The efficacy and tolerability of tarafenacin, a new muscarinic acetylcholine receptor M3 antagonist in patients with overactive bladder; randomised, double-blind, placebo-controlled phase 2 study

Abstract

Tarafenacin 0.4 mg decreased the number of micturitions in patients with OAB after 12 weeks compared with placebo, and the dose-response relationship of tarafenacin 0.2 and 0.4 mg was confirmed. Both dose levels of tarafenacin were well tolerated.

Potential Primary Endpoint for Exploratory Clinical Trial in Patients with Overactive Bladder: A Systematic Literature Review

“…). The full texts of 119 trials were reviewed, and 38 were ultimately included in the analysis . Of the 39 potentially relevant trials additionally identified from http://ClinicalTrials.gov, three were included in the analysis .…”

“…We retrieved a total of 41 trials involving 22 328 patients (14 292 randomized to a treatment group and 8036 to a placebo group) that met the selection criteria. The number of participants used in analyses of the mean number of micturitions in 24 h, mean number of incontinence episodes in 24 h, mean number of urgency episodes in 24 h, mean volume voided/micturition,, mean number of urgency incontinence episodes in 24 h,, and mean number of nocturia episodes were 22 311, 8738, 14 178, 18 763, 10 072, and 9072 patients, respectively. The main characteristics of the 41 trials are described in Table .…”

Perspectives for the pharmacological treatment of overactive bladder syndrome

“…The initial results seem to indicate that the action of the drug begins quickly, reaching maximum blood concentration within 4h after swallowing, and T 1/2 -within 35 h, as a result of which it can be taken once a day. No significant cardiovascular adverse events have been noted so far [2].…”

Expected Next-Generation Drugs Under Development in Relation to Voiding Symptoms

“…A representative candidate antimuscarinic agent, tarafenacin, is known to have superior selectivity to M3 in comparison with M2; it was shown to have 200 times greater selectivity [18] and its characteristics include less constipation than conventional anticholinergic agents and dry mouth as the most common side effect [19]. THVD-201 (Tolenix) and THVD-202 have been developed for a once daily or twice daily regimen, which is combination of tolterodine, an antimuscarinics, and pilocarpine, a modified-release muscarinic agonist [20].…”