This project seeks to develop a novel disease-modifying compound for Alzheimer's disease (AD).
The primary objective of this study is to evaluate the safety, tolerability, and pharmacokinetics of BMS-984923 in healthy participants. A secondary objective of this study is to conduct a receptor occupancy sub-study aimed at determining drug receptor occupancy at each dose using \[18F\]FPEB Positron Emission Tomography.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
36
Day 1: Admission, administration of study drug, and 2 night in-patient stay; Day 3: Discharge following the completion of all scheduled procedures.
Yale University
New Haven, Connecticut, United States
Count of Treatment Emergent Adverse Events (TEAEs)
A count of participants that experience any adverse events found to be associated with treatment. All adverse events are summarized in the adverse events section.
Time frame: Up to 7 days after last dose
Count of Lab Abnormalities
Count of participants with clinical lab abnormalities.
Time frame: Up to 7 days after last dose
Count of Clinically Significant Changes in Safety Assessments
A count of participants that experienced any clinically significant changes in: Vital Signs, Physical Exam, Electrocardiogram, Neuropsychiatric Inventory - Q, Geriatric Depression Scale, Glasgow Coma Scale, Montreal Cognitive Assessment
Time frame: Up to 7 days after last dose
Maximum Plasma Concentration (Cmax)
Maximum plasma concentration as determined by pharmacokinetic modeling
Time frame: Up to 7 days after last dose
Time of Cmax (Tmax)
Time of Cmax as determined by pharmacokinetic modeling
Time frame: Up to 7 days after last dose
Area Under the Curve From 0 to 24h (AUC 24h)
Plasma drug exposure as determined by pharmacokinetic modeling, AUC is represented as ng∙h/mL.
Time frame: Up to 7 days after last dose
Receptor Occupancy
Metabotropic glutamate receptor subtype 5 (mGluR5) occupancy using \[18F\]FPEB Positron Emission Tomography calculated using the percentage of total mGluR5 availability and plasma concentrations of study drug were used to model the relationship between plasma concentration (CP) and receptor occupancy with the conventional sigmoidal maximum receptor occupancy (r\_max) model where IC50 is the CP required to produce 50% of the r\_max. A nonlinear least squares analysis was used to estimate the parameters from all scans. The data supported a model with 1 parameter (IC50, r\_max = 100%). IC80 is the CP required to produce 80% of the r\_max. The outcomes of relevance are the IC50 and IC80 calculated for the model.
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Time frame: Up to 24 hours after last dose