Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 58, Issue 10, Pages 4131-4164Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm5013227
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- Catholic University of the Sacred Heart
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Inhaled bronchodilators, including long-acting muscarinic receptor antagonists (LAMA) and long-acting beta(2)-adrenoreceptor agonists (LABA), are the mainstay of pharmacological treatment of stable chronic obstructive pulmonary disease (COPD). Among approved LAMA, tiotropium bromide, glycopyrronium bromide, and umeclidinium bromide at administered once daily, whereas aclidinium bromide is administered every 12 h. New LAMA are Under development for COPD. Among the approved LABA, indacaterol has a 24 h duration of action, whereas salmeterol and formoterol require twice-daily administration. New once-daily LABA, including vilanterol, olodaterol, milveterol, carmoterol, and abediterol, are in development. LAMA/LABA fixed dose combinations (FDCs) provide the convenience of two bronchodilators with different mechanism of action in a single inhaler. Indacaterol/glycopyrronium, umeclidinium/vilanterol, and olodaterol/tiotropium FDCs have been approved or are under approval and are likely to become a standard pharmacological Strategy for COPD. Inhaled dual-pharmacology compounds, combining muscarinic antagonism and beta(2)-agonism (MABA) in a single molecule, potentially provide additive or synergistic bronchodilation over either inhaled antimuscarinic or beta(2)-agonist monotherapy.
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