RGX-019 is a preclinical monoclonal antibody-drug conjugate (ADC) program that targets MERTK to selectivity kill cancer cells and activate tumor myeloid cells. The RNA-DRIVEr™ platform revealed that RNA dysregulation results in activation (increased expression) of MERTK in breast cancer (TNBC).
In addition to TNBC, MERTK is highly expressed in several other solid and liquid cancers, including NSCLC, melanoma, AML, and MM. MERTK activation causes direct effects on cancer cells (proliferation, migration) as well as immune suppressive effects through its action on tumor associated macrophages (TAMs).
MERTK is also required for maintenance of the retinal pigment epithelium (RPE) of the eye, hampering development of MERTK inhibitors which can result in retinal toxicity.
RGX-019 is a novel MERTK targeting monoclonal antibody that drives internalization of the MERTK receptor with partial-agonist activity. RGX-019’s unique mechanism-of-action provides a wide therapeutic window that avoids retinal toxicity and enables an antibody-drug conjugate approach for effective targeting of MERTK expressing tumors.
RGX-104 is an oral small molecule activator of LXR/APOE that inhibits the growth of tumor blood vessels (angiogenesis) and activates tumor myeloid cells to enhance the immune response against tumors.
Ompenaclid (RGX-202) is an oral small molecule inhibitor of SLC6A8 that induces apoptosis (cell death) of colorectal cancer cells.