Clinical trial NCT01634412: Comparative Bioavailability of Sublingual TNX-102, Oral and Intravenous Cyclobenzaprine in Healthy Adults
Official title: A Single-Dose, Open-Label, Randomized Study of the Comparative Pharmacokinetics of Sublingual TNX-102 2.4 mg at pH 3.5 and 7.1, Oral Cyclobenzaprine 5 mg Tablets, and Intravenous Cyclobenzaprine 2.4 mg in Healthy Adults
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy Adults
Lead sponsor: Tonix Pharmaceuticals, Inc.
Sponsor class: INDUSTRY
First posted: 2012-07-06
Enrollment: 24
Sex: ALL
Minimum age (years): 18
Maximum age (years): 65
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: PARALLEL
Primary purpose: TREATMENT

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).


Eligibility criteria: Inclusion Criteria: Healthy adults

* 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.

Primary outcomes:
measure: • Measured levels of cyclobenzaprine and norcyclobenzaprine in plasma and urine
timeFrame: 27 time points per period for blood assessment ; 3 pooled analyses in urine.
measure: Safety and tolerability of sublingual TNX-102 2.4 mg at pH 3.5 and pH 7.1.
timeFrame: Continuously until the end (day 4) of the study period + Telephone follow-up 7-13 days after dosing (total duration: about 1 month)
Secondary outcomes:
Other outcomes:
Locations:
city: Quebec City
country: Canada
facility: PharmaNet, Inc.
state: Quebec
Study officials:
affiliation: Tonix Pharmaceuticals, Inc.
name: Seth M. Lederman, MD
role: STUDY_CHAIR
affiliation: Tonix Pharmaceuticals, Inc.
name: Jeffrey P. Kitrelle, MD
role: STUDY_DIRECTOR
affiliation: PharmaNet
name: Denis Audet, MD
role: PRINCIPAL_INVESTIGATOR
References: