Emactuzumab

Emactuzumab
Emactuzumab light (purple) and heavy (orange) chains complexed with CSF-1R (green)
Monoclonal antibody
TypeWhole antibody
SourceHumanized (from mouse)
TargetCSF1R
Clinical data
Other namesRG7155, RO5509554
Routes of
administration
intravenous infusion
ATC code
  • none
Pharmacokinetic data
Elimination half-life1.5 - 9 days
Identifiers
CAS Number
DrugBank
UNII
KEGG
Chemical and physical data
FormulaC6398H9908N1704O2020S44
Molar mass144430.19 g·mol−1

Emactuzumab[1] (RG-7155) is a humanized monoclonal antibody directed against colony stimulating factor 1 receptor (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]

  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): 846–859. 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): 949–956. doi:10.1016/S1470-2045(15)00132-1. PMID 26179200.