
- Development of the novel GlyT1 inhibitor, iclepertin (BI 425809), for the treatment of cognitive impairment associated with schizophrenia.European archives of psychiatry and clinical neuroscience · 2023Review
- The Absolute Bioavailability, Absorption, Distribution, Metabolism, and Excretion of BI 425809 Administered as an Oral Dose or an Oral Dose with an Intravenous Microtracer Dose of [Clinical drug investigation · 2022Article
- Role of Mitophagy in the Pathogenesis of Stroke: From Mechanism to Therapy.Oxidative medicine and cellular longevity · 2022Review
- Effects of Cytochrome P450 3A4 Induction and Inhibition on the Pharmacokinetics of BI 425809, a Novel Glycine Transporter 1 Inhibitor.European journal of drug metabolism and pharmacokinetics · 2022Article
- Drugs Based on NMDAR Hypofunction Hypothesis in Schizophrenia.Frontiers in neuroscience · 2021Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND AND
objectivesSchizophrenia and Alzheimer's disease are characterised by glutamatergic pathway abnormalities related to N-methyl-D-aspartate (NMDA) receptor hypofunction and cognitive impairment. Glycine is an NMDA receptor co-agonist; inhibition of glycine transporter 1 (GlyT1) should improve NMDA receptor hypofunction. This study evaluated safety and pharmacokinetic properties of BI 425809-a potent and selective GlyT1 inhibitor.
methodsIn the single-rising dose (SRD) component of this study, subjects were randomised to a single dose of BI 425809 [doses (mg): 0.5, 1, 2, 5, 10, 25, 50, 100 and 150], or placebo. The bioavailability/food effect (BA/FE) component investigated BI 425809 pharmacokinetics following single dosing (25-mg tablet) after overnight fasting or with a high-calorie meal or as solution (25 mg) after overnight fasting.
resultsOverall, 33/83 (39.8%) subjects had ≥ 1 treatment-related adverse event (AE); there were no deaths or serious AEs. Reported SRD part AEs trended towards dose dependency, occurring at the higher doses (mostly central nervous system related). BI 425809 plasma concentration-time profiles were similarly shaped across all doses and plasma exposure increased proportional to dose. In the BA/FE component, geometric mean ratios for the area under the concentration-time curve from time zero to the last measurable concentration and the maximum plasma concentration for tablet fasted versus solution fasted were 80.5 and 50.0%, respectively, and for tablet fed versus fasted were 125.9 and 142.1%, respectively.
conclusionBI 425809 was generally well-tolerated at doses expected to be clinically relevant. The AE profile suggested possible GlyT1-inhibiting effects. CLINICAL TRIAL IDENTIFIER: NCT02068690.
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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.