GlaxoSmithKline and Theravance commence MABA Phase IIb COPD study

Issued: Philadelphia PA

GlaxoSmithKline (GSK) and Theravance (NASDAQ:  THRX) announced today that the first patient has started treatment with an investigational inhaled bifunctional compound GSK961081 (‘081) in a Phase IIb study to evaluate efficacy and safety in patients with moderate to severe chronic obstructive pulmonary disease (COPD).

‘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.

Study design

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.

GlaxoSmithKline – one of the world’s leading research-based pharmaceutical and healthcare companies – is committed to improving the quality of human life by enabling people to do more, feel better and live longer.  For further information please visit www.gsk.com.

Theravance - is a biopharmaceutical company with a pipeline of internally discovered product candidates. Theravance is focused on the discovery, development and commercialization of small molecule medicines across a number of therapeutic areas including respiratory disease, bacterial infections and gastrointestinal motility dysfunction. The company's key programmes include: the RELOVAIR™ programme and Bifunctional Muscarinic Antagonist-Beta2 Agonist (MABA) programme, both with GlaxoSmithKline plc, and VIBATIV™ (telavancin) with Astellas Pharma Inc. By leveraging its proprietary insight of multivalency toward drug discovery, Theravance is pursuing a best-in-class strategy designed to discover superior medicines in areas of significant unmet medical need. For more information, please visit the company's web site at www.theravance.com.

THERAVANCE®, the Theravance logo, and MEDICINES THAT MAKE A DIFFERENCE® are registered trademarks of Theravance, Inc.

VIBATIV is a trademark of Astellas Pharma Inc.

RELOVAIR is a trademark of Glaxo Group Limited.  Mark is intended for U.S. and subject to FDA approval.

GlaxoSmithKline enquiries:

Theravance, Inc. enquiries:

Michael W. Aguiar
Senior Vice President and Chief Financial Officer
(650) 808 4100
Investor.relations@theravance.com