Affiliation:
1. Certara USA Princeton NJ USA
2. Biohaven Pharmaceuticals, Inc. New Haven CT USA
3. Pfizer Inc. Groton CT USA
Abstract
AbstractRimegepant is a small‐molecule calcitonin gene‐related peptide receptor antagonist approved for the acute treatment of migraine ± aura and preventive treatment of migraine in adults. The pharmacokinetics of rimegepant in elderly and nonelderly subjects were evaluated. In an open‐label Phase 1 study, 14 elderly (aged 65 years or older) and 14 nonelderly (aged 18 to less than 45 years) subjects each received a single oral dose of rimegepant 75 mg. Blood samples were collected before dosing and through 96 hours after dosing. The pharmacokinetic parameters of rimegepant after a single dose were similar in both age groups. Geometric least‐squares mean ratios (elderly/nonelderly) of the natural log‐transformed maximum observed plasma concentration and natural log‐transformed area under the plasma concentration–time curve from time 0 extrapolated to infinity were 96.6 and 104.6, respectively. Eight (28.6%) subjects (4 elderly, 4 nonelderly) experienced 1 or more adverse events (AEs); all AEs were mild in intensity, and no serious AEs or AEs leading to discontinuation were reported. Following a single 75‐mg dose of oral rimegepant, pharmacokinetic parameters were similar in elderly and nonelderly adults; no dose adjustment is warranted in elderly subjects.
Subject
Pharmacology (medical),Pharmaceutical Science