Emibetuzumab

Emibetuzumab (LY2875358) is a humanized bivalent MET antibody (IgG4 type). Emibetuzumab shows high neutralization and internalization activities, resulting in inhibition of both HGF-dependent and HGF-independent MET pathway activation and tumor growth. Emibetuzumab can be used in study of cancer[1].

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR

MET[1].

Emibetuzumab (LY2875358) (100 nmol/L; 6 days) inhibits HGF-stimulated proliferation of H596[1]. Cell Proliferation Assay[1] Cell Line: H596 cells (HGF-stimulated) Concentration: 100 nmol/L Incubation Time: 6 days Result: Suppressed cell proliferation.

Emibetuzumab (LY2875358) (10 mg/kg; i.v.; once a week for 5 weeks) inhibits in vivo growth of glioblastoma U87MG xenograft tumors in mice[1]. Emibetuzumab (10 or 20 mg/kg; i.v.; single) downregulates levels of MET and pMET in the tumors of mice[1]. Emibetuzumab (10 mg/kg; i.v.; once a week for 3, 5 or 6 weeks) exhibits antitumor effects on MET-amplified xenograft mouse tumor models[1]. Animal Model: Athymic nude mice (U87MG tumor xenograft model)[1]. Dosage: 10 mg/kg Administration: Intravenous injection, once a week for 5 weeks. Result: Demonstrated a significant inhibition of tumor growth. Animal Model: Athymic nude mice (MKN45 xenograft tumor model)[1]. Dosage: 10 or 20 mg/kg Administration: Intravenous injection, single. Result: Reduced MET and pMET in the tumors by approximately 50% at both the 10 and 20 mg/kg doses by 72 hours post dose, and the reductions persisted to 14 days. Animal Model: Athymic nude mice (MET-amplified xenograft mouse tumor models)[1]. Dosage: 10 mg/kg Administration: Intravenous injection, once a week for 3, 5 or 6 weeks. Result: Resulted in a marked reduction in tumor growth in the MKN45/SNU-5/EBC-1 gastric xenograft tumors.

[1]. Liu L, et al. LY2875358, a neutralizing and internalizing anti-MET bivalent antibody, inhibits HGF-dependent and HGF-independent MET activation and tumor growth. Clin Cancer Res. 2014 Dec 1;20(23):6059-70.