aprutumab ixadotin

Aprutumab ixadotin (BAY1187982) is an antibody-drug conjugate (ADC) developed by Bayer for the treatment of cancer. It consists of a fully human monoclonal antibody targeting fibroblast growth factor receptor 2 (FGFR2), conjugated via a noncleavable linker to a novel auristatin-based cytotoxic payload. The drug specifically binds to FGFR2 isoforms IIIb and IIIc, which are overexpressed in various solid tumors such as breast, gastric, and ovarian cancers. Upon binding to FGFR2-expressing tumor cells, the ADC is internalized and releases its cytotoxic payload intracellularly, leading to microtubule disruption and cell death. Preclinical studies demonstrated high selectivity and potent antitumor activity in FGFR2-positive models. Aprutumab ixadotin entered phase I clinical trials for advanced solid tumors expressing FGFR2 but development was discontinued due to unexpected toxicities at subtherapeutic doses[1][2][5][7].

Other names

FGFR2-ADCFGFR-2-ADCFGFR 2-ADCAbrutumab ixadotine