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BREZTRI AEROSPHERE – an ICS, LABA, LAMA combination inhaler1

The BREZTRI AEROSPHERE inhaler and packaging

BREZTRI AEROSPHERE contains 3 active substances; budesonide (ICS), glycopyrronium (LAMA), and formoterol fumarate dihydrate (LABA) 
in 1 pMDI device.*

The combination of these substances—with different mechanisms of action—results in increased efficacy compared to use with any of the dual component therapies.

Budesonide, glycopyrronium, and formoterol fumarate dihydrate mechanisms of action (MOAs)

Budesonide Inhaled corticosteroid (ICS)

  • Budesonide is a glucocorticosteroid that when inhaled, has a rapid onset of action (within hours) and dose dependent anti-inflammatory action in the airways.
    • This results in reduced symptoms, and fewer COPD exacerbations.
  • Inhaled budesonide has less severe effects than systemic corticosteroids.

Glycopyrronium Long-acting muscarinic antagonist (LAMA)

  • Glycopyrronium is a bronchodilator with a rapid onset of action, and a similar affinity to the muscarinic receptor subtypes M1 to M5.
    • This results in the inhibition of the M3 receptor at the smooth muscle.

Formoterol fumarate dihydrate Long-acting beta2-andrenergic agonist (LABA)

  • Formoterol fumarate dihydrate is a bronchodilator with a rapid onset of action.
    • This results in the direct relaxation of smooth muscle in the airways, because of the increase in cAMP through activation of adenylate cyclase.

As a consequence of the differential density of muscarinic receptors and beta2-adrenoceptors in the central and peripheral airways of the lung:

  • Muscarinic antagonists are more effective in relaxing central airways
  • Beta2-adrenergic agonists are more effective in relaxing peripheral airways

Relaxation of both central and peripheral airways with combination treatment may contribute to its beneficial effects on lung function.

Pharmacodynamics:Pharmaco-dynamics: BREZTRI AEROSPHERE achieved rapid onset of action*

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Improvement in FEV1 was within 5 minutes of the first dose on Day 1 (median time to ≥100 mL)

See the lung function outcomes from the BREZTRI AEROSPHERE clinical trials.

View data

* Clinical significance has not been established.

cAMP: cyclic adenosine monophosphate; COPD: chronic obstructive pulmonary disease; FEV1: forced expiratory volume in one second; ICS: inhaled corticosteroid; LABA: long-acting beta2-adrenergic agonist; LAMA: long-acting muscarinic antagonist; MOA: mechanism of action; pMDI: pressurized metered-dose inhaler.

Reference:

  1. BREZTRI AEROSPHERE Product Monograph. AstraZeneca Canada Inc.