Bibliographic
Year of Publication:
2007
Contact PI Name:
Josien Hubert
Primary Reference (PubMED ID):
Funding Source:
Not Reported
Study Goal and Principal Findings:
The design and development of a new class of small 2,6-disubstituted piperidine N-arylsulfonamide γ-secretase inhibitors is reported. Lowering molecular weight including the use of conformational constraint led to compounds with less CYP 3A4 liability compared to early leads. Compounds active orally in lowering Aβ levels in Tg CRND8 mice were identified as potential treatments for Alzheimer’s disease.
Therapeutic Agent
Therapeutic Information:
Therapy Type:
Small Molecule
Therapeutic Target:
gamma Secretase
Animal Model
Model Information:
Experimental Design
Is the following information reported in the study?:
Power/Sample Size Calculation
Randomized into Groups
Blinded for Treatment
Blinded for Outcome Measures
Pharmacokinetic Measures
Pharmacodynamic Measures
Toxicology Measures
ADME Measures
Biomarkers
Dose
Formulation
Route of Delivery
Duration of Treatment
Frequency of Administration
Age of Animal at the Beginning of Treatment
Age of Animal at the End of Treatment
Sex as a Biological Variable
Study Balanced for Sex as a Biological Variable
Number of Premature Deaths
Number of Excluded Animals
Statistical Plan
Genetic Background
Inclusion/Exclusion Criteria Included
Conflict of Interest
Outcomes
Outcome Measured
Outcome Parameters
ADME
CYP450 Inhibition
Pharmacokinetics
Area Under the Curve (AUC)
Pharmacodynamics
Target Engagement (Reduction beta Amyloid Peptide 40-Plasma)
Biomarker
Plasma-beta Amyloid Peptides
Spectroscopy
Nuclear Magnetic Resonance Spectroscopy