Emactuzumab

Emactuzumab
Monoclonal antibody
Type	Whole antibody
Source	Humanized (from mouse)
Target	CSF1R
Clinical data
Other names	RG7155, RO5509554
Routes of; administration	intravenous infusion
ATC code	none;
Pharmacokinetic data
Elimination half-life	1.5 - 9 days
Identifiers
CAS Number	1448221-67-7;
DrugBank	DB14905;
UNII	6FY6EI1X8R;
KEGG	D11234;
Chemical and physical data
Formula	C6398H9908N1704O2020S44
Molar mass	144430.19 g·mol−1

Emactuzumab[1] (RG-7155) is a humanized monoclonal antibody directed against CSF-1R expressed on macrophages[2][3] and has demonstrated a profound antitumor effect through interference with the CSF-1/CSF-1R axis, along with a manageable safety profile in patients with diffuse-type tenosynovial giant cell tumors (d-TGCT)[4]

History

This drug was originally developed by Roche/Genentech. In August 2020, Celleron Therapeutics signed a deal to acquire an exclusive worldwide license for the asset.[5]

Mechanism of Action

Emactuzumab is a humanized monoclonal antibody directed against the tyrosine kinase receptor colony stimulating factor 1 receptor (CSF1R; CSF-1R; CD115), also known as macrophage colony-stimulating factor receptor (M-CSFR), with potential antineoplastic and immunomodulating activities. Upon administration, emactuzumab binds to CSF1R expressed on macrophages and inhibits the binding of colony-stimulating factor-1 (CSF-1) to CSF1R. This prevents CSF1R activation and CSF1R-mediated signaling in these cells, which blocks the production of inflammatory mediators by macrophages and reduces inflammation. By blocking both the activity of CSF1R-dependent tumor-associated macrophages (TAMs) and the recruitment of TAMs to the tumor microenvironment, emactuzumab enhances T-cell infiltration and antitumor T-cell immune responses, which inhibits the proliferation of tumor cells. TAMs play key roles in immune suppression and promoting inflammation, tumor cell proliferation and survival.[6]

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References

World Health Organization (2014). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 111" (PDF). WHO Drug Information. 28 (2).
Ries CH, Cannarile MA, Hoves S, Benz J, Wartha K, Runza V, et al. (June 2014). "Targeting tumor-associated macrophages with anti-CSF-1R antibody reveals a strategy for cancer therapy". Cancer Cell. 25 (6): 846–59. doi:10.1016/j.ccr.2014.05.016. PMID 24898549.
Ries CH, Hoves S, Cannarile MA, Rüttinger D (August 2015). "CSF-1/CSF-1R targeting agents in clinical development for cancer therapy". Current Opinion in Pharmacology. 23: 45–51. doi:10.1016/j.coph.2015.05.008. PMID 26051995.
Cassier PA, Italiano A, Gomez-Roca CA, Le Tourneau C, Toulmonde M, Cannarile MA, et al. (August 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". The Lancet. Oncology. 16 (8): 949–56. doi:10.1016/S1470-2045(15)00132-1. PMID 26179200.
"Roche offloads clinical-phase cancer drug to Celleron". FierceBiotech.
"NCI Drug Dictionary: Emactuzumab". NCI Drug Dictionary. U.S. Department of Health and Human Services, National Institutes of Health, National Cancer Institute (NCI). 2011-02-02.

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[1] World Health Organization (2014). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 111" (PDF). WHO Drug Information. 28 (2).

[2] Ries CH, Cannarile MA, Hoves S, Benz J, Wartha K, Runza V, et al. (June 2014). "Targeting tumor-associated macrophages with anti-CSF-1R antibody reveals a strategy for cancer therapy". Cancer Cell. 25 (6): 846–59. doi:10.1016/j.ccr.2014.05.016. PMID 24898549.

[3] Ries CH, Hoves S, Cannarile MA, Rüttinger D (August 2015). "CSF-1/CSF-1R targeting agents in clinical development for cancer therapy". Current Opinion in Pharmacology. 23: 45–51. doi:10.1016/j.coph.2015.05.008. PMID 26051995.

[4] Cassier PA, Italiano A, Gomez-Roca CA, Le Tourneau C, Toulmonde M, Cannarile MA, et al. (August 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". The Lancet. Oncology. 16 (8): 949–56. doi:10.1016/S1470-2045(15)00132-1. PMID 26179200.

[5] "Roche offloads clinical-phase cancer drug to Celleron". FierceBiotech.

[6] "NCI Drug Dictionary: Emactuzumab". NCI Drug Dictionary. U.S. Department of Health and Human Services, National Institutes of Health, National Cancer Institute (NCI). 2011-02-02.