Which genes does brigatinib target?

Brigatinib is a highly efficient and selective second-generation tyrosine kinase inhibitor that has shown significant effects in the treatment of lung cancer, especially targeting certain genetic mutations.

ALKGene:

The ALK (Anaplastic Lymphoma Kinase, anaplastic lymphoma kinase) gene is a key target in non-small cell lung cancer. When the ALK gene is rearranged or fused, it becomes abnormally activated, driving tumor growth.

Brigatinib can precisely inhibit the activity of ALK, thereby blocking the proliferation signals of tumor cells. Clinical trials have shown that brigatinib can significantly prolong progression-free survival (PFS) and overall survival (OS) for patients with ALK-positive non-small cell lung cancer.

ROS1Gene:

ROS1 (c-ros oncogene 1, proto-oncogene1tyrosine kinase) is another commonly mutated gene in non-small cell lung cancer. Similar to ALK, ROS1 gene fusion can also lead to abnormal proliferation of tumor cells.

Brigatinib can also inhibit the activity of ROS1 and has a good therapeutic effect on ROS1 positive lung cancer patients. Studies have shown that brigatinib can significantly shrink tumors and delay disease progression in these patients.

EGFRGene:

Mutations in the EGFR (Epidermal Growth Factor Receptor, epidermal growth factor receptor) gene are also common in non-small cell lung cancer. Although brigatinib was not originally designed for EGFR, studies have found that it also has certain inhibitory effects on certain EGFR mutations.

This means that brigatinib may provide an additional treatment option for some patients with EGFR mutations. However, its effectiveness may be more limited compared with inhibitors that specifically target EGFR.

References:

https://go.drugbank.com/drugs/DB12267