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.

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.[5]

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 (June 1, 2014). "Targeting tumor-associated macrophages with anti-CSF-1R antibody reveals a strategy for cancer therapy". Cancer Cell. 25 (6): 846–859. doi:10.1016/j.ccr.2014.05.016.
Ries, CH; Hoves, S (4 June 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.
Cassier, PA; Italiano, A (12 July 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): 949–956. doi:10.1016/S1470-2045(15)00132-1.
National Cancer Institute. "NCI Drug Dictionary: Emactuzumab". Cite journal requires |journal= (help)

This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.

[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 (June 1, 2014). "Targeting tumor-associated macrophages with anti-CSF-1R antibody reveals a strategy for cancer therapy". Cancer Cell. 25 (6): 846–859. doi:10.1016/j.ccr.2014.05.016.

[3] Ries, CH; Hoves, S (4 June 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.

[4] Cassier, PA; Italiano, A (12 July 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): 949–956. doi:10.1016/S1470-2045(15)00132-1.

[5] National Cancer Institute. "NCI Drug Dictionary: Emactuzumab". Cite journal requires |journal= (help)