Exploratory Bioavailability of Fentanyl Sublingual Spray Under Fasting Conditions

• ClinicalTrials.gov Identifier: NCT02138396
• Recruitment Status: Completed
• First Posted: May 14, 2014
• Last Update Posted: December 12, 2014
• Sponsor: INSYS Therapeutics Inc
• Information provided by (Responsible Party): INSYS Therapeutics Inc

Study Description

Brief Summary:

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.

Condition or disease	Intervention/treatment	Phase
Bioavailability	Drug: Fentanyl Sublingual Spray (FSS); Drug: Fentanyl Citrate Injection (FCI); Drug: Naltrexone	Not Applicable

Study Design

• Study Type: Interventional (Clinical Trial)
• Actual Enrollment: 12 participants
• Allocation: Randomized
• Intervention Model: Crossover Assignment
• Masking: None (Open Label)
• Primary Purpose: Basic Science
• Official Title: 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
• Study Start Date: January 2014
• Actual Primary Completion Date: January 2014
• Actual Study Completion Date: January 2014

Arms and Interventions

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 Name: 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 Name: 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.

Outcome Measures

Primary Outcome Measures :

1. Maximum concentration (Cmax) by mode of administration [ Time Frame: within 36 hours after dosing ]

Secondary Outcome Measures :

1. Area under the concentration-time curve [AUC(last)] by mode of administration [ Time Frame: 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 ]
2. Area under the curve extrapolated to infinity [AUC(inf)] by mode of administration [ Time Frame: 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 ]

Eligibility Criteria

• Ages Eligible for Study: 18 Years to 55 Years (Adult)
• Sexes Eligible for Study: All
• Accepts Healthy Volunteers: Yes

Criteria

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

Contacts and Locations

Locations

United States, Texas

Worldwide Clinical Trials Early Phase Services, LLC

San Antonio, Texas, United States, 78217

Sponsors and Collaborators

INSYS Therapeutics Inc

Investigators

• Principal Investigator: George J Atiee, MD; Worldwide Clinical Trials Early Phase Services, LLC

More Information

• Responsible Party: INSYS Therapeutics Inc
• ClinicalTrials.gov Identifier: NCT02138396 History of Changes
• Other Study ID Numbers: INS-13-019
• First Posted: May 14, 2014
• Last Update Posted: December 12, 2014
• Last Verified: December 2014

Additional relevant MeSH terms:

Fentanyl; Naltrexone; Citric Acid; Sodium Citrate; Analgesics, Opioid; Narcotics; Central Nervous System Depressants; Physiological Effects of Drugs; Analgesics; Sensory System Agents; Peripheral Nervous System Agents; Adjuvants, Anesthesia; Anesthetics, Intravenous; Anesthetics, General; Anesthetics; Anticoagulants; Calcium Chelating Agents; Chelating Agents; Sequestering Agents; Molecular Mechanisms of Pharmacological Action; Alcohol Deterrents; Narcotic Antagonists