Reference Detail

Ref Type
PMID
Authors Dayong Zhai, Wei Deng, Zhongdong Huang, Evan Rogers, J. Jean Cui.
Title The novel, rationally-designed, ALK/SRC inhibitor TPX-0005 overcomes multiple acquired resistance mechanisms to current ALK inhibitors
Journal AACR
Vol
Issue
Date
URL http://www.abstractsonline.com/Plan/ViewAbstract.aspx?sKey=055d4461-9793-4f83-b663-f356d9ae0fdb&cKey=ff6f8d25-f06a-4ae4-9dbf-7e390ef45123&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 Therapy Description
Repotrectinib Repotrectinib (TPX-0005) is a multi-kinase inhibitor that demonstrates strong activity against Ros1, Ntrk1/2/3, and Alk, and also inhibits Jak2 and Src family kinases, resulting in tumor cell death (PMID: 30093503).
Drug Name Trade Name Synonyms Drug Classes Drug Description
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
ALK G1202R Advanced Solid Tumor sensitive Repotrectinib Preclinical - Cell line xenograft Actionable In a preclinical study, Repotrectinib (TPX-0005) inhibited ALK G1202R and suppressed tumor growth in cell line xenograft models with ALK G1202R (AACR, Cancer Res: April 2016; Volume 57, Abstract #2132). detail...
EML4-ALK SRC pos lung cancer resistant Crizotinib Preclinical - Cell culture Actionable In a preclinical study, lung cancer cell lines harboring EML4-ALK and elevated Src activity were resistant to Xalkori (crizotinib) induced growth inhibition in culture (AACR, Cancer Res: April 2016; Volume 57, Abstract #2132). detail...
ALK wild-type Advanced Solid Tumor sensitive Repotrectinib Preclinical - Cell line xenograft Actionable In a preclinical study, Repotrectinib (TPX-0005) inhibited cell proliferation in transformed cell lines over expressing wild-type ALK in culture and suppressed tumor growth in xenograft models (AACR, Cancer Res: April 2016; Volume 57, Abstract #2132). detail...
EML4-ALK SRC pos lung cancer sensitive Repotrectinib Preclinical - Cell culture Actionable In a preclinical study, TPX-0005 inhibited Alk and Src signaling, and cell proliferation in lung cancer cell lines harboring EML4-ALK and elevated Src activity in culture (AACR, Cancer Res: April 2016; Volume 57, Abstract #2132). detail...
ALK L1196M Advanced Solid Tumor sensitive Repotrectinib Preclinical - Cell culture Actionable In a preclinical study, Repotrectinib (TPX-0005) inhibited cell proliferation in transformed cell lines over expressing ALK L1196M in culture (AACR, Cancer Res: April 2016; Volume 57, Abstract #2132). detail...
EML4-ALK SRC pos Advanced Solid Tumor resistant Ceritinib Preclinical - Cell culture Actionable In a preclinical study, lung cancer cell lines harboring EML4-ALK and elevated Src activity were resistant to Zykadia (ceritinib) induced growth inhibition in culture (AACR, Cancer Res: April 2016; Volume 57, Abstract #2132). detail...