Quantum Leap Healthcare Collaborative

Agent Information Sheet

Widely hailed as the future of phase II drug development, the adaptive I-SPY 2 platform trial has set a new benchmark for
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I-SPY Trial Manuscript
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pexidartinib

Trade Name:
PLX3397
Company:
Status:
Halted for Toxicity
Agent Chaperone(s):
Treatment Protocol:
PLX 3397 is a Kinase Inhibitor. PLX3397 is orally administered at 1200mg/day (600mg, BID) twice a day with paclitaxel administered at 80 mg/m2 once a week for 12 total weeks.This regimen is followed by AC (q2w or q3w) for four weeks.
Date Entered I-SPY:
August 17, 2015
Date Left I-SPY:
October 22, 2015
No. Participants in Arm:
9
Graduating Subtypes:
Agent Description:

Pexidartinib is a capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity. Pexidartinib binds to and inhibits phosphorylation of stem cell factor receptor (KIT), colony-stimulating factor-1 receptor (CSF1R) and FMS-like tyrosine kinase 3 (FLT3), which may result in the inhibition of tumor cell proliferation and down-modulation of macrophages, osteoclasts and mast cells involved in the osteolytic metastatic disease. FLT3, CSF1R and FLT3 are overexpressed or mutated in many cancer cell types and play major roles in tumor cell proliferation and metastasis.

Notes:
Final pCR Probabilities:
Primary Manuscript:
 
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