The influence of renal impairment on the pharmacokinetics of rimegepant: Results of a phase 1, open-label, single-dose, parallel-group study
Abstract
OBJECTIVE: The objective of this study was to investigate the pharmacokinetics of rimegepant in participants with mild, moderate, or severe renal impairment compared to healthy adults with normal renal function.
BACKGROUND: Rimegepant is a calcitonin gene-related peptide receptor antagonist approved in the United States for treatment of acute and preventive treatment of migraine.
METHODS: In this Phase 1, open-label, four-group, pharmacokinetic study, 36 participants were grouped by degree of renal impairment according to estimated glomerular filtration rate (eGFR): normal; mild (60-89 mL/min/1.73 m2); moderate (30-59 mL/min/1.73 m2); and severe (<30 mL/min/1.73 m2). Participants received a single 75-mg oral rimegepant tablet to determine total and unbound plasma rimegepant concentrations using both matched and pooled control analysis. The study enrollment period began on October 17, 2017, and concluded on March 27, 2018.
RESULTS: For mild, moderate, and severe renal impairment groups, respectively, compared with matched control groups, total geometric least-square mean ratios (90% confidence intervals) were 1.06 (0.75-1.52), 1.40 (0.97-2.02), and 1.04 (0.70-1.57) for area under the concentration-time curve from time zero to infinity (AUC0-inf) and 1.20 (0.75-1.92), 0.76 (0.42-1.37), and 0.90 (0.50-1.62) for maximum observed concentration (Cmax). Geometric mean ratios of unbound AUC0-inf were 1.22 (0.82-1.82), 1.84 (1.30-2.61), and 2.57 (1.86-3.56) in the mild, moderate, and…
How strong is the evidence?
Evidence Hub reads this as a clinical trial, done in people. Its evidence level is 3 of 5 (Moderate · trial / cohort / secondary analysis). Trials without a large randomized design, cohorts and secondary analyses give moderate evidence. Reported size: 36 participants or records.
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