INS-19

INS-19 is a first-in-class, orally bioavailable small molecule inhibitor of the mitochondrial citrate carrier (SLC25A1), currently under development by Inspirna for the treatment of advanced solid tumors. SLC25A1 is a critical transporter that moves mitochondrial-derived citrate into the cytoplasm, where it serves as a primary substrate for de novo lipogenesis and a precursor for acetyl-CoA, thereby influencing both cellular metabolism and epigenetic regulation through histone acetylation. By blocking this transport mechanism, INS-19 disrupts the metabolic adaptations of cancer cells, particularly those that are highly dependent on SLC25A1 for survival and proliferation. Preclinical data have demonstrated that inhibition of SLC25A1 leads to metabolic stress, reduced lipid synthesis, and significant tumor growth inhibition. The drug is currently being evaluated in Phase 1 clinical trials to assess its safety, tolerability, and preliminary anti-tumor activity in patients with various solid malignancies.