Reference Detail

Ref Type
PMID
Authors Francois Gonzalvez, Xiaotian Zhu, Wei-Sheng Huang, Theresa E. Baker, Yaoyu Ning, Scott D. Wardwell, Sara Nadworny, Sen Zhang, Biplab Das, Yongjin Gong, Matthew T. Greenfield, Hyun G. Jang, Anna Kohlmann, Feng Li, Paul M. Taslimi, Meera Tugnait, Yongjin Xu
Title AP32788, a potent, selective inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, in preclinical models
Journal
Vol
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Date
URL http://www.abstractsonline.com/Plan/ViewAbstract.aspx?mID=4017&sKey=407e597a-33c8-4936-87f4-08ee4b23e8b9&cKey=34ee7ebf-07c6-40ea-825f-28fb5018ec92&mKey=1d10d749-4b6a-4ab3-bcd4-f80fb1922267
Abstract Text

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
AP32788 AP32788 2 1
Drug Name Trade Name Synonyms Drug Classes Drug Description
AP32788 TAK-788 EGFR Inhibitor (Pan) 43 HER2 Inhibitor 22 AP32788 inhibits EGFR and ERBB2 (HER2), with selectivity for mutant forms including EGFR exon 20 insertions, potentially resulting in growth inhibition in EGFR or ERBB2-mutant cancer cells (AACR, Cancer Res: April 2016; Volume 57, Abstract #2644).
Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
ERBB2 exon 20 ins Advanced Solid Tumor sensitive AP32788 Preclinical - Pdx & cell culture Actionable In a preclinical study, AP32788 inhibited growth of transformed cell lines over expressing ERBB2 (HER2) exon 20 insertions in culture, and induced tumor regression in PDX models (AACR, Cancer Res: April 2016; Volume 57, Abstract #2644). detail...
ERBB2 G776V Advanced Solid Tumor sensitive AP32788 Preclinical - Cell culture Actionable In a preclinical study, AP32788 inhibited growth of transformed cell lines over expressing ERBB2 (HER2) G776V in culture (AACR, Cancer Res: April 2016; Volume 57, Abstract #2644). detail...