Drug intelligence / Profile preview

REGN3124-PBD

Development stage
Preclinical
Lead developer
Regeneron Pharmaceuticals
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

REGN3124-PBD is an antibody-drug conjugate (ADC) developed by Regeneron Pharmaceuticals for the treatment of glioblastoma multiforme (GBM). It consists of REGN3124, a fully human monoclonal antibody that selectively targets the epidermal growth factor receptor variant III (EGFRvIII), a tumor-specific mutation frequently expressed in GBM. The antibody is conjugated to the pyrrolobenzodiazepine (PBD) dimer linker-payload SG-3249. Upon binding to EGFRvIII-expressing cells, the ADC is internalized, and the PBD payload is released to crosslink DNA, leading to potent cytotoxicity. REGN3124-PBD has demonstrated significant anti-tumor activity in preclinical patient-derived xenograft (PDX) models, including those with heterogeneous EGFRvIII expression, due to its ability to induce bystander killing of neighboring tumor cells.

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)EGFRvIII (Epidermal growth factor receptor variant III)

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