Rgenix is a privately-held clinical-stage biopharmaceutical company developing first-in-class drugs that target key pathways in cancer progression.

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RGX-202 is an oral small molecule inhibitor of SLC6A8 that induces apoptosis (cell death) of colorectal cancer cells.

Mechanism of Action

Creatine Kinase-B (CKB) was revealed as an RNA dysregulated cancer driver in KRAS mutant colorectal cancer (CRC) by the RNA-DRIVEr™ platform.​ CKB is activated in response to tumor hypoxia (low oxygen) to enable cancer cells to generate ATP and other nucleotides via phospho-creatine. ​



Phospho-creatine is imported into CKB expressing (CKB+) cancer cells via the creatine transporter SLC6A8.​ RGX-202 is an oral first-in-class creatine mimetic NCE that acts as a competitive inhibitor of the creatine transporter SLC6A8. ​​

In the setting of tumor hypoxia (which is a common feature of CRC) RGX-202-mediated depletion of phospho-creatine (P-Cr) impairs synthesis of ATP and other nucleotides that are required for colorectal cancer cell survival, resulting in potent induction of apoptosis (cancer cell death).​

Since healthy (non-tumor) tissue is not hypoxic under normal conditions, inhibition of SLC6A8 by RGX-202 largely leaves healthy tissue unaffected, providing a wide therapeutic window.​​

RGX-202 is currently being tested in combination with the standard-of-care regimen FOLFIRI and bevacizumab in a Phase 1b clinical trial for the 2nd line treatment of patients with advanced colorectal cancer whose tumors express CKB (~65% of colorectal cancers).


Abequolixron (RGX-104)

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.



RGX-019 is a monoclonal antibody-drug conjugate (ADC) that targets MERTK to selectivity kill cancer cells and activate tumor myeloid cells.