On April 3, 2019 Rgenix, Inc., a clinical stage biopharmaceutical company developing first-in-class small molecule and antibody cancer therapeutics, reported it is presenting pre-clinical data from ongoing research of RGX-019, a monoclonal antibody that targets MERTK, for the treatment of advanced cancer (Press release, Rgenix, APR 3, 2019, View Source [SID1234534968]). In a presentation of a late-breaking abstract, "Characterization of the anti-cancer and immunologic activity of RGX-019, a novel pre-clinical stage humanized monoclonal antibody targeting the MERTK receptor," which was accepted for the 2019 American Association of Cancer Research Annual Meeting, Isabel Kurth Ph.D., Rgenix VP of Research, discussed data showing RGX-019 to be a potent and selective inhibitor of MERTK signaling, resulting in suppression of cancer growth and activation of the innate immune response.

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RGX-019 is a humanized monoclonal antibody that selectively targets MERTK, a receptor tyrosine kinase of the TYRO3/AXL/MERTK (TAM) family. MERTK is expressed in immune cells such as macrophages, dendritic cells and NK cells, and is also overexpressed in a wide variety of liquid and solid cancers.

Activation of MERTK on cancer cells via ligand binding activates several tumor-promoting signaling pathways, stimulating tumor proliferation, migration and angiogenesis, and decreasing apoptosis and chemosensitivity. When activated on macrophages, MERTK promotes an immune-suppressive M2 phenotype.

RGX-019 binds to human MERTK with high affinity and selectivity, without detectible binding to other related TAM kinases. RGX-019 has a unique mechanism of action that not only leads to blockade of ligand binding, but also to MERTK degradation via receptor internalization.

This novel mechanism of action leads to inhibition of cancer growth in vitro and in vivo as well as activation of M1 (pro-inflammatory) cytokine release from immune-suppressive M2 macrophages.

Masoud Tavazoie, MD, PhD, and Chief Executive Officer of Rgenix, said, "We are excited to have an opportunity to reveal the pre-clinical data that demonstrates the positive progress we are making with the development of RGX-019, our third proprietary program. The ability of RGX-019 to selectivity degrade MERTK in cancers cells and M2 macrophages provides a distinct advantages over current small-molecule approaches to targeting MERTK which are hampered by off-target binding to other related kinases. This data provides a strong foundation for IND enabling studies."

Sohail Tavazoie, MD, PhD, and Chair of Rgenix’s Scientific Advisory Board, said, "RGX-019 shows great potential as a cancer therapeutic and its ability to selectively modulate both cancer growth and innate immune activation is illustrative of that possibility. We look forward to continuing our research on this antibody and its impact on various MERTK expressing cancers."