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Therapy Name | Pexidartinib + PLX9486 |
Synonyms | |
Therapy Description | |
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). | |
Pexidartinib | Turalio | PLX3397|CML-261 | CSF1R Inhibitor 28 FLT3 Inhibitor 69 KIT Inhibitor 57 | Turalio (pexidartinib) inhibits multiple receptor tyrosine kinases, including KIT, CSF1R, FLT3, and FLT3/ITD, which may inhibit growth in cancer cells (PMID: 22294205, PMID: 25993548, PMID: 25847190). Turalio (pexidartinib) is FDA approved for use in patients with symptomatic tenosynovial giant cell tumor (FDA.gov). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
KIT exon11 | gastrointestinal stromal tumor | predicted - sensitive | Pexidartinib + PLX9486 | Phase I | Actionable | In a Phase I trial, PLX9486 and Pexidartinib (PLX3397) combination therapy demonstrated safety and preliminary efficacy, resulted in a partial response rate of 8.3% (1/12) and progression-free survival not yet reached in patients with advanced solid tumors, 11 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 exon17 | gastrointestinal stromal tumor | predicted - sensitive | Pexidartinib + PLX9486 | Phase I | Actionable | In a Phase I trial, PLX9486 and Pexidartinib (PLX3397) combination therapy demonstrated safety and preliminary efficacy, resulted in a partial response rate of 8.3% (1/12) and progression-free survival not yet reached in patients with advanced solid tumors, 11 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... |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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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 |