Bioequivalence of rimegepant, a small molecule CGRP receptor antagonist, administered as an oral tablet, a sublingual orally disintegrating tablet, and a supralingual orally disintegrating tablet: two phase 1 randomized studies in healthy adults.

BACKGROUND

Rimegepant is an orally administered small molecule calcitonin gene-related peptide receptor antagonist indicated for the acute and preventive treatment of migraine.

METHODS

Two single-center, phase 1, open-label, randomized bioequivalence studies were conducted in healthy adult non-smokers, aged 18-55 years. One study compared the rate and extent of absorption of the marketed formulation of rimegepant 75 mg orally disintegrating tablet (ODT) administered sublingually with rimegepant 75 mg oral tablet, an earlier development formulation; the second compared the rate and extent of absorption of 75 mg rimegepant ODT administered supralingually with rimegepant oral tablet.

RESULTS

The ln-transformed geometric mean ratios for the area under the curve (AUC) from time 0 to the last available concentration time point (time

CONCLUSIONS

Rimegepant 75 mg ODT, administered sublingually or supralingually, and rimegepant 75 mg oral tablet were bioequivalent.

Déclaration de conflit d'intérêts

Declaration of conflicting interestsRobert Croop was an employee of Biohaven Pharmaceuticals, owns stock in Biohaven Ltd, was an employee of Pfizer, has received research payments from Pfizer and provides services to Collima LLC, which has had consulting agreements with Pfizer, Aptose Biosciences Inc., Manistee Therapeutics and Vida Ventures Management Co., L.L.C. Jennifer Hould and Richard Bertz are employed by and own stock/stock options in Biohaven Pharmaceuticals. Jing Liu and Kyle T. Matschke are employed by and own stock/stock options in Pfizer Inc. Rajinder Bhardwaj, PhD, and Matt S. Anderson, PhD, are employed by Certara USA, which was a paid consultant of Biohaven Pharmaceuticals. Richard B. Lipton serves on the editorial board of