Drug intelligence / Profile preview

pexidartinib + temozolomide

Development stage
Phase 2
Lead developer
Daiichi Sankyo
Modality
Small Molecules
Administration
Oral
01

Overview

Pexidartinib + temozolomide is an investigational combination therapy studied primarily in newly diagnosed glioblastoma. Pexidartinib is an orally bioavailable small-molecule tyrosine kinase inhibitor targeting colony-stimulating factor 1 receptor (CSF1R), KIT, and FMS-like tyrosine kinase 3 (FLT3). It modulates the tumor microenvironment by inhibiting CSF1R signaling, which can reduce tumor-associated macrophages and potentially sensitize tumors to standard therapies. Temozolomide is an oral alkylating agent that induces DNA damage in cancer cells. The combination has been evaluated alongside radiation therapy to assess whether altering the tumor microenvironment with pexidartinib enhances the efficacy of standard-of-care chemoradiation with temozolomide. Clinical trials have established recommended dosing regimens but have not demonstrated significant improvement in progression-free or overall survival compared to historical controls[1][3][5][6].

Other names
pexidartinib and temozolomidePEX + TMZ
02

Targets

CSF1R (Macrophage colony-stimulating factor receptor)DNAFLT3-ITD (Fms-like tyrosine kinase 3 with internal tandem duplication)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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