Lorlatinib/Lorlatinib: Functional Analysis and Main Therapeutic Areas

Lorlatinib/Lorlatinib (Lorlatinib) is a drug with significant anti-tumor effects. It mainly inhibits multiple tyrosine kinases such as anaplastic lymphoma kinase (ALK) and c-ros oncogene-1 (ROS1). In 2018, lorlatinib successfully obtained approval from the U.S. Food and Drug Administration (FDA) with its unique third-generation macrocyclic ALK/ROS1 inhibition mechanism. The FDA specifically designated it as an orphan drug for the treatment of ALK-positive or ROS-1-positive metastatic non-small cell lung cancer (NSCLC).

According to statistics, approximately 3-7% of patients with non-small cell lung cancer are ALK positive. Such patients tend to be non-smokers or light smokers, are relatively young, and most of them have adenocarcinoma. However, the effectiveness of some traditional ALK inhibitors (such as alectinib, crizotinib, etc.) in long-term treatment is limited due to factors such as ALK resistance mutations, gene amplification, activation of alternative signaling pathways, and the development of brain metastases.

Lorlatinib is unique in its excellent brain penetration, which makes it particularly responsive in treating the central nervous system. Lorlatinib has shown significant efficacy in patients whose disease has progressed on other ALK inhibitors. Therefore, clinical guidelines usually recommend that in the first-line treatment of non-small cell lung cancer, if the ALK inhibitor is not effective, lorlatinib can be considered in the second-line or third-line treatment setting.

Before starting lorlatinib treatment, doctors will ensure that the patient's tumor sample is positive for ALK. To ensure optimal results, patients are advised to take it at a fixed time every day, regardless of food intake. It should be noted that lorlatinib tablets should be swallowed whole and should not be crushed, chewed or divided. Tablets should not be taken if they are damaged.