On April 18, 2018 Rgenix, Inc., a clinical stage biopharmaceutical company developing first-in-class small molecule and antibody cancer therapeutics, reported that it is presenting pre-clinical data from ongoing research of RGX-202, a small molecule compound in development designed to inhibit SLC6a8, a creatine transporter, integral to cancer cell energy metabolism (Press release, Rgenix, APR 18, 2018, View Source [SID1234525519]). In a poster presentation today at the 2018 American Association of Cancer Research Annual Meeting, "RGX-202, a first-in-class small-molecule inhibitor of the creatine transporter SLC6a8, is a robust suppressor of cancer growth and metastatic progression", the data showed RGX-202 to be a robust inhibitor of creatine uptake in cancer cells and to be active in several pre-clinical gastrointestinal cancer models both as a single agent and in combination with chemotherapy.

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RGX-202 is a small molecule that inhibits a novel cancer metabolism target, SLC6a8, which is involved in supplying energy to cancer cells. SLC6a8 is over-expressed in several prevalent cancer types, including gastrointestinal malignancies such as colorectal cancer.

More than 140,000 patients are diagnosed with colorectal cancer annually in the U.S. With approximately 50,000 deaths in the U.S. attributed to the condition annually, it is a leading cause of cancer deaths. Creatine metabolism has been shown to spur the growth of colon cancer. This pathway is activated by colon cancer cells to allow uptake of phosphorylated creatine that can be converted to ATP to fuel survival of cancer cells as they proliferate and spread. RGX-202 inhibits this pathway by blocking the ability of SLC6a8 to import phosphocreatine into cancer cells.

In the pre-clinical research presented today, the impact of RGX-202 was studied alone, and in combination with standard of care chemotherapy agents such as 5-FU.

On its own, RGX-202 induced cancer cell death in vivo and demonstrated anti-tumor activity in both KRAS mutant and KRAS wild-type models of gastrointestinal cancer. RGX-202 also suppressed colon cancer and pancreatic cancer liver metastatic colonization, a model of metastatic cancer progression. Importantly, RGX-202 significantly extended survival of tumor-bearing mice as a single agent.

Studies combining RGX-202 with 5-FU resulted in additive anti-tumor activity, with complete tumor regressions among 50% of treated mice and significantly prolonged survival versus 5-FU treatment alone.

Masoud Tavazoie, MD, PhD, and Chief Executive Officer of Rgenix, said, "The data presented today is just a snapshot of our pre-clinical progress on our research of RGX-202. These data show the strong potential for RGX-202 and support further research of the compound. With these data, we are building a strong foundation for future clinical development of RGX-202, which, with regulatory approval, would diversify our clinical pipeline."