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Ref Type

PMID

Authors

Andrew J. Wagner, William D. Tap, Anthony Frank Shields, Amita Patnaik, Rashmi Chugh, Gabriel Tinoco,

Title

A phase I pharmacokinetic (PK) and pharmacodynamic (PD) study of PLX9486 alone and in combination (combo) with the KIT inhibitors pexidartinib (pexi) or sunitinib (su) in patients (Pts) with advanced solid tumors and gastrointestinal stromal tumor (GIST).

Journal	Vol	Issue	Date	Pages	Journal Short Title
Journal of Clinical Oncology

URL

http://ascopubs.org/doi/abs/10.1200/JCO.2018.36.15_suppl.11509#affiliationsContainer

Abstract Text

Journal of Clinical Oncology 36, no. 15_suppl (May 20 2018) 11509-11509

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Therapy Name	Drugs	Efficacy Evidence	Clinical Trials
PLX9486	PLX9486	9	4

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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	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	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 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...

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