Entrectinib (Rozlytrek) is a kinase inhibitor, primarily used to treat ROS1-positive metastatic non-small cell lung cancer and solid tumors positive for NTRK gene fusion.

What Are the Precautions for Taking Entrectinib (Rozlytrek)?

Patient Selection Requirements

Entrectinib is indicated for adult patients with ROS1-positive metastatic non-small cell lung cancer (confirmed by an FDA-approved detection method), as well as adult and pediatric patients aged over 1 month with solid tumors positive for NTRK gene fusion.

Patient selection must be based on the presence of ROS1 rearrangement or NTRK gene fusion in tumor or plasma samples.

Plasma samples may only be used for testing when tumor tissue samples are unavailable.

Baseline Assessment Items

Evaluate left ventricular ejection fraction (LVEF) in patients with heart failure symptoms or known risk factors.

Measure serum uric acid levels.

Assess QT interval and electrolyte levels.

Central Nervous System (CNS) Effects

Potential neurological adverse reactions include cognitive impairment (27%), mood disorders (10%), dizziness (38%), and sleep disturbances (14%).

Among these, 4.5% of patients experience Grade 3 cognitive adverse events.

Patients are advised to avoid driving or operating hazardous machinery during the period of experiencing CNS adverse reactions.

Standard Dosage for Adults

ROS1-positive non-small cell lung cancer: 600 mg orally, once daily.

Solid tumors positive for NTRK gene fusion: 600 mg orally, once daily.

Basis for Dosage Form Selection

Capsules swallowed whole: Suitable for patients who can swallow capsules and require a dose that is a multiple of 100 mg.

Capsules reconstituted into suspension: Used for patients with dysphagia or those requiring enteral administration.

Oral granules: Suitable for patients who can swallow soft food but cannot swallow capsules.

Administration Time Management

Administer once daily, with or without food.

Missed dose handling: If the next dose is not due within 12 hours, take the missed dose; otherwise, skip it.

Vomiting handling: If vomiting occurs immediately after administration, repeat the dose.

Medication Monitoring for Entrectinib (Rozlytrek)

Laboratory Monitoring Frequency

Liver function: Every 2 weeks for the first 4 weeks, then monthly thereafter.

Serum uric acid levels: Monitor regularly before and during treatment.

Electrolyte levels: Determine monitoring frequency based on risk assessment factors.

Specialist Assessment Requirements

Cardiac function: Baseline assessment for patients with symptoms or risk factors.

Neurological symptoms: Regular assessment of cognitive function and emotional status.

Special Monitoring Items

Liver function: Monitor every 2 weeks for the first month of treatment, then monthly thereafter.

Electrocardiogram (ECG): Monitor QT interval at baseline and regularly during treatment.