Despite advances in the development of molecularly targeted
therapies, limited improvements in overall survival have been noted among many
cancer patients with solid
tumors, primarily due to development of drug resistance. Accordingly, there is an unmet need for new targeted
therapies and treatment approaches for
cancer, especially for overcoming resistance. Expression of the
folate receptor is upregulated in many
tumor types and thus represents an ideal target for
cancer treatment. Several
folate receptor targeted
therapies are in development, including the small molecule
drug conjugate
vintafolide, the
monoclonal antibody farletuzumab, and the
antibody-drug conjugate IMGN853. The role of the
folate receptor as a target in
cancer progression and resistance as well as emerging preclinical and clinical data from studies on those
folate receptor targeted agents that are in development with a focus on
vintafolide are reviewed. The
folate receptor has several unique properties, such as high expression in several
tumor types, that make it a rational target for
cancer treatment, and allow for selective delivery of
folate receptor targeted agents. Early-stage clinical data in lung and
ovarian cancer suggest that
vintafolide has the potential for combination with other standard approved agents.