INA03

INA03 is an antibody-drug conjugate (ADC) composed of a humanized monoclonal IgG4 antibody targeting CD71 (transferrin receptor, TfR1), conjugated to the cytotoxic payload monomethyl auristatin E (MMAE) via a 3-arylpropiolonitrile-valine-citrulline linker. The drug exploits the overexpression of CD71 on malignant cells, particularly in acute leukemias, to deliver MMAE selectively to cancer cells. Upon binding to CD71, INA03 is internalized and trafficked into lysosomes where MMAE is released following cathepsin B cleavage, resulting in cell death. Preclinical studies have shown that INA03 effectively reduces tumor burden and increases survival in leukemia models with minimal toxicity. Early clinical trials indicate tolerability and preliminary antileukemic activity in relapsed or refractory acute leukemia patients[1][2][3][5].