Pebezertinib

DB21705InvestigationalSmall molecule

Pebezertinib is a small molecule drug. The usage of the INN stem '-ertinib' in the name indicates that Pebezertinib is a epidermal growth factor receptor (EGFR) inhibitor. Pebezertinib is under... Pebezertinib is under investigation in clinical trial NCT05241873 ((Concerto) Study of BLU-451 in Advanced Cancers With EGFR Exon 20 Insertion Mutations).

Mechanism: Pharmacologically active on Epidermal growth factor receptor
Curator reviewed
Formula / weight: C₂₄H₁₉F₄N₇O · 497.458 g/mol (avg)
Code names: BLU-203139; · BLU-451

Resolves to

Compound

UNIIG8G5AU5GLJCAS2769954-39-2ChEMBLCHEMBL6068412ChEBI760324PubChem163280903

Structure

InChIKeyXIMJCWSFLXXQMZ-UHFFFAOYSA-NSMILESCN1C=C(NC2=NC=C(C(NC3=C(F)C=CC(NC(=O)C=C)=C3)=N2)C2=CC=C(C=C2)C(F)(F)F)C=N1

Targets

P00533EGFR

What you can answer from here — as of September 23, 2026

1Protein targetEach mapped to UniProt, with action and pharmacological action

Listed above

1Clinical trialPhase, status and sponsor resolved per trial

2+ReferencesStructured and connected to the statements they support

Which drugs share a target with Pebezertinib, and which of those have an active Phase 3 trial?

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