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AVA6207 is a first-in-class dual-payload peptide drug conjugate (PDC) developed by Avacta Therapeutics using its proprietary pre|CISION® platform. It is designed to target the tumor microenvironment by leveraging the enzymatic activity of fibroblast activation protein (FAP), which is highly expressed in the stroma of many solid tumors. The molecule remains inert in systemic circulation and selectively releases two distinct cytotoxic payloads—exatecan (a topoisomerase I inhibitor) and monomethyl auristatin E (MMAE, a microtubule inhibitor)—upon cleavage by FAP at the tumor site. This dual-mechanism approach is intended to overcome drug resistance and enhance anti-tumor efficacy while minimizing off-target toxicities. AVA6207 is currently in preclinical development for the treatment of resistant solid tumors, with clinical trials anticipated to commence in 2026.
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