EU Grants Patent to TNX-102 SL, Oral Muscle Relaxant for Fibromyalgia in New Phase 3 Trial

EU Grants Patent to TNX-102 SL, Oral Muscle Relaxant for Fibromyalgia in New Phase 3 Trial

The European Patent Office (EPO) has issued a patent covering the intellectual rights to the composition and formulation of TNX-102 SL, Tonix Pharmaceuticals’ investigational under-the-tongue muscle relaxant now in pivotal clinical trials to treat fibromyalgia and other disorders.

The company is currently enrolling adults with fibromyalgia into the Phase 3  RELIEF (NCT04172831) study, testing TNX-102 SL as a sublingual tablet taken at bedtime. Criteria for eligible patients are available here; U.S. trial locations and contacts are here.

“The issuance of this European patent is an important step forward in our efforts to broaden our intellectual property estate on a global basis for TNX-102 SL,” Seth Lederman, MD, president and chief executive officer of Tonix Pharmaceuticals, said in a press release.

The patent (EP2968992A2), “Eutectic Formulations of Cyclobenzaprine Hydrochloride and Mannitol,” includes 14 claims pertaining to compositions comprising the eutectics (mixture) of cyclobenzaprine hydrochloride and mannitol, as well as protocols detailing how to make these compositions.

TNX-102 SL is based on a proprietary eutectic (a homogeneous, solid mixture of two or more substances) formulation of cyclobenzaprine (sold under the brand name Flexeril, among others), a potent muscle relaxant used to treat muscle spasms and similar conditions.

A tablet, it is designed to be placed under the tongue (sublingual administration) once daily at bedtime. According to the company, this mode of administration will aid cyclobenzaprine’s absorption and avoid it being quickly metabolized in the liver (first pass liver metabolism), potentially allowing for longer use than is possible with available oral medications based on cyclobenzaprine, approved to treat muscle spasms.

First pass is a phenomenon in which the concentration of a drug is greatly reduced before reaching the bloodstream. This normally happens because a large fraction of the medication is absorbed and processed in the liver or in the intestines before it has the chance to enter systemic circulation.

Recent results from the Phase 3 AFFIRM (NCT02436096) trial showed that TNX-102 SL had a significant beneficial impact on sleep quality and fatigue, although it did not reduce pain levels in fibromyalgia patients.

The company is now enrolling patients into two randomized, double-blind and placebo-controlled Phase 3 trials — RECOVERY (NCT03841773) and RELIEF (NCT04172831) — that will investigate the safety and efficacy of higher doses of TNX-102 SL tablets (5.6 mg, taken daily as two 2.8 mg tablets) in treating people with post-traumatic stress disorder (PTSD; RECOVERY) and fibromyalgia (RELIEF).

Both 12-week trials, RECOVERY is recruiting participants from 30 sites across the U.S.; RELIEF has 40 locations in the U.S.

 In addition to fibromyalgia and PTSD, the therapy is being developed as a potential treatment for agitation in Alzheimer’s disease and alcohol use disorder.