Entrectinib (Rozlytrek) is a kinase inhibitor approved for the treatment of ROS1-positive metastatic non-small cell lung cancer (NSCLC) and solid tumors positive for NTRK gene fusion. As a highly effective targeted therapeutic drug, entrectinib exerts significant anti-tumor activity while being accompanied by a series of adverse reactions that require close monitoring.

What Are the Side Effects of Entrectinib (Rozlytrek)?

Systemic Reactions

Fatigue is one of the most common side effects, with an incidence rate of 48%, of which 5% are of Grade 3 or higher severity.

Fatigue symptoms may persist and significantly affect patients’ quality of life, requiring full attention and supportive treatment during the treatment process.

Neurological Effects

The incidence of dysgeusia is 44%, manifested as changes in or loss of the sense of taste.

The incidence of dizziness is 38%, of which 2.2% are of Grade 3 severity.

10% of patients require dose adjustment due to dizziness, 7% require dose interruption, and 0.7% discontinue the drug permanently because of dizziness.

Digestive System Reactions

The incidence rates are 46% for constipation, 35% for diarrhea, 34% for nausea, and 24% for vomiting.

These gastrointestinal symptoms are usually more obvious in the early stage of medication, and most patients can be relieved through symptomatic treatment.

Severe Side Effects of Entrectinib (Rozlytrek)

Risk of Congestive Heart Failure

The incidence of congestive heart failure is 3.4%, of which 2.3% are Grade 3 severe events.

Before using entrectinib, left ventricular ejection fraction (LVEF) must be evaluated in patients with heart failure symptoms or known risk factors.

Management Plan: For newly developed or worsening heart failure, suspend entrectinib administration.

Conduct appropriate medical management and re-evaluate LVEF.

Depending on the severity of heart failure or the deterioration of LVEF, resume treatment at a reduced dose after returning to the baseline level or discontinue the drug permanently.

Central Nervous System (CNS) Effects

The incidence of cognitive impairment is 27%, with symptoms including cognitive disorder (8%), confusional state (7%), attention deficit (4.8%), memory impairment (3.7%), etc.

Hepatotoxic Reactions

The incidence of elevated AST is 44%, and the incidence of elevated ALT is 38%.

2.5-2.9% of patients experience Grade 3-4 elevation of AST or ALT.

Monitoring Plan: Monitor liver function every 2 weeks in the first month of treatment.

After that, monitor once a month.

Suspend or permanently discontinue the drug according to the severity.

Precautions for Taking Entrectinib (Rozlytrek)

CYP3A Inhibitors

Adults and children aged 2 years and above: If concurrent use cannot be avoided, the dose of entrectinib needs to be reduced.

Children under 2 years old: Avoid concurrent use with entrectinib.

CYP3A Inducers

Avoid concurrent use with entrectinib.

Avoid concurrent use with entrectinib.

Regular Monitoring

Blood pressure monitoring: Every 2 weeks and at least once a month.

Liver function monitoring: Including ALT and AST.

Uric acid level assessment.

Electrocardiogram (ECG) and electrolyte monitoring.