Entretinib is an oral tyrosine kinase inhibitor targeting the fusion of ROS1 and NTRK genes, mainly used for the treatment of ROS1 positive non-small cell lung cancer and NTRK gene fusion positive solid tumors, with significant central nervous system permeability and clinical efficacy.

1. Indications for treatment

(1) ROS1 positive non-small cell lung cancer: suitable for adult patients with locally advanced or metastatic ROS1 positive non-small cell lung cancer.

(2) NTRK gene fusion positive solid tumor: used to treat NTRK gene fusion positive solid tumor patients in adults and children over 12 years old.

2 Clinical effects

(1) Objective response rate: 57% in NTRK fused solid tumors and 77% in ROS1 positive NSCLC, demonstrating excellent anti-tumor activity.

(2) Therapeutic effect on brain metastases: It has a significant control effect on central nervous system metastases, with an objective remission rate of over 50%.

(3) Duration of remission: The median remission time was 24.6 months, significantly prolonging the progression free survival of patients.

3 mechanisms of action

(1) Targeted inhibition: Selective inhibition of TRKA/B/C, ROS1, and ALK kinase activity, blocking downstream signaling pathways.

(2) Blood brain barrier penetration: It has excellent central nervous system permeability, with cerebrospinal fluid concentration reaching 15-20% of plasma concentration.

4 Security Features

(1) Common adverse reactions: including dizziness, constipation, diarrhea, fatigue, etc., mostly grade 1-2, well tolerated.

(2) Medication for special populations: prohibited during pregnancy, breastfeeding should be suspended during lactation, and medication for children should be carefully evaluated.