Nurtec (formerly BHV-0223) is a new formulation of riluzole that is placed under the tongue and dissolves in the mouth. The therapy is being developed by Biohaven Pharmaceuticals for treating amyotrophic lateral sclerosis (ALS).

How Nurtec works

Riluzole is a glutamate-modulating agent. Its exact mechanism of action is unknown, but it is thought to block the release of glutamate from nerve cells. Glutamate is a neurotransmitter, a key molecule that transmits information from one nerve cell to another and plays a crucial role in normal brain function.

One of the causes of nerve damage in ALS is thought to be glutamate dysfunction wherein toxic levels of glutamate are released and damage the surrounding nerve cells. Glutamate-modulating agents are thought to have neuroprotective properties in diseases such as ALS, as they may prevent glutamate from reaching damaging levels.

Nurtec, the new formulation of riluzole, is intended to address some of the problems associated with the therapy, such as dysphagia (difficulty swallowing) by using the Zydis ODT (orally dissolving tablet) technology developed by Catalent. Nurtec is designed to be placed under the tongue, where it will dissolve and be absorbed quickly. Because it is absorbed by the oral mucosa (the lining of the mouth) rather than by the gastrointestinal system, researchers think Nurtec also will prevent the need for restrictions associated with pill-form riluzole, such as having to take it on an empty stomach and avoiding caffeinated products.

Nurtec in clinical trials

Biohaven Pharmaceuticals successfully completed a Phase 1 clinical trial to test the pharmacokinetics (movement in the body), safety, and tolerability of Nurtec in 138 healthy volunteers. The results were presented in a poster at the American Association of Neuromuscular & Electrodiagnostic Medicine (AANEM) annual meeting in 2018. They showed that a 40 mg dose of Nurtec had bioequivalence with 50 mg of riluzole, but with less variability in pharmacokinetics, leading to more predictable treatment levels in the body.

Biohaven has an open treatment protocol through the expanded access program of the U.S. Food and Drug Administration (FDA). This clinical trial (NCT03537807), which is currently enrolling patients, is designed to allow physicians access to prescribing Nurtec to their ALS patients who might benefit more from taking it rather than swallowing oral riluzole tablets.

Next steps for Nurtec

Biohaven rebranded BHV-0223 as Nurtec and submitted a 505(b)(2) NDA (new drug application) to the FDA in November 2018. If the FDA approves the sublingual treatment, it should be available on the market later in 2019.

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