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Table 2 Clinical trials with CSF1/CSF1R inhibitors in combination with anti-tumor therapies (excluding cancer-immunotherapy doublets)

From: Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy

Class Target Compound Combination partner Clinical phase Sponsor Indication identifier Status/Results Reference
Small molecules CSF1R (and cKIT, Flt3) Pexidartinib
(PLX3397, PLX108-01)
Androgen-deprivation therapy plus external radiotherapy 1 Plexxikon/Daiichi Sankyo Prostate cancer NCT02472275 Ongoing -
Paclitaxel 1 Plexxikon/Daiichi Sankyo Solid tumors NCT01525602 ORR: 4/23 (17%)
CBR: 14/23 (61%)
Eribulin 1/2 Plexxikon/Daiichi Sankyo Breast cancer NCT01596751 Ongoing -
Temozolomide plus external radiotherapy 1/2 Plexxikon/Daiichi Sankyo GBM NCT01790503 Not yet reported -
Vemurafenib 1 Plexxikon/Daiichi Sankyo BRAF-mutated melanoma NCT01826448 Terminated -
PLX9486 (KIT inhibitor) 1/2 Plexxikon/Daiichi Sankyo GIST NCT02401815 Ongoing -
Sirolimus 1/2 Plexxikon/Daiichi Sankyo Advanced sarcomas, MPNST NCT02584647 Ongoing, not yet reported [73]
Monoclonal antibodies CSF1R Emactuzumab (RG7155) Paclitaxel 1 Roche Ovarian and breast cancer NCT01494688 Not yet reported -
CSF1R Emactuzumab (RG7155) Paclitaxel plus bevacizumab 2 Roche Ovarian cancer NCT02923739 Ongoing -
CSF1 MCS110 Carboplatin plus gemcitabine 2 Novartis TNBC NCT02435680 Ongoing -
CSF1 PD-0360324 Cyclophosphamide 2 Pfizer Recurrent platinum-resistant epithelial ovarian, peritoneal, or fallopian tube cancer NCT02948101 Ongoing -
  1. CBR clinical benefit rate, CSF1 colony-stimulating factor 1, CSF1R colony-stimulating factor 1 receptor, dt-GCT diffuse-type tenosynovial giant cell tumor, GBM glioblastoma, GIST gastrointestinal stromal tumor, MPNST malignant peripheral nerve sheath tumor, ORR objective response rate, TNBC triple-negative breast cancer