{"entity":{"id":"bezuclastinib","kind":"drug","name":"Bezuclastinib","aka":[],"tldr":"Bezuclastinib is an experimental small-molecule drug from Cogent Biosciences in phase 3 trials for gastrointestinal stromal tumour, aimed at KIT and MET.","summary":"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.","status":"phase-3","asOf":"2026-09-11","links":[{"label":"ClinicalTrials.gov: trials of Bezuclastinib","url":"https://clinicaltrials.gov/search?intr=Bezuclastinib"},{"label":"Sponsor pipeline page","url":"https://www.cogentbio.com/pipeline"}],"tags":["pipeline","ctgov-ingest"],"related":[],"cancers":["gist","indolent-systemic-mastocytosis","advanced-systemic-mastocytosis"],"sections":[],"technologies":[],"targets":["kit","met"],"drugs":[],"companies":["cogent-biosciences"],"institutions":[],"pathways":[],"terms":[],"trials":["nct05208047","nct05186753","nct04996875"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"provenance":{"editedBy":"OnCo ingestion (ClinicalTrials.gov v2 + sponsor pipeline pages)","editedOn":"2026-09-11"},"code":"CGT9486","modality":"small molecule","mechanism":"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.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},"route":"/drugs/bezuclastinib/","neighbours":{"cancer":[{"id":"advanced-systemic-mastocytosis","kind":"cancer","name":"Advanced systemic mastocytosis (aggressive SM, SM with an associated haematological neoplasm, mast cell leukaemia)","route":"/cancers/advanced-systemic-mastocytosis/"},{"id":"gist","kind":"cancer","name":"Gastrointestinal stromal tumour (GIST)","route":"/cancers/gist/"},{"id":"gist-imatinib-resistant","kind":"cancer","name":"Imatinib-resistant GIST","route":"/cancers/gist-imatinib-resistant/"},{"id":"indolent-systemic-mastocytosis","kind":"cancer","name":"Indolent and smouldering systemic mastocytosis","route":"/cancers/indolent-systemic-mastocytosis/"},{"id":"gist-kit-exon-11","kind":"cancer","name":"KIT exon 11-mutant GIST","route":"/cancers/gist-kit-exon-11/"}],"target":[{"id":"kit","kind":"target","name":"KIT","route":"/targets/kit/"},{"id":"met","kind":"target","name":"MET","route":"/targets/met/"}],"company":[{"id":"cogent-biosciences","kind":"company","name":"Cogent Biosciences","route":"/companies/cogent-biosciences/"}],"trial":[{"id":"nct04996875","kind":"trial","name":"(Apex) Bezuclastinib in Patients With Advanced Systemic Mastocytosis","route":"/trials/nct04996875/"},{"id":"nct05208047","kind":"trial","name":"(Peak) A Phase 3 Randomized Trial of CGT9486+Sunitinib vs. Sunitinib in Subjects With Gastrointestinal Stromal Tumors","route":"/trials/nct05208047/"},{"id":"nct05186753","kind":"trial","name":"(Summit) A Study to Evaluate the Efficacy and Safety of CGT9486 Versus Placebo in Patients With Indolent or Smoldering Systemic Mastocytosis","route":"/trials/nct05186753/"}]}}