What does lorlatinib/lorlatinib treat?

Lorlatinib/lorlatinib (Lorlatinib) is a novel third-generation tyrosine kinase inhibitor (TKI) that targets anaplastic lymphoma kinase (ALK) and the receptor tyrosine kinase C-ROS oncogene 1 (ROS1). A key limitation of traditional ALK/ROS tkis is that they are associated with acquired resistance mutations in the ALK or ROS1 genes (particularly ALK G1202R and ROS1 G2032R), although these are not the only resistance mechanisms. Another limitation of this class of drugs is their insufficient potency against CNS metastasis, which may be attributed to the blood-brain barrier (BBB).

Therefore, lorlatinib was developed to overcome these limitations and was more effective, selective, and penetrating across the BBB than previous generation ALK/ROS1 TKIs, and subsequently received Breakthrough Therapy designation from the U.S. Food and Drug Administration (FDA) in April 2017. In September 2018, Japan became the first country to approve lorlatinib for the treatment of patients with ALK-rearranged non-small cell lung cancer. Ultimately, the FDA approved lorlatinib, and its use is expected to become increasingly important due to its good efficacy in clinical trials.

The original drug is marketed in China as lorlatinib tablets. The common specifications are 25mg*90 tablets and 100mg*30 tablets. The price of each box may be around 10,000 to 20,000 RMB. The price of the original Hong Kong version may be 30,000 to 50,000 RMB per box (the price may fluctuate due to the exchange rate), which is relatively expensive. There are relatively cheap generic drugs sold overseas, and their drug ingredients are basically the same as the original drugs. Taking the ones produced by relevant pharmaceutical factories in Laos as an example, the price of each box of 100mg*30 tablets may be around 3,000 yuan (the price may fluctuate due to the exchange rate).