Comparative Bioavailability of Sublingual TNX-102, Oral and Intravenous Cyclobenzaprine in Healthy Adults

NCT ID: NCT01634412

Last Updated: 2014-09-26

Basic Information

• Recruitment Status: COMPLETED
• Clinical Phase: PHASE1
• Total Enrollment: 24 participants
• Study Classification: INTERVENTIONAL
• Study Start Date: 2012-06-30
• Study Completion Date: 2014-01-31

Brief Summary

Very low dose (VLD) cyclobenzaprine at bedtime has shown promise as a treatment for fibromyalgia, but the chemistry of cyclobenzaprine requires new formulation technology for bedtime use. The present trial is designed to assess the safety and tolerability of sublingual TNX-102 2.4 mg (a new formulation of cyclobenzaprine designed to result in increased dosage precision and decreased potential for morning grogginess) at pH 3.5 and 7.1 and to compare the bio-availability of sublingual TNX-102 2.4 mg at pH 3.5 and 7.1 and cyclobenzaprine (5 mg tablets, or 2.4 mg iv).

Conditions

Healthy Adults

Study Design

• Allocation Method: RANDOMIZED
• Intervention Model: PARALLEL
• Primary Study Purpose: TREATMENT
• Blinding Strategy: NONE

Study Groups

SL TNX-102 at pH 3.5

2.4 mg TNX-102 sublingual solution (2.4 mg/mL) in PBS at pH 3.5

Group Type: EXPERIMENTAL

SL TNX-102 2.4 mg at pH 3.5

Intervention Type: DRUG

1 dose of 2.4 mg TNX-102 sublingual solution (2.4 mg/mL) in PBS at pH 3.5, administered as 1 mL held under the tongue for 90 seconds without swallowing

SL TNX-102 at pH 7.1

2.4 mg TNX-102 sublingual solution (2.4 mg/mL) in PBS at pH 7.1

Group Type: EXPERIMENTAL

SL TNX-102 2.4 mg at pH 7.1

Intervention Type: DRUG

1 dose of 2.4 mg TNX-102 sublingual solution (2.4 mg/mL) in PBS at pH 7.1, administered as 1 mL held under the tongue for 90 seconds without swallowing

Cyclobenzaprine tablets

5 mg cyclobenzaprine tablet once

Group Type: ACTIVE_COMPARATOR

Cyclobenzaprine Tablet

Intervention Type: DRUG

1 x 5 mg cyclobenzaprine tablet, swallowed with 240 mL of room-temperature water

Cyclobenzaprine IV

2.4 mg cyclobenzaprine USP in PBS (0.6 mg/mL) at pH 7.4

Group Type: ACTIVE_COMPARATOR

Cyclobenzaprine IV

Intervention Type: DRUG

1 dose of 2.4 mg cyclobenzaprine USP in PBS (0.6 mg/mL) at pH 7.4, administered intravenously as a 4 mL bolus injection over 30 seconds

Interventions

SL TNX-102 2.4 mg at pH 3.5

1 dose of 2.4 mg TNX-102 sublingual solution (2.4 mg/mL) in PBS at pH 3.5, administered as 1 mL held under the tongue for 90 seconds without swallowing

Intervention Type: DRUG

SL TNX-102 2.4 mg at pH 7.1

1 dose of 2.4 mg TNX-102 sublingual solution (2.4 mg/mL) in PBS at pH 7.1, administered as 1 mL held under the tongue for 90 seconds without swallowing

Intervention Type: DRUG

Cyclobenzaprine Tablet

1 x 5 mg cyclobenzaprine tablet, swallowed with 240 mL of room-temperature water

Intervention Type: DRUG

Cyclobenzaprine IV

1 dose of 2.4 mg cyclobenzaprine USP in PBS (0.6 mg/mL) at pH 7.4, administered intravenously as a 4 mL bolus injection over 30 seconds

Intervention Type: DRUG

Eligibility Criteria

Inclusion Criteria

• Male or female
• Non-smoker
• 18-65 years old
• BMI > 18.5 and < 30.0
• With medically acceptable form of contraception (female only)
• With signed informed consent

Exclusion Criteria

• Any clinically significant abnormality including ECG abnormalities or vital sign abnormalities (systolic blood pressure < 90 or > 140 mmHg, diastolic blood pressure lower < 50 or > 90 mmHg, or heart rate < 50 or > 100 BPM)
• Any abnormal laboratory test (including positivity for Hep B, Hep C, HIV, and Hemoglobin < 128 g/L (males) or < 115 g/L (females) and hematocrit < 0.37 L/L (males) or < 0.32 L/L (females))
• History of alcohol or drug abuse or dependence within 1 year and/or positive drug, cotinine, or alcohol tests
• Use of any drug (within 30 days), supplement, or food (within 14 days) known to induce or inhibit hepatic drug metabolism prior to study medication
• Positive pregnancy test, breastfeeding or lactating
• Use of medication other than hormonal contraceptives or topical products, including OTC, natural health products, MAO inhibitors
• Participation in an investigational study within 30 days prior to dosing
• Donation of plasma (within 7 days), or donation or loss of blood of 50-499 mL (within30 days), or of > 499 mL (within 56 days) prior to dosing.

• Minimum Eligible Age: 18 Years
• Maximum Eligible Age: 65 Years
• Eligible Sex: ALL
• Accepts Healthy Volunteers: Yes

Sponsors

Tonix Pharmaceuticals, Inc.

INDUSTRY

Sponsor Role: lead

Responsible Party

Responsibility Role: SPONSOR

Principal Investigators

Seth M. Lederman, MD

Role: STUDY_CHAIR

Tonix Pharmaceuticals, Inc.

Jeffrey P. Kitrelle, MD

Role: STUDY_DIRECTOR

Tonix Pharmaceuticals, Inc.

Denis Audet, MD

Role: PRINCIPAL_INVESTIGATOR

PharmaNet

Locations

PharmaNet, Inc.

Québec, Quebec, Canada

Countries

Canada

Other Identifiers

TNX-CY-F102

Identifier Type: -

Identifier Source: org_study_id