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Taletrectinib (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).
|Drug Name||Trade Name||Synonyms||Drug Classes||Drug Description|
|Taletrectinib||DS6051b|DS-6051B|DS-6051|AB-106||ROS1 Inhibitor 19 Trk Receptor Inhibitor (Pan) 29||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, Taletrectinib (DS6051b) treatment resulted in a partial response in 3 patients and stable disease in 1 patient out of 4 patients with non-small cell lung cancer harboring ROS1 fusions with secondary ROS1 G2032R mutations ((J Clin Oncol 2022 40:16_suppl, 8572; NCT04395677).||detail...|
|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|
|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 July 15 2016 (76) (14 Supplement) CT024).||detail...|
|ROS1 fusion||lung non-small cell carcinoma||predicted - sensitive||Taletrectinib||Phase II||Actionable||In a Phase II trial, Taletrectinib (DS6051b) treatment in non-small cell lung cancer patients with ROS1 fusions resulted in a 90% (36/40) overall response rate (ORR) and 95% disease control rate (DCR) in TKI-naive patients and 47.6% (10/21) ORR and 76.2% DCR in crizotinib-pretreated patients, intracranial ORR of 83.3% (5/6) and DCR of 100% in patients with baseline brain lesions, and partial responses in 3 of 4 patients with secondary ROS1 G2032R mutations (J Clin Oncol 2022 40:16_suppl, 8572; NCT04395677).||detail...|
|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|
|Clinical Trial||Phase||Therapies||Title||Recruitment Status||Covered Countries||Other Countries|
|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 | ITA | FRA||3|