Biohaven Pharmaceutical announced positive results from its bioequivalence study with rimegepant Zydis orally dissolving tablets (ODT). Rimegepant is a small molecule, oral, calcitonin gene-related peptide (CGRP) receptor antagonist currently in two pivotal Phase 3 trials for the acute treatment of migraine using a tablet formulation. Biohaven has been working with Catalent U.K. Swindon Zydis, a subsidiary of Catalent, to develop a new ODT formulation of rimegepant which dissolves on the tongue without the need for fluid intake.
The purpose of the bioequivalence study was to demonstrate pharmacokinetic equivalence of the rimegepant Zydis ODT formulation compared to the rimegepant tablet formulation used in the Phase 3 program. Topline results demonstrate that the rimegepant Zydis ODT achieves bioequivalent exposures relative to the current Phase 3 tablet fomulation. In the study, 34 healthy volunteers were administered rimegepant 75mg Zydis ODT and the current rimegepant 75mg tablet. In the pre-specified primary analysis, rimegepant Zydis ODT achieved area-under-the-curve and peak exposures of approximately 97% and 105%, respectively, compared to those generated by rimegepant tablet. The 90% confidence intervals were within the 80% to 125% range that is commonly used to define bioequivalence.
"We are very excited about the favorable results from the study establishing the bioequivalence of our innovative rimegepant Zydis ODT with the tablet formulation used in the Phase 3 trials. The fast-dissolving Zydis rimegepant formulation is designed to enable patients with migraine to start their acute treatment promptly, without a need for swallowing liquids,” Vlad Coric, M.D., Chief Executive Officer of Biohaven, said. “The characteristics of this formulation are particularly advantageous for the acute treatment of migraine because many individuals with migraine often experience concurrent nausea or vomiting. Our rimegepant Zydis ODT is a convenient formulation that can be taken wherever and whenever a migraine occurs. We are progressing multiple formulations across our small molecule CGRP receptor antagonist platform in an effort to meet patient needs across the spectrum of migraine treatment."
Based upon these bioequivalence results, Biohaven is planning to initiate a Phase 3 trial with rimegepant Zydis ODT in the first quarter of 2018 to assess onset of action and patient satisfaction with the Zydis ODT formulation. Biohaven's development program enables the potential to bring rimegepant to market with this new formulation while staying on track with its original rimegepant development timeline. Biohaven expects to receive topline results from its two pivotal Phase 3 trials examining the efficacy of rimegepant 75mg oral tablet versus placebo in the acute treatment of migraine by the end of the first quarter of 2018.
Biohaven has an exclusive worldwide license agreement with Catalent to provide Catalent's Zydis ODT fast-dissolving technology for the development of Biohaven's lead CGRP receptor antagonist product candidate, rimegepant. The agreement also provides exclusive rights for developing additional small molecule CGRP receptor antagonists with the Zydis ODT technology. Catalent's proprietary Zydis technology creates a unique, freeze-dried, oral solid dosage form that disperses almost instantly in the mouth, without the need for water. With more than 20 products launched in 50 countries and a dispersion speed of three seconds or less, Zydis ODT is the world's fastest and best-in-class orally dissolving tablet.