Entrectinib (Rozlytrek) is a targeted kinase inhibitor indicated for the treatment of ROS1‑positive non‑small cell lung cancer (NSCLC) and NTRK gene fusion‑positive solid tumors.

I. Dosage and Administration: Individualized and Precise Dosing

1. Patient Selection

(1) ROS1‑positive NSCLC: Confirm the presence of ROS1 gene rearrangement in tumor or plasma specimens using an FDA‑approved test.

(2) NTRK gene fusion‑positive solid tumors: Confirm the presence of NTRK gene fusion using an FDA‑approved test, with no known acquired resistance mutations.

2. Recommended Dosage

(1) Adults with ROS1‑positive NSCLC: 600 mg orally once daily, until disease progression or unacceptable toxicity.

(2) Adults with NTRK gene fusion‑positive solid tumors: 600 mg orally once daily.

(3) Pediatric patients (>1 month): Dosage adjusted based on body surface area (BSA) or age (see Tables 1 and 2 in the Prescribing Information for details).

3. Administration Methods

(1) Capsules: Swallow whole; do not chew or crush.

(2) Oral suspension: Prepare by mixing capsule contents with room‑temperature water or milk; let stand for 15 minutes before administration. For patients with swallowing difficulties or those requiring enteral feeding.

(3) Oral granules: Sprinkle onto soft foods (e.g., applesauce, yogurt) and consume within 20 minutes; do not chew.

4. Management of Missed Doses and Vomiting

(1) Missed dose: If the next scheduled dose is more than 12 hours away, take the missed dose; otherwise, skip the missed dose.

(2) Vomiting: If vomiting occurs immediately after dosing, repeat the dose.

II. Precautions: Safety First

1. Congestive Heart Failure

(1) Monitor for new or worsening symptoms such as dyspnea and edema during treatment.

(2) For symptomatic heart failure or decreased left ventricular ejection fraction, interrupt treatment for evaluation; reduce dose or permanently discontinue based on severity.

2. Central Nervous System (CNS) Effects

(1) May cause cognitive impairment, mood disorders, dizziness, and sleep disturbances.

(2) Patients should avoid driving or operating hazardous machinery until symptoms resolve.

(3) Interrupt, reduce dose, or permanently discontinue based on severity.

3. Risk of Skeletal Fractures

(1) Fracture incidence: up to 25% in pediatric patients and 5% in adult patients.

(2) Promptly evaluate patients presenting with pain, limited mobility, or deformity.

4. Hepatotoxicity

(1) Monitor liver function (ALT, AST) every 2 weeks for the first month, then monthly thereafter.

(2) Permanently discontinue for significant transaminase elevation accompanied by bilirubin elevation.

5. Hyperuricemia

(1) Monitor serum uric acid levels before and periodically during treatment.

(2) For symptomatic hyperuricemia, interrupt treatment and initiate urate‑lowering therapy.

6. QT Interval Prolongation

(1) Monitor ECG and electrolytes before and periodically during treatment.

(2) Avoid concomitant use with drugs known to prolong the QT interval.

7. Visual Disturbances

For symptoms such as blurred vision, diplopia, or photophobia, interrupt treatment and perform an ophthalmologic evaluation.

8. Embryo‑Fetal Toxicity

(1) May cause fetal harm. Females of reproductive potential must use effective contraception during treatment and for 5 weeks after the last dose.

(2) Males with female partners of reproductive potential must use contraception during treatment and for 3 months after the last dose.

9. Drug Interactions

(1) CYP3A inhibitors: Avoid concomitant use with strong or moderate CYP3A inhibitors. If unavoidable, reduce dose and limit use to ≤14 days.

(2) CYP3A inducers: Avoid concomitant use, as efficacy may be reduced.

(3) Grapefruit products: Avoid consumption during treatment.

III. Patient Healthy Lifestyle: Comply with Treatment and Improve Quality of Life

1. Dietary Recommendations

(1) Balanced nutrition: Ensure adequate intake of protein and vitamins to enhance physical fitness.

(2) Avoid grapefruit: May increase drug exposure by affecting CYP3A metabolism.

(3) Soft food for administration: Granules may be sprinkled on soft foods (e.g., applesauce, yogurt) to facilitate swallowing.

2. Exercise and Bone Health

(1) Moderate exercise: Such as walking and yoga to strengthen muscles, improve balance, and reduce fall risk.

(2) Fracture risk awareness: Especially in pediatric patients; avoid high‑risk activities and seek medical attention promptly for pain.

For additional information, please refer to the Entrectinib (Rozlytrek) Prescribing Information.