Lorlatinib/lorlatinib (Borina) main efficacy and clinical effects

Lorlatinib/ Lorlatinib ( Lorlatinib) is a new generation of ALK and ROS1 dual-target inhibitors and is a third-generation oral small molecule tyrosine kinase inhibitor (TKI). The drug was developed by Pfizer and is used to treat patients with ALK-positive or ROS1-positive non-small cell lung cancer, especially those who have developed resistance to previous generation drugs such as Crizotinib, Alectinib, and Brigatinib. The biggest feature of lorlatinib is its high selectivity and strong penetration. It can effectively inhibit multiple ALK resistance mutations, penetrate the blood-brain barrier at the same time, and show significant efficacy in brain metastatic lesions.

In terms of molecular mechanism, lorlatinib inhibits downstream signaling and blocks tumor cell proliferation and metastasis by targetingALK (anaplastic lymphoma kinase) and ROS1 (c-ros proto-oncogene 1 receptor) pathways. Compared with previous generation drugs, lorlatinib not only has stronger inhibitory effect on ALK mutant strains, but also maintains activity against highly resistant mutations such as G1202R, making it an important back-line option for the treatment of advanced ALK-positive NSCLC. The more prominent advantage is that it can effectively control brain metastases. Because of its excellent central nervous system penetration ability, it can significantly reduce the risk of brain recurrence.

In clinical application, lorlatinib is used for patients who have progressed after previously receiving one or more ALK inhibitor treatments. It can also be used as one of the initial treatment options to help prolong disease control time and improve quality of life. Some studies have pointed out that after patients use lorlatinib, the duration of tumor shrinkage and symptom relief is significantly prolonged, especially in the control of brain metastases. In addition, lorlatinib also shows the potential to inhibit tumor activity in ROS1-positive lung cancer, providing more treatment options for patients with this rare type.

References：https://www.lorbrena.com/