Which generation of drugs are brigatinib/brigatinib? Is it a targeted drug?

Brigatinib is a second-generation targeted drug that is an ALK inhibitor. Targeted drugs refer to drugs that specifically act on specific molecules or signaling pathways in tumor cells to achieve therapeutic effects. Brigatinib can inhibit the ALK protein, thereby blocking the growth and spread of tumor cells. Compared with traditional chemotherapy, targeted drugs are more selective and specific, can reduce damage to normal cells and improve treatment effects. The emergence of brigatinib provides a new treatment option for patients with ALK-positive non-small cell lung cancer.

Brigatinib is an orally active tyrosine kinase inhibitor (TKI) that is 12 times more potent than crizotinib in inhibiting the kinase. It also inhibits ROS1 kinase and has shown preclinical activity against several ALK mutations that underlie the clinical impermeability of crizotinib. Multiple doses of brigatinib (30-300 mg) evaluated in the clinical trial phase found an objective response rate (ORR) of 72% in 71 patients with ALK-positive progressive non-small cell lung cancer pretreated with crizotinib, with a higher ORR of 54% in the 180 mg group and 45% in the 90 mg group. Likewise, the median progression-free survival was 12.9 months and 9.2 months, respectively.

Brigatinib is considered a miracle drug because it is ineffective against all otherALK inhibitors such as oxirtinib, lorlatinib, etc. Specifically, spatially arranged mutations in ALK represent the majority of cases that are resistant to other ALK inhibitors. Examination of all preclinical data demonstrates that brigatinib is more active and survivable against various drugs that cause G1202R and L1196M mutations in ALK than other established inhibitors.