Product Description
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AI Product Description
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Entrectinib is a novel, orally bioavailable, small-molecule tyrosine kinase inhibitor (TKI) designed to target multiple oncogenic drivers. Its chemical structure is defined by the molecular formula C28H30N6O4S, and it is registered under the CAS number 1175994-58-1. This agent functions as a potent inhibitor of ROS1, ALK, and NTRK1/2/3 kinases, which are critical fusion proteins driving the growth of various malignancies. By binding to the ATP-binding pocket of these kinases, Entrectinib prevents phosphorylation and downstream signaling, effectively halting tumor cell proliferation and inducing apoptosis.
A distinguishing feature of Entrectinib is its ability to cross the blood-brain barrier, making it particularly valuable for treating central nervous system metastases associated with ROS1-positive non-small cell lung cancer (NSCLC), ALK-positive NSCLC, and TRK fusion-positive solid tumors. Clinical trials have demonstrated significant objective response rates in patients who have progressed on prior therapies or who are treatment-naïve. The drug was approved by regulatory agencies such as the FDA and EMA for specific indications involving ROS1-positive NSCLC and NTRK gene fusion-positive solid tumors.
Common side effects include dizziness, edema, constipation, dysgeusia, and elevated liver enzymes. While generally well-tolerated, monitoring for cardiac toxicity, including QT interval prolongation, and neurologic events like cognitive impairment is essential during treatment. As precision medicine advances, Entrectinib represents a paradigm shift in targeting rare genetic alterations across diverse tumor types, offering hope where traditional chemotherapy has failed. Its broad spectrum activity against multiple kinase fusions positions it as a cornerstone therapy in the evolving landscape of targeted oncology, providing durable responses and improved quality of life for patients with advanced solid tumors harboring specific driver mutations.