Used in the treatment of ALK-positive non-small cell lung cancer, LDK378 (also known as ceritinib) is a potent inhibitor of the anaplastic lymphoma kinase (ALK) receptor tyrosine kinase. It is specifically designed to target tumors that have developed resistance to earlier ALK inhibitors, making it effective in patients who have progressed on prior therapies. The compound also shows activity against insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1 kinases, broadening its potential therapeutic use. Administered orally, it achieves high concentrations in the central nervous system, offering clinical benefit in patients with brain metastases. Its development represents a significant advancement in personalized medicine for lung cancer patients with specific genetic alterations.