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Therapy Name | Taletrectinib |
Synonyms | |
Therapy Description |
Taletrectinib (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). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Taletrectinib | DS6051b|DS-6051B|DS-6051|AB-106 | ROS1 Inhibitor 22 Trk Receptor Inhibitor (Pan) 33 | Taletrectinib (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). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
ROS1 fusion ROS1 G2032R | lung non-small cell carcinoma | predicted - sensitive | Taletrectinib | Case Reports/Case Series | Actionable | In a Phase II trial (TRUST-I), Taletrectinib (DS6051b) treatment resulted in an objective response rate of 66.7% (8/12, all partial responses) in patients with non-small cell lung cancer harboring ROS1 fusions with secondary ROS1 G2032R mutations (PMID: 38822758; NCT04395677). | 38822758 |
ROS1 rearrange | lung non-small cell carcinoma | predicted - sensitive | Taletrectinib | Phase I | Actionable | In a Phase I trial, Taletrectinib (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 |
EML4 - ALK | Advanced Solid Tumor | sensitive | Taletrectinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing EML4-ALK were sensitive to treatment with Taletrectinib (DS6051b) in culture, demonstrating cell growth inhibition (PMID: 31399568). | 31399568 |
ROS1 fusion | lung non-small cell carcinoma | predicted - sensitive | Taletrectinib | Phase II | Actionable | In a Phase II trial (TRUST-I), Taletrectinib (DS6051b) treatment in non-small cell lung cancer patients with ROS1 fusions resulted in a 90.6% (96/106) overall response rate (ORR) and 95.3% disease control rate (DCR) in TKI-naive patients and 51.5% (34/66) ORR and 83.3% DCR in crizotinib-pretreated patients, intracranial ORR of 87.5% (7/8) and DCR of 100% in patients with baseline brain lesions, and partial responses in 8 of 12 patients with secondary ROS1 G2032R mutations (PMID: 38822758; NCT04395677). | 38822758 |
ROS1 fusion | lung non-small cell carcinoma | predicted - sensitive | Taletrectinib | Phase I | Actionable | In a Phase I trial, Taletrectinib (DS6051b) 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 2016;76(14 Suppl):Abstract nr CT024; NCT02279433). | detail... |
ROS1 fusion | lung non-small cell carcinoma | predicted - sensitive | Taletrectinib | Phase II | Actionable | In a Phase II trial (TRUST-II), Taletrectinib (DS6051b) treatment demonstrated safety in ROS1 fusion-positive non-small cell lung cancer patients and resulted in a confirmed investigator-assessed objective response rate (cORRinv) of 94% (17/18) and a disease control rate (DCR) of 100% in the treatment-naive cohort and a cORRinv of 55% (12/22) and DCR of 91% in the previously treated cohort (Ann Oncol (2023) 34 (suppl_2):S788-S789; NCT04919811). | detail... |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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NCT02279433 | Phase I | Taletrectinib | A First-in-human Study to Evaluate the Safety, Tolerability and Pharmacokinetics of DS-6051b | Completed | USA | 0 |
NCT04919811 | Phase II | Taletrectinib | Taletrectinib Phase 2 Global Study in ROS1 Positive NSCLC (TRUST-II) | Recruiting | USA | POL | ITA | FRA | ESP | CAN | 3 |
NCT06214793 | Phase II | Taletrectinib | Taletrectinib in Previously Treated Metastatic CDH1-mutated Invasive Lobular Cancer (ILC) | Suspended | USA | 0 |