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TS-104 is a first-in-class, multi-specific peptide-drug conjugate (PDC) developed by TwoStep Therapeutics for the treatment of advanced solid tumors. It consists of a polyspecific integrin-binding peptide (PIP), which is an engineered, ultra-stable knottin peptide, conjugated to the cytotoxic microtubule inhibitor monomethyl auristatin E (MMAE). PIP selectively targets five tumor-associated integrins (including αvβ3, αvβ5, αvβ6, αvβ1, and α5β1) that are highly expressed in active conformations on solid tumors. This multi-targeting approach is designed to overcome tumor heterogeneity and resistance associated with single-antigen targeting. Upon binding and rapid internalization, TS-104 delivers MMAE directly into cancer cells, leading to cell cycle arrest and apoptosis.
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