Ensartinib is an ALK inhibitor targeted therapy primarily used to treat locally advanced or metastatic non-small cell lung cancer with ALK gene fusions. It inhibits tumor growth by blocking abnormal ALK protein activity. It received FDA approval in late 2024 and is currently also being explored for adjuvant therapy after surgery.
Indications and Mechanism of Action
Indicated as a first-line treatment for 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, blocking tumor cell proliferation signals.
Dosage and Administration
The standard recommended dose is 225 mg once daily, taken orally. It can be taken with or without food, and should be taken at a fixed time each day.
Capsules must be swallowed whole; chewing or crushing is prohibited. If a dose is missed by more than 12 hours, it may be made up; if less than 12 hours, skip the missed dose. Do not take an extra dose if vomiting occurs after administration.
Common Adverse Reactions
Skin reactions: Rash, pruritus, and photosensitivity. Patients should avoid sun exposure and use sunscreen during treatment.
Gastrointestinal system: Nausea, vomiting, constipation, or diarrhea; a light diet is recommended.
Liver function abnormalities: Elevated transaminases; liver function tests must be monitored regularly.
Others: Visual disturbances, fatigue, and lower extremity edema. Rare but serious interstitial lung disease requires immediate medical attention.
Important Precautions
ALK-positive status must be confirmed via genetic testing before treatment; contraindicated in pregnant women.
Avoid concomitant use with strong CYP3A4 inducers (such as rifampin) or inhibitors to prevent affecting drug efficacy.
Stop the medication immediately and seek medical attention if symptoms such as persistent dyspnea, severe skin reactions, or jaundice occur.
