[ad_1]
Vibegron (Gemtesa) has also been shown to be effective in the treatment of overactive bladder (OAB) when a tablet is crushed and mixed with applesauce. Recent studies have shown that the pill can be crushed to help treat OAB in those with difficulty swallowing.1
“The fact that Hemteza can be crushed and given with applesauce suggests that it could be used in older patients, particularly in the long-term care setting, as OAB and swallowing difficulties increase with age. This will allow Urovant to develop OAB treatment options tailored to meet different management needs.” and is consistent with the goal of commercialization,” said Sef Kurstjens, PhD, Chief Medical Officer of Urovant Sciences, in a press release on the findings.2
In phase 1 of the study, vibegron was given to participants in a single 75 mg dose as an intact tablet or as a crushed tablet with 1 tablespoon of apple juice. Participants were healthy individuals between the ages of 18 and 50 years. In total, there were 30 participants and 29 had sufficient plasma samples for pharmacokinetic (PK) analysis. Each was randomly assigned to 1 of 2 sequences: whole tablet in the first period and crushed in the second, or crushed in the first period and not whole in the second. There were 13 days between periods.
Primary endpoints evaluated included PK parameters of maximum observed plasma concentration (Cmax), area under the plasma concentration-time curve (AUC) from time 0 to last measured concentration (AUC0-t), and AUC from time 0. infinity (AUC0‒∞). Cmax and AUC0‒∞ decreased by ≈30% and ≈10%, respectively, when using the crushed tablet, but this decrease was not considered clinically significant due to the results of a phase 2 study, which showed a low level of efficacy.
Additional endpoints evaluated included additional PC parameters, taste, safety and tolerability parameters, and durability. Additional PK parameters include several endpoints, such as time to Cmax, terminal half-life, total clearance after oral administration, and volume of distribution in the terminal phase after oral administration. Results for taste were assessed using a questionnaire, in which approximately half (53.3%) of the participants reported that the tablet/apple mixture tasted as expected.
Safety and tolerability measures included adverse events (AEs) and clinical laboratory and vital sign assessments. Treatment-emergent AEs (TEAEs) occurred in 9 (30%) patients, and the most common TEAE was headache, which occurred in 4 (13.3%) participants. The crushed tablet was also found to be stable for 4 hours under ambient conditions.
These results indicate that there is no clinically significant change in PK parameters or stability by mixing vibegrone ground and mixed with applesauce.
The authors wrote: “The lack of clinically significant differences with vibegron in crushing and administration is particularly important because few oral pharmacotherapies for OAB retain their essential properties when crushed.”
According to the authors, these findings may improve long-term treatment compliance for patients with OAB, as they indicate that giving vibegron tablets crushed and mixed with applesauce may be a safe and viable solution for patients with swallowing difficulties. Vibegron is currently FDA approved for the treatment of symptoms of OAB in adults.
References
1. King J, Walker A, Aikin D, Haag-Molkenteller C, Kankam M. Pharmacokinetics and safety of vibegron 75 mg administered as intact or crushed tablets in healthy adults. Clin Pharmacol Drug Dev. Published November 14, 2022. Accessed November 3, 2022. doi.org/10.1002/cpdd.1169
2. Urovant Sciences announces the publication of pharmacokinetic data for GEMTESA (vibegron 75mg) administered as whole or crushed tablets. News release. Urovant Sciences. October 27, 2022. Available: November 3, 2022. https://www.businesswire.com/news/home/20221027005843/en/Urovant-Sciences-Announces-Public
[ad_2]
Source link