GSK2239633 FTIH Study

GSK2239633 is a human chemokine receptor 4 (CCR4) antagonist with a novel anti-inflammatory profile acting mainly on a subset of Th2 cells, with potential for the oral treatment of all severities of asthma. Inhibition of the CCR4 receptor represents a target for asthma because of the potential to inhibit Th2 cell chemotaxis and the subsequent effects of limiting Th2 cell involvement in both the acute and chronic inflammatory response. Recent data in man suggests that the CCR4 receptor ligands (thymus and activation-regulated chemokine (TARC) and macrophage-derived chemokine (MDC)) may be important in asthma and in the development of Allergic Bronchopulmonary Aspergillosis (ABPA). This will provide a unique opportunity to differentiate GSK2239633 significantly from other oral non-steroidal asthma treatments. This study is the first administration of oral GSK2239633 in humans. Two alternating cohorts of 12 subjects will receive 3 single, ascending doses of oral GSK2239633 or placebo. In addition, one cohort will receive a single dose of GSK2239633 or placebo following the standard FDA high fat/high calorie meal. Safety will be monitored (ECGs, telemetry, vital signs, clinical laboratory assessments, adverse events), and blood samples will be taken for pharmacokinetic and pharmacodynamic analysis.