EGFR-KSPi-ADC

EGFR-KSPi-ADC is an experimental antibody-drug conjugate (ADC) developed by Bayer AG. It consists of a monoclonal antibody targeting the Epidermal Growth Factor Receptor (EGFR) conjugated to a novel pyrrole-based inhibitor of the kinesin spindle protein (KSP, also known as Eg5 or KIF11). KSP is a microtubule motor protein essential for the formation of a bipolar spindle during mitosis; its inhibition leads to mitotic arrest and subsequent apoptosis. By targeting EGFR, which is frequently overexpressed in various solid tumors, the ADC is designed to deliver the cytotoxic KSP inhibitor specifically to cancer cells, potentially improving the therapeutic index compared to systemic small-molecule KSP inhibitors. Preclinical studies presented at AACR 2017 demonstrated potent anti-tumor efficacy and complete regressions in xenograft models of non-small cell lung cancer (NSCLC), urothelial cell carcinoma, and renal cell carcinoma.