Novel dual PDE3/PDE4 inhibitor shows promise in COPD

In the treatment of patients with chronic obstructive pulmonary disease (COPD), the investigational dual phosphodiesterase (PDE) 3 and 4 inhibitor TQC3721 helps improve lung function, according to a phase 2 PACER-II study.

PACER-II was conducted across 27 tertiary centres in China and included COPD patients receiving background therapy with single or dual long-acting bronchodilators. Patients were required to have post-bronchodilator FEV1 of 30% to 70% of predicted and FEV1/FVC <0.7.

A total of 240 patients were randomly assigned to receive TQC3721 at 3 or 6 mg or placebo twice daily for 4 weeks. Change in peak FEV1 at week 4 was assessed as the primary endpoint.

Of the patients, 28.8 percent and 71.2 percent were receiving concomitant long-acting muscarinic antagonists (LAMAs) or long-acting β2-agonists (LABAs)/LAMAs, respectively, at baseline.

At week 4, peak FEV1 significantly improved with TQC3721 at both 3 and 6 mg than with placebo (mean differences, 100 and 147 mL, respectively; p=0.0011 and p<0.0001).

Compared with placebo, 6-mg TQC3721 was also associated with substantial improvements in average FEV1 area under the curve at 0–12 h (87 mL; p<0.0001) and symptoms (St George’s Respiratory Questionnaire score, –5.09; p=0.0031).

In subgroup analyses, 6-mg TQC3721 was associated with significantly greater improvement in peak FEV1 at week 4 compared with placebo for patients on background LAMA (mean difference, 239 mL; p<0.0001) and for those on background LABA/LAMA (mean difference, 109 mL; p=0.0006).

Safety findings did not significantly differ between TQC3721 and placebo.