TONIX is developing TNX-102 SL as a sublingual (SL) or under-the-tongue tablet (TNX-102 SL) at a novel dose. The TNX-102 SL tablet is based on novel technology that rapidly delivers cyclobenzaprine into the body. The tablet quickly dissolves and releases cyclobenzaprine under the tongue, which is absorbed across the mucous membrane into the patient’s bloodstream. The rapid absorption of TNX-102 SL is due to the tablet’s proprietary design and formula. Patients cannot get the same rapid absorption simply by crushing existing cyclobenzaprine products and placing the powder under their tongues. cyclobenzaprine is a widely prescribed muscle relaxant with an established safety profile. Several large clinical studies have confirmed cyclobenzaprine’s safety and tolerability.
TNX-102 SL is in development as a treatment for fibromyalgia syndrome (FM). Very low dose cyclobenzaprine(VLDC) already has been tested as a bedtime treatment for FM. This treatment improved FM outcomes in a Phase 2a, randomized, double-blinded, placebo-controlled clinical study. Thirty-six FM patients were given escalating doses of cyclobenzaprine (1mg – 4mg), or placebo, once daily between dinner and bedtime for 8 weeks. VLDC treatment demonstrated statistically significant improvements in a number of FM clinical outcome measures, recognized by the American College of Rheumatology and/or by OMERACT (Outcome Measures in Rheumatoid Arthritis Clinical Trials). 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 cyclobenzaprine products. The unique qualities of TNX-102 SL provide for rapid absorption into the bloodstream and rapid excretion from the system. This is ideal for a bedtime medicine to reduce next day somnolence. In addition, since TNX-102 SL avoids first-pass metabolism by the liver, a psychoactive metabolite of cyclobenzaprine, norcyclobenzaprine, is not generated. TONIX believes that this metabolite contributes to reduced long term efficacy with the off-label use of generic cyclobenzaprine in FM.
Tonix began enrollment in a pivotal trial of TNX-102 SL for the treatment fibromyalgia in September 2013.