Gemtesa (vibegron) / Merck (MSD), Kissei, Kyorin, Sumitomo Pharma, Jeil, Pierre Fabre, Knight Therap - LARVOL DELTA

Synergistic CRISPR-Cas9 Host Engineering and Enzyme Evolution for Enantioselective Synthesis of a Vibegron Pyrrolidine Intermediate. (PubMed, Org Lett) - "Here we report an imine reductase (IRED) catalyzed asymmetric imine reduction to access a key vibegron intermediate. Directed evolution afforded a highly efficient variant delivering 94% conversion and >99% d.e. Combined enzyme and host engineering enabled clean whole cell catalysis, establishing a robust and scalable biocatalytic platform."

Journal

Efficacy and Safety of Vibegron Add-On Therapy for Persistent Overactive Bladder Symptoms in Benign Prostatic Hyperplasia Patients With α1-Blocker Treatment: A Multi-Center Prospective Randomized Controlled Study (VATON Study). (PubMed, Low Urin Tract Symptoms) - "Vibegron add-on therapy to an α1-blocker may be effective and safe for treating BPH with persistent OAB symptoms."

Clinical • Journal • Benign Prostatic Hyperplasia • Overactive Bladder

Evaluating sexual function in men treated with vibegron for overactive bladder while on pharmacological therapy for benign prostatic hyperplasia: exploratory analysis from the phase 3 COURAGE trial (AUA 2026) - No abstract available

P3 data • Benign Prostatic Hyperplasia • Overactive Bladder

Efficacy and safety of vibegron in men =75 years of age with symptoms of overactive bladder on pharmacotherapy for benign prostatic hyperplasia: a subgroup analysis of the COURAGE trial (AUA 2026) - No abstract available

Clinical • Benign Prostatic Hyperplasia • Overactive Bladder

The effect of anticholinergics and β-3 agonists on erectile function: a narrative review. (PubMed, Sex Med Rev) - "OAB pharmacotherapy may influence male sexual health; however, evidence remains mixed. Further high-quality research is needed to elucidate these relationships and guide individualized treatment strategies that address both urinary and sexual function in men."

Journal • Overactive Bladder

Microwave-assisted N,S doped carbon quantum dots as fluorescent nanoprobes for vibegron determination: face-centered design optimization, validation, and green chemistry assessment. (PubMed, RSC Adv) - "Furthermore, spiked human plasma analysis demonstrated recoveries ranging from 96.44% to 104.28% with RSD values below 4%, confirming applicability to biological matrices for therapeutic drug monitoring. Comprehensive green chemistry assessment using AGREE (0.65), CaFRI (80/100), and BAGI (70.0/100) metrics demonstrated favorable environmental sustainability characterized by minimal hazardous reagent consumption, low carbon footprint, reduced waste generation, and excellent practical applicability, providing an environmentally benign analytical tool for routine pharmaceutical quality control and therapeutic drug monitoring applications."

Journal

Effects of Vibegron, a β3-Adrenoceptor Agonist, on Lower Urinary Tract Dysfunction in Diabetic Rats. (PubMed, Low Urin Tract Symptoms) - "These findings suggest that vibegron may be a promising therapeutic option for addressing detrusor overactivity, ischemia, and inflammation of the bladder associated with diabetes mellitus."

Journal • Preclinical • Cardiovascular • Diabetes • Metabolic Disorders • Oncology • HIF1A • TGFB1 • TNFA

Persistent bothersome urinary frequency following stereotactic body radiation therapy for clinically localized prostate cancer: rationale for prophylactic β3-agonist in men with elevated baseline international prostate symptom scores. (PubMed, Front Oncol) - "Answers to question 4E and tamsulosin usage were recorded at regular follow-ups to assess, and demographic factors as well as baseline prostate volume, alpha-adrenergic antagonist usage and IPSS score severity were used as modifiers. Prophylactic alpha-adrenergic antagonists do not protect against bothersome acute urinary frequency. This paper makes the case that urinary frequency may be better addressed with a prophylactic beta-3 agonist, like vibegron, which is designed to treat storage-related LUTS concerns."

Journal • Genito-urinary Cancer • Oncology • Overactive Bladder • Prostate Cancer • Solid Tumor

Validated LC-MS/MS Method for Vibegron Quantification in Human Plasma via a Selective Fragment Ion (m/z 135.1): Addressing Matrix Interference and Sample Instability. (PubMed, Biomed Chromatogr) - "The method demonstrated excellent linearity (0.500-400.223 ng/mL), precision (0.58%-3.34%), and accuracy (98.26%-102.29%), using only 100 μL of plasma. Fully compliant with ICH M10 guidelines, the method is well suited for future pharmacokinetic, bioavailability, and bioequivalence studies."

Journal

Exploring the therapeutic potential of beta-3 adrenergic agonists in overactive bladder: A comprehensive review. (PubMed, Med J Armed Forces India) - "The objective of this review was to understand the beta-3 signaling mechanisms in OAB and analyze the results of studies comparing mirabegron either as monotherapy or in combination with antimuscarinics for OAB treatment...In patients who are resistant to monotherapy, a combination therapy consisting of antimuscarinic agents and beta-3-agonists may be attempted. Primarily, this review emphasizes the role of beta-3 agonists in OAB in terms of their mechanism, safety, and efficacy in comparison with those of antimuscarinic drugs."

Journal • Review • Overactive Bladder • Urinary Incontinence • Urology

A novel electrochemical sensor for the analysis of vibegron as a newly approved FDA drug: a rational computational design and cleaning validation application. (PubMed, Anal Methods) - "The theoretical assumptions were practically verified by studying the selectivity of various electrodes with different studied ionophores towards vibegron and another structurally related molecule, mirabegron. This work also demonstrated the first use of electrochemistry during a cleaning validation protocol for monitoring any drug residues to ensure the effective cleaning of pharmaceutical manufacturing equipment with satisfactory recovery values. The proposed sensor was found to be a more sustainable, portable and faster sensing platform for these residues than conventional chromatographic methods."

FDA event • Journal

Effects of Treatment and Weather Variables on Nocturnal Enuresis: Long-Term Analysis Using the Classification and Regression Trees Model. (PubMed, Cureus) - "Our findings suggest that effective long-term management of NE may require individualized treatment plans that account for clinical and weather-related variables. Among weather-related variables, consideration of seasonal and environmental factors may be especially important in managing NE."

Journal • Pediatrics • Urinary Incontinence

Editorial Comment on: Use and Persistence of Beta-3 Adrenoceptor Agonists for the Treatment of Overactive Bladder. (PubMed, Int J Urol) - No abstract available

Journal • Overactive Bladder

Role of Combination Therapy in Women With Refractory Overactive Bladder (clinicaltrials.gov) - P=N/A | N=0 | Withdrawn | Sponsor: University of Alabama at Birmingham | N=54 ➔ 0 | Trial completion date: Dec 2026 ➔ Jan 2026 | Not yet recruiting ➔ Withdrawn | Trial primary completion date: Aug 2026 ➔ Jan 2026

Enrollment change • Trial completion date • Trial primary completion date • Trial withdrawal • Overactive Bladder

Restoring Control: A Medication Use Evaluation of Vibegron in the Treatment of Overactive Bladder (ASHP 2025) - No abstract available

Overactive Bladder

An updated meta-analysis of head-to-head trials comparing the efficacy, safety, and adherence of mirabegron and vibegron in overactive bladder. (PubMed, Medicine (Baltimore)) - "Recent data indicated that vibegron demonstrated superior efficacy in reducing urgency and UUI episodes while maintaining a safety profile comparable to mirabegron. Furthermore, vibegron is associated with improved treatment adherence. However, additional RCTs are necessary to confirm these findings."

Clinical • Head-to-Head • Journal • Retrospective data • Review • Overactive Bladder • Urinary Incontinence

Safety and efficacy of vibegron in pediatric patients with treatment-resistant nocturnal enuresis: a multicenter retrospective study. (PubMed, Transl Pediatr) - "Although enuresis alarms and desmopressin are the first-line treatments recommended by clinical guidelines, 20-40% of affected children demonstrate inadequate response and require additional therapeutic interventions. Add-on strategies-particularly triple therapy-were more effective than monotherapy switching, strengthening the incorporation of vibegron as part of multimodal treatment strategies. Given the retrospective nature of the study, prospective randomized trials are warranted to confirm these findings and optimize the treatment protocols."

Journal • Retrospective data • Pediatrics • Urinary Incontinence • Urology

Bladder Function and Safety of Vibegron in Men With Overactive Bladder Receiving Treatment for Benign Prostatic Hyperplasia: Outcomes From the Phase 3 Randomized Controlled COURAGE Trial. (PubMed, Neurourol Urodyn) - P3 | "There were no safety signals related to bladder function identified by urodynamics; risk of protocol-defined AEs of urinary retention or residual urine volume increase was not increased with vibegron compared with placebo in this population."

Journal • P3 data • Benign Prostatic Hyperplasia • Overactive Bladder

Use and Persistence of Beta 3-Adrenoceptor Agonists for the Treatment of Overactive Bladder. (PubMed, Int J Urol) - "The higher discontinuation rate of mirabegron may reflect the availability of vibegron as an alternative treatment option. The complementary use of both β3 agonists could play a key role in optimizing OAB management."

Journal • Overactive Bladder

Exploratory randomized comparison of mirabegron and vibegron as first-line therapy for overactive bladder in elderly women. (PubMed, Urology) - "Over 12 weeks, mirabegron and vibegron showed comparable efficacy and safety in pharmacotherapy-naïve elderly women with OAB. Given the single-center design and limited statistical power, these findings provide preliminary insights that may help guide the selection of first-line β3-adrenergic receptor agonists and highlight the need for larger multicenter trials."

Journal • Constipation • Gastroenterology • Gastrointestinal Disorder • Overactive Bladder • Xerostomia

Radiation Nephritis Associated with Lutetium-177 Prostate-Specific Membrane Antigen (KIDNEY WEEK 2025) - "His outpatient medications include tadalafil 5 mg, vibegron 75 mg, testosterone cypionate 0.3 ml every 7 days, ezetimibe 10 mg, rosuvastatin 5 mg and insulin. Nephropathy attributed to binding of the drug to PSMA-like proteins expressed in the tubules leading to retention of beta emitter in the kidneys. Radiation renal injury is typically evident several months after irradiation."

Acute Kidney Injury • Diabetes • Genito-urinary Cancer • Hypertension • Metabolic Disorders • Nephrology • Prostate Cancer • Renal Disease • Solid Tumor

β3-Adrenoceptor Agonists for Neurogenic Lower Urinary Tract Dysfunction: Evidence and Clinical Rationale for First-Line Therapy. (PubMed, Neurourol Urodyn) - "β3-adrenoceptor agonists represent a safe, effective, and well-tolerated first-line option in NLUTD management. They preserve bladder safety and continence with fewer systemic side effects. OnabotulinumtoxinA remains an important escalation therapy for refractory cases but carries higher procedural and retention risks. A β3-agonist-based strategy offers a rational, patient-centered foundation for treatment."

Journal • Review • Cardiovascular • CNS Disorders • Multiple Sclerosis • Orthopedics

Target and off-target effects of vibegron on smooth muscle contraction of human detrusor and prostate tissues. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "Similar to mirabegron, improvements of storage symptoms by vibegron involve mechanisms beyond inhibition of voiding contractions. Off-target effects occur with 10 µM, and include inhibition of neurogenic contractions and antagonism of prostatic α1A-adrenoceptors. Vibegron effects in the prostate may differ between patients with low BPH progression, and patients needing surgery for BPH."

Journal • Benign Prostatic Hyperplasia • Overactive Bladder

Main pharmacological differences between mirabegron and vibegron for the treatment of overactive bladder. (PubMed, Actas Urol Esp (Engl Ed)) - No abstract available

Journal • Overactive Bladder

Comparative assessment of oral medications for overactive bladder in older adults: a systematic review and network meta-analysis. (PubMed, Aging Male) - "In terms of reducing Micturitions, the interventions were ranked: trospium chloride (TRO), fesoterodine (FES) 4/8 mg, vibegron (VIB), mirabegron (MIR) 25/50 mg, tolterodine ER (TOL) 4 mg, placebo (PBO), of which only TOL showed no significant difference compared to placebo; Forsafety, the TEAE of TOL 4/8 mg had the highest incidence and was significantly different from others; MIR, VIB, and FES 4mg were well-tolerated regarding dry mouth and constipation; TOL 4 mg, FES 4/8 mg, and VIB showed a statistically increase from placebo for headache and FES 4/8mg and MIR 25 mg showed a statistically increase for dizziness. TRO 60 mg has the best efficacy in reducing micturitions, but increases the incidence of dry mouth and constipation; VIB and MIR are well tolerated in dry mouth and constipation, but may increase the risk of headache or dizziness."

Clinical • Journal • Retrospective data • Review • Constipation • Gastroenterology • Gastrointestinal Disorder • Overactive Bladder • Pain • Xerostomia • MIR25