Detailed description of the main targets and mechanisms of action of Ceritinib/Ceritinib (Zanda)

Ceritinib (Ceritinib) is an oral small molecule targeted drug that mainly acts on anaplastic lymphoma kinase (ALK). In some patients with non-small cell lung cancer (NSCLC), rearrangement of the ALK gene can lead to abnormal proliferation and survival of tumor cells. Seritinib inhibits tumor cell proliferation and promotes apoptosis by highly selectively inhibiting ALK tyrosine kinase activity and blocking downstream signaling pathways such as PI3K/AKT, RAS/MAPK and JAK/STAT.

At the molecular level, ceritinib can tightly bind to the ATP binding pocket of ALK and directly inhibit its kinase function. This high-affinity binding allows the abnormal signals of tumor cells to be effectively blocked, which is especially advantageous for patients who overcome resistance to first-generation ALK inhibitors. At the same time, ceritinib also has a certain inhibitory effect on ROS1, providing treatment options for patients with related gene rearrangements.

In addition, ceritinib can penetrate the blood-brain barrier and is also effective in patients with central nervous system (CNS) metastasis. ALK Patients with positive lung cancer have a higher risk of brain metastasis, and ceritinib has a high concentration in the brain, which can inhibit the growth of brain tumors and delay disease progression. This property makes it show unique clinical value in patients with drug resistance or brain metastasis.

In general, ceritinib exerts anti-tumor effects by precisely inhibiting ALK and ROS1 related pathways, while reducing the impact on non-target sites and improving drug safety. Combined with molecular testing to clarify the patient's genetic status and regular follow-up, individualized treatment can be achieved, efficacy can be optimized, and drug resistance or disease progression can be detected in a timely manner, providing a scientific basis for subsequent treatment.

Reference materials:https://www.drugs.com/