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Bezuclastinib is an experimental small-molecule drug from Cogent Biosciences in phase 3 trials for gastrointestinal stromal tumour, aimed at KIT and MET.
Bezuclastinib (CGT9486) is a small-molecule drug developed by Cogent Biosciences. Its targets are KIT and MET (the sponsor names KIT (including KIT D816V)). The sponsor states: Bezuclastinib (CGT9486/PLX9486) is a selective tyrosine kinase inhibitor designed to potently inhibit KIT driver mutations, including the KIT D816V mutation that drives systemic mastocytosis, and is combined with sunitinib versus sunitinib alone in gastrointestinal stromal tumours. ClinicalTrials.gov describes the intervention as: Participants will receive CGT9486 orally until study stopping rules are met. It is the investigational product in 1 recruiting or active industry-led phase 2 and phase 3 interventional cancer trial, including the phase 3 study NCT05208047 ((Peak) A Phase 3 Randomised Trial of CGT9486+Sunitinib vs. Sunitinib in Subjects With Gastrointestinal Stromal Tumours), in gastrointestinal stromal tumour. The largest, NCT05208047, plans to enrol 482 participants with primary completion was scheduled for 2025-09-30 on the registry. Status reflects the highest phase registered on ClinicalTrials.gov; no efficacy results are recorded here.
Bezuclastinib (CGT9486/PLX9486) is a selective tyrosine kinase inhibitor designed to potently inhibit KIT driver mutations, including the KIT D816V mutation that drives systemic mastocytosis, and is combined with sunitinib versus sunitinib alone in gastrointestinal stromal tumours. Connects to KIT and MET.
1.Bezuclastinib slips into a pocket on KIT.
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Query for this drug: (TITLE:"Bezuclastinib" OR ABSTRACT:"Bezuclastinib" OR TITLE:"CGT9486" OR ABSTRACT:"CGT9486") 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 Bezuclastinib, not a curated reading list.
Shares KIT exon 11-mutant GIST, Imatinib-resistant GIST, Gastrointestinal stromal tumour (GIST) and the tag pipeline.
Shares KIT exon 11-mutant GIST, Imatinib-resistant GIST, Gastrointestinal stromal tumour (GIST) and the tag pipeline.
Shares Imatinib-resistant GIST, Gastrointestinal stromal tumour (GIST) and the tag pipeline.
Shares Cogent Biosciences and the tag pipeline.
Shares Cogent Biosciences and the tag pipeline.
Shares Indolent and smouldering systemic mastocytosis and the tag pipeline.
Shares Gastrointestinal stromal tumour (GIST) and the tag pipeline.