MYRBETRIQ- mirabegron tablet, film coated, extended release
Astellas Pharma US, Inc.
1 INDICATIONS AND USAGE
MYRBETRIQ� is a beta-3 adrenergic agonist indicated for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency.
2 DOSAGE AND ADMINISTRATION
2.1 Dosing Information
The recommended starting dose of MYRBETRIQ� is 25 mg once daily with or without food. MYRBETRIQ� 25 mg is effective within 8 weeks. Based on individual patient efficacy and tolerability the dose may be increased to 50 mg once daily [see Clinical Studies (14)].
MYRBETRIQ� should be taken with water, swallowed whole and should not be chewed, divided, or crushed.
2.2 Dose Adjustments in Specific Populations
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) [see Use in Specific Populations (8.6) and Clinical Pharmacology (12.3)].
�
Patients with moderate hepatic impairment (Child-Pugh Class B) [see Use in Specific Populations (8.7) and Clinical Pharmacology (12.3)].
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) [see Use in Specific Populations (8.6, 8.7) and Clinical Pharmacology (12.3)].
3 DOSAGE FORMS AND STRENGTHS
MYRBETRIQ� extended-release tablets are supplied in two different strengths as described below:
� 25 mg oval, brown, film coated tablet, debossed with the Astellas logo (Astellas logo) and "325"
� 50 mg oval, yellow, film coated tablet, debossed with the Astellas logo (Astellas logo) and "355"
DESCRIPTION
Mirabegron is a beta-3 adrenergic agonist. The chemical name is 2-(2-aminothiazol-4-yl)-N-[4-(2-{[(2R)-2-hydroxy-2-phenylethyl]amino}ethyl)phenyl]acetamide having an empirical formula of C21 H24 N4 O2 S and a molecular weight of 396.51
Mirabegron is a white powder. It is practically insoluble in water (0.082 mg/mL). It is soluble in methanol and dimethyl sulfoxide.
Each MYRBETRIQ� extended-release tablet, for oral administration contains either 25 mg or 50 mg of mirabegron and the following inactive ingredients: polyethylene oxide, polyethylene glycol, hydroxypropyl cellulose, butylated hydroxytoluene, magnesium stearate, hypromellose, yellow ferric oxide, and red ferric oxide (25 mg tablet only).
12 CLINICAL PHARMACOLOGY
12.1 Mechanism of Action
Mirabegron is an agonist of the human beta-3 adrenergic receptor (AR) as demonstrated by in vitro laboratory experiments using the cloned human beta-3 AR. Mirabegron relaxes the detrusor smooth muscle during the storage phase of the urinary bladder fill-void cycle by activation of beta-3 AR which increases bladder capacity. Although mirabegron showed very low intrinsic activity for cloned human beta-1 AR and beta-2 AR, results in humans indicate that beta-1 AR stimulation occurred at a mirabegron dose of 200 mg.
