In 2020, lung cancer was the second most common type of cancer in the world and the most lethal. Due to the high mortality rate and the low efficiency of available treatments, there is the need for more efficient approaches to fight this disease. In this regard, the use of already approved pharmaceuticals for other purposes can be valuable. Thus, the study aimed to assess the potential application of beta-blockers, alone or combined with cytostatic drugs. The effects of the β-blockers propranolol (10, 25, 50, 100, 125, 150, 200 and 250 µM) and carvedilol (0.1, 1, 5, 10, 20, 60, 75 and 100 µM) and cytostatic drugs cisplatin (1, 5, 20, 50, 100, 150, 200, and 250 µM) and etoposide (0.005, 0.1, 0.5, 1, 2.5, 5, 7.5 and 10 µM) were evaluated in cancer cell lines, A549 and H460, at different time points (24/48/72h), through cell viability. Overall, A549 demonstrated higher sensitivity to propranolol, cisplatin, and etoposide and H460 was more sensitive to carvedilol. The study of combined effects of beta-blockers and cytostatic drugs revealed the potential value of beta-blockers in the treatment of cancer.