A potent and selective cFMS inhibitor EI-1071 inhibits CSF1R signaling and regulates tumor associated macrophages

Scholarly Communication
2018/09/14
A potent and selective cFMS inhibitor EI-1071 inhibits CSF1R signaling and regulates tumor associated macrophages

Preclinical studies show that so-called M2 tumor-associated macrophages (TAMs) forge an immunosuppressive microenvironment at metastatic niches to facilitate tumor cell colonization. Colony-stimulating factor 1 receptor (CSF-1R) signaling is known to regulate the survival and maintenance of M2 TAMs, suggesting that targeting CSF-1R might have therapeutic potential in halting cancer progression. To this end, we developed an orally active, selective small-molecule CSF-1R inhibitor, EI-1071. Preclinical characterization of EI-1071 demonstrated that it is a potent and selective CSF-1R inhibitor and has favorable drug properties for clinical evaluation.

The abstract for this presentation at the American Association for Cancer Research 2019 Annual Meeting can be found here and the poster here: AACR poster

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