Bisoprolol Fumarate

The Bisoprolol in COPD Study (BICS) randomized 515 high‑risk COPD patients to bisoprolol or placebo. Despite a standardized titration protocol, the primary outcome — annualized patient‑reported exacerbations treated with corticosteroids or antibiotics — showed no difference between groups (2.03 vs. 2.01, adjusted rate ratio 0.97, 95% CI 0.84‑1.13; P=0.72). Serious adverse events were similar. The trial was underpowered due to COVID‑19‑related suspension. Bisoprolol does not reduce COPD exacerbation frequency in this population.

Fig. 1 Freedom From Exacerbation of Chronic Obstructive Pulmonary Disease in the 2 Trial Groups. (Devereux G, et al., 2024)

Two bisoprolol derivatives, N‑acetyl bisoprolol and N‑formyl bisoprolol, were synthesized with yields of 32.4% and 20.2%. In silico docking showed highest binding affinity to the beta‑1 adrenergic receptor (PDB: 4BVN), with binding energies of −6.74, −7.03, and −7.63 kcal/mol for bisoprolol and the two derivatives, respectively. Molecular dynamics confirmed complex stability. SwissADME predicted similar properties to the parent drug. These derivatives may have antihypertensive potential.

Fig. 2 Binding energy of bisoprolol (compound 1, blue), N-acetyl bisoprolol (compound 3, yellow) and N-formyl bisoprolol (compound 5, green) with six target proteins through molecular docking simulations. (Oktaviani NPS, et al., 2023)