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Therapy Name	PLX9486
Synonyms
Therapy Description	PLX9486 is a Kit inhibitor with selective activity against primary (exon 9 and 11) and secondary (exon 17 and 18) Kit mutations, which may lead to growth inhibition in tumor cells expressing mutant c-Kit (Journal of Clinical Oncology 36, no. 15_suppl (May 20 2018) 11509-11509, PMID: 30523507).

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Drug Name	Trade Name	Synonyms	Drug Classes	Drug Description
PLX9486		PLX-9486\|PLX 9486\|Bezuclastinib\|CGT-9486\|CGT9486\|CGT 9486	KIT Inhibitor 57	PLX9486 is a Kit inhibitor with selective activity against primary (exon 9 and 11) and secondary (exon 17 and 18) Kit mutations, which may lead to growth inhibition in tumor cells expressing mutant c-Kit (Journal of Clinical Oncology 36, no. 15_suppl (May 20 2018) 11509-11509, PMID: 30523507).

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Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
KIT exon11	gastrointestinal stromal tumor	predicted - sensitive	PLX9486	Phase I	Actionable	In a Phase I trial, PLX9486 demonstrated safety and preliminary efficacy, resulted in a progression-free survival of more than 24 weeks and partial response in 8.3% (2/24) of patients with advanced solid tumors, 20 of these patients had gastrointestinal stromal tumor that progressed on Gleevec (imatinib mesylate), and most harbored KIT exon 11 and exon 17 mutations (Journal of Clinical Oncology 36, no. 15_suppl (May 20 2018) 11509-11509; NCT02401815).	detail...
KIT exon11 KIT exon17	gastrointestinal stromal tumor	predicted - sensitive	PLX9486	Phase I	Actionable	In a Phase I trial, PLX9486 treatment resulted in partial response with 33% decrease of tumor size after 4 cycles of therapy in a patient with gastrointestinal stromal tumor harboring a primary KIT exon 11 mutation and a secondary KIT exon 17 mutation, who progressed on prior Gleevec (imatinib mesylate) and Sutent (sunitinib) therapies (CTOS Annual Meeting, Nov 2017, abstract # 2771952).	detail...
KIT exon17	gastrointestinal stromal tumor	predicted - sensitive	PLX9486	Phase I	Actionable	In a Phase I trial, PLX9486 demonstrated safety and preliminary efficacy, resulted in a progression-free survival of more than 24 weeks and partial response in 8.3% (2/24) of patients with advanced solid tumors, 20 of these patients had gastrointestinal stromal tumor that progressed on Gleevec (imatinib mesylate), and most harbored KIT exon 11 and exon 17 mutations (Journal of Clinical Oncology 36, no. 15_suppl (May 20 2018) 11509-11509; NCT02401815).	detail...
KIT W557_K558del KIT Y823D	gastrointestinal stromal tumor	sensitive	PLX9486	Preclinical - Pdx	Actionable	In a preclinical study, PLX9486 treatment decreased Mapk phosphorylation, inhibited proliferation, and reduced tumor growth and induced regression in a Gleevec (imatinib)-resistant patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT W557_K558del and Y823D (PMID: 30523507).	30523507
KIT W557Lfs*5 KIT P577del KIT D820G	gastrointestinal stromal tumor	sensitive	PLX9486	Preclinical - Pdx	Actionable	In a preclinical study, PLX9486 treatment decreased Mapk phosphorylation and Kit downstream signaling, inhibited proliferation, and reduced tumor growth in a Gleevec (imatinib)-resistant patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT P577del, W557Lfs*5, and D820G (PMID: 30523507).	30523507
KIT D816V	Advanced Solid Tumor	sensitive	PLX9486	Preclinical - Cell culture	Actionable	In a preclinical study, PLX9486 treatment inhibited proliferation of Gleevec (imatinib)-resistant transformed cells expressing KIT D816V in culture (PMID: 30523507).	30523507
KIT V560G KIT D816V	Advanced Solid Tumor	sensitive	PLX9486	Preclinical - Cell culture	Actionable	In a preclinical study, PLX9486 treatment inhibited proliferation of Gleevec (imatinib)-resistant transformed cells expressing KIT V560G and D816V in culture (PMID: 30523507).	30523507
KIT wild-type	Advanced Solid Tumor	sensitive	PLX9486	Preclinical - Cell culture	Actionable	In a preclinical study, PLX9486 treatment inhibited proliferation of ligand-stimulated cells expressing wild-type KIT in culture (PMID: 30523507).	30523507
KIT act mut	Advanced Solid Tumor	sensitive	PLX9486	Preclinical	Actionable	In a preclinical study, PLX9486 inhibited KIT mutations, including exon 17 mutations, and demonstrated in vivo and in vitro activity against tumors harboring KIT exon 17 mutations (Cancer Res February 1, 2016 76; IA32).	detail...

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Clinical Trial	Phase	Therapies	Title	Recruitment Status	Covered Countries	Other Countries
NCT05186753	Phase II	PLX9486	(Summit) A Study to Evaluate the Efficacy and Safety of CGT9486 Versus Placebo in Patients With Indolent or Smoldering Systemic Mastocytosis	Active, not recruiting	USA \| POL \| NOR \| NLD \| ITA \| IRL \| GRC \| GBR \| FRA \| ESP \| DEU \| CZE \| CHE \| CAN \| BEL \| AUT \| AUS	0
NCT05208047	Phase III	Sunitinib PLX9486 + Sunitinib PLX9486	(Peak) a Phase 3 Randomized Trial of CGT9486+Sunitinib Vs. Sunitinib in Subjects with Gastrointestinal Stromal Tumors	Active, not recruiting	USA \| SWE \| POL \| NOR \| NLD \| ITA \| HUN \| GBR \| FRA \| ESP \| DNK \| DEU \| CZE \| CAN \| BRA \| AUS \| ARG	5
NCT02401815	Phase Ib/II	PLX9486 + Sunitinib Pexidartinib + PLX9486 PLX9486	PLX9486 as a Single Agent and in Combination With PLX3397 or PLX9486 With Sunitinib in Patients With Advanced Solid Tumors	Completed	USA	0
NCT04996875	Phase II	PLX9486	(Apex) Bezuclastinib in Patients With Advanced Systemic Mastocytosis	Recruiting	USA \| POL \| NOR \| NLD \| ITA \| GBR \| FRA \| ESP \| DEU \| CHE \| CAN \| BEL \| AUT \| AUS	0

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