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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 . 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 , 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 Charts
These 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.✖
1. Cassier PA, Italiano A, Gomez-Roca CA, Le Tourneau C, Toulmonde M, Cannarile MA, Ries C, Brillouet A, Müller C, Jegg AM et al.. (2015)
CSF1R inhibition with emactuzumab in locally advanced diffuse-type tenosynovial giant cell tumours of the soft tissue: a dose-escalation and dose-expansion phase 1 study.
Lancet Oncol, 16 (8): 949-56. [PMID:26179200]
2. Dimoudis N, Fertig G, Fidler A, Pickl M, Ries C, Seeber S, Lanzendoerfer M, Krueger K. (2011)
Antibodies against human csf-1r and uses thereof.
Patent number: US20110165156 A1. Assignee: Dimoudis N, Fertig G, Fidler A, Pickl M, Ries C, Seeber S, Lanzendoerfer M, Krueger K.. Priority date: 10/12/2009. Publication date: 07/07/2011.
3. Gomez-Roca CA, Italiano A, Le Tourneau C, Cassier PA, Toulmonde M, D'Angelo SP, Campone M, Weber KL, Loirat D, Cannarile MA et al.. (2019)
Phase I study of emactuzumab single agent or in combination with paclitaxel in patients with advanced/metastatic solid tumors reveals depletion of immunosuppressive M2-like macrophages.
Ann Oncol, 30 (8): 1381-1392. [PMID:31114846]
4. Goswami KK, Ghosh T, Ghosh S, Sarkar M, Bose A, Baral R. (2017)
Tumor promoting role of anti-tumor macrophages in tumor microenvironment.
Cell Immunol, 316: 1-10. [PMID:28433198]
5. Pradel LP, Ooi CH, Romagnoli S, Cannarile MA, Sade H, Rüttinger D, Ries CH. (2016)
Macrophage Susceptibility to Emactuzumab (RG7155) Treatment.
Mol Cancer Ther, 15 (12): 3077-3086. [PMID:27582524]
6. Ries CH, Cannarile MA, Hoves S, Benz J, Wartha K, Runza V, Rey-Giraud F, Pradel LP, Feuerhake F, Klaman I et al.. (2014)
Targeting tumor-associated macrophages with anti-CSF-1R antibody reveals a strategy for cancer therapy.
Cancer Cell, 25 (6): 846-59. [PMID:24898549]
7. Smart K, Bröske AM, Rüttinger D, Mueller C, Phipps A, Walz AC, Ries C, Baehner M, Cannarile M, Meneses-Lorente G. (2020)
PK/PD Mediated Dose Optimization of Emactuzumab, a CSF1R Inhibitor, in Patients With Advanced Solid Tumors and Diffuse-Type Tenosynovial Giant Cell Tumor.
Clin Pharmacol Ther, 108 (3): 616-624. [PMID:32575160]