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PLX73086 is a selective small molecule inhibitor of the colony-stimulating factor 1 receptor (CSF1R), developed as an antineoplastic agent. It acts by binding to CSF1R and blocking its activation and downstream signaling pathways, leading to reduced proliferation and survival of peripheral macrophages while sparing central nervous system microglia due to poor blood-brain barrier penetration[1][2][4][5]. This selectivity makes PLX73086 valuable for research into immune modulation in cancer and neuroinflammatory conditions. The drug was developed by Plexxikon (a subsidiary of Daiichi Sankyo) with Ambit Biosciences Corporation as the originator[3]. Clinical development reached phase 1 for indications such as giant cell tumour of tendon sheath and advanced solid tumors but was discontinued before approval[3][7].
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