This is a single-center study incorporating 2 parts: A Multiple Ascending Dose Study (Part A) and a comparative Bioavailability/Bioequivalence and Food Effect study (Part B). Both parts of the study will be conducted in healthy adult subjects.
This study is intended to evaluate the pharmacokinetics of OxyContin (oxycodone ER) and PF614, as well as PF614 fragments, following administration of multiple ascending doses of PF614, and to compare to steady-state pharmacokinetics to those of OxyContin. (Part A) In addition, oral bioavailability of oxycodone derived from single doses of PF614 of the to-be-marketed capsule formulation will be compared to that of the reference drug, OxyContin, in the fasted and fed condition. A pivotal food effect assessment will be incorporated into the study to determine the impact of a high fat meal on the bioavailability of oxycodone, following oral single-dose administration of PF614 (Part B).
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
84
PRA Health Sciences-Early Development Services
Salt Lake City, Utah, United States
Incidence of Treatment-Emergent Adverse Events [Safety and Tolerability]
Adverse Events, Significant Adverse Events, Adverse Events leading to discontinuation
Time frame: 30 days
Pharmacokinetics AUC [Area Under the Curve]
Area under the concentration-time curve from the time of dosing to the start of the next dosing interval using PF614 concentrations and oxycodone concentrations in plasma.
Time frame: Full PK sampling time points will be 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Cmax [Maximum Plasma Concentration]
Maximum (peak) plasma concentration first dose
Time frame: PK sampling time points will be 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Tlag [Time to first measurable plasma concentration]
Time prior to the time corresponding to the first measurable (non-zero) concentration
Time frame: PK sampling time points will be 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Tmax [Time to maximum plasma concentration]
Time to maximum plasma concentration on Day 1 (first dose)
Time frame: PK sampling time points 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics AUC, Steady State
Steady-state (Day 5) area under the concentration-time curve from the time of dosing extrapolated to time infinity
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics CL/F [Clearance]
Apparent total systemic clearance
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Pharmacokinetics Cmax, Steady State
Maximum (peak) plasma concentration at steady-state on Day 5
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Tmax, Steady State
Time to maximum plasma concentration on Day 5
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics t1/2 [Half-life]
Terminal elimination half-life
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Vz/F [Volume of Distribution]
Apparent volume of distribution during the terminal-elimination phase
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics elimination rate
Terminal elimination rate/constant
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Ctrough [Minimum Plasma Concentration before next dose]
Concentrations prior to dosing
Time frame: Prior to dosing on Days 2, 3, and 4
Pharmacokinetics Part B AUC
Area under the concentration-time curve from the time of dosing extrapolated to time infinity in fed vs fasted state
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Part B AUC 0-t
Area under the concentration-time curve from the time of dosing to the last measurable concentration in fed vs fasted state
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Part B Cmax
Maximum (peak) plasma concentration in fed vs fasted state
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Bioavailability and Bioequivalence
Bioavailability and Bioequivalence of single oral doses of PF614 prodrug and oxycodone derived from from PF614 vs. oxycodone derived from OxyContin in healthy adult subjects (Part B)
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Part B CL/F
Apparent total systemic clearance
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Part B pAUC
Partial area under the concentration-time curve from the time of dosing to 12 hours post dose
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Part B Tlag
Time prior to the time corresponding to the first measurable dose (non-zero) concentration
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Part B Tmax
Time to maximum plasma concentration on Day 1 (first dose)
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Part B t1/2
Terminal elimination half life
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Part B Vz/F
Apparent volume of distribution during the terminal elimination phase
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Pharmacokinetics Part B Terminal elimination rate
Terminal elimination rate constant
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Plasma Concentration of inactive metabolic fragment #1
Evaluate plasma concentrations of PFR06082 (Part A only)
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours
Plasma Concentration of inactive metabolic fragment #2
Evaluate plasma concentrations of PFR06110 (Part A only)
Time frame: PK sampling time points 0, 30 minutes; 1, 2, 3, 4, 6, 8, and 12 hours