GGFG-eribulin

GGFG-eribulin is a linker-payload intermediate developed by Chongqing Sintaho for use in the construction of antibody-drug conjugates (ADCs). It consists of the cytotoxic payload eribulin, a synthetic analogue of halichondrin B that acts as a microtubule inhibitor, conjugated to a tetrapeptide linker (Gly-Gly-Phe-Gly). This specific linker is designed to be cleaved by lysosomal enzymes, such as cathepsin B, within target cancer cells to release the active drug. Eribulin exerts its antineoplastic effect by binding to the plus ends of microtubules, inhibiting their growth phase without affecting the shortening phase. This leads to irreversible mitotic block in the G2/M phase and subsequent apoptosis. GGFG-eribulin is part of a portfolio of toxin-linkers intended for the development of XDC (any-drug conjugate) therapeutics.