batefenterol (GSK961081) / GSK - LARVOL DELTA

Pharmacological Characterization of MABA, GSK961081 on Human Airway Smooth Muscle Cells (ATS 2017) - "The dual-acting muscarinic receptor antagonist and β2-adrenoceptor agonist (MABA) GSK961081 is a considerably more potent activator of cAMP release from ASMC than either salbutamol or GSK1143101A the LABA-containing portion of the MABA molecule.nStudy sponsored by GlaxoSmithKline, UK."

Combination therapy • Asthma • Biosimilar • Chronic Obstructive Pulmonary Disease • Immunology

A randomized, controlled, repeat-dose study of batefenterol/fluticasone furoate compared with placebo in the treatment of COPD. (PubMed, BMC Pulm Med) - P2 | "Six weeks of BAT/FF 300/100 treatment was non-inferior to placebo for change from baseline in HR, with no new clinically relevant general or cardiovascular safety signals."

Clinical • Journal

Pharmacological profile of AZD8871 (LAS191351), a novel inhaled dual M3 receptor antagonist/b2-adrenoceptor agonist molecule with long-lasting effects and favorable safety profile. (PubMed, J Pharmacol Exp Ther) - "AZD8871 exhibits a higher muscarinic component than batefenterol in human bronchi, with a shift in potency under propranolol blockade of 2- and 6-fold, respectively, together with a persisting relaxation (5.3% recovery at 8 hours). Thus, AZD8871 has the potential to be a next generation of inhaled bronchodilators in respiratory diseases. SIGNIFICANCE STATEMENT: N/A."

Clinical • Journal

Randomized dose-finding study of batefenterol via dry powder inhaler in patients with COPD (Dovepress) - P=NA, N=323; "Batefenterol 300 µg may represent the optimal dose for Phase III studies."

Clinical data