Drug intelligence / Profile preview

GSK2849330

Development stage
Phase 1
Lead developer
GSK
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

GSK2849330 is a novel humanized IgG1/IgG3 monoclonal antibody developed to target the human epidermal growth factor receptor 3 (HER3; also known as ERBB3). It binds with high affinity and specificity to the extracellular domain III of HER3, preventing neuregulin 1 (NRG1) ligand binding and thereby inhibiting receptor dimerization and downstream signaling. The antibody is glycoengineered for enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) via high-affinity binding to FcγRIIIA and further modified for increased complement-dependent cytotoxicity (CDC) through high-affinity binding to complement protein C1q. These modifications maximize its potential antitumor activity. In clinical studies, GSK2849330 demonstrated a favorable safety profile but limited antitumor activity in unselected HER3-expressing cancers; however, an exceptional response was observed in a patient with CD74-NRG1-rearranged non-small cell lung cancer. The drug was developed by GSK primarily for advanced solid tumors expressing HER3[2][5][6].

Other names
anti-HER3 monoclonal antibodyanti-HER-3 monoclonal antibodyanti-HER 3 monoclonal antibodyAnti-HER3-monoclonal-antibodyAnti-HER-3-monoclonal-antibodyAnti-HER 3-monoclonal-antibody
02

Targets

ERBB3 (Erb-b2 receptor tyrosine kinase 3)

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