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12 Diseases |  |
1 Trial |
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1 Trial |  |
83 News |  |
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- | basmisanil (RG1662) / Roche, darigabat (CVL-865) / AbbVie
Journal: New Insights Into Pharmacology of GABAA Receptor Alpha Subunits-Selective Modulators. (Pubmed Central) - Jan 10, 2025
Future drug discovery efforts are encouraged to focus on positive allosteric modulators that selectively target the ?2, ?3 subunits and negative/positive allosteric modulators that target the ?5 subunit of the GABAA receptor. The pursuit of ligands possessing only anxiolytic effects or those enhancing cognition continues to be an important focus for future research, with promising advancements depicted in recent studies.
- | basmisanil (RG1662) / Roche
Preclinical, Journal: Basmisanil, an ?5-GABAAR negative allosteric modulator, produces rapid and sustained antidepressant-like responses in male mice. (Pubmed Central) - Jun 2, 2024
Bioanalysis of plasma and brain samples confirms effective blood-brain barrier penetration by Basmisanil and extrapolation to previously published data suggest that effects were observed at doses (10 and 30?mg/kg i.p.) corresponding to relatively modest levels of ?5-GABAAR occupancy (40-65?%). These results suggest that Basmisanil exhibits a combination of rapid and sustained antidepressant-like effects highlighting the potential of ?5-NAMs as a novel therapeutic strategy for depression.
- basmisanil (RG1662) / Roche
Trial termination: A Study to Evaluate the Safety and Efficacy of Basmisanil Treatment in Children Aged 2-14 Years With Dup15q Syndrome (clinicaltrials.gov) - May 14, 2024
P2, N=7, Terminated, Sponsor: Hoffmann-La Roche
These results suggest that Basmisanil exhibits a combination of rapid and sustained antidepressant-like effects highlighting the potential of ?5-NAMs as a novel therapeutic strategy for depression. Completed --> Terminated; The study was terminated due to sponsor decision and not related to safety or tolerability.
- basmisanil (RG1662) / Roche
Trial completion: A Study to Evaluate the Safety and Efficacy of Basmisanil Treatment in Children Aged 2-14 Years With Dup15q Syndrome (clinicaltrials.gov) - Apr 8, 2024
P2, N=7, Completed, Sponsor: Hoffmann-La Roche
Completed --> Terminated; The study was terminated due to sponsor decision and not related to safety or tolerability. Terminated --> Completed
- | basmisanil (RG1662) / Roche
Enrollment change, Trial completion date, Trial termination, Trial primary completion date: A Study to Evaluate the Safety and Efficacy of Basmisanil Treatment in Children Aged 2-14 Years With Dup15q Syndrome (clinicaltrials.gov) - Mar 17, 2024
P2, N=7, Terminated, Sponsor: Hoffmann-La Roche
Terminated --> Completed N=90 --> 7 | Trial completion date: Jan 2026 --> Mar 2024 | Recruiting --> Terminated | Trial primary completion date: Jan 2026 --> Mar 2024; The study was terminated due to sponsor decision and not related to safety or tolerability.
- ||| basmisanil (RG1662) / Roche
Enrollment open: A Study to Evaluate the Safety and Efficacy of Basmisanil Treatment in Children Aged 2-14 Years With Dup15q Syndrome (clinicaltrials.gov) - Mar 15, 2024
P2, N=90, Recruiting, Sponsor: Hoffmann-La Roche
N=90 --> 7 | Trial completion date: Jan 2026 --> Mar 2024 | Recruiting --> Terminated | Trial primary completion date: Jan 2026 --> Mar 2024; The study was terminated due to sponsor decision and not related to safety or tolerability. Active, not recruiting --> Recruiting
- || basmisanil (RG1662) / Roche
Enrollment closed: A Study to Evaluate the Safety and Efficacy of Basmisanil Treatment in Children Aged 2-14 Years With Dup15q Syndrome (clinicaltrials.gov) - Feb 7, 2024
P2, N=90, Active, not recruiting, Sponsor: Hoffmann-La Roche
Active, not recruiting --> Recruiting Recruiting --> Active, not recruiting
- basmisanil (RG1662) / Roche
Quindecim, a Phase II, double-blind, randomized, placebo-controlled trial of basmisanil in children with Dup15q syndrome (A4) - Apr 21, 2023 - Abstract #EAN2023EAN_1164;
- || basmisanil (RG1662) / Roche, midazolam hydrochloride / Generic mfg., diazepam / Generic mfg.
PK/PD data, Preclinical, Journal: A 'middle-out approach' for the prediction of human drug disposition from preclinical data using simplified physiologically based pharmacokinetic (PBPK) models. (Pubmed Central) - Mar 16, 2023
For basmisanil, the sparse preclinical data available could have affected the model performance for fitting and the subsequent extrapolation to human. Overall, this work provides a rational strategy to predict human drug distribution using preclinical PK data within the PBPK modelling strategy.
- | basmisanil (RG1662) / Roche
Retrospective data, Journal: Physiologically Based Biopharmaceutics Modeling of Food Effect for Basmisanil: A Retrospective Case Study of the Utility for Formulation Bridging. (Pubmed Central) - Jan 22, 2023
However, there is need for further evaluation of the approach and a definition of what formulation changes are minor in this context. In addition, this work highlights some uncertainties in the handling of solubility in PBBM, in particular around temperature dependency of solubility and the parameterization of bile salt solubilization using measurements in biorelevant media.
- ||| basmisanil (RG1662) / Roche
Enrollment open: A Study to Evaluate the Safety and Efficacy of Basmisanil Treatment in Children Aged 2-14 Years With Dup15q Syndrome (clinicaltrials.gov) - Jul 18, 2022
P2, N=90, Recruiting, Sponsor: Hoffmann-La Roche
In addition, this work highlights some uncertainties in the handling of solubility in PBBM, in particular around temperature dependency of solubility and the parameterization of bile salt solubilization using measurements in biorelevant media. Not yet recruiting --> Recruiting
- |||| basmisanil (RG1662) / Roche
New P2 trial: A Study to Evaluate the Safety and Efficacy of Basmisanil Treatment in Children Aged 2-14 Years With Dup15q Syndrome (clinicaltrials.gov) - Apr 1, 2022
P2, N=90, Not yet recruiting, Sponsor: Hoffmann-La Roche
- || basmisanil (RG1662) / Roche
Clinical, P2 data, Journal: A randomized, double-blind, placebo-controlled phase II trial to explore the effects of a GABA-α5 NAM (basmisanil) on intellectual disability associated with Down syndrome. (Pubmed Central) - Mar 23, 2022
P2
Basmisanil did not meet the primary efficacy objective of concomitant improvement on cognition and adaptive functioning after 6 months of treatment, despite evidence for target engagement. This study provides key learnings for future clinical trials in Down syndrome.
- basmisanil (RG1662) / Roche
The GABAA α5 Receptor as a Therapeutic Target for Dup15q Syndrome ([VIRTUAL]) - Nov 28, 2021 - Abstract #ACNP2021ACNP_1242;
The converging evidence reported here strongly suggests that excess GABAA receptor function contributes to the pathophysiology of Dup15q syndrome and points to the GABAA α5 receptor subtype as a novel and tractable target for the treatment of Dup15q syndrome. Roche is planning a randomized-controlled phase 2 trial in children with Dup15q syndrome to evaluate the effects of a GABAA α5 NAM (basmisanil) on core symptoms of Dup15q syndrome.
- | basmisanil (RG1662) / Roche
Preclinical, Journal: Basmisanil, a highly selective GABA-α5 negative allosteric modulator: preclinical pharmacology and demonstration of functional target engagement in man. (Pubmed Central) - Nov 11, 2021
An exploratory EEG study provided evidence for functional activity of basmisanil in human brain. Therefore, these preclinical and early clinical studies show that basmisanil has an ideal profile to investigate potential clinical benefits of GABA-α5 receptor negative modulation.
- | itraconazole / Generic mfg.
Journal: PKPD and cardiac single cell modeling of a DDI study with a CYP3A4 substrate and itraconazole to quantify the effects on QT interval duration. (Pubmed Central) - Sep 22, 2021
The results of the two approaches were in agreement, suggesting that the effect of basmisanil on QT interval duration can be attributed to the effect on hERG alone. The C-QT model for basmisanil can be used to derive the QT interval corrected changes in heart rate (QTc) and thus inform cardiac safety strategy in later development without the need for a separate, dedicated study.
- | basmisanil (RG1662) / Roche
Journal: Inhibition of a tonic inhibitory conductance in mouse hippocampal neurones by negative allosteric modulators of α5 subunit-containing γ-aminobutyric acid type A receptors: implications for treating cognitive deficits. (Pubmed Central) - Mar 9, 2021
Basmisanil was markedly less potent than the other α5-NAMs, an unexpected result based on studies of recombinant α5 GABA receptors. Studying the effects of α5 GABA receptor-selective drugs on the tonic inhibitory current in neurones could inform the selection of compounds for future clinical trials.
- basmisanil (RG1662) / Roche
[VIRTUAL] Results of a 24- Week Phase 2 Trial with Basmisanil, a Potent Selective Negative Allosteric Modulator of Gabaa α5 Receptors, in Cognitive Impairment Associated with Schizophrenia (CIAS) () - Mar 1, 2021 - Abstract #SIRS2021SIRS_596;
P2b
Discussion Overall, basmisanil did not improve cognitive deficits and functional impairment compared to placebo in a 24week study. However, subgroup analyses indicate that the cognitive subtype of patients may be associated with distinct profiles of treatment response.
- basmisanil (RG1662) / Roche
[VIRTUAL] Results of a 24- Week Phase 2 Trial with Basmisanil, a Potent Selective Negative Allosteric Modulator of Gabaa α5 Receptors, in Cognitive Impairment Associated with Schizophrenia (CIAS) () - Mar 1, 2021 - Abstract #SIRS2021SIRS_476;
P2b
Discussion Overall, basmisanil did not improve cognitive deficits and functional impairment compared to placebo in a 24week study. However, subgroup analyses indicate that the cognitive subtype of patients may be associated with distinct profiles of treatment response.
- basmisanil (RG1662) / Roche
[VIRTUAL] Results of a 24- Week Phase 2 Trial with Basmisanil, a Potent Selective Negative Allosteric Modulator of Gabaa α5 Receptors, in Cognitive Impairment Associated with Schizophrenia (CIAS) () - Mar 1, 2021 - Abstract #SIRS2021SIRS_459;
P2, P2b
Discussion Overall, basmisanil did not improve cognitive deficits and functional impairment compared to placebo in a 24week study. However, subgroup analyses indicate that the cognitive subtype of patients may be associated with distinct profiles of treatment response.
- || basmisanil (RG1662) / Roche
Clinical, Journal: A de novo variant of CHD8 in a patient with autism spectrum disorder. (Pubmed Central) - Apr 21, 2020
Whole exome sequencing for parent-child trio revealed a de novo heterozygous loss-of-function mutation (c.4984C>T, p.Arg1662Ter) in CHD8 gene. Our findings elaborate the genotype-phenotype correlation and confirm that the CHD8 disruptions represent a clinical ASD subtype and further highlight the significance of implementing genomic medicine in clinical practice for an early intervention and necessary support for the families.
- basmisanil (RG1662) / Roche
Evaluation of the Efficacy, Safety and Tolerability of basmisanil, a Selective GABAA 5 Negative Allosteric Modulator in Cognitive Impairment Associated with Schizophrenia: A Randomized, Double-Blind, Placebo-Controlled Phase 2b Study. (Spadolini - Ground Floor) - Apr 4, 2020 - Abstract #SIRS2020SIRS_1150;
P2b
Operational learnings such as key factors driving screening failures and discontinuation rates and their ties to compliance will also be discussed. As the study is still ongoing, full results and discussion thereof will be disclosed during the presentation (after clinical data base lock).
- | basmisanil (RG1662) / Roche
Preclinical, Journal: Comprehensive analysis of long non-coding RNAs and mRNAs in skeletal muscle of diabetic Goto-Kakizaki rats during the early stage of type 2 diabetes. (Pubmed Central) - Feb 26, 2020
Our study could provide more comprehensive knowledge of mRNAs and lncRNAs in skeletal muscle of GK rats at 3 and 4 weeks of age. And our study may provide deeper understanding of the underlying mechanism in T2D of GK rats at the age of 3 and 4 weeks.
- | basmisanil (RG1662) / Roche
Journal: HIV gp120 upregulates tonic inhibition through α5-containing GABARs. (Pubmed Central) - Jan 29, 2020
The increased current resulted from upregulation of extrasynaptic α5-containing GABARs, as indicated by inhibition with the selective inverse agonist basmisanil...Increased tonic inhibition impairs neuroplasticity and inhibition of α5-containing GABARs improves cognitive function in disease models. Thus, gp120-induced upregulation of α5-containing GABARs presents a novel therapeutic target for HAND.
- |||| basmisanil (RG1662) / Roche
Trial completion: A Study to Evaluate the Effects of Basmisanil in Participants With Cognitive Impairment Associated With Schizophrenia (CIAS) Treated With Antipsychotics (clinicaltrials.gov) - Jan 2, 2020
P2b, N=240, Completed, Sponsor: Hoffmann-La Roche
Thus, gp120-induced upregulation of α5-containing GABARs presents a novel therapeutic target for HAND. Active, not recruiting --> Completed
- | basmisanil (RG1662) / Roche
Enrollment closed: A Study to Evaluate the Effects of Basmisanil in Participants With Cognitive Impairment Associated With Schizophrenia (CIAS) Treated With Antipsychotics (clinicaltrials.gov) - Jul 9, 2019
P2b, N=240, Active, not recruiting, Sponsor: Hoffmann-La Roche
Active, not recruiting --> Completed Recruiting --> Active, not recruiting
- basmisanil (RG1662) / Roche
Preclinical and Early Clinical Pharmacological Profile of Basmisanil, a Gaba-A 5 Receptor Negative Allosteric modulator, Currently in a Phase 2 Clinical Trial for Cognitive Impairment Associated with Schizophrenia (Regency S-V) - Apr 3, 2019 - Abstract #SIRS2019SIRS_788;
Key aspects of the study design and baseline data will be presented. Discussion These data suggest basmisanil is a promising candidate drug with a unique pharmacological and safety profile for further clinical testing in conditions associated with cognitive impairment such as schizophrenia.
- basmisanil (RG1662) / Roche
Preclinical and Early Clinical Pharmacological Profile of Basmisanil, a Gaba-A 5 Receptor Negative Allosteric modulator, Currently in a Phase 2 Clinical Trial for Cognitive Impairment Associated with Schizophrenia (Regency P-Q) - Apr 3, 2019 - Abstract #SIRS2019SIRS_765;
Key aspects of the study design and baseline data will be presented. Discussion These data suggest basmisanil is a promising candidate drug with a unique pharmacological and safety profile for further clinical testing in conditions associated with cognitive impairment such as schizophrenia.
- | basmisanil (RG1662) / Roche
Trial completion date, Trial primary completion date: A Study to Evaluate the Effects of Basmisanil in Participants With Cognitive Impairment Associated With Schizophrenia (CIAS) Treated With Antipsychotics (clinicaltrials.gov) - Sep 27, 2018
P2b, N=240, Recruiting, Sponsor: Hoffmann-La Roche
Discussion These data suggest basmisanil is a promising candidate drug with a unique pharmacological and safety profile for further clinical testing in conditions associated with cognitive impairment such as schizophrenia. Trial completion date: Apr 2019 --> Dec 2019 | Trial primary completion date: Aug 2018 --> Dec 2019
- | basmisanil (RG1662) / Roche
Trial primary completion date: A Study to Evaluate the Effects of Basmisanil in Participants With Cognitive Impairment Associated With Schizophrenia (CIAS) Treated With Antipsychotics (clinicaltrials.gov) - Aug 1, 2018
P2b, N=240, Recruiting, Sponsor: Hoffmann-La Roche
Trial completion date: Apr 2019 --> Dec 2019 | Trial primary completion date: Aug 2018 --> Dec 2019 Trial primary completion date: Apr 2019 --> Aug 2018
- basmisanil (RG1662) / Roche
Enrollment change, Trial termination, Trial primary completion date: A Study to Evaluate the Safety and Efficacy of Basmisanil in Adults With Severe Motor Impairment Following an Ischemic Stroke (clinicaltrials.gov) - Jan 8, 2018
P2, N=5, Terminated, Sponsor: Hoffmann-La Roche
Trial primary completion date: Apr 2019 --> Aug 2018 N=95 --> 5 | Recruiting --> Terminated | Trial primary completion date: Sep 2018 --> Nov 2017; Low participant enrolment
- ||| basmisanil (RG1662) / Roche
Enrollment change, Trial primary completion date: A Study to Evaluate the Effects of Basmisanil in Participants With Cognitive Impairment Associated With Schizophrenia (CIAS) Treated With Antipsychotics (clinicaltrials.gov) - Dec 2, 2017
P2b, N=240, Recruiting, Sponsor: Hoffmann-La Roche
N=95 --> 5 | Recruiting --> Terminated | Trial primary completion date: Sep 2018 --> Nov 2017; Low participant enrolment N=180 --> 240 | Trial primary completion date: Aug 2018 --> Apr 2019
- basmisanil (RG1662) / Roche
Trial termination: A Study of RO5186582 in Down Syndrome Among Children 6 to 11 Years of Age (clinicaltrials.gov) - Mar 27, 2017
P2, N=45, Terminated, Sponsor: Hoffmann-La Roche
Active, not recruiting --> Terminated; Study was terminated due to data from another study showing no efficacy. There were no safety issues of concern.
- |||| basmisanil (RG1662) / Roche
Enrollment open: A Study to Evaluate the Effects of Basmisanil in Participants With Cognitive Impairment Associated With Schizophrenia (CIAS) Treated With Antipsychotics (clinicaltrials.gov) - Mar 20, 2017
P2b, N=180, Recruiting, Sponsor: Hoffmann-La Roche
There were no safety issues of concern. Not yet recruiting --> Recruiting
- |||| basmisanil (RG1662) / Roche
Enrollment open: A Study to Evaluate the Safety and Efficacy of Basmisanil in Adults With Severe Motor Impairment Following an Ischemic Stroke (clinicaltrials.gov) - Dec 14, 2016
P2, N=95, Recruiting, Sponsor: Hoffmann-La Roche
Not yet recruiting --> Recruiting Not yet recruiting --> Recruiting
- |||||| basmisanil (RG1662) / Roche
New P2b trial: A Study to Evaluate the Effects of Basmisanil in Participants With Cognitive Impairment Associated With Schizophrenia (CIAS) Treated With Antipsychotics (clinicaltrials.gov) - Nov 3, 2016
P2b, N=180, Not yet recruiting, Sponsor: Hoffmann-La Roche
- ||||| basmisanil (RG1662) / Roche
New P2 trial: A Study to Evaluate the Safety and Efficacy of Basmisanil in Adults With Severe Motor Impairment Following an Ischemic Stroke (clinicaltrials.gov) - Oct 11, 2016
P2, N=95, Not yet recruiting, Sponsor: Hoffmann-La Roche
- | basmisanil (RG1662) / Roche
Trial completion: A Study to Investigate the Effect of CYP3A Inhibition on the Pharmacokinetics of RG1662 in Healthy Subjects (clinicaltrials.gov) - Aug 26, 2016
P1, N=12, Completed, Sponsor: Hoffmann-La Roche
Not yet recruiting --> Recruiting Recruiting --> Completed
- basmisanil (RG1662) / Roche
Trial primary completion date: A Study of RO5186582 in Down Syndrome Among Children 6 to 11 Years of Age (clinicaltrials.gov) - Aug 8, 2016
P2, N=45, Active, not recruiting, Sponsor: Hoffmann-La Roche
Recruiting --> Completed Trial primary completion date: Jan 2017 --> Aug 2016
- |||| basmisanil (RG1662) / Roche
Trial completion: A Study of RG1662 in Adults and Adolescents With Down Syndrome (CLEMATIS) (clinicaltrials.gov) - Jul 5, 2016
P2, N=173, Completed, Sponsor: Hoffmann-La Roche
Trial primary completion date: Jan 2017 --> Aug 2016 Recruiting --> Completed
- | basmisanil (RG1662) / Roche
Enrollment closed, Trial primary completion date: A Study of RO5186582 in Down Syndrome Among Children 6 to 11 Years of Age (clinicaltrials.gov) - Jul 5, 2016
P2, N=44, Active, not recruiting, Sponsor: Hoffmann-La Roche
Recruiting --> Completed Recruiting --> Active, not recruiting | Trial primary completion date: Jun 2017 --> Jan 2017
- | basmisanil (RG1662) / Roche
Enrollment change: A Study of RO5186582 in Down Syndrome Among Children 6 to 11 Years of Age (clinicaltrials.gov) - Apr 6, 2016
P2, N=46, Recruiting, Sponsor: Hoffmann-La Roche
Recruiting --> Active, not recruiting | Trial primary completion date: Jun 2017 --> Jan 2017 N=36 --> 46
- |||| basmisanil (RG1662) / Roche
Enrollment open: A Study of RG1662 in Adults and Adolescents With Down Syndrome (CLEMATIS) (clinicaltrials.gov) - Feb 2, 2016
P2, N=180, Recruiting, Sponsor: Hoffmann-La Roche
N=36 --> 46 Active, not recruiting --> Recruiting
- ||| basmisanil (RG1662) / Roche
Enrollment closed: A Study of RG1662 in Adults and Adolescents With Down Syndrome (CLEMATIS) (clinicaltrials.gov) - Nov 5, 2015
P2, N=173, Active, not recruiting, Sponsor: Hoffmann-La Roche
Active, not recruiting --> Recruiting Recruiting --> Active, not recruiting
- basmisanil (RG1662) / Roche
Trial completion: Basmisanil Positron Emission Tomography Study in Japanese Volunteers (clinicaltrials.gov) - Nov 3, 2015
P1, N=6, Completed, Sponsor: Hoffmann-La Roche
Recruiting --> Active, not recruiting Recruiting --> Completed
- | basmisanil (RG1662) / Roche
Enrollment open: A Study of RO5186582 in Down Syndrome Among Children 6 to 11 Years of Age (clinicaltrials.gov) - Sep 2, 2015
P2, N=36, Recruiting, Sponsor: Hoffmann-La Roche
Recruiting --> Completed Not yet recruiting --> Recruiting
- basmisanil (RG1662) / Roche
New P1 trial: Basmisanil Positron Emission Tomography Study in Japanese Volunteers (clinicaltrials.gov) - Aug 27, 2015
P1, N=8, Recruiting, Sponsor: Hoffmann-La Roche
- | basmisanil (RG1662) / Roche
Trial completion: A Study of the Effect of RG1662 on Metformin in Healthy Volunteers (clinicaltrials.gov) - Jul 2, 2015
P1, N=17, Completed, Sponsor: Hoffmann-La Roche
Not yet recruiting --> Recruiting Active, not recruiting --> Completed
- | basmisanil (RG1662) / Roche
New P2 trial: A Study of RO5186582 in Down Syndrome Among Children 6 to 11 Years of Age (clinicaltrials.gov) - Jun 30, 2015
P2, N=36, Not yet recruiting, Sponsor: Hoffmann-La Roche
- | basmisanil (RG1662) / Roche
New P1 trial: A Study to Investigate the Effect of CYP3A Inhibition on the Pharmacokinetics of RG1662 in Healthy Subjects (clinicaltrials.gov) - Jun 12, 2015
P1, N=12, Recruiting, Sponsor: Hoffmann-La Roche