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

Tonix Pharmaceuticals

Status and phase: Completed; Phase 1

Conditions: Healthy Adults

Treatments: Drug: Cyclobenzaprine IV; Drug: Cyclobenzaprine Tablet; Drug: SL TNX-102 2.4 mg at pH 3.5; Drug: SL TNX-102 2.4 mg at pH 7.1

Study type: Interventional

Funder types: Industry

Identifiers

NCT01634412

TNX-CY-F102

Details and patient eligibility

About

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).

Enrollment: 24 patients

Sex: All

Ages: 18 to 65 years old

Volunteers: Accepts Healthy Volunteers

Inclusion and exclusion 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.

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Parallel Assignment

Masking: None (Open label)

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24 participants in 4 patient groups

SL TNX-102 at pH 3.5

Experimental group

Description:

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

Treatment:

Drug: SL TNX-102 2.4 mg at pH 3.5

SL TNX-102 at pH 7.1

Experimental group

Description:

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

Treatment:

Drug: SL TNX-102 2.4 mg at pH 7.1

Cyclobenzaprine tablets

Active Comparator group

Description:

5 mg cyclobenzaprine tablet once

Treatment:

Drug: Cyclobenzaprine Tablet

Cyclobenzaprine IV

Active Comparator group

Description:

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

Treatment:

Drug: Cyclobenzaprine IV