Tigozertinib

DB19239InvestigationalSmall molecule

Tigozertinib (BLU-945) is currently under investigation in clinical trial NCT04862780 (Phase 1/​2 Study Targeting EGFR Resistance Mechanisms in NSCLC) for the treatment of NSCLC.

Chemical structure of Tigozertinib
Mechanism
Curator reviewed
Formula / weight
C28H37FN6O3S · 556.7 g/mol (avg)
Also known as
3-ISOQUINOLINAMINE, N-(2-((3S,4R)-3-FLUORO-4-METHOXY-1-PIPERIDINYL)-4-PYRIMIDINYL)-5-(1-METHYLETHYL)-8-((2R,3S)-2-METHYL-3-((METHYLSULFONYL)METHYL)-1-AZETIDINYL)- · EGFR MUTANT-SELECTIVE INHIBITOR BLU-945 · N-{2-[(3S,4R)-3-fluoro-4-methoxypiperidin-1-yl]pyrimidin-4-yl}-5-(propan-2-yl)-8-[(2R,3S)-2-methyl-3-[(methanesulfonyl)methyl]azetidin-1-yl]isoquinolin-3-amine
Code names
BLU-945

Resolves to

Structure
InChIKeyLIMFPAAAIVQRRD-BCGVJQADSA-NSMILESCO[C@@H]1CCN(C[C@@H]1F)C1=NC=CC(NC2=CC3=C(C=CC(N4C[C@H](CS(C)(=O)=O)[C@H]4C)=C3C=N2)C(C)C)=N1
Targets
Transporters

What you can answer from here — as of July 09, 2026

1Protein targetEach mapped to UniProt, with action and pharmacological action
Listed above
1TransporterSubstrate / inhibitor direction, not just membership
Listed above
1Clinical trialPhase, status and sponsor resolved per trial
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4+ReferencesStructured and connected to the statements they support
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