Definition

An orally available, small molecule inhibitor of the creatine transporter, solute carrier family 6, member 8 (SLC6a8), with potential antineoplastic activity. Upon oral administration, RGX-202 inhibits phosphocreatine uptake by SLC6a8, thereby reducing intracellular levels of phosphocreatine available for ATP synthesis in tumor cells. SLC6a8 is overexpressed in some cancer types and inhibition of its activity may potentially limit tumor cell growth and metastasis.