For your patients with overactive bladder (OAB)

Rethinq OAB Treatment Rethinq OAB Treatment

Myrbetriq is a β3‑adrenergic agonist indicated for patients with OAB symptoms of urge urinary incontinence, urgency, and urinary frequency.1

Mechanism of Action

Think β3. Think Myrbetriq.

The first and only FDA‑approved β3‑adrenergic agonist.

Myrbetriq is not an antimuscarinic agent.1
It targets a different receptor signaling pathway—
the β3‑adrenergic receptor (AR) pathway.

  • Overactive bladder (OAB) is characterized by involuntary contraction of the detrusor muscle during the storage phase.3
  • Myrbetriq relaxes the detrusor smooth muscle during the storage phase of the urinary bladder fill‑void cycle by activation of the β3‑AR.

As a result, bladder capacity is increased.

  • Mirabegron is an agonist of the human β3‑AR as demonstrated by in vitro laboratory experiments using the cloned human β3‑AR.1
  • Although mirabegron showed very low intrinsic activity for cloned human β1‑AR and β2‑AR, results in humans indicate that β1‑AR stimulation occurred at a mirabegron dose of 200 mg.1

See how Myrbetriq targets the β3‑AR pathway.

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Behavioral therapies may be combined with pharmacologic management as a first‑line treatment option for OAB, according to AUA/SUFU guidelines4

Adapted from AUA/SUFU (American Urological Association/Society of Urodynamics, Female Pelvic Medicine, & Urogenital Reconstruction) guidelines.

Efficacy Summary

Study Design1

Myrbetriq® (mirabegron) was evaluated in three 12‑week, double‑blind, randomized,
placebo‑controlled, parallel‑group, multicenter clinical trials in patients with OAB
with symptoms of urge urinary incontinence, urgency, and urinary frequency (Studies 1, 2, and 3).

Entry Criteria:

  • OAB symptoms for ≥3 months
  • ≥8 micturitions per day
  • ≥3 episodes of urgency with or without incontinence over a 3 day period
MYRBETRIQ Efficacy Summary MYRBETRIQ Efficacy Summary

Patients were randomized to receive:

Efficacy Study 1:

Myrbetriq 50 mg, placebo, or an active control once daily

Efficacy Study 2:

Myrbetriq 50 mg or placebo once daily

Efficacy Study 3:

Myrbetriq 25 mg, Myrbetriq 50 mg, or placebo once daily


Co-primary efficacy endpoints in Studies 1, 2 and 3

Change from baseline to end of treatment (Week 12) in:

Mean number of incontinence episodes per 24 hours

Mean number of micturitions
per 24 hours, based on a
3‑day micturition diary

Secondary endpoint: Change from baseline to end of treatment (Week 12)
in mean volume voided per micturition.


Efficacy evaluated in three 12‑week,
double‑blind, placebo‑controlled Phase III studies1

Demonstrated efficacy for incontinence,
micturition frequency, and volume voided per micturition1


In three 12‑week, double‑blind, placebo‑controlled Phase III studies

Mean change from baseline to final visit§

Placebo (grey), Myrbetriq 25 mg (yellow), Myrbetriq 50 mg (green)
Placebo (grey), Myrbetriq 25 mg (yellow), Myrbetriq 50 mg (green)

Incontinence episodes (co‑primary endpoint||)

Incontinence Episodes: Study 1 Incontinence Episodes: Study 2 Incontinence Episodes: Study 3

Micturition frequency (co‑primary endpoint)

Micturition Frequency: Study 1 Micturition Frequency: Study 2 Micturition Frequency: Study 3

Volume voided per micturition (secondary endpoint)

Volume voided per micturition: Study 1 Volume voided per micturition: Study 2 Volume voided per micturition: Study 3

Myrbetriq was effective in treating
the symptoms of overactive bladder (OAB):

Myrbetriq 25 mg: Within 8 weeks
Myrbetriq 50 mg: Within 4 weeks

The efficacy of
Myrbetriq 25 MG and 50 MG
was maintained through the
12-Week treatment period.1

§Adjusted mean for baseline, gender, and geographic region.
||For incontinence episodes per 24 hours, the analysis population is restricted to patients with ≥1 episode of incontinence at baseline.
This population includes patients randomized to placebo and Myrbetriq 50 mg in Studies 1 and 2.

Safety Profile

Safety evaluated in three 12‑week, double‑blind, placebo‑controlled Phase III studies1**

Percent of patients with adverse reactions derived from all
adverse events >placebo and reported by ≥1% of patients treated with Myrbetriq® (mirabegron) 25 mg or 50 mg once daily in Studies 1, 2, and 31

Placebo Myrbetriq Myrbetriq
(%) 25 mg (%) 50 mg (%)
Number of Patients 1380 432 1375
Hypertensiona 7.6 11.3 7.5
Nasopharyngitis 2.5 3.5 3.9
Urinary Tract Infection (UTI) 1.8 4.2 2.9
Headache 3.0 2.1 3.2
Constipation 1.4 1.6 1.6
Upper Respiratory Tract Infection 1.7 2.1 1.5
Arthralgia 1.1 1.6 1.3
Diarrhea 1.3 1.2 1.5
Tachycardia 0.6 1.6 1.2
Abdominal Pain 0.7 1.4 0.6
Fatigue 1.0 1.4 1.2
aIncludes reports of blood pressure (BP) above the normal range and BP increased from baseline, occuring predominantly in subjects with baseline hypertension.
  • Atrial fibrillation (0.2%) and prostate cancer (0.1%) were reported as serious adverse events by >1 patient and at a rate greater than placebo.
  • The most frequent adverse events (0.2%) leading to discontinuation in Studies 1, 2, and 3 for the 25 mg or 50 mg dose were nausea, headache, hypertension, diarrhea, constipation, dizziness, and tachycardia.

Safety evaluated in a 1‑year, randomized, fixed‑dose, double‑blind, active‑controlled study1††

Percent of patients with adverse reactions derived from all adverse events, reported by >2% of patients treated with Myrbetriq® (mirabegron) 50 mg once daily in the 1‑year safety study1

Myrbetriq Active Controlb
50 mg (%) (%)
Number of Patients 812 812
Hypertension 9.2 9.6
Urinary Tract Infection (UTI) 5.9 6.4
Headache 4.1 2.5
Nasopharyngitis 3.9 3.1
Back Pain 2.8 1.6
Constipation 2.8 2.7
Dry Mouth 2.8 8.6
Dizziness 2.7 2.6
Sinusitis 2.7 1.5
Influenza 2.6 3.4
Arthralgia 2.1 2.0
Cystitis 2.1 2.3
bThe active control in this study was tolterodine extended-release (ER) 4 mg.5
  • Serious adverse events (reported by ≥2 patients and >active control) included cerebrovascular accident (0.4%) and osteoarthritis (0.2%).
  • Serum ALT/AST increased from baseline by greater than 10‑fold in 2 patients (0.3%) taking Myrbetriq 50 mg; these markers subsequently returned to baseline while both patients continued Myrbetriq.
  • Serious adverse events of neoplasm were reported by 0.1%, 1.3%, and 0.5% of patients treated with Myrbetriq 50 mg, 100 mg, and active control once daily, respectively. Neoplasms reported by 2 patients treated with Myrbetriq 100 mg included breast cancer, lung neoplasm malignant, and prostate cancer.
  • Adverse reactions leading to discontinuation in patients treated with Myrbetriq 50 mg (reported by >2 patients and >active control) included constipation (0.9%), headache (0.6%), dizziness (0.5%), hypertension (0.5%), dry eyes (0.4%), nausea (0.4%), vision blurred (0.4%), and urinary tract infection (0.4%).

**In Studies 1, 2, and 3, Myrbetriq was evaluated for safety in 2736 patients. Study 1 also included an active control. For the combined Studies 1, 2, and 3, 432 patients received Myrbetriq 25 mg, 1375 received Myrbetriq 50 mg, and 929 received Myrbetriq 100 mg once daily.
††Myrbetriq was also evaluated for safety in 1632 patients who received Myrbetriq 50 mg once daily (n=812 patients) or Myrbetriq 100 mg (n=820 patients) in a 1‑year study in patients with OAB (Study 4). • Of these patients, 731 received Myrbetriq in a previous 12‑week study. • In Study 4, 1385 patients received Myrbetriq continuously for at least 6 months, 1311 patients received Myrbetriq for at least 9 months, and 564 patients received Myrbetriq for at least 1 year.

Dosing

Convenient, once-daily oral therapy

The recommended starting dose of
Myrbetriq® (mirabegron) is 25 mg orally, once daily1

25 mg, once daily. 50 mg, once daily.
  • Myrbetriq 25 mg can be effective within 8 weeks.1
  • Based on individual patient efficacy and tolerability, the dose may be increased to 50 mg, once daily.1
  • Myrbetriq can be taken with or without food.1
  • Myrbetriq should be taken with water, swallowed whole, and should not be chewed, divided, or crushed.1

There is no generic equivalent
to Myrbetriq

Dose adjustments in special populations1

  • The daily dose of Myrbetriq should not exceed 25 mg once daily in the following populations:
    • Patients with severe renal impairment (CLcr 15 to 29 mL/min or eGFR 15 to 29 mL/min/1.73 m2).
    • Patients with moderate hepatic impairment (Child‑Pugh Class B).
  • Myrbetriq is not recommended for use in patients with end-stage renal disease (ESRD) or in patients with severe hepatic impairment (Child‑Pugh Class C).
  • No dose adjustment is necessary for the elderly.
  • The safety and effectiveness of Myrbetriq in pediatric patients have not been established.

INDICATIONS AND USAGE

Myrbetriq® (mirabegron) is a beta‑3 adrenergic agonist indicated for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency.

IMPORTANT SAFETY INFORMATION

Myrbetriq® (mirabegron) is contraindicated in patients who have known hypersensitivity reactions to mirabegron or any component of the tablet.

Myrbetriq can increase blood pressure. Periodic blood pressure determinations are recommended, especially in hypertensive patients. Myrbetriq is not recommended for use in severe uncontrolled hypertensive patients (defined as systolic blood pressure ≥ 180 mm Hg and/or diastolic blood pressure ≥ 110 mm Hg).

Urinary retention in patients with bladder outlet obstruction (BOO) and in patients taking antimuscarinic medications for the treatment of OAB has been reported in postmarketing experience in patients taking mirabegron. A controlled clinical safety study in patients with BOO did not demonstrate increased urinary retention in Myrbetriq patients; however, Myrbetriq should be administered with caution to patients with clinically significant BOO. Myrbetriq should also be administered with caution to patients taking antimuscarinic medications for the treatment of OAB.

Angioedema of the face, lips, tongue and/or larynx has been reported with Myrbetriq. In some cases angioedema occurred after the first dose. Cases of angioedema have been reported to occur hours after the first dose or after multiple doses. Angioedema associated with upper airway swelling may be life threatening. If involvement of the tongue, hypopharynx, or larynx occurs, promptly discontinue Myrbetriq and initiate appropriate therapy and/or measures necessary to ensure a patent airway.

Since Myrbetriq is a moderate CYP2D6 inhibitor, the systemic exposure to CYP2D6 substrates such as metoprolol and desipramine is increased when co‐administered with Myrbetriq. Therefore, appropriate monitoring and dose adjustment may be necessary, especially with narrow therapeutic index drugs metabolized by CYP2D6, such as thioridazine, flecainide, and propafenone.

In clinical trials, the most commonly reported adverse reactions (> 2% and > placebo) for Myrbetriq 25 mg and 50 mg versus placebo, respectively, were hypertension (11.3%, 7.5% vs 7.6%), nasopharyngitis (3.5%, 3.9% vs 2.5%), urinary tract infection (4.2%, 2.9% vs 1.8%), and headache (2.1%, 3.2% vs 3.0%).

In postmarketing experience, the following events have also occurred: constipation, diarrhea, and dizziness.

Please see accompanying complete Prescribing Information for Myrbetriq® (mirabegron)

REFERENCES

1. Myrbetriq [Prescribing Information]. Northbrook, IL: Astellas Pharma US, Inc. 2. Astellas Pharma US, Inc. Data on File. 3. Chu FM, Dmochowski R. Pathophysiology of overactive bladder. Am J Med. 2006;119(3):3S‑8S. 4. Gormley EA, Lightner DJ, Burgio KL, et al. Diagnosis and Treatment of Overactive Bladder (Non-Neurogenic) in Adults: AUA/SUFU guideline. Linthicum, MD: American Urological Association Education and Research, Inc.; 2014:1‑57. 5. Khullar V, Amarenco G, Angulo JC, et al. Efficacy and tolerability of mirabegron, a β3‑adrenoceptor agonist, in patients with overactive bladder: results from a randomised European–Australian phase 3 trial. Eur Urol. 2013;63:283‑295.

Important Safety Information,
Indications and Usage

INDICATIONS AND USAGE

Myrbetriq® (mirabegron) is a beta‑3 adrenergic agonist indicated for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency.

IMPORTANT SAFETY INFORMATION

Myrbetriq® (mirabegron) is contraindicated in patients who have known hypersensitivity reactions to mirabegron or any component of the tablet.

Myrbetriq can increase blood pressure. Periodic blood pressure determinations are recommended, especially in hypertensive patients. Myrbetriq is not recommended for use in severe uncontrolled hypertensive patients (defined as systolic blood pressure ≥ 180 mm Hg and/or diastolic blood pressure ≥ 110 mm Hg).

Urinary retention in patients with bladder outlet obstruction (BOO) and in patients taking antimuscarinic medications for the treatment of OAB has been reported in postmarketing experience in patients taking mirabegron. A controlled clinical safety study in patients with BOO did not demonstrate increased urinary retention in Myrbetriq patients; however, Myrbetriq should be administered with caution to patients with clinically significant BOO. Myrbetriq should also be administered with caution to patients taking antimuscarinic medications for the treatment of OAB.

Angioedema of the face, lips, tongue and/or larynx has been reported with Myrbetriq. In some cases angioedema occurred after the first dose. Cases of angioedema have been reported to occur hours after the first dose or after multiple doses. Angioedema associated with upper airway swelling may be life threatening. If involvement of the tongue, hypopharynx, or larynx occurs, promptly discontinue Myrbetriq and initiate appropriate therapy and/or measures necessary to ensure a patent airway.

Since Myrbetriq is a moderate CYP2D6 inhibitor, the systemic exposure to CYP2D6 substrates such as metoprolol and desipramine is increased when co‐administered with Myrbetriq. Therefore, appropriate monitoring and dose adjustment may be necessary, especially with narrow therapeutic index drugs metabolized by CYP2D6, such as thioridazine, flecainide, and propafenone.

In clinical trials, the most commonly reported adverse reactions (> 2% and > placebo) for Myrbetriq 25 mg and 50 mg versus placebo, respectively, were hypertension (11.3%, 7.5% vs 7.6%), nasopharyngitis (3.5%, 3.9% vs 2.5%), urinary tract infection (4.2%, 2.9% vs 1.8%), and headache (2.1%, 3.2% vs 3.0%).

In postmarketing experience, the following events have also occurred: constipation, diarrhea, and dizziness.

Please see accompanying complete Prescribing Information for Myrbetriq® (mirabegron)