Tonix Pharmaceuticals has been granted a U.S. patent for its investigational therapy TNX-102 SL (cyclobenzaprine HCl sublingual tablets), designed to treat fibromyalgia, among other indications.
Issued by the U.S. Patent and Trademark Office under the title “Eutectic Formulations of Cyclobenzaprine Hydrochloride,” the patent includes claims about the pharmaceutical composition and manufacturing of the eutectics in TNX-102 SL. Eutectic refers to a mixture of substances that melt and freeze at the same temperature.
The therapy — for the treatment of fibromyalgia (FM), post-traumatic stress disorder (PTSD), and agitation in Alzheimer’s disease — remains under patent law until 2035, giving Tonix market exclusivity in the United States until then.
TNX-102 SL is a proprietary under-the-tongue (or sublingual) eutectic formulation of cyclobenzaprine. The medicine inhibits different receptors that are involved in pain, sleep, and stress, including the serotonin-2A, alpha-1 adrenergic, and histamine H1 receptors.
The therapy was designed to deliver a small dose of cyclobenzaprine to the bloodstream without it being metabolized in the liver, which can otherwise greatly decrease the concentration of the medicine. Furthermore, the formulation decreases the body’s exposure to an active breakdown product known as norcyclobenzaprine, which has a long half-life in blood plasma.
In contrast, currently marketed cyclobenzaprine-based therapies are oral therapies, which means that they undergo high levels of liver metabolism. They are mainly limited to short-term use of two to three weeks and are used to treat muscle spasm relief.
However, TNX-102 SL has a different pharmacokinetic profile — what the body does to a therapy — compared with current cyclobenzaprine therapies.
Tonmya has been conditionally accepted by the U.S. Food and Drug Administration (FDA) as the trade name for TNX-102 SL in 2.8 mg doses for the treatment of PTSD.
The potential of TNX-102 SL for treating FM has been assessed in the Phase 2/3 BESTFIT (NCT01903265), and the Phase 3 AFFIRM (NCT02436096) and BESTFIT-OLE (NCT02015234) trials.
The results suggested that daily administration of TNX-102 SL at a 2.8 mg dosage could reduce patients’ pain, improve their sleep quality, and have beneficial effects on other FM-related symptoms.
Tonix is now launching a Phase 3 clinical trial to assess the safety and efficacy of a higher 5.6 mg dose of TNX-102 SL in FM patients.
“We are committed to building our intellectual property covering the unique properties of TNX-102 SL in multiple markets around the world,” Seth Lederman, president and CEO of Tonix said in a press release.
“These newly issued claims strengthen and expand TNX-102 SL’s overall patent portfolio and provide Tonix with significant intellectual property protection for TNX-102 SL in the U.S.,” he said.