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The receptor that macrophages depend on; blocking it shrinks tenosynovial giant cell tumour (a CSF1-driven tumour) and depletes tumour-supporting macrophages, though the latter has not yet helped patients with common cancers.
CSF1R signalling sustains macrophages and microglia. Tenosynovial giant cell tumour is driven by CSF1 translocation in a minority of cells that recruit a CSF1R-positive mass: pexidartinib (2019) and vimseltinib (2025) are approved; emactuzumab and cabiralizumab (antibodies) showed activity. In solid tumours, CSF1R blockade to deplete tumour-associated macrophages and combine with PD-1 inhibitors (cabiralizumab-nivolumab in pancreatic cancer) was disappointing. Axatilimab (anti-CSF1R) was approved in 2024 for chronic GVHD, targeting macrophage-driven fibrosis.
In plain words · The receptor that macrophages depend on; blocking it shrinks tenosynovial giant cell tumour (a CSF1-driven tumour) and depletes tumour-supporting macrophages, though the latter has not yet helped patients with common cancers.
The receptor that macrophages depend on; blocking it shrinks tenosynovial giant cell tumour (a CSF1-driven tumour) and depletes tumour-supporting macrophages, though the latter has not yet helped patients with common cancers.
Type III receptor tyrosine kinase for CSF1 and IL-34; controls differentiation, survival and function of monocytes, macrophages, osteoclasts and microglia.
4 products aim at CSF1R: antibodies and small molecules. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
Immune or microenvironment target: its medicines act on immune, stromal or bone cells rather than on the tumour cell (drug mechanisms in the corpus). HPA CSF1R: RNA tissue enhanced (lymphoid tissue 107 nTPM, placenta 97 nTPM); blood lineage lineage enriched (monocytes 650 nTPM); no normal tissue stained high; highest cancer staining ovarian cancer (1 of 9 high). Distribution: 3 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Sarcomas (soft tissue, bone, GIST), Pancreatic ductal adenocarcinoma, Brain and spinal cord tumours (all types)); Open Targets associates it with 5 specific cancer types at or above 0.5 (gastrointestinal stromal tumor, renal cell carcinoma, pigmented villonodular synovitis, soft tissue sarcoma, tenosynovial giant cell tumor). (Rule 1 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas CSF1R tissue; UniProt P07333; Open Targets ENSG00000182578 associations
First described 1985. Earliest sequence paper UniProt cites for the protein: Nienhuis A.W. et al, Cell, 1985, "Expression of the human c-fms proto-oncogene in hematopoietic cells and its deletion in the 5q- syndrome". Source.
Type III receptor tyrosine kinase for CSF1 and IL-34; controls differentiation, survival and function of monocytes, macrophages, osteoclasts and microglia.
RNA: tissue enhanced (lymphoid tissue 107 nTPM, placenta 97 nTPM), detected in all normal tissues. Blood: lineage enriched (monocytes 650 nTPM).
No normal tissue stained high; medium in Adrenal gland, Appendix, Bone marrow, Bronchus, Cerebellum, Cerebral cortex and more.
Medium only: breast cancer, cervical cancer, endometrial cancer, lung cancer.
HPA CSF1R tissue · HPA CSF1R pathology · HPA protein class: CD markers, FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Chiauranib is an experimental small-molecule drug from Chipscreen Biosciences in phase 3 trials for ovarian cancer, aimed at VEGF / VEGFR and KIT.
Emactuzumab is an experimental monoclonal antibody from SynOx Therapeutics in phase 3 trials for tenosynovial giant cell tumour, aimed at CSF1R.
Pexidartinib is the first drug for tenosynovial giant cell tumour, a benign but destructive joint tumour; it is effective but has liver toxicity that requires a restricted programme.
Surufatinib is HUTCHMED's angio-immuno kinase inhibitor, approved in China in 2020 for non-pancreatic and in 2021 for pancreatic neuroendocrine tumours.
One cancer page, one trial page, one treatment page and one target page on OnCo cite this paper by its DOI; this record gives the citation a page of its own so a reader can follow it without leaving OnCo. Read the abstract above alongside the citing pages listed under Related; the record was created automatically from the Europe PMC entry and its figures have not been checked by hand.
This review is the standard map of the tumour microenvironment and the reason microenvironment-directed drugs, from anti-angiogenics to macrophage and fibroblast targeting agents, are developed alongside tumour-cell-directed ones.
Query for this target: (TITLE:"CSF1R" OR ABSTRACT:"CSF1R") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about CSF1R, not a curated reading list.
Shares Vimseltinib, Pexidartinib, Surufatinib, Tenosynovial giant cell tumour (TGCT).
Shares The pre-metastatic niche, Complement in cancer, Nutrient competition & metabolic immunosuppression, Myeloid suppression: TAMs, MDSCs & don't-eat-me signals.
Shares Vimseltinib, Tenosynovial giant cell tumour (TGCT), Sarcomas (soft tissue, bone, GIST), Small-molecule kinase inhibitors.
Shares Pexidartinib, Tenosynovial giant cell tumour (TGCT), Small-molecule kinase inhibitors.
Shares Vimseltinib, Tenosynovial giant cell tumour (TGCT), Small-molecule kinase inhibitors.
Shares Quail and Joyce 2013: microenvironmental regulation of tumour progression and metastasis, Nutrient competition & metabolic immunosuppression, Myeloid suppression: TAMs, MDSCs & don't-eat-me signals.
Shares Nutrient competition & metabolic immunosuppression, The angiogenic switch & tumour vessels, Sarcomas (soft tissue, bone, GIST), Pancreatic ductal adenocarcinoma.