Therapy Detail

Therapy Name Repotrectinib
Therapy Description

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).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Repotrectinib TPX-0005 ALK Inhibitor 19 JAK2 Inhibitor 17 ROS1 Inhibitor 14 SRC Inhibitor 26 Trk Receptor Inhibitor (Pan) 23 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).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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 ALK L1196M Advanced Solid Tumor sensitive Repotrectinib Preclinical - Cell culture Actionable In a preclinical study, Repotrectinib (TPX-0005) inhibited Alk activity and proliferation of transformed cells over expressing ALK L1196M in the context of EML4-ALK in culture (European Journal of Cancer , Volume 69, S32). detail...
ALK fusion Advanced Solid Tumor predicted - sensitive Repotrectinib Phase I Actionable In a Phase I (TRIDENT-1) trial, Repotrectinib (TPX-0005) treatment resulted in stable disease in 25% (4/16) of patient with advanced solid tumor harboring ALK fusions who completed 2 cycles of treatment (J Clin Oncol 36, 2018 (suppl; abstr 2513); NCT03093116). detail...
ROS1 fusion ROS1 G2032R Advanced Solid Tumor predicted - sensitive Repotrectinib Phase I Actionable In a Phase I (TRIDENT-1) trial, Repotrectinib (TPX-0005) treatment resulted in partial response in a patient with advanced solid tumor harboring ROS1 G2032R in the context of ROS1 fusion (J Clin Oncol 36, 2018 (suppl; abstr 2513); NCT03093116). detail...
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...
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...
ETV6-NTRK2 Advanced Solid Tumor sensitive Repotrectinib Preclinical - Cell culture Actionable In a preclinical study, Repotrectinib (TPX-0005) inhibited proliferation of transformed cells expressing ETV6-NTRK2 in culture (PMID: 30093503). 30093503
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...
ROS1 fusion Advanced Solid Tumor predicted - sensitive Repotrectinib Phase I Actionable In a Phase I (TRIDENT-1) trial, Repotrectinib (TPX-0005) treatment resulted in partial response in 21.6% (8/37) of patients with advanced solid tumors harboring ROS1 or NTRK fusions (J Clin Oncol 36, 2018 (suppl; abstr 2513); NCT03093116). detail...
EML4-ALK ALK G1202R Advanced Solid Tumor sensitive Repotrectinib Preclinical - Cell line xenograft Actionable In a preclinical study, Repotrectinib (TPX-0005) inhibited Alk activity and proliferation of transformed cells expressing ALK G1201R in the context of EML4-ALK in culture, resulted in tumor growth inhibition in cell line xenograft models (PMID: 30093503). 30093503 detail...
ETV6-NTRK3 Advanced Solid Tumor sensitive Repotrectinib Preclinical - Cell culture Actionable In a preclinical study, Repotrectinib (TPX-0005) inhibited proliferation of transformed cells expressing ETV6-NTRK3 in culture (PMID: 30093503). 30093503
EML4-ALK Advanced Solid Tumor sensitive Repotrectinib Preclinical - Cell line xenograft Actionable In a preclinical study, Repotrectinib (TPX-0005) inhibited growth of transformed cells expressing EML4-ALK in culture, led to tumor growth inhibition in cell line xenograft models (PMID: 30093503). 30093503
Clinical Trial Phase Therapies Title Recruitment Status
NCT03093116 Phase Ib/II Repotrectinib A Study of TPX-0005 in Patients With Advanced Solid Tumors Harboring ALK, ROS1, or NTRK1-3 Rearrangements Recruiting