Belapectin (GR-MD-02) is a Galectin-3 (Gal-3) inhibitor. Belapectin drives tumor-induced immunosuppression by inducing T cell Apoptosis. Belapectin promotes tumor regression and improves survival of tumor-bearing mice through a CD8+ T cell-dependent mechanism. Belapectin binds to Gal-3 with affinity Ki of 2.8 μM.
Belapectin (0.2 mg/mL, 2 mg/mL; 48 h) inhibits the proliferation of 4T1 and MCA-205 cells and induced apoptosis[1].
Belapectin (2.4 mg/mouse; i.p.; 3 times per week for 3 weeks) only exerts function under the combination with anti-OX40 mAb, does cause a significant reduction in tumor growth and a corresponding increase in survival. The combined treatment also produces lasting long-term memory, and 100 percent of the tumor-free mice were protected from subsequent tumor reattacks[1].
References:
[1]. Sturgill ER, et al. Galectin-3 inhibition with belapectin combined with anti-OX40 therapy reprograms the tumor microenvironment to favor anti-tumor immunity. Oncoimmunology. 2021 Mar 1;10(1):1892265.
[2]. Capasso D, et al. Galectins detection for the diagnosis of chronic diseases: An emerging biosensor approach[J]. TrAC Trends in Analytical Chemistry, 2023: 116952.