Zidesamtinib is a brain-penetrant, ROS1-selective kinase inhibitor with activity against ROS1 resistance mutations, indicated for locally advanced or metastatic ROS1-positive NSCLC after a prior ROS1 kinase inhibitor. ROS1 gene fusions drive a small subset of non-small cell lung cancers, and while several ROS1 inhibitors are available, treatment is limited over time by two recurring problems: the emergence of resistance mutations, particularly the...
- Mechanism
- Curator reviewed · 4 references
Zidesamtinib is an inhibitor of the tyrosine kinase ROS1, including ROS1 resistance mutations. In a biochemical assay, zidesamtinib inhibited ROS1 (IC50 = 0.7 nM) and also showed inhibitory effects on ALK (IC50 = 3 nM) and the tropomyosin receptor kinases TRKB (IC50 = 54 nM), TRKC (IC50 = 193 nM) and TRKA (IC50 = 258 nM). In vitro, zidesamtinib inhibited the viability of cultured cells expressing ROS1 fusion genes and resistance mutations (G2032R, S1986F, F2004C/V, L2026M, D2033N, and G2101A). In mice with subcutaneously implanted tumors harboring ROS1 fusions, including the G2032R mutation, zidesamtinib inhibited tumor growth, and it had antitumor activity in an intracranial NSCLC xenograft model harboring a ROS1 fusion.
- Primary indication
- Zidesamtinib is indicated for the treatment of adult patients with locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC) who received a prior ROS1 kinase inhibitor.Curator reviewed · 2 structured indications
- Formula / weight
- C22H22FN7O · 419.464 g/mol (avg)
- First approval
- United States, 2026
- Code names
- NU-0002362 · NU-0002362-009 · NU-2362-010 · NU-520 · NUV-520 · NVL-520
- Brand names
Resolves to
DTWUUAFTYSMNQX-GFCCVEGCSA-NSMILESCCN1N=CC2=C1C1=CN=C(N)C(O[C@H](C)C3=CC(F)=CC=C3C3=NN(C)N=C3C2)=C1What you can answer from here — as of November 03, 2026
Which drugs share a target with Zidesamtinib, and which of those have an active Phase 3 trial?
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