Entrectinib (Rozlytrek) is a targeted anticancer drug indicated for cancer patients with specific gene mutations.

Indications of Entrectinib 

Entrectinib is mainly used for the treatment of the following two groups of patients:

1. Adult patients with ROS1-positive non-small cell lung cancer (NSCLC)

(1) Indicated for adult patients with metastatic ROS1-positive NSCLC confirmed by an FDA-approved test.

(2) This drug can effectively inhibit the activity of ROS1 kinase and block tumor growth signals.

2. Patients with NTRK gene fusion-positive solid tumors

(1) Indicated for adult and pediatric patients aged 1 month and above with NTRK gene fusion-positive tumors and no known acquired drug-resistant mutations.

(2) Patients must have metastatic tumors or tumors for which surgical resection may lead to severe complications, and have failed previous treatments or lack satisfactory alternative treatment options.

(3) This indication was granted accelerated approval based on tumor response rate and duration of response.

Contraindications and Contraindicated Foods

1. Contraindications

A comprehensive assessment of the patient's condition is required before administration, especially for patients with underlying diseases of the heart, liver, nervous system and other organs.

2. Contraindicated Foods and Drug Interactions

Grapefruit and its products: Grapefruit can inhibit CYP3A enzymes, significantly increase the blood concentration of entrectinib and raise the risk of adverse reactions. Consumption should be avoided during medication.

3. Other Contraindicated Drugs

(1) Strong or moderate CYP3A inhibitors (e.g., itraconazole, clarithromycin): Concomitant use should be avoided; if unavoidable, the dose of entrectinib needs to be adjusted.

(2) CYP3A inducers (e.g., rifampicin, carbamazepine): May reduce the efficacy of entrectinib, and concomitant use should be avoided.

(3) Drugs that prolong the QT interval: Concomitant use may increase the risk of arrhythmias, and a careful assessment is required.

Administration in Special Populations

1. Pregnant and Lactating Women

(1) Entrectinib may cause fetal harm and is contraindicated in pregnant women.

(2) Reproductive-aged females should use effective contraceptive measures during treatment and for at least 5 weeks after the last dose.

(3) Female partners of fertile male patients should also use contraception during the patient's treatment and for 3 months after the last dose.

(4) Lactating women should discontinue breastfeeding until 7 days after the last dose.

2. Pediatric Patients

(1) Entrectinib has been approved for pediatric patients aged 1 month and above with NTRK gene fusion-positive solid tumors, and the dose must be accurately calculated based on body surface area.

(2) Pediatric patients have a higher risk of fractures, and close monitoring of skeletal symptoms is required.

(3) The safety and efficacy of entrectinib in pediatric patients with ROS1-positive NSCLC have not been established.

3. Geriatric Patients

(1) Approximately 25% of patients in clinical studies were aged 65 years and above, but the available data are limited, and no significant difference in response was observed between geriatric and younger patients.

(2) Medication should be administered with a careful assessment based on the patient's overall health status.

4. Patients with Hepatic or Renal Impairment

(1) Hepatic impairment: Dose adjustment is generally not required for patients with mild to moderate hepatic impairment; however, clinical data are insufficient for patients with moderate to severe hepatic impairment, and close monitoring of adverse reactions is necessary.

(2) Renal impairment: Dose adjustment is not required for patients with mild to moderate renal impairment; no studies have been conducted in patients with severe renal impairment, and cautious use is advised.

5. Patients with Cardiac or Nervous System Diseases

Patients with a history of heart failure, QT interval prolongation, epilepsy, mental disorders and other related diseases should use the drug under close monitoring; dose adjustment or treatment suspension should be implemented if necessary.