Smac Mimetic/XIAP/IAP Antagonist (S016-1348) as Solid Tumor Therapeutics

• Orally active, monovalent IAP (Inhibitor of Apoptosis Protein) antagonist demonstrating anti-tumor efficacy as a single agent
• Exhibits nanomolar-level target binding and nanomolar in vitro efficacy in colony formation assays
• Oral bioavailability of 55%

• S-016-1348 is a novel SMAC mimetic targeting XIAP and other IAPs
• Induces cancer cell death independently of TNF-α, overcoming limitations of current SMAC mimetics
• Upregulates DR5, enabling effective monotherapy across various tumor types
• Shows strong anti-tumor activity in PDX models of colon, head & neck, and TNBC
• Demonstrates excellent oral bioavailability and favorable pharmacokinetics across species
• Well tolerated in preclinical studies with high safety margins

• Effective against multiple cancer types, including colon cancer, head & neck cancers, and triple-negative breast cancer (TNBC)
• Shows superior preclinical efficacy and bioavailability compared to existing Phase II clinical trial candidates