GSK159802 is a potent, inhaled, long acting selective beta-2-receptor agonist (LABA), which
is being developed for once daily treatment of asthma and COPD as part of a combination
product with a once daily inhaled corticosteroid and also as a standalone product for the
treatment of COPD. Stimulation of the beta-2-agonist in the lung mainly relaxes bronchial
smooth muscle cells which results in bronchodilation. Unwanted systemic side effects related
with beta-2-agonist treatment such as tachycardia, tremor, hyperglycemia and hypokalemia are
limited by local administration and also tend to show tachyphylaxis.
The LABAs that are currently available (e.g., salmeterol, formoterol) require twice-daily
administration, given their duration of action. Therefore, there is significant opportunity
for a once-daily inhaled medication to improve patient compliance and overall disease
management by providing sustained, 24-hour bronchodilation.