Clinical Trial Confirms GEMTESA Can Maintain Therapeutic Properties When Administered in Crushed Form with Applesauce

A recently published Phase 1 clinical study demonstrates that vibegron, the active ingredient in GEMTESA, preserves its pharmacokinetic profile when formulated as a crushed tablet mixed with applesauce. The research, featured in the peer-reviewed journal Clinical Pharmacology in Drug Development, provides important evidence for expanding treatment options for patients with overactive bladder who face swallowing challenges.

Study Design and Key Findings

The investigation enrolled 30 healthy adult participants, with 29 completing the pharmacokinetic analysis. Each subject received both an intact 75-mg GEMTESA tablet and a crushed formulation prepared with applesauce in randomized sequence. The primary research endpoints focused on maximum plasma concentration (Cmax) and area under the curve (AUC) measurements.

While modest reductions in Cmax and AUC0–∞ were observed when vibegron was crushed and mixed with applesauce, these decreases were not deemed clinically significant. Earlier Phase 2 efficacy data indicated that vibegron maintained therapeutic effectiveness at these reduced plasma levels. Additionally, stability testing confirmed that GEMTESA retained its chemical integrity for up to 4 hours when suspended in applesauce.

Safety and Tolerability Profile

Treatment-emergent adverse events (TEAEs) occurred in 9 participants (30.0%) following intact tablet administration compared to 12 participants (43.3%) in the crushed formulation group. The most frequently reported adverse effect was headache, affecting 4 subjects (13.3%) in each cohort. Other notable TEAEs included constipation (crushed 13.3% vs. intact 6.7%) and nausea (crushed 6.7% vs. intact 0%). No trial discontinuations resulted from either adverse events or taste-related concerns.

Participant feedback regarding taste perception revealed that approximately half of the study population (53.3%) found the GEMTESA-applesauce mixture palatable as formulated. Among those reporting taste discrepancies, 50% characterized the flavor as bitter, though 80% of this subgroup expressed displeasure with the preparation. Notably, taste considerations did not prompt any study withdrawals.

Clinical Significance for Older Patient Populations

This finding carries particular relevance for geriatric populations, as both overactive bladder and dysphagia—difficulty swallowing—increase substantially with advancing age. Approximately 30 million Americans experience bothersome OAB symptoms, with prevalence escalating significantly in older adults residing in long-term care facilities. The research suggests that the ability to administer vibegron via crushed formulation addresses a significant barrier to medication adherence, since older patients often skip doses or resort to non-prescribed administration methods when faced with tablet-swallowing difficulties.

The authors emphasized that “few oral pharmacotherapies for OAB maintain their essential properties when crushed,” making vibegron’s stability profile distinctive within the therapeutic class.

GEMTESA Market Timeline and Current Status

GEMTESA received FDA approval in December 2020 and entered the U.S. market in April 2021, establishing approximately 3 years of commercial availability to date. The medication is indicated for adults with OAB presenting with urge incontinence, urgency, and urinary frequency. Ongoing clinical evaluations are exploring its efficacy in treating OAB symptoms in men with concurrent benign prostatic hyperplasia.

Urovant Sciences, the biopharmaceutical subsidiary of Sumitovant Biopharma Ltd., is advancing a second-generation pipeline candidate, URO-902, a novel gene therapy designed for OAB patients who have exhausted conventional oral pharmacologic interventions.

Understanding Overactive Bladder

OAB develops when the bladder muscle undergoes involuntary contraction, manifesting as urinary urgency, urgency incontinence, polyuria (≥8 voids per 24 hours), and nocturia. The condition substantially compromises quality of life and daily functional capacity across affected patient populations.

This Phase 1 pharmacokinetic investigation strengthens the clinical evidence supporting vibegron’s versatility as an oral therapeutic option tailored to diverse patient administration requirements and unmet clinical needs in urology.