Part 1 of the study evaluates the safety and tolerability as well as pharmacokinetic properties of a single oral dose of BOS172767 enantiomer E1 and BOS172767 enantiomer E2 following administration to healthy participants. Part 2 of the study was to be conducted to assess the safety and tolerability as well as pharmacokinetic properties of one selected enantiomer (BOS172767-Ex) following multiple ascending doses over 14 days of dosing in healthy participants.
The study design of Part 1 was a double-blind, placebo-controlled, randomized, single-dose, two-way crossover, followed by two sequential ascending dose periods in 12 healthy participants. Part 2 was designed to be a double-blind, placebo-controlled, randomized multiple ascending dose (MAD) study in 36 healthy participants (12 per study cohort). Part 2 was to progress following completion of Part 1, but was not conducted.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
TRIPLE
Enrollment
12
Oral tablets
Oral tablets
Quotient Sciences
Nottingham, United Kingdom
Part 1: Relative bioavailability of E1 versus E2 (Frel; exposure) of a single oral dose of BOS172767 enantiomer 1 (E1) and enantiomer 2 (E2) following administration to healthy participants based on Cmax, AUC(0-last), and AUC (0-inf)
Cmax is defined as the maximum observed concentration. AUC(0-last) is defined as the area under the curve from 0 time to the last measurable concentration. AUC (0-inf) is defined as the area under the curve from 0 time extrapolated to infinity.
Time frame: 24 hours post-dose for each of the four 6-day Periods
Part 1: Number of participants with any treatment-emergent adverse event
Time frame: up to Day 6 of each Period; up to a 10-day Follow-up Period after last dose (up to Study Day 59)
Part 1: Number of participants with abnormal, clinically significant physical examination findings
Time frame: up to Day 6 of each Period; up to a 10-day Follow-up Period after last dose (up to Study Day 59)
Part 1: Number of participants with abnormal, clinically significant safety laboratory test findings
Time frame: up to Day 6 of each Period; up to a 10-day Follow-up Period after last dose (up to Study Day 59)
Part 1: Number of participants with abnormal, clinically significant vital sign values
Time frame: up to Day 6 of each Period; up to a 10-day Follow-up Period after last dose (up to Study Day 59)
Part 1: Number of participants with abnormal, clinically significant electrocardiogram findings
Time frame: up to Day 6 of each Period; up to a 10-day Follow-up Period after last dose (up to Study Day 59)
Part 1: Plasma concentration of BOS172767 enantiomers 1 and 2
Time frame: 24 hours post-dose for each of the four 6-day Periods
Part 1: Slope estimates (β) from the power model analysis on Cmax, AUC(0-last), and AUC(0-inf), as a measure of dose proportionality
Time frame: 24 hours post-dose for each of the four 6-day Periods
Part 2: Plasma concentration of BOS172767-Ex (enantiomer E1 or E2)
Time frame: 24 hours post-dose
Part 2: Number of participants with any treatment-emergent adverse event
Time frame: up to Day 24 of Part 2 (up to approximately 18 study weeks)
Part 2: Number of participants with abnormal, clinically significant physical examination findings
Time frame: up to Day 24 of Part 2 (up to approximately 18 study weeks)
Part 2: Number of participants with abnormal, clinically significant safety laboratory test findings
Time frame: up to Day 24 of Part 2 (up to approximately 18 study weeks)
Part 2: Number of participants with abnormal, clinically significant vital sign values
Time frame: up to Day 24 of Part 2 (up to approximately 18 study weeks)
Part 2: Number of participants with abnormal, clinically significant electrocardiogram findings
Time frame: up to Day 24 of Part 2 (up to approximately 18 study weeks)
Part 2: Slope estimates (β) from the power model analysis on Cmax, AUC(0-last), and AUC(0-inf), as a measure of dose proportionality
Time frame: 24 hours post-dose
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