Therapy Detail
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| Therapy Name | Repotrectinib |
| Synonyms | |
| 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 26 JAK2 Inhibitor 16 ROS1 Inhibitor 17 SRC Inhibitor 31 Trk Receptor Inhibitor (Pan) 26 | 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, PMID: 32269053). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| 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... |
| 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... |
| 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 | 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 |
| ROS1 rearrange | lung non-small cell carcinoma | sensitive | Repotrectinib | Guideline | Actionable | Repotrectinib (TPX-0005) is included in guidelines as first-line therapy for patients with metastatic non-small cell lung cancer harboring a ROS1 rearrangement, or as a next-line therapy in patients with ROS1-rearranged non-small cell lung cancer who have not received prior ROS1 inhibitor therapy (PMID: 32169226, Version Update 15 Sept 2020; ESMO.org). | detail... 32169226 |
| 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 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... |
| 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 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... |
| 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... |
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- Use quotes to match a longer phrase which contains spaces "mtor c1483f"
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT03093116 | Phase Ib/II | Repotrectinib | A Study of Repotrectinib (TPX-0005) in Patients With Advanced Solid Tumors Harboring ALK, ROS1, or NTRK1-3 Rearrangements (TRIDENT-1) | Recruiting | USA | ITA | FRA | ESP | DEU | CAN | BEL | 12 |
| NCT04094610 | Phase Ib/II | Repotrectinib | A Study of Repotrectinib in Pediatric and Young Adult Subjects Harboring ALK, ROS1, OR NTRK1-3 Alterations | Recruiting | USA | CAN | 4 |
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