Therapy Detail
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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 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 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 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 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 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 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... |
| 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 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 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 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT05208047 | Phase III | Sunitinib PLX9486 + Sunitinib PLX9486 | (Peak) A Phase 3 Randomized Trial of CGT9486+Sunitinib vs. Sunitinib in Subjects With Gastrointestinal Stromal Tumors | Recruiting | USA | SWE | POL | NOR | NLD | ITA | HUN | GBR | FRA | ESP | DNK | DEU | CZE | CAN | BRA | AUS | ARG | 5 |
| 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 |
| 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 | Recruiting | USA | POL | NOR | NLD | ITA | IRL | GRC | GBR | FRA | ESP | DEU | CZE | CHE | CAN | BEL | AUT | AUS | 0 |
| 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 |
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