Basic Information
Developed by GlaxoSmithKline (GSK), sulphide bromide was first approved by Health Canada on April 17, 2014, and then obtained by the European Medicines Agency (EMA) on April 28, 2014. Approved for listing, then approved by the US Food and Drug Administration (FDA) on April 30, 2014, and later approved by the Japan Pharmaceutical and Medical Device Administration (PMDA) on March 26, 2015. Marketed by GSK under the trade names Incruse Ellipta®, Incruse® and Encruse®.
Indole bromide is a long-acting, competitive and reversible muscarinic choline receptor antagonist (mAChRs) that maintains bronchiectasis. This drug is indicated for the treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD).
Incruse Ellipta® is an inhaled powder containing 62.5 μg of indole bromide. The recommended dose is 62.5 μg per inhalation (inhalation once) once daily.
Structural formula
Mechanism
Indole bromide is a long-acting choline receptor antagonist (LAMA) that relaxes bronchial smooth muscle. The kinetic selectivity for the M3 receptor is higher than that of the M2 receptor, and the dissociation with the M3 receptor is slower than M2. It has anti-parasympathetic effects and can inhibit the action of the M3 receptor.
synthetic route
Research key data
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