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hD16F7-MMAE is an antibody-drug conjugate (ADC) consisting of the humanized monoclonal antibody hD16F7, which targets vascular endothelial growth factor receptor-1 (VEGFR-1), conjugated to the cytotoxic payload monomethyl auristatin E (MMAE). VEGFR-1 is a tyrosine kinase receptor involved in pathological angiogenesis, tumor invasiveness, and the recruitment of protumoral M2 macrophages. The hD16F7 antibody component specifically binds to VEGFR-1 on tumor cells and cells within the tumor microenvironment, facilitating the internalization of the ADC and the subsequent release of MMAE. MMAE then inhibits tubulin polymerization, leading to cell cycle arrest and apoptosis. Preclinical studies have demonstrated significant antitumor activity in melanoma and glioblastoma models, including patient-derived xenografts, where it targets both the tumor cells and the tumor microenvironment components like endothelial cells and M2 macrophages.
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