Pharmacokinetic Study of Fentanyl 400 µg Sublingual Spray, Actiq® 400 µg Transmucosally, and Fentanyl Citrate Injection 100 µg Intravenously (iv)

INSYS Therapeutics

Status and phase: Completed; Phase 1

Conditions: Pain

Treatments: Drug: Naltrexone 50 mg; Drug: Fentanyl citrate injection 100 µg intravenously; Drug: Actiq® 400 µg transmucosally; Drug: Fentanyl 400 µg sublingual spray

Study type: Interventional

Funder types: Industry

Identifiers

NCT01780233

INS-06-003

Details and patient eligibility

About

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.

Full 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.

Enrollment: 40 patients

Sex: All

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

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.

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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40 participants in 3 patient groups

Fentanyl 400 µg sublingual spray + naltrexone 50 mg

Experimental group

Description:

Patients received a single administration of 400 µg of fentanyl spray sublingually + naltrexone hydrochloride 50 mg orally.

Treatment:

Drug: Naltrexone 50 mg

Drug: Fentanyl 400 µg sublingual spray

Actiq® 400 µg transmucosally + naltrexone 50 mg

Active Comparator group

Description:

Patients received a single administration of 400 µg of Actiq® transmucosally + naltrexone hydrochloride 50 mg orally.

Treatment:

Drug: Actiq® 400 µg transmucosally

Drug: Naltrexone 50 mg

Fentanyl citrate injection 100 µg iv + naltrexone 50 mg

Active Comparator group

Description:

Patients received a single administration of 100 µg of fentanyl citrate intravenously + naltrexone hydrochloride 50 mg orally.

Treatment:

Drug: Naltrexone 50 mg

Drug: Fentanyl citrate injection 100 µg intravenously