886 the Efficacy and Tolerability of Mirabegron in Patients With Overactive Bladder – Results From a European–australian Phase Iii Trial

Khullar, Vik; Cambronero, J.; Ströberg, Peter; Angulo, Javier; Boerrigter, Peter J.; Blauwet, Mary Beth; Wooning, M.

doi:10.1016/s1569-9056(11)60870-1

Cited by 37 publications

(20 citation statements)

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“…The results of two pivotal phase 3 clinical trials for mirabegron confirmed that mirabegron significantly improves key OAB symptoms, urinary incontinence and frequency of micturition (Khullar et al, 2011;Nitti et al, 2011). Overall, the incidence of treatment-emergent adverse events in mirabegron groups was low across studies, and mirabegron was generally well tolerated (Chapple et al, 2010;Khullar et al, 2011;Nitti et al, 2011). The therapeutic dose is 50 mg in extended-release formulations once daily.…”

Section: Introductionmentioning

confidence: 92%

“…In a phase 2 dose-ranging study to evaluate the efficacy of mirabegron versus placebo in patients with OAB, mirabegron at doses of 50, 100, and 200 mg in extended-release formulations once daily had superior efficacy results compared with placebo (Chapple et al, 2010). The results of two pivotal phase 3 clinical trials for mirabegron confirmed that mirabegron significantly improves key OAB symptoms, urinary incontinence and frequency of micturition (Khullar et al, 2011;Nitti et al, 2011). Overall, the incidence of treatment-emergent adverse events in mirabegron groups was low across studies, and mirabegron was generally well tolerated (Chapple et al, 2010;Khullar et al, 2011;Nitti et al, 2011).…”

Section: Introductionmentioning

confidence: 93%

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Absorption, Metabolism and Excretion of [¹⁴C]Mirabegron (YM178), a Potent and Selective β₃-Adrenoceptor Agonist, after Oral Administration to Healthy Male Volunteers

Takusagawa¹,

Lier²,

Suzuki³

et al. 2012

Drug Metab Dispos

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ABSTRACT:The mass balance and metabolite profiles of 2-(2- total of 10 metabolites were found in urine. On the basis of the metabolites found in urine, major primary metabolic reactions of mirabegron were estimated to be amide hydrolysis (M5, M16, and M17), accounting for 48% of the identified metabolites in urine, followed by glucuronidation (M11, M12, M13, and M14) and N-dealkylation or oxidation of the secondary amine (M8, M9, and M15), accounting for 34 and 18% of the identified metabolites, respectively. In feces, the radioactivity was recovered almost entirely as the unchanged form. Eight of the metabolites characterized in urine were also observed in plasma. These findings indicate that mirabegron, administered as a solution, is rapidly absorbed after oral administration, circulates in plasma as the unchanged form and metabolites, and is recovered in urine and feces mainly as the unchanged form.amino

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Section: Introductionmentioning

confidence: 92%

Section: Introductionmentioning

confidence: 93%

Absorption, Metabolism and Excretion of [¹⁴C]Mirabegron (YM178), a Potent and Selective β₃-Adrenoceptor Agonist, after Oral Administration to Healthy Male Volunteers

Takusagawa¹,

Lier²,

Suzuki³

et al. 2012

Drug Metab Dispos

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“…These data were presented for the first time at the 26th Annual Congress of the European Association of Urology, in Vienna, Austria, 18-22 March 2011 [9,10]. After 12 weeks of treatment with mirabegron once-daily, significant improvements from baseline were seen in the co-primary end points, incontinence episodes per 24 h and micturitions per 24 h, compared with placebo (p < 0.05).…”

Section: Mirabegronmentioning

confidence: 99%

Industry Update: the Latest Developments in Therapeutic Delivery

Rees¹

2011

Therapeutic Delivery

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The present Industry Update covers the period 16 March to 15 April 2011, with information sourced from company press releases, media newswires, regulatory agencies and relevant patent offices. There was considerable activity in the area of ‘Business development’; however for reasons of brevity, only those, which in my view, are most relevant are included. Cephalon continues to build its business through acquisitions, in this case the privately held company Gemin X, which has a promising portfolio of targeted cancer therapeutics. SuperGen and Astex Therapeutics have agreed a merger from which Astex Pharmaceuticals will emerge as a stronger commercial entity with critical mass that may find itself a prospective acquisition in the future. Pfizer have agreed to off-load Capsugel to KKR at a cost of US$2.375 billion in cash. A significant number of licensing deals have also taken place, a notable number involving large Japanese pharmaceutical companies. A rash of product approvals occurred both in the EU and the USA following the pre- and post-christmas lull, and positive top-line results from two Phase III multiple sclerosis trials involving laquinimod and dimethyl fumarate, were of particular interest. An exciting range of journal publications also appeared relating to potential therapeutic targets or targeting strategies including the LNA-based compounds developed by Santaris Pharma, identification of inhibitors of the Wnt signaling pathway, and the synthesis and evaluation of the multimodal porphysome nanovesicles.

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“…A phase III trial in Europe and Australia examined the efficacy and tolerability of mirabegron in patients with OAB 14. Patients received either placebo, mirabegron 50 mg, mirabegron 100 mg, or extended-release tolterodine 4 mg once daily for 4 weeks.…”

Section: Efficacy Studies Including Comparative Studiesmentioning

confidence: 99%

“…The larger phase III European-Australian RCT14 reported incidence rates for adverse events to be 43.3%, 46.7%, 42.8%, and 40.1%, for the placebo, tolterodine slow-release, and mirabegron 50 and 100 mg groups, respectively. The incidence of hypertension was 7.7%, 8.1%, 5.9%, and 5.4%, dry mouth was 2.6%, 10.1%, 2.8%, and 2.8%, and headache was 2.8%, 3.6%, 3.7%, and 1.8% for the respective groups.…”

Section: Safety and Tolerability Patient-focused Perspectives Qol mentioning

confidence: 99%

Mirabegron – a selective ß3-adrenoreceptor agonist for the treatment of overactive bladder

Bhide¹,

Digesu²,

Fernando³

et al. 2012

RRU

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Overactive bladder is a common condition that significantly impacts overall quality of life. Antimuscarinics are the current main pharmacological option for treatment; however, many patients fail to adhere to therapy due to troublesome side effects. Mirabegron is a new beta-3 adrenoreceptor agonist which causes detrusor smooth muscle relaxation and has been proposed to be effective for treating overactive bladder symptoms. Mirabegron has been shown to be superior to placebo for reducing the mean number of incontinence episodes per 24 hours and the mean number of micturitions per 24 hours. Side effects such as dry mouth were observed at similar or lower rates than those seen for placebo and antimuscarinics. Higher doses of mirabegron were associated with minor increases in pulse rate and mean blood pressure. Mirabegron offers a new alternative for treating overactive bladder in patients for which antimuscarinics are either not tolerated or not appropriate.

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886 the Efficacy and Tolerability of Mirabegron in Patients With Overactive Bladder – Results From a European–australian Phase Iii Trial

Cited by 37 publications

References 0 publications

Absorption, Metabolism and Excretion of [¹⁴C]Mirabegron (YM178), a Potent and Selective β₃-Adrenoceptor Agonist, after Oral Administration to Healthy Male Volunteers

Absorption, Metabolism and Excretion of [¹⁴C]Mirabegron (YM178), a Potent and Selective β₃-Adrenoceptor Agonist, after Oral Administration to Healthy Male Volunteers

Industry Update: the Latest Developments in Therapeutic Delivery

Mirabegron – a selective ß3-adrenoreceptor agonist for the treatment of overactive bladder

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886 the Efficacy and Tolerability of Mirabegron in Patients With Overactive Bladder – Results From a European–australian Phase Iii Trial

Cited by 37 publications

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Absorption, Metabolism and Excretion of [14C]Mirabegron (YM178), a Potent and Selective β3-Adrenoceptor Agonist, after Oral Administration to Healthy Male Volunteers

Absorption, Metabolism and Excretion of [14C]Mirabegron (YM178), a Potent and Selective β3-Adrenoceptor Agonist, after Oral Administration to Healthy Male Volunteers

Industry Update: the Latest Developments in Therapeutic Delivery

Mirabegron &ndash; a selective &szlig;3-adrenoreceptor agonist for the treatment of overactive bladder

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Absorption, Metabolism and Excretion of [¹⁴C]Mirabegron (YM178), a Potent and Selective β₃-Adrenoceptor Agonist, after Oral Administration to Healthy Male Volunteers

Absorption, Metabolism and Excretion of [¹⁴C]Mirabegron (YM178), a Potent and Selective β₃-Adrenoceptor Agonist, after Oral Administration to Healthy Male Volunteers

Mirabegron – a selective ß3-adrenoreceptor agonist for the treatment of overactive bladder