'081 is a single molecule functioning as both a muscarinic antagonist and a beta2 receptor agonist (MABA).
Darrell Baker, SVP, Respiratory & Immuno-Inflammation, Medicines Development Centre, GSK said "We are excited with the progress that we are making with this molecule, which has the potential to be an important new treatment option for patients living with COPD."
Mathai Mammen, SVP, Research & Early Clinical Development of Theravance said, "This MABA compound was developed through Theravance's research of secondary binding clefts on both the beta2 and muscarinic receptors."
'081 is an investigational compound within the inhaled bifunctional muscarinic antagonist-beta2 agonist (MABA) programme that was licensed to GSK from Theravance in 2005 under the terms of the companies' Strategic Alliance Agreement.
The overall aim of this Phase IIb study is to evaluate the safety and efficacy of '081 administered both once daily, QD and twice daily, BID, over a 28 day period to allow the selection of a well tolerated and efficacious dose and dosing interval to take forward into Phase III development.
The study is a multi-centre, randomised, double-blind and double dummy, placebo and active-controlled, eight-arm, parallel-group study with '081.
Approximately 425 patients with moderate/severe COPD will be randomised in order to achieve 357 evaluable patients.
The primary objective is to evaluate dose response, dose interval, efficacy, and safety of '081 by studying three QD doses (100mcg, 400mcg, and 800mcg) and three BID doses (100mcg, 200mcg, 400mcg) and the active comparator salmeterol 50mcg BID compared with placebo delivered by DISKUS™ in patients with COPD.
The primary efficacy endpoint will be change from baseline in a.m. trough forced expiratory volume in one second (FEV1) on Day 29. Secondary endpoints will include serial FEV1 measures and use of salbutamol rescue medication.
The study is being conducted in centres throughout Europe and South Africa.