PLX038

PLX038 is a long-acting, PEGylated prodrug of SN-38, the active metabolite of irinotecan and sacituzumab govitecan. It is designed to slowly release SN-38 in the body, providing sustained inhibition of DNA topoisomerase I (TOP1), an enzyme crucial for DNA repair in cancer cells. By inhibiting TOP1, PLX038 prevents cancer cells from repairing damaged DNA, leading to cell death. The drug’s unique formulation allows for prolonged exposure at lower peak concentrations compared to conventional irinotecan therapy, potentially improving efficacy and reducing toxicity. Preclinical studies have shown that PLX038 can penetrate the blood-brain barrier and accumulate in tumors with high retention time[2][4][7]. It is being developed primarily for solid tumors including glioblastoma and other primary CNS tumors (especially those with MYC or MYCN amplification), triple-negative breast cancer (TNBC), platinum-resistant ovarian cancer, small cell lung cancer (SCLC), and other refractory solid tumors[2][4][6][7][8].

Other names

PEGylated SN-38PEG40kDa~SN-38