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Comparative Pharmacokinetics and Safety of TNX-102 SL Tablets and Cyclobenzaprine Oral Tablet in Healthy Adults

Phase 1
Completed
Conditions
Healthy Adults
Interventions
Drug: SL TNX-102-A at 2.4 mg
Drug: SL TNX-102 at 2.4 mg
Drug: SL TNX-102 at 4.8 mg
Registration Number
NCT01689259
Lead Sponsor
Tonix Pharmaceuticals, Inc.
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 TNX-102 2.4 mg SL Tablets (a new formulation of cyclobenzaprine designed to result in increased dosage precision and decreased potential for morning grogginess) at 2.4 mg and 4.8 mg and to compare the bio-availability of TNX-102 2.4 mg SL Tablets at 2.4 mg and 4.8 mg to that of TNX-102-A 2.4 mg SL Tablets (without phosphate) at 2.4 mg and cyclobenzaprine (5 mg tablets).

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
24
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 (within 30 days), or of > 499 mL (within 56 days) prior to dosing.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
SL TNX-102-A at 2.4 mgSL TNX-102-A at 2.4 mg1 x TNX-102-A (without phosphate) SL Tablet at 2.4 mg
Cyclobenzaprine tabletsCyclobenzaprine tablets1 x 5 mg cyclobenzaprine oral tablet
SL TNX-102 at 2.4 mgSL TNX-102 at 2.4 mg1 x TNX-102 SL Tablets at 2.4 mg
SL TNX-102 at 4.8 mgSL TNX-102 at 4.8 mg2 x TNX-102 SL Tablets at 2.4 mg
Primary Outcome Measures
NameTimeMethod
Measured levels of cyclobenzaprine and norcyclobenzaprine in plasma and urine27 time points per period for blood assessment ; 3 pooled analyses in urine.

Blood samples will be taken per period: within 30 minutes pre-dose and 2, 3.5, 5, 10, 20, 30, and 45 minutes and 1, 2, 2.5, 3, 3.33, 3.67, 4, 4.33, 4.67, 5, 5.5, 6, 8, 12, 16, 24, 36, 48, and 72 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 and 48-72 hours post-dose.

Safety and tolerability of TNX-102 SL Tablets at 2.4 mg and 4.8 mg.Continuously until the end (day 4) of the study period + Telephone follow-up 7-13 days after dosing (total duration: about 1 month)

Every adverse events occurring during the study period will be reported.

Secondary Outcome Measures
NameTimeMethod

Trial Locations

Locations (1)

PharmaNet, Inc.

🇨🇦

Quebec City, Quebec, Canada

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