Application of Ripotinib in the treatment of NTRK fusion-positive tumors

Introduction: Ripotinib is a new second-generation ROS1/NTRK inhibitor that has shown significant potential and effect in the treatment of NTRK fusion-positive tumors. Ripotinib not only targets ROS1-positive tumors but also has therapeutic effects on NTRK fusion-positive tumors, making it a broad-spectrum anticancer drug, especially for the treatment of adult patients with locally advanced or metastatic ROS1-positive non-small cell lung cancer. Ripotinib can overcome the known ALK, ROS1 and NTRK resistance problems that have emerged in clinical practice, providing a new treatment option for drug-resistant patients.

Application in the treatment of NTRK fusion-positive tumors

In the TRIDENT-1 study, achieved an objective response rate (cORR) of 41% in NTRK fusion-positive patients who had not received TKI treatment and a cORR of 48% in patients who had received TKI treatment. Especially among patients carrying solvent front mutations, the cORR assessed by the researchers reached 62%. Ripotinib demonstrated favorable safety and tolerability in clinical trials, with most treatment-related adverse events (TRAEs) grade 1/2 and no grade 5 TRAEs observed.

Efficacy in the treatment of ROS1 lung cancer

In a global, multicenter, single-arm, open-label, multi-cohort clinical trial, patients with ROS1-positive locally advanced or metastatic non-small cell lung cancer were included. Efficacy was evaluated in 71 ROS1 tyrosine kinase inhibitor-naive patients (who had received up to 1 prior platinum-based chemotherapy or immunotherapy) and 56 patients who had received 1 ROS1 tyrosine kinase inhibitor but no platinum-based chemotherapy or immunotherapy.

It was confirmed that the overall response rate in the group not using ROS1 tyrosine kinase inhibitors was 79%, while the overall response rate in patients previously treated with ROS1 inhibitors was 38%. The median duration of response in the two groups was 34.1 months and 14.8 months, respectively. Responses were observed in intracranial lesions in patients with measurable central nervous system metastases and in patients who developed resistance mutations after treatment with tyrosine kinase inhibitors.

Medication Reference Guide

1. Based on the presence of ROS1 rearrangement in tumor specimens, it is selected for the treatment of patients with locally advanced or metastatic non-small cell lung cancer.

2. The recommended dose is 160 mg once a day for 14 days, then increased to 160 mg twice a day, with or without food.