Aprutumab ixadotin (BAY 1187982) is the first antibody-drug conjugate (ADC) targeting FGFR2, and is also the inaugural ADC to employ an auristatin-based active payload.

Aprutumab ixadotin exhibits an antigen-binding affinity of 0.29 nM for FGFR2 and demonstrates inhibitory activity across several cancer cell lines with an IC50 ranging from 0.097 to 0.83 nM over 72 hours. Additionally, Aprutumab ixadotin induces apoptosis in FGFR2-positive cells (SUN-52PE, SUN-16).

Aprutumab ixadotin administered intravenously at doses of 5 mg/kg or 7.5 mg/kg weekly for 30 days was well tolerated and led to partial regression of tumors in mouse xenograft models of SNU-16, MFM-223, or NCI-H716.

Human

Monoclonal