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Updated: Apr 11, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
CSF-1/CSF-1R targeting agents in clinical development for cancer therapy
Carola H Ries1, Sabine Hoves1, Michael A Cannarile1
1Roche Pharmaceutical Research and Early Development, Roche Innovation Center Penzberg, Nonnenwald 2, 82377 Penzberg, Germany.
Abstract:
Macrophage infiltration has been identified as an independent poor prognostic factor for several cancer entities. In mouse tumor models macrophages orchestrate various tumor-promoting processes. This observation sparked an interest to therapeutically target these plastic innate immune cells. To date, blockade of colony stimulating factor-1 or its receptor represents the only truly selective approach to manipulate macrophages in cancer patients. Here, we discuss the currently available information on efficacy and safety of various CSF-1/CSF-1R inhibitors in cancer patients and highlight potential combination partners emerging from preclinical studies while considering the differences between mouse and human macrophage biology.
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