Drug intelligence / Profile preview

robatumumab + gemcitabine + erlotinib

Development stage
Unknown
Lead developer
Merck
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

Robatumumab + gemcitabine + erlotinib is an investigational combination regimen of three agents: - **Robatumumab** is a fully human IgG1 monoclonal antibody that selectively targets and inhibits insulin-like growth factor 1 receptor (IGF-1R), impeding IGF signaling and inducing receptor downregulation and tumor cell killing, including by antibody-dependent cellular cytotoxicity[1][3][9]. - **Gemcitabine** is a nucleoside analog (antimetabolite) that inhibits DNA synthesis, resulting in apoptosis in rapidly dividing cells such as tumors[2][4][8]. - **Erlotinib** is an oral small molecule inhibitor of epidermal growth factor receptor (EGFR), blocking EGFR tyrosine kinase activity and downstream oncogenic signaling[4][10]. The combination is studied in oncology, primarily advanced pancreatic cancer. Erlotinib + gemcitabine is an approved regimen for first-line therapy in pancreatic cancer, while addition of robatumumab has been studied in early-phase protocols, but not approved for this indication[7]. The combination aims to block both growth factor-receptor signaling (EGFR and IGF-1R) and DNA synthesis, potentially overcoming resistance mechanisms.

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)IGF-1R (Insulin-like growth factor 1 receptor)

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