What are the precautions for taking entrectinib?

Entrectinib is an anti-tumor drug. Entrectinib works by interfering with the growth of cancer cells, and the cancer cells will eventually be eliminated. Entrectinib was developed by Roche and was first approved in Japan in 2019 for the treatment of pediatric and adult patients with NTRK fusion-positive, recurrent or advanced solid tumors. Entrectinib is also applicable to ROS1positive adults with metastatic non-small cell lung cancer.

What are the precautions for taking entrectinib?

1.Congestive heart failure:Assess left ventricular ejection fraction (LVEF) before initiating entrectinib in patients with symptoms of congestive heart failure or known risk factors. Monitor patients for clinical signs and symptoms of congestive heart failure. In patients with myocarditis with or without reduced ejection fraction, MRI or cardiac biopsy may be needed for diagnosis. For new or worsening congestive heart failure, discontinue entrectinib, reassess LVEF, and implement appropriate medical therapy. Reduce dose or permanently discontinue entrectinib based on severity of congestive heart failure or LVEF deterioration.

2.Central nervous system effects: Entrectinib may cause central nervous system adverse reactions, including cognitive impairment, mood disorders, dizziness and sleep disorders. Withhold medication and then resume at the same or reduced dose when condition improves, or permanently discontinue entrectinib based on severity.

3.Bone fracture: Entrectinib will increase the risk of fracture, evaluate patients with signs or symptoms of fracture promptly.

4.Hepatotoxicity:Monitor liver tests, including ALT and AST, every 2 weeks during the first month of treatment, and then monthly as clinically indicated. Withhold or permanently discontinue entrectinib based on severity. If discontinued, resume entrectinib at the same or reduced dose based on severity.

5.Excessive uric acid:At the beginning of useAssess serum uric acid levels before and periodically during treatment with entrectinib Monitor patients for signs and symptoms of hyperuricemia. Initiate treatment with urate-lowering medications as clinically indicated and discontinue entrectinib for signs and symptoms of hyperuricemia. After improvement based on severity, resume the same or reduce dose.

6.QTinterval prolongation:MonitorQTc patients with prolongation of the QTc interval or who are at risk of QTc interval prolongation. Assess QT interval and electrolytes at baseline and periodically during treatment. Withhold and then resume the same or reduced dose, or permanently discontinue entrectinib based on severity.

7.Visual Impairment:Suppress new visual changes or changes that interfere with activities of daily living until they improve or stabilize. Obtain ophthalmic evaluation as appropriate. Resume at the same or reduced dose after condition improves or stabilizes.

8.Embryo-Fetal Toxicity:Can cause fetal harm. Inform women of the potential risks to the fetus and the use of effective contraception.

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