EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor.

doi:10.1158/0008-5472.CAN-15-2581

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Article

EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor.

Cancer research - 15 Mar 2016

Jia Yong, Juarez Jose, Li Jie, Manuia Mari, Niederst Matthew J, Tompkins Celin, Timple Noelito, Vaillancourt Mei-Ting, Pferdekamper AnneMarie Culazzo, Lockerman Elizabeth L, Li Chun, Anderson Jennifer, Costa Carlotta, Liao Debbie, Murphy Eric, DiDonato Michael, Bursulaya Badry, Lelais Gerald, Barretina Jordi, McNeill Matthew, Epple Robert, Marsilje Thomas H, Pathan Nuzhat, Engelman Jeffrey A, Michellys Pierre-Yves, McNamara Peter, Harris Jennifer, Bender Steven, Kasibhatla Shailaja

Abstract excerpt

Non-small cell lung cancer patients carrying oncogenic EGFR mutations initially respond to EGFR-targeted therapy, but later elicit minimal response due to dose-limiting toxicities and acquired resistance. EGF816 is a novel, irreversible mutant-selective EGFR inhibitor that specifically targets EGFR-activating mutations arising de novo and upon resistance acquisition, while sparing wild-type (WT) EGFR. EGF816...

Topics

Animals
Antineoplastic Agents
Carcinoma, Non-Small-Cell Lung
Cell Line, Tumor
Drug Resistance, Neoplasm
ErbB Receptors
Female

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Lung Neoplasms

Mice

Mice, Nude

Mutation

Phosphorylation

Rats

Xenograft Model Antitumor Assays

Source

Open in PubMed

Identifiers

PMID: 26825170
DOI: 10.1158/0008-5472.CAN-15-2581

Genes

EGFR
EGF

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 30 Aug 2026.

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