This is a phase 1, first in human, randomized, double-blind, placebo-controlled, single ascending dose (SAD) study in healthy adult male and female subjects 18 to 55 years of age, inclusive.
Subjects will provide written informed consent and undergo a screening visit within 28 days of receiving study drug. Eligible subjects must have a negative urine drug screen (UDS) and a negative naloxone challenge test at Screening and at the check-in visit (Day -1). Upon completion of screening, eligible subjects will be admitted to the clinical research unit (CRU) on Day -1 and remain confined in the CRU through completion of all scheduled procedures on Day 4 to allow for safety labs, pharmacokinetic (PK) blood draws, ECGs, injection site assessments, and adverse event monitoring. Study medication dosing will occur in the morning on Day 1 and serial blood samples for plasma concentration determination for PK analysis will be taken during this time at pre-dose and 0.25, 0.50, 1, 1.5, 2, 4, 8, 10, 12, 24 (day 2), 48 (day 3), and 72 (day 4) hours post dose. Additional blood PK samples will be taken at follow-up visits. A Safety Review Committee (SRC) will review blinded, preliminary data from Cohort 1 to make recommendations regarding escalation to Cohorts 2 and 3.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
24
Frontage Clinical Research Center
Secaucus, New Jersey, United States
Incidence of Treatment Emergent Adverse Events (TEAEs)
Number of Participants with TEAEs
Time frame: From predose through end of study visit, assessed up to study completion, an average of 15 months
Severity of TEAEs
Severity of TEAEs
Time frame: From predose through end of study visit, assessed up to study completion, an average of 15 months
Serious Adverse Events (SAEs)
Number of Participants with SAEs
Time frame: From predose through end of study visit, assessed up to study completion, an average of 15 months
Discontinuation Due to Adverse Events (AEs)
Number of Participants who discontinue the study due to AEs
Time frame: From predose through end of study visit, assessed up to study completion, an average of 15 months
Pharmacokinetics: AUC0-last
Area under the plasma concentration-time curve (AUC) from time 0 to last measurable plasma concentration
Time frame: From predose through end of study visit, assessed up to study completion, an average of 15 months
Pharmacokinetics: AUC0-infinity
Area under the plasma concentration-time curve from time 0 to infinity, calculated as AUC0-last + AUCt-inf
Time frame: From predose through end of study visit, assessed up to study completion, an average of 15 months
Pharmacokinetics: AUC0-inf %extrapolation
Percentage of AUC0-inf due to extrapolation from Tlast to infinity
Time frame: From predose through end of study visit, assessed up to study completion, an average of 15 months
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Pharmacokinetics: Cmax
Maximum observed plasma concentration (Cmax)
Time frame: From predose through end of study visit, assessed up to study completion, an average of 15 months
Pharmacokinetics: Tmax
Time of Cmax
Time frame: From predose through end of study visit, assessed up to study completion, an average of 15 months
Pharmacokinetics: t1/2
Terminal half-life (t1/2)
Time frame: From predose through end of study visit, assessed up to study completion, an average of 15 months
Pharmacokinetics: Kel (λz)
Apparent terminal rate-constant, calculated using linear regression on the terminal portion of the Log-concentration versus time curve
Time frame: From predose through end of study visit, assessed up to study completion, an average of 15 months
Pharmacokinetics: Vz/F
Apparent volume of distribution (Vz/F)
Time frame: From predose through end of study visit, assessed up to study completion, an average of 15 months
Pharmacokinetics: CL/F
Apparent clearance (CL/F)
Time frame: From predose through end of study visit, assessed up to study completion, an average of 15 months