Clinical trial NCT01780233: Pharmacokinetic Study of Fentanyl 400 µg Sublingual Spray, Actiq® 400 µg Transmucosally, and Fentanyl Citrate Injection 100 µg Intravenously (iv)
Official title: A Single-dose Crossover Study of Fentanyl Sublingual Spray 400 Mcg Versus Actiq® 400 Mcg Versus Fentanyl Citrate Injection (iv) 100 Mcg Under Fasted Conditions
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Pain
Lead sponsor: INSYS Therapeutics Inc
Sponsor class: INDUSTRY
First posted: 2013-01-31
Enrollment: 40
Sex: ALL
Minimum age (years): 18
Maximum age (years): 55
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: CROSSOVER
Primary purpose: TREATMENT

Brief summary: The objective of this study was to compare the rate of absorption and bioavailability of fentanyl 400 µg sublingual spray, Actiq® 400 µg transmucosally, and fentanyl citrate injection 100 µg intravenously.

Detailed description: This was a Phase I, single-dose, open-label, randomized, 3-period, 3-treatment cross over study in which 21 healthy subjects received single doses of fentanyl 400 µg sublingual spray, Actiq® 400 µg transmucosally, and fentanyl citrate injection 100 µg intravenously following a 10-hour overnight fast. There was a 7 day washout period between treatments.

Eligibility criteria: Inclusion Criteria:

* Male or non-pregnant, non-breast-feeding female between the ages of 18-55 inclusive.
* Body Mass Index (BMI) between 18-30 kg/m\^2, inclusive, and body weight of at least 60 kg (132 lbs).
* Subject was healthy according to the medical history, laboratory results, and physical examination.

Exclusion Criteria:

* Had a presence or history of clinically significant cardiovascular, pulmonary, hepatic, renal, hematologic, gastrointestinal, endocrine, immunologic, dermatologic, neurologic, oncologic, or psychiatric disease or any other condition which, in the opinion of the Investigator would jeopardize the safety of the subject or the validity of the study results.
* Had a clinically significant abnormal finding on the physical exam, medical history, electrocardiogram (ECG), or clinical laboratory results at screening.
* Had a significant history of hypersensitivity to opioid analgesics, fentanyl or any related products, naltrexone, or severe hypersensitivity reactions (like angioedema) to any drugs.
* Had a significantly abnormal diet during the 4 weeks preceding the first dose of study medication.
* Had donated blood or plasma within 30 days prior to the first dose of study medication or during the course of this study.
* Had participated in another clinical trial within 30 days prior to the first dose of study medication or during the course of this study.
* Had used any over-the-counter (OTC) medication, including nutritional supplements, within 7 days prior to the first dose of study medication or during the course of this study.
* Had used any prescription medication, except hormonal contraceptive or hormonal replacement therapy, within 14 days prior to the first dose of study medication or during the course of this study.
* Had used enzyme altering drugs such as barbiturates, corticosteroids, phenothiazines, cimetidine, carbamazepine, etc, within 30 days prior to the first dose of study medication or during the course of this study.
* Had used opioid analgesics within the last 30 days.

Primary outcomes:
measure: Time to reach the maximum drug concentration (Tmax) in plasma
timeFrame: Up to 60 minutes pre-dose to 36 hours post-dose
Secondary outcomes:
measure: Maximum drug concentration (Cmax) in plasma
timeFrame: Up to 60 minutes pre-dose to 36 hours post-dose
measure: Area under the plasma concentration-time curve from time-0 to the time of the last quantifiable concentration (AUClast)
timeFrame: Up to 60 minutes pre-dose to 36 hours post-dose
measure: Area under the plasma concentration-time curve from time-0 extrapolated to infinity (AUCinf)
timeFrame: Up to 60 minutes pre-dose to 36 hours post-dose
measure: Percentage of AUCinf based on extrapolation (AUCextrap)
timeFrame: Up to 60 minutes pre-dose to 36 hours post-dose
measure: Observed elimination rate constant (λz)
timeFrame: Up to 60 minutes pre-dose to 36 hours post-dose
measure: Observed terminal elimination half-life (T1/2)
timeFrame: Up to 60 minutes pre-dose to 36 hours post-dose
measure: Time of the last measurable concentration of drug (Tlast) in plasma
timeFrame: Up to 60 minutes pre-dose to 36 hours post-dose
measure: Last quantifiable drug concentration (Clast) in plasma
timeFrame: Up to 60 minutes pre-dose to 36 hours post-dose
Other outcomes:
Locations:
city: Austin
country: United States
facility: CEDRA Clinical Research, LLC
state: Texas
Study officials:
affiliation: INSYS Therapeutics Inc
name: Neha Parikh
role: STUDY_DIRECTOR
affiliation: CEDRA Clinical Research
name: Frederick A. Bieberdorf, MD
role: PRINCIPAL_INVESTIGATOR
References:
citation: Parikh N, Goskonda V, Chavan A, Dillaha L. Single-dose pharmacokinetics of fentanyl sublingual spray and oral transmucosal fentanyl citrate in healthy volunteers: a randomized crossover study. Clin Ther. 2013 Mar;35(3):236-43. doi: 10.1016/j.clinthera.2013.02.017.