Exploratory Bioavailability of Fentanyl Sublingual Spray Under Fasting Conditions

Single-Dose, Open-Label, Two-Period, Two-Treatment, Two-Sequence Crossover Exploratory Bioavailability Study of Subsys® (Fentanyl Sublingual Spray), 400 mcg, and Fentanyl Citrate Injection 2 mL x 0.05 mg/mL (Total Dose 100 mcg) Under Fasted Conditions

The objective of this study is to compare the rate of absorption and bioavailability of fentanyl sublingual spray 400 mcg to fentanyl citrate 100 mcg by intramuscular injection.

Study Overview

• Status: Completed
• Conditions: Bioavailability
• Intervention / Treatment: Drug: Fentanyl Sublingual Spray (FSS); Drug: Fentanyl Citrate Injection (FCI); Drug: Naltrexone

• Study Type: Interventional
• Enrollment (Actual): 12
• Phase: Not Applicable

Contacts and Locations

Study Locations

• United States
  • Texas
    • San Antonio, Texas, United States, 78217
      • Worldwide Clinical Trials Early Phase Services, LLC

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 16 years to 53 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Meets protocol-specified criteria for qualification and contraception
• Good access to veins on both sides
• Willing and able to remain confined in the study unit for the entire duration of each treatment period and comply with restrictions related food, drink and medications
• Voluntarily consents to participate and provides written informed consent prior to any protocol-specific procedures

Exclusion Criteria:

• Intolerance to venipuncture or injections
• Presence or history of oral disease, irritation or piercings
• Allergy or adverse response to fentanyl, naltrexone, or related drugs
• Tattoos, scarring, or other skin abnormality at planned injection sites
• History or current use of over-the-counter medications, dietary supplements, or drugs (including nicotine and alcohol) outside protocol-specified parameters
• Signs, symptoms or history of any condition that, per protocol or in the opinion of the investigator, might compromise: 1) the safety or well-being of the participant or study staff; 2) the safety or well-being of the participant's offspring (such as through pregnancy or breast-feeding); 3) the analysis of results

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: FSS first, then FCI; At each of two treatment visits participants fast for 10 hours before dosing, and receive naltrexone before and after dosing. Participants in this group receive a single dose of fentanyl sublingual spray (FSS) at the first visit. After a washout period of at least seven days, they receive a single intramuscular fentanyl citrate injection (FCI) at the second treatment visit.	Drug: Fentanyl Sublingual Spray (FSS); A single dose of fentanyl, 400 mcg per sublingual spray; Other Names: Subsys®; Drug: Fentanyl Citrate Injection (FCI); A single dose of fentanyl citrate, 100 mcg per intramuscular injection; Drug: Naltrexone; Naltrexone is provided as a 50 mg tablet before and after product dosing to minimize unacceptable adverse effects of fentanyl.
Experimental: FCI first, then FSS; At each of two treatment visits participants fast for 10 hours before dosing, and receive naltrexone before and after dosing. Participants in this group receive a single intramuscular fentanyl citrate injection (FCI) at the first visit. After a washout period of at least seven days, they receive a single dose of fentanyl sublingual spray (FSS) at the second treatment visit.	Drug: Fentanyl Sublingual Spray (FSS); A single dose of fentanyl, 400 mcg per sublingual spray; Other Names: Subsys®; Drug: Fentanyl Citrate Injection (FCI); A single dose of fentanyl citrate, 100 mcg per intramuscular injection; Drug: Naltrexone; Naltrexone is provided as a 50 mg tablet before and after product dosing to minimize unacceptable adverse effects of fentanyl.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Maximum concentration (Cmax) by mode of administration	within 36 hours after dosing

Secondary Outcome Measures

Outcome Measure	Time Frame
Area under the concentration-time curve [AUC(last)] by mode of administration	prior to the intial dose, at 5, 10, 20, 30, and 40 minutes postdose, and at 1.0, 1.25, 1.5, 2.0, 4.0, 6.0, 8.0, 10.0, 12.0, 16.0, 24.0, and 36 hours post-dose
Area under the curve extrapolated to infinity [AUC(inf)] by mode of administration	prior to the intial dose, at 5, 10, 20, 30, and 40 minutes postdose, and at 1.0, 1.25, 1.5, 2.0, 4.0, 6.0, 8.0, 10.0, 12.0, 16.0, 24.0, and 36 hours post-dose

Collaborators and Investigators

• Sponsor: INSYS Therapeutics Inc
• Investigators: Principal Investigator: George J Atiee, MD, Worldwide Clinical Trials Early Phase Services, LLC

Study record dates

Study Major Dates

• Study Start: January 1, 2014
• Primary Completion (Actual): January 1, 2014
• Study Completion (Actual): January 1, 2014

Study Registration Dates

• First Submitted: May 12, 2014
• First Submitted That Met QC Criteria: May 12, 2014
• First Posted (Estimate): May 14, 2014

Study Record Updates

• Last Update Posted (Estimate): December 12, 2014
• Last Update Submitted That Met QC Criteria: December 11, 2014
• Last Verified: December 1, 2014

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Central Nervous System Depressants; Peripheral Nervous System Agents; Analgesics; Sensory System Agents; Anesthetics, Intravenous; Anesthetics, General; Anesthetics; Analgesics, Opioid; Narcotics; Adjuvants, Anesthesia; Narcotic Antagonists; Alcohol Deterrents; Fentanyl; Naltrexone
• Other Study ID Numbers: INS-13-019