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Synonyms: RG7155 | RO5509554
Compound class:
Antibody
Comment: Emactuzumab is a humanized, IgG1κ anti-colony stimulating factor 1 receptor (CSF1R) monoclonal antibody, being investigated for its anti-cancer potential.
Peptide sequence and structural information for this antibody are available from its IMGT/mAb-db record. Peptide sequence analysis using the heavy and light chain variable regions of emactuzumab reveals 100% matches to sequences 39 and 40 respectively from patent US20110165156 [2]. These two sequences belong to the clone named hMab 2F11-e7 (or simply 2F11) in the patent document. In 2018 Roche terminated their emactuzumab development programme. In August 2020 they announced that they were licensing emactuzumab to Celleron Therapeutics who intent to progress the drug as a treatment for diffuse tenosynovial giant cell tumours (TGCT), for which Roche have alreaady published efficacy [7], TGCT is driven by cells that overproduce the CSF1 protein which attracts the macrophages that ultimately cause the inflammatory damage that characterises the disease. 
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| No information available. |
Summary of Clinical Use  |
| Emactuzumab has progressed to Phase 2 clinical evaluation in patients with a range of advanced/metastatic solid tumours (as of November 2018). Click here to link to ClinicalTrials.gov's full list of emactuzumab trials. |
| Clinical Trials | |||||
| Clinical Trial ID | Title | Type | Source | Comment | References |
| NCT01494688 | A Study of RO5509554 as Monotherapy and in Combination With Paclitaxel in Participants With Advanced Solid Tumors | Phase 1 Interventional | Hoffmann-La Roche | Although emactuzumab reduced immunosuppressive tumour-associated macrophages in the tumours of trial participants, it showed no antitumor efficacy. The drug did however exhibit signs of benefit in a cohort of patients with TGCT in a dose-escalation and dose-expansion of the study. | 1,3 |
