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Comparative Bioavailability of TNX-102 and Cyclobenzaprine and Effect of Food on the Pharmacokinetics of TNX-102 in Healthy Adults

This study is ongoing, but not recruiting participants.
Sponsor:
Information provided by (Responsible Party):
Tonix Pharmaceuticals, Inc.
ClinicalTrials.gov Identifier:
NCT01490788
First received: December 7, 2011
Last updated: June 6, 2013
Last verified: June 2013
History of Changes
  Purpose

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 TNX-102 2.4 mg (a new formulation of cyclobenzaprine designed to result in increased dosage precision and decreased potential for morning grogginess) and to compare the bio-availability of TNX-102 2.4 mg and cyclobenzaprine 5 mg tablets under fasting or fed conditions.


Condition Intervention Phase
Healthy
 Drug: TNX-102 2.4 mg, Fasting conditions
Drug: TNX-102 2.4 mg, Fed conditions
Drug: Cyclobenzaprine 5 mg, Fasting conditions
 Phase 1

Study Type: Interventional
Study Design: Allocation: Randomized
Endpoint Classification: Bio-availability Study
Intervention Model: Crossover Assignment
Masking: Open Label
Primary Purpose: Treatment
Official Title: A Single-Dose, Open-Label, Randomized, Three-Way Crossover Study of the Comparative Bioavailability of TNX-102 2.4 mg and Cyclobenzaprine 5 mg Tablets and of the Effect of Food on the Pharmacokinetics of TNX-102 in Healthy Adults.

Resource links provided by NLM:

U.S. FDA Resources

Further study details as provided by Tonix Pharmaceuticals, Inc.:

Primary Outcome Measures:
  • Measured levels of cyclobenzaprine and norcyclobenzaprine in plasma and urine [ Time Frame: 23 time points per period for blood assessment ; 4 pooled analyses in urine, safety monitoring throughout the shoe study period.. ] [ Designated as safety issue: No ]
    Blood samples will be taken per period: within 30 minutes pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 3.33, 3.67, 4,4.33, 4.67, 5, 5.5, 6, 8, 12, 16, 24, 36, 48, 72, and 96 hours post-dose. A single urine sample will be collected within 30 minutes pre-dose (one sample), and urine will be pooled from 0-24, 24-48, 48-72, and 72-96 hours post-dose.

  • Safety and tolerability of TNX-102 2.4 mg [ Time Frame: Continuously until the end (day 5) of each study period + 8-10 days after end of last period (total duration: about 1 month) ] [ Designated as safety issue: Yes ]
    Every adverse events occurring during the study period will be reported.


Enrollment: 30
Study Start Date: December 2011
Estimated Study Completion Date: March 2014
Estimated Primary Completion Date: September 2013 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: TNX-102 FAST
2.4 mg gelcap once
 Drug: TNX-102 2.4 mg, Fasting conditions
TNX-102 2.4 mg - 1 gelcap once under fasting conditions.
Experimental: TNX-102 FED
2.4 mg gelcap once
 Drug: TNX-102 2.4 mg, Fed conditions
TNX-102 2.4 mg, 1 gelcap once given under fed conditions.
Active Comparator: cyclobenzaprine FAST
generic cyclobenzaprine 5 mg tablet once or FLEXERIL 5 mg tablet once
 Drug: Cyclobenzaprine 5 mg, Fasting conditions
Cyclobenzaprine 5 mg, 1 tablet once under fasting conditions

Detailed Description:

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. Employing a proprietary mixture of approved lipids with cyclobenzaprine, TNX-102, is designed to provide predictable absorption of cyclobenzaprine and to result in increased dosage precision and decreased potential for morning grogginess.

As a first step in the development of TNX-102 in the treatment of fibromyalgia, the present single-center, randomized, open-label, single-dose, three-way-crossover trial is designed to assess the safety and tolerability of TNX-102 2.4 mg (a dose based on the results of a previous Phase 2a, proof-of-concept study - VPI-CY-0001.1) and to compare the rate and extent of absorption of TNX-102 2.4 mg and cyclobenzaprine 5 mg tablets under fasting or fed conditions.

  Eligibility

Ages Eligible for Study:   18 Years to 55 Years
Genders Eligible for Study:   Both
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria: Healthy adults

  • Male or female
  • Non-smoker
  • 18-55 years old
  • BMI > 18.5 and < 30.0
  • With medically acceptable form of contraception (female only).

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.
  Contacts and Locations
Please refer to this study by its ClinicalTrials.gov identifier: NCT01490788

Locations
Canada, Quebec
PharmaNet, Inc.
Québec City, Quebec, Canada, G1P 0A2
Sponsors and Collaborators
Tonix Pharmaceuticals, Inc.
Investigators
Principal Investigator: Denis Audet, MD PharmaNet
Study Chair: Seth M. Lederman, MD Tonix Pharmaceuticals, Inc.
Study Director: Jeffrey P. Kitrelle, MD Tonix Pharmaceuticals, Inc.
  More Information

No publications provided

Responsible Party: Tonix Pharmaceuticals, Inc.
ClinicalTrials.gov Identifier: NCT01490788     History of Changes
Other Study ID Numbers: TNX-CY-F101
Study First Received: December 7, 2011
Last Updated: June 6, 2013
Health Authority: United States: Food and Drug Administration
Canada: Health Canada

Additional relevant MeSH terms:
Cyclobenzaprine
Amitriptyline
Antidepressive Agents, Tricyclic
Antidepressive Agents
Psychotropic Drugs
Central Nervous System Agents
Therapeutic Uses
Pharmacologic Actions
Muscle Relaxants, Central
Physiological Effects of Drugs
Neuromuscular Agents
 Peripheral Nervous System Agents
Tranquilizing Agents
Central Nervous System Depressants
Analgesics, Non-Narcotic
Analgesics
Sensory System Agents
Adrenergic Uptake Inhibitors
Adrenergic Agents
Neurotransmitter Agents
Molecular Mechanisms of Pharmacological Action
Neurotransmitter Uptake Inhibitors

ClinicalTrials.gov processed this record on June 17, 2013