Taletrectinib is a small molecule ROS1 inhibitor for use in patients with advanced forms of ROS1-positive non-small cell lung cancer. It is targeted against ROS1, including resistant mutant forms, and shows some inhibitor activity against tropomyosin receptor kinases (TRKs) TRKA, TRKB, and TRKC.
- Mechanism
- Curator reviewed · 1 reference
Taletrectinib is an inhibitor of tyrosine kinase ROS1, including ROS1 resistance mutations. It also exhibits inhibitory effects on tropomyosin receptor kinases (TRKs) TRKA, TRKB, and TRKC. Fusion proteins that include ROS1 domains can drive tumorigenic potential through hyperactivation of downstream signaling pathways, leading to unconstrained cell proliferation.
- Primary indication
- Taletrectinib is indicated for the treatment of adult patients with locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC).Curator reviewed · 2 structured indications
- Formula / weight
- C23H24FN5O · 405.477 g/mol (avg)
- First approval
- United States, 2025
- Code names
- AB-106 · DS-6051 · DS-6051A
- Brand names
Resolves to
HEVHTYMYEMEBPX-HZPDHXFCSA-NSMILES[H][C@](C)(N)COC1=CC=C(C=C1)C1=CN=C2C=C\C(NN12)=N\[C@]([H])(C)C1=CC(F)=CC=C1What you can answer from here — as of September 13, 2026
Which drugs share a target with Taletrectinib, and which of those have an active Phase 3 trial?
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