GSK Initiates Phase I Study With Theravance Medicine for COPD

Theravance has announced that GlaxoSmithKline (GSK) has enrolled the first subjects in a Phase I clinical study designed to assess the safety, tolerability and pharmacokinetics of Theravance's investigational, inhaled bronchodilator, GSK656398 (formerly known as TD-5742), for the treatment of chronic obstructive pulmonary disease (COPD).

GSK656398 is an inhaled, long-acting muscarinic antagonist (LAMA) discovered by Theravance through the application of multivalent drug design in a drug discovery program dedicated to finding new medicines for respiratory disease such as COPD and asthma. The LAMA program is one of three respiratory programs under joint development by GSK and Theravance. Inhaled muscarinic antagonists are among the most frequently used bronchodilators for COPD and work by inhibiting muscarinic receptors on lung airways, which lead to bronchodilation and improved lung function.

Theravance's intent with the research program was to discover inhaled LAMAs that produce prolonged blockade of airway muscarinic receptors as a result of being highly lung-retained. Higher lung retention should also lead to lower concentrations of drug in the systemic circulation, an approach that could result in improved tolerability over the market leader at doses with comparable efficacy.