Drug intelligence / Profile preview

PLX3397 + eribulin

Development stage: Phase 2
Lead developer: Daiichi Sankyo
Modality: Small Molecules
Administration: Oral, Intravenous

Overview

PLX3397 (pexidartinib) is a selective inhibitor of the colony-stimulating factor 1 receptor (CSF1R, also known as FMS) and KIT tyrosine kinases. It modulates the tumor microenvironment by depleting tumor-associated macrophages and myeloid-derived suppressor cells, potentially overcoming resistance to chemotherapy. Eribulin mesylate (Halaven) is a microtubule inhibitor approved for metastatic breast cancer after prior chemotherapy regimens. The combination of PLX3397 and eribulin is being investigated in clinical trials for metastatic breast cancer to determine safety, tolerability, and efficacy[3][4][5].

Targets

CSF1R (Macrophage colony-stimulating factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)TUBB (Tubulin (alpha and beta subunits))

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