Given that folate receptor 1 (FOLR1) is selectively overexpressed in epithelial ovarian cancer cells, initial clinical trials of FOLR1-targeting agents explored the efficacy of farletuzumab (MORAb-003), an anti-FOLR1 antibody, and vintafolide, a conjugate of folic acid (FA) and the vinca alkaloid desacetylvinblastine hydrazide (1–3). Here, FOLR1 is linked to ovarian carcinoma.