The purpose of this study is to assess the safety and tolerability of a novel positron emission tomography (PET) tracer \[11C\]BMT-136088 in healthy adult subjects for measurement of availability of Lysophosphatidic Acid (LPA1) receptors in the human lung and to use this tracer to assess LPA1 receptor occupancy using \[11C\]BMT-136088 in the human lung following oral administration of Bristol Myers Squibb (BMS)-986020.
End point Classification: Pharmacokinetics/Pharmacodynamics
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
20
Yale Pet Center
New Haven, Connecticut, United States
Overall safety and tolerability of novel tracer [11C]BMT-136088
The following safety endpoints will be considered, the incidence of adverse events (AEs), serious AEs, AEs leading to discontinuation from the study, and death as well as marked abnormalities in clinical laboratory tests, vital sign measurements, electrocardiograms (ECGs), and physical examinations occurring from screening up to study discharge.
Time frame: Approximately up to 90 days
Lung LPA1 percentage receptor occupancy of BMS-986020
Assessed by \[11C\]BMT-136088 tracer lung volume of distribution (VT) before and after single oral dose of BMS-986020.
Time frame: Up to 2 days post BMS-986020 administration
Exposure-response relationship between lung LPA1 percentage receptor occupancy and BMS-986020 plasma concentration.
Time frame: Up to 48 hr postdose (Approximately up to Day 3)
Maximum observed concentration (Cmax) of BMS-986020
Time frame: 13 timepoints up to Day 3
Time of maximum observed concentration (Tmax) of BMS-986020
Time frame: 13 timepoints up to Day 3
Area under the concentration-time curve from time zero to the time of the last quantifiable concentration [AUC(0-T)] of BMS-986020
Time frame: 13 timepoints up to Day 3
Area under the concentration-time curve from time zero extrapolated to infinite time [AUC(INF)] of BMS-986020
Time frame: 13 timepoints up to Day 3
Half life (T-HALF) of BMS-986020
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Time frame: 13 timepoints up to Day 3
Safety of single oral dose of BMS-986020 where [11C]BMT-136088 is administered to healthy subjects
Safety based on incidence of AEs, serious AEs, AEs leading to discontinuation, and death as well as marked abnormalities in clinical laboratory tests, vital sign measurements, ECGs, and physical examinations
Time frame: Approximately up to 90 days