Therapy Detail
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| Therapy Name | DS6051b |
| Synonyms | |
| Therapy Description |
DS6051b is an inhibitor of NTRK1/2/3 and ROS1 fusion proteins, which inhibits downstream signaling and may lead to decreased tumor cell growth (Cancer Res 2016;76(14 Suppl):Abstract nr CT024). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| DS6051b | DS-6051B|DS-6051|AB-106|Taletrectinib | ROS1 Inhibitor 14 Trk Receptor Inhibitor (Pan) 23 | DS6051b is an inhibitor of NTRK1/2/3 and ROS1 fusion proteins, which blocks downstream signaling and may lead to inhibition of tumor cell growth (PMID: 32591465). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| ETV6 - NTRK3 | Advanced Solid Tumor | sensitive | DS6051b | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ETV6-NTRK3 were sensitive to treatment with DS6051b in culture, demonstrating cell growth inhibition (PMID: 31399568). | 31399568 |
| ROS1 fusion | lung non-small cell carcinoma | predicted - sensitive | DS6051b | Phase I | Actionable | In a Phase I clinical trial, DS-6051b was well-tolerated and demonstrated some preliminary efficacy in patients with advanced solid tumors, including a partial response in a patient with non-small cell lung cancer liver metastases harboring a ROS1 fusion (Cancer Res July 15 2016 (76) (14 Supplement) CT024). | detail... |
| Unknown unknown | neuroendocrine carcinoma | not applicable | DS6051b | Phase I | Actionable | In a Phase I clinical trial, treatment with DS-6051b was well-tolerated in patients with advanced solid tumors, and resulted in partial responses in two patients, including a patient with neuroendocrine carcinoma (Cancer Res July 15 2016 (76) (14 Supplement) CT024). | detail... |
| EML4 - ALK | Advanced Solid Tumor | sensitive | DS6051b | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing EML4-ALK were sensitive to treatment with DS6051b in culture, demonstrating cell growth inhibition (PMID: 31399568). | 31399568 |
| Unknown unknown | neuroendocrine tumor | not applicable | DS6051b | Phase I | Actionable | In a Phase I trial, DS6051b demonstrated manageable toxicity, resulted in an objective response rate of 8.3% (1/12) in patients with advanced neuroendocrine tumors (NET), with 1 patient with small bowel NET achieving a partial response with a median progression-free survival of 10.2 months (PMID: 32591465). | 32591465 |
| ETV6 - NTRK2 | Advanced Solid Tumor | sensitive | DS6051b | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ETV6-NTRK2 were sensitive to treatment with DS6051b in culture, demonstrating cell growth inhibition (PMID: 31399568). | 31399568 |
| Unknown unknown | Advanced Solid Tumor | not applicable | DS6051b | Phase I | Actionable | In a Phase I clinical trial, DS-6051b was well-tolerated and demonstrated some preliminary efficacy in patients with advanced solid tumors (Cancer Res July 15 2016 (76) (14 Supplement) CT024). | detail... |
| ROS1 rearrange | lung non-small cell carcinoma | predicted - sensitive | DS6051b | Phase I | Actionable | In a Phase I trial, DS6051b demonstrated manageable toxicity, resulted in an objective response rate of 33.3% (2/6) in patients with advanced non-small cell lung cancer harboring ROS1 rearrangements (PMID: 32591465). | 32591465 |
| ETV6 - NTRK1 | Advanced Solid Tumor | sensitive | DS6051b | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ETV6-NTRK1 were sensitive to treatment with DS6051b in culture, demonstrating cell growth inhibition (PMID: 31399568). | 31399568 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status |
|---|---|---|---|---|
| NCT02279433 | Phase I | DS6051b | A First-in-human Study to Evaluate the Safety, Tolerability and Pharmacokinetics of DS-6051b | Active, not recruiting |
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