Pharmacokinetics and Safety of Vibegron 75 mg Administered as an Intact or Crushed Tablet in Healthy Adults. Issue 11 (14th September 2022)

• Record Type: Journal Article
• Authors: King, Jennifer; Walker, Ann; Aikin, Dorothy; Haag‐Molkenteller, Cornelia; Kankam, Martin
• Is Part Of: Clinical pharmacology in drug development. Volume 11:Issue 11(2022)
• Page Start: 1349
• Page End: 1355
• Publication Date: 2022-09-14
• Subjects: adrenergic β3‐receptor agonist -- bioavailability -- dysphagia -- long‐term care -- overactive bladder; Drugs -- Testing -- Periodicals; Drug development -- Periodicals; Clinical pharmacology -- Periodicals; 615.580724
• DOI: 10.1002/cpdd.1169
• Languages: English
• ISSNs: 2160-7648

Abstract

Abstract: Oral pharmacotherapy for overactive bladder, a condition that increases with age, includes anticholinergics and β3 ‐adrenergic receptor agonists. Older adults, including those with dysphagia, may have difficulty swallowing tablets. In this phase 1 study in healthy adults, we assessed the pharmacokinetic profile of the β3 ‐adrenergic receptor agonist vibegron administered as a single 75‐mg dose as an intact tablet versus crushed and mixed with applesauce. Additional end points included safety (assessed by adverse events), perception of taste (assessed via questionnaire), and stability over 4 hours after crushing and mixing in applesauce (assessed by chromatography). Overall, 30 participants were randomized, and 29 were included in the pharmacokinetic analysis. Crushing a vibegron tablet and mixing with applesauce decreased vibegron maximum observed plasma concentration and area under the plasma concentration–time curve from time 0 to infinity by ≈30% and ≈10%, respectively; however, these decreases were not considered clinically significant. Treatment‐emergent adverse events were reported in 16 (53.3%) participants. Approximately half of participants reported the vibegron and applesauce mixture tasted as expected; of those reporting the taste was different than expected, 50% reported the taste as bitter. The mixture was stable for 4 hours in applesauce. The results of this study showed that crushing and administering vibegron with applesauce may be an appropriate option for patients with overactive bladder and swallowing difficulties.