Enqutinib is a multi-target tyrosine kinase inhibitor used for NTRK fusion positive solid tumors and ROS1 positive non-small cell lung cancer. The following is the core clinical information.

1、 Usage and dosage

1.1 Standard Dose

Adults: 600mg, once daily, orally.

Children (≥ 1 month): Calculated based on body surface area (BSA ≥ 1.5m ²: 600mg/day); 1.1-1.5m ²: 500mg/day; 0.9-1.1m ²: 400mg/day).

1.2 Usage

Taken with meals, it can reduce gastrointestinal reactions such as nausea and vomiting.

Take the medicine at a fixed time every day, swallow the whole pill, and do not crush or chew it.

1.3 Dose adjustment

Adverse reactions ≥ grade 3: Suspend medication and reduce to 400mg/day after recovering to ≤ grade 1.

Abnormal liver function: Pause when transaminase>5 × ULN or bilirubin>3 × ULN, and reduce dosage after recovery.

QTc>500ms: Pause, evaluate restart and reduction after correcting electrolyte.

Strong CYP3A4 inhibitor: If used in combination, reduce the dosage of Enrvatinib to 400mg/day.

2、 Therapeutic effect

2.1 Objective relief rate

NTRK fusion positive solid tumor: ORR of approximately 57% to 63% in multiple studies, and remission can last for 12 to 24 months.

ROS1 positive NSCLC: first-line treatment has an ORR of about 67% to 73% and a median PFS of about 15 to 19 months.

2.2 Central nervous system activity

The drug can penetrate the blood-brain barrier and is equally effective for patients with brain metastases, with an intracranial ORR of approximately 50% to 60%.

3、 Precautions

3.1 Congestive heart failure

Regularly monitor LVEF before and during treatment, and discontinue medication when LVEF is less than 50% or decreases by ≥ 10% from baseline.

3.2 Central nervous system side effects

Common dizziness, taste disorders, and cognitive impairments. Avoid driving and working at heights; Severe CNS symptoms require discontinuation of medication for screening.

3.3 Risk of Fracture

Assess bone density and supplement calcium and vitamin D before treatment for high-risk populations (≥ 55 years old or those with osteoporosis).

3.4 Drug Interactions

Prohibit potent CYP3A4 inducers (rifampicin, phenytoin sodium). When used in combination with potent CYP3A4 inhibitors, the dosage should be reduced.