Drug intelligence / Profile preview

pf-06459988

Development stage: Discontinued
Lead developer: Pfizer
Modality: Small Molecules
Administration: Oral

Overview

PF-06459988 is a third-generation, orally active, irreversible and mutant-selective inhibitor of the epidermal growth factor receptor (EGFR), specifically designed to target EGFR mutants containing the T790M resistance mutation. It demonstrates high potency and specificity for double-mutant EGFRs (such as L858R/T790M or Del19/T790M) while exhibiting minimal activity against wild-type EGFR. This selectivity aims to reduce adverse effects associated with wild-type EGFR inhibition. The drug was developed by Pfizer for the treatment of cancers—primarily non-small cell lung cancer (NSCLC)—harboring these resistant mutations[1][3][5][7][9].

Other names: PF-06459988PF06459988PF 06459988PF 6459988PF6459988PF-6459988

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)

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