SETDB1 is a chromatin-modifying enzyme linked to cancer drug resistance, immune evasion, and metastatic progression. Our SETDB1 inhibitor lead compound, MSETC, is an optimized bicyclic peptide designed to reverse immune evasion and restore anti-tumor immune response at the chromatin level.
| Study / Indication | Preclinical | Phase 1 | Phase 2 | Phase 3 | Market | Sponsor |
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| Advanced Solid Tumors |
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Kazia Therapeutics |
SETDB1 is a key chromatin regulator implicated in immune evasion, treatment resistance, and tumor progression, making it an attractive target for therapeutic intervention at the epigenetic level. MSETC, our lead candidate, is a highly selective bicyclic peptide discovered and optimized using an AI-enabled epigenetic drug discovery platform. Designed to target a novel disease-associated nuclear SETDB1 complex, MSETC has the potential to restore immune signaling and overcome resistance to immunotherapies, including checkpoint inhibitors.
The field of oncology is advancing beyond first-generation inhibitors toward next-generation precision targets that modulate immune resistance, tumor plasticity, and transcriptional control, with SETDB1 positioned at the forefront. Enhanced understanding of tumor biology now enables precise, mechanism-driven strategies to address specific drivers of adaptation and immune evasion, offering broader applicability, improved outcomes, and strong potential in combination with immunotherapy.