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Prof. Suzie Chen and her colleagues at Rutgers University have recently discovered that the metabotropic glutamate receptor 1 (GRM1, mGluR1) plays a significant role in the development and growth of melanoma tumors.  They found that riluzole, the only drug approved by the U.S. FDA for the treatment of amyotrophic lateral sclerosis (ALS), which also blocks glutamate release from GRM1 cells, inhibits melanoma growth and proliferation both in vitro, in mouse xenograft models, and in limited human clinical trials in melanoma patients.  However, the clinical use of riluzole for ALS, and potentially for melanoma, is severely limited by variable CYP1A2-mediated first pass metabolism.  Fox Chase Chemical Diversity Center, Inc. has developed novel and innovative prodrug derivatives of riluzole which avoid CYP1A2 in vitro metabolism and are expected to provide more regular pharmacokinetics and exposure in patients, with a longer half-life, allowing for once daily oral dosing versus the current twice daily dosing that is required, and potentially greater patient compliance.  

The company has filed several PCT provisional U.S. patent applications on riluzole prodrugs, with additional composition of matter patent filings anticipated. Other than riluzole, there are no compounds that target the glutamate pathway for treatment of metastatic melanoma.  The company has raised more than $2.2 million specifically for this program since 2010, and is looking to raise an additional $3 million by the third quarter of 2015, in order to perform the required IND-enabling studies for an IND application and enter Phase I clinical trials at the Cancer Center of New Jersey