Description
SGI-110 (guadecitabine) is a second-generation DNA methyltransferase inhibitor designed as a prodrug of decitabine with enhanced stability and prolonged exposure. This hypomethylating agent has been evaluated in metastatic colorectal cancer, particularly in combination with immunotherapy approaches and standard chemotherapy regimens. The compound represents an epigenetic therapy approach that aims to reverse aberrant DNA methylation patterns commonly found in colorectal tumors.
Mechanism of Action
SGI-110 works by inhibiting DNA methyltransferases (DNMT1, DNMT3A, and DNMT3B), enzymes responsible for adding methyl groups to cytosine bases in DNA. By blocking these enzymes, the drug prevents hypermethylation of tumor suppressor gene promoters, potentially restoring normal gene expression and enhancing immune recognition of cancer cells. The prodrug formulation provides more stable delivery compared to decitabine, allowing for sustained demethylating activity.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.