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SB02024 is a potent, selective, and orally active small molecule inhibitor of vacuolar protein sorting 34 (Vps34), also known as PIK3C3. Developed by Sprint Bioscience, it acts as an ATP-competitive inhibitor that blocks the initiation of autophagy in tumor cells. By inhibiting Vps34, SB02024 reprograms the tumor microenvironment, increasing the infiltration of immune cells through the induction of chemokines like CCL5 and CXCL10 via the STAT1/IRF7 and cGAS-STING pathways. Preclinical studies have demonstrated its efficacy in reducing tumor growth and enhancing the activity of tyrosine kinase inhibitors (such as sunitinib and erlotinib) and immune checkpoint inhibitors in models of breast cancer, melanoma, and colorectal cancer.
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