Folate Receptor Targeted Therapeutics for Cancer

Case ID:

WSU researchers, in collaboration with Duquesne University, have developed a series of novel folate analogs that show selective toxicity toward tumor cells expressing high levels of the surface protein folate receptor.  This invention has potential in the development of targeted antitumor drugs. 

Background & Unmet Need:

Folate metabolism plays an important role in DNA synthesis and cell proliferation.  This important role makes it a viable target for cancer chemotherapy.  Typically, normal cells express low levels of folate receptors.  Inhibitory folate analogs show essentially negligible affinity and substrate activity toward the ubiquitously expressed reduced folate carrier (RFC), the major transport system in tissues and tumors.  Loss of RFC expression or function may have profound consequences including cancer.


Technology Description:

This invention involves a series of folate analogs that show selective cytotoxicity toward tumor cells (such as ovarian cancer) that express high levels of the surface protein folate receptor (FR), which binds and transports folic acid and related folates into mammalian cells.  Typically normal cells express low levels of FRs.  This selectivity toward FR expressing tumors versus RFC would confer a remarkable therapeutic selectivity.


Commercial Applications:

  • Development of antitumor drugs that selectively target tumors
  • Treatments for ovarian cancer, uterine cancer, breast cancer, and acute myeloid leukemia


Stage of Development:



Competitive Advantages:

  • Analogs are far more potent than other folate receptor analogs
  • Analogs show greater uptake activity in folate receptor expressing cells


Intellectual Property Status:

Patent application filed


Related Publications or Citations of Work:

Gangjee A, Jain HD, McGuire JJ, Kisliuk RL. (2004) Benzoyl ring halogenated classical 2-amino-6-methyl-3,4-dihydro-4-oxo-5-substituted thiobenzoyl-7H-pyrrolo[2,3-d]pyrimidine antifolates as inhibitors of thymidylate synthase and as antitumor agents. J Med Chem. 47(27):6730-9.

Gangjee A, Zeng Y, McGuire JJ, Kisliuk RL. (2005) Synthesis of classical, four-carbon bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates. J Med Chem. 48(16):5329-36.


Patent Information:
For Information, Contact:
Nicole Grynaviski
Commercialization Principal
Wayne State University
Larry Matherly
Aleem Gangjee
Cancer Therapies