VIP236

VIP236 is a first-in-class small molecule-drug conjugate (SMDC) designed for targeted cancer therapy. It consists of an αvβ3 integrin small molecule binder, a peptide linker cleavable by neutrophil elastase in the tumor microenvironment, and a camptothecin-derived topoisomerase I inhibitor payload (VIP126). The drug is engineered to selectively deliver its cytotoxic payload to tumors expressing αvβ3 integrins, with extracellular release triggered by neutrophil elastase activity in the tumor microenvironment. This targeted approach aims to maximize antitumor efficacy while minimizing systemic toxicity. Preclinical studies have demonstrated significant antitumor activity and reduction of metastases in various solid tumor models, including non-small cell lung cancer, colon cancer, renal cell carcinoma, triple-negative breast cancer, and gastric cancer[2][4][5][7]. VIP236 is currently being evaluated in Phase 1 clinical trials for advanced or metastatic solid tumors[5][7].

Other names

αvβ3 integrin antagonist-camptothecin SMDcintegrin-targeted SMDC