Ensartinib is a targeted drug classified as an ALK inhibitor, primarily used for the treatment of ALK fusion-positive locally advanced or metastatic non-small cell lung cancer. It inhibits tumor growth by blocking the activity of abnormal ALK proteins. It was approved by the FDA for marketing in late 2024 and is currently being explored for postoperative adjuvant therapy.
I. Indications and Mechanism of Action
It is indicated for the first-line treatment of adult patients with ALK-positive non-small cell lung cancer, or for patients whose disease has progressed after treatment with other ALK inhibitors.
As a tyrosine kinase inhibitor, it potently inhibits targets such as ALK, MET, and ROS1, thereby blocking tumor cell proliferation signals.
II. Dosage and Administration
The standard recommended dose is 225 mg orally once daily, which can be taken with or without food, and should be administered at a fixed time each day.
Capsules must be swallowed whole; do not chew or crush. If a dose is missed by more than 12 hours, it can be taken as a makeup dose, but if the interval is less than 12 hours, the missed dose should be skipped. Do not take an additional dose if vomiting occurs after administration.
III. Common Adverse Reactions
Skin reactions: Rash, pruritus, and photosensitivity; patients should avoid sun exposure and use sunscreen during treatment.
Digestive system: Nausea, vomiting, constipation, or diarrhea; a light diet is recommended.
Abnormal liver function: Elevated transaminases; liver function indicators must be monitored regularly.
Others: Visual disturbances, fatigue, and lower extremity edema; rare but severe interstitial lung disease requires immediate medical attention.
IV. Important Precautions
ALK-positive status must be confirmed via genetic testing prior to treatment initiation, and it is contraindicated in pregnant women.
Avoid concomitant use with strong CYP3A4 inducers (such as rifampin) or inhibitors to prevent compromising the drug's efficacy.
Discontinue the medication immediately and seek medical attention if symptoms such as persistent dyspnea, severe skin reactions, or jaundice occur.
