Lorlatinib/lorlatinib version
Lorlatinib is a third-generation small molecule TKI that is a new, reversible ATP-competitive ALK and ROS1 inhibitor. It exerts an inhibitory effect by mediating the disruption of the ALK and ROS1 signaling pathways. In the United States and Europe, lorlatinib has been approved for the treatment of ALK-positive non-small cell lung cancer. Importantly, lorlatinib also has favorable effects in patients who develop brain metastases across the blood-brain barrier. Animal studies have shown that lorlatinib is more effective than alectinib against CNS lesions.
Lorlatinib is a targeted drug called a tyrosine kinase inhibitor (TKI). Tyrosine kinases are proteins that cells use to signal each other to promote growth. They act as chemical messengers. Blocking these signals can help slow or stop cancer growth. If a patient has previously been treated with an ALK-targeting drug and the cancer has begun to grow again (get worse), the patient may need to receive lorlatinib for NSCLC. Before receiving treatment, doctors will need to test for cancer cells. These tests look for changes in these proteins and genes. They used lorlatinib to look for changes in the ALK gene.
Clinical studies have shown that the cumulative incidence of central nervous system progression and non-central nervous system progression was lower in the alectinib group than in the crizotinib group at any time point. NCT01970865 is an open-label, multicenter Phase I/II study demonstrating that alectinib has systemic activity and prevents intracranial metastasis in patients with advanced ALK- or ROS1-positive non-small cell lung cancer.
In short, lorlatinib, as an efficient and safe anti-cancer drug, provides new treatment hope for NSCLC patients. By precisely inhibiting the activity of ALK and ROS1 proteins, lorlatinib can effectively control the growth and spread of tumors and improve patients' quality of life.
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