Sgi-110 (Not yet branded)

Other Medications

US Experimental EU Experimental ES med_spain_not_available IV 2 Clinical Trials
DNMT1 DNMT3A DNMT3B

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

Neutropenia Thrombocytopenia Anemia Fatigue Nausea Febrile neutropenia Injection site reactions Diarrhea

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT01966289 med_phase_prefix1
Archived
SGI-110 in Combination With an Allogeneic Colon Cancer Cell Vaccine (GVAX) and Cyclophosphamide (CY) in Metastatic Colorectal Cancer (mCRC)
United States
NCT01896856 med_phase_prefix1
Archived
Phase I/II Study of SGI-110 With Irinotecan Versus Regorafenib or TAS-102 in Metastatic Colorectal Cancer
United States, Netherlands