MSETC

MSETC is a first-in-class, highly selective bicyclic peptide designed to target the nuclear SETDB1 (SET domain bifurcated histone lysine methyltransferase 1) complex. Discovered and optimized using an AI-integrated epigenetic drug discovery engine, MSETC is being developed for oncology applications. SETDB1 is an epigenetic enzyme that plays a crucial role in gene silencing, particularly of transposable elements, and is frequently upregulated in various cancers, contributing to immune evasion and tumor progression. By inhibiting the SETDB1 complex, MSETC aims to trigger an anti-tumor immune response and sensitize tumors to other therapies. Kazia Therapeutics acquired the global rights to the SETDB1 platform, including MSETC, in 2023.