EC0225 (Endocyte)

EC0225 is a first-in-class folate-targeted small molecule drug conjugate (SMDC) developed by Endocyte for the treatment of refractory or metastatic solid tumors. The molecule is engineered with a single folic acid targeting moiety attached to a hydrophilic peptide-based spacer, which is further linked to two distinct cytotoxic payloads: a vinca alkaloid (desacetylvinblastine hydrazide) and mitomycin. These payloads are attached via separate disulfide-containing linkers designed to be cleaved in the reducing environment of the cytoplasm. EC0225 specifically targets the folate receptor (FR), which is highly expressed on the surface of many cancer cells. Upon binding to the receptor, the conjugate is internalized through receptor-mediated endocytosis, where the release of the two cytotoxic agents allows for a synergistic anti-tumor effect by simultaneously inhibiting microtubule assembly and cross-linking DNA.

Other names

Folic acid desacetylvinblastine hydrazide conjugate