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ROS1 inhibitors (for patients with ROS1 rearrangements)

Source: Non-Small Cell Lung Cancer Treatment (PDQ®)–Health Professional Version, National Cancer Institute.

Source updated: May 15, 2025 · Captured 2026-09-09.

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Context: Treatment of Newly Diagnosed Stage IV, Relapsed, and Recurrent NSCLC / Treatment Options for Newly Diagnosed Stage IV, Relapsed, and Recurrent NSCLC (First-Line Therapy)

ROS1 rearrangements occur in approximately 1% to 2% of patients with NSCLC.[73] ROS1 TKI therapy is the current standard of care for patients with locally advanced or metastatic NSCLC and a ROS1 variant. Crizotinib, entrectinib, and repotrectinib are all approved by the FDA for patients with NSCLC and ROS1 fusions. Notably, repotrectinib is the only ROS1 TKI that is approved by the FDA for patients previously treated with a ROS1 TKI. Entrectinib and repotrectinib have both shown intracranial activity, while repotrectinib also appears to be active in patients with known ROS1 resistance variants, including G2032R.

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Entrectinib →Crizotinib →Repotrectinib (for both ROS1 TKI-naïve and ROS1 TKI-treated patients) →

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PubMed 23814043 · Original source

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