GSK-2269557 (nemiralisib), a PI3Kδ inhibitor, is in development as an anti-inflammatory drug for the treatment of inflammatory airways disease. Studies in moderate or severe stable COPD patients have shown an acceptable safety and tolerability profile when GSK-2269557 was administered via inhalation. Cough was the most commonly reported adverse event.

Cevipabulin is a synthetic, water-soluble tubulin-binding agent with potential antineoplastic activity. Cevipabulin appears to bind at the vinca-binding site on tubulin but seems to act more similar to taxane-site binding agents in that it enhances tubulin polymerization and does not induce tubulin depolymerization. The disruption in microtubule dynamics may eventually inhibit cell division and reduce cellular growth.

Sanofi aventis developed saredutant (also known as SR 48968C) as a tachykinin neurokinin-2 (NK2) receptor antagonist for the treatment of depressive disorders and generalized anxiety disorder. This drug participated in phase III clinical trials in patients with a generalized anxiety disorder and as Combination Treatment for major depressive disorder, however, the drug failed to meet efficacy endpoints. It is known that NK-2 receptor mediates airway obstruction that is why saredutant was studied as a potential treatment of asthma. However, all studies of the drug were discontinued.

Batefenterol, previously known as GSK961081, a bifunctional muscarinic (M2 and M3 receptors) antagonist β2-agonist that is developed for chronic obstructive pulmonary disease (COPD). The drug has successfully completed phase II clinical trials with clinically significant improvements in lung function. No new or unexpected safety signals were observed in this COPD population. The conclusion from the trial was following that batefenterol 300 µg might represent the optimal dose for Phase III studies.

PF-04634817 is a small molecule chemokine CCR2 and CCR5 receptor dual antagonist. Treatment with PF-04634817 was associated with a modest improvement in best-corrected visual acuity, which was inferior to intravitreal ranibizumab. Analysis of the primary endpoint, Urine Albumin-to-Creatinine Ratio, indicated a modest effect of PF-04634817 in reducing albuminuria in subjects with type 2 diabetes who received angiotensin receptor blocker therapy after 12 weeks of treatment. Despite the tolerable safety profile shown by PF-04634817, clinical development was discontinued in light of the modest efficacy observed.