Sublingual Formulation of Riluzole Bioequivalent to Tablet Formulation

Tuesday, January 09, 2018

Biohaven announced positive results from its bioequivalence study of BHV-0223, an innovative sublingual formulation of riluzole, currently available as a 50-mg tablet, which is currently the standard-of-care treatment for patients with Amyotrophic Lateral Sclerosis (ALS), but can be difficult for patients with ALS to swallow. Topline results in a study with 138 healthy volunteers who were administered 40 mg of BHV-0223 sublingually and 50 mg of riluzole in tablet form under fasted conditions showed area-under-the-curve and peak exposures of approximately 90% and 113%, respectively, compared to those generated by generic riluzole. The 90% confidence intervals were within the 80% to 125% range used to define bioequivalence. 

Biohaven is developing BHV-0223 as a potential treatment for patients with ALS and received regulatory feedback from the Food and Drug Administration (FDA) that no additional efficacy or toxicology studies are necessary for submission of a new drug application (NDA) for this indication. Biohaven anticipates completing an NDA submission in the first half of 2018. 

While riluzole is FDA-approved for ALS, conventional tablets may be difficult to administer to paatients with ALS, who often have dysphagia. The sublingual BHV-0223 dissolves in seconds and does not require swallowing. In addition, riluzole is associated with dose-dependent effects on liver tests (transaminases), which is significant because BHV-0223 offers bioequivalent exposures with a 20% lower dose. Based on this observation and reduced drug exposure to the liver, BHV-0223 may have a lessened risk for causing liver enzyme elevations. 

Vlad Coric, MD, Chief Executive Officer of Biohaven, commented, “Sublingual BHV-0223 is unique in that it is . . . optimized to allow administration to patients with dysphagia and to provide therapeutic blood levels at a lower dose for all patients suffering from ALS."

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