Tonix Pharmaceuticals Testing
New Sublingual Medication for Fibromyalgia

A sublingual, under-the-tongue, cyclobenzaprine (Flexeril) tablet for the treatment of fibromyalgia is being developed by Tonix Pharmaceuticals. A new more efficient delivery system compared to the pill form of cyclobenzaprine (CBP), this muscle relaxant medication that has been a mainstay of fibromyalgia treatment for more than twenty years. The sublingual tablet (TNX-102 SL) is based on novel technology that rapidly delivers CBP into the body. It quickly dissolves and releases the drug under the tongue, which is absorbed across the mucous membrane into the patient's bloodstream. CBP is a widely prescribed medication with an established safety record. Several large clinical trials throughout the years have confirmed its safety and tolerability.

At the 2013 August International MYOPAIN Meeting in Seattle, Bruce Daugherty, PhD, MBA from Tonix Pharmaceuticals gave a presentation about the success of preliminary TNX-102 studies determining the efficacy of CPB on reducing FM symptoms. He reported that CPB is a potent antagonist of 5HT2A and α1A andrenergic receptors (a class of G protein-coupled receptors that are targets for norepinephrine [noradrenaline] and epinephrine [adrenaline] as well as 5HT norepinephrine reuptake.
The new CPB treatment has demonstrated improved FM outcomes in a Phase 2a, randomized, double-blinded, placebo-controlled clinical study. In the study 36 FM patients were given escalating doses of CPB (1mg-4mg), or placebo, once daily between dinner and bedtime for 8 weeks. The treatment demonstrated statistically significant improvements in a number of FM clinical outcome measures recognized by the American College of Rheumatology. These included reductions in musculoskeletal pain, pain sensitivity, fatigue and altered mood.

Tonix expects TNX-102 SL to have an improved tolerability and efficacy profile versus currently available generic CPB products. The uniqueness of TNX-102 SL has been shown to provide for rapid absorption into the bloodstream and rapid excretion from the system. As a bedtime medication this is ideal since it reduces next day symptoms of drowsiness. In addition, since this medication avoids metabolism problems in the liver, a psychoactive metabolite of cyclobenzaprine, norcyclobezaprine is not generated. Tonix believes production of this metabolite in generic cyclobenzaprine contributes to reduced long-term efficacy in the treatment of FM.

In September 2013 Tonix began enrollment in a pivotal trial of TNX-102 SL for the treatment of fibromyalgia.