TK216
TK216 was an attempt to hit the fusion protein that causes Ewing sarcoma directly, something long thought impossible for a transcription factor. In early trials with vincristine it produced a few responses but not enough to carry the drug forward.
Overview
TK216 was Oncternal Therapeutics' first-in-class small molecule aimed at EWS-FLI1, the fusion transcription factor present in about 85 percent of Ewing sarcomas. It was given as a continuous intravenous infusion, alone and with vincristine, in a phase 1/2 trial in relapsed or refractory Ewing sarcoma. A minority of heavily pretreated patients had objective responses, including some complete responses, but the response rate did not meet the threshold for a registrational study and the sponsor did not continue development.
The Ewing sarcoma page names it with IGF-1R antibodies and PARP inhibitors among the targeted approaches that have not yet succeeded, while lurbinectedin and combinations remain in trials.
Designed from the YK-4-279 series to bind the EWS-FLI1 fusion oncoprotein and prevent its interaction with RNA helicase A, disabling the transcription factor that drives Ewing sarcoma; it also disrupts microtubules. Connects to EWSR1-FLI1 fusion.
1.TK216 slips into a pocket on EWSR1-FLI1 fusion.
Trials
topTrials recruiting now
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Latest papers
topQuery for this drug: (TITLE:"TK216" OR ABSTRACT:"TK216" OR TITLE:"TK-216" OR ABSTRACT:"TK-216") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about TK216, not a curated reading list.
Similar pages
not linked directly; found by shared links- TrialStudy of Lurbinectedin Monotherapy in Pediatric and Young Adult Participants With Relapsed/Refractory Ewing Sarcoma
Shares Lurbinectedin, Ewing sarcoma.
- TermHistological response to induction chemotherapy (osteosarcoma and Ewing sarcoma)
Shares EWSR1-FLI1 fusion, Ewing sarcoma, Vincristine.
- CompanyPharmaMar
Shares Lurbinectedin, Ewing sarcoma.
- CompanyJazz Pharmaceuticals
Shares Lurbinectedin, Ewing sarcoma.
- PathwayTranscriptional machinery & addiction
Shares EWSR1-FLI1 fusion, Ewing sarcoma.
- TermGene fusion
Shares EWSR1-FLI1 fusion, Ewing sarcoma.