Folate receptor α (FRα) is a member of a family of cell-surface glycoproteins that facilitate the transport and accumulation of folate, through endocytosis, into cells. FRα is expressed in the germinal epithelium of the ovary, the epithelium of the fallopian tube, the surface epithelium of the uterus, the surface epithelium of the endocervix and the glandular epithelium of the cervix.1-5


FRα is an attractive target due to its overexpression in multiple epithelial malignancies including ovarian, endometrial, triple negative breast, and non-small cell lung cancer, with limited expression on normal tissues.1-5

  1. Elnakat H, Ratnam M. Distribution, functionality and gene regulation of folate receptor isoforms: Implications in targeted therapy. Adv Drug Deliv Rev. 2004;56:1067-1084.
  2. Salazar MD, Ratnam M. The folate receptor: What does it promise in tissue-targeted therapeutics? Cancer Metastasis Rev. 2007;26:141-152.
  3. Ledermann JA, Canevari S, Thigpen T. Targeting the folate receptor: Diagnostic and therapeutic approaches to personalize cancer treatments. Ann Oncol. 2015;26:2034-2043.
  4. Kalli KR, Oberg AL, Keeney GL, et al. Folate receptor alpha as a tumor target in epithelial ovarian cancer. Gynecol Oncol. 2008;108:619-626.
  5. Toffoli G, Russo A, Gallo A, et al. Expression of folate binding protein as a prognostic factor for response to platinum-containing chemotherapy and survival in human ovarian cancer. Int J Cancer. 1998;79:121-126.