Entretinib: Usage, Dosage, Efficacy, and Precautions
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.
Disclaimer：《Entretinib: Usage, Dosage, Efficacy, and Precautions》Edited and sorted by Seagull Pharmacy's editors. Please contact us in time if there is any infringement. In addition, the suggestions for drug usage, dosage and disease mentioned in the article are only for medical staff's reference, and can not be used as any basis for medication！