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FAP-exatecan (AVA6103) is an investigational peptide drug conjugate (PDC) developed by Avacta Therapeutics using its proprietary pre|CISION® tumor-activated oncology delivery platform. The drug consists of the potent topoisomerase I inhibitor exatecan linked to a peptide that is specifically cleaved by Fibroblast Activation Protein (FAP), a protease highly expressed in the tumor microenvironment of many solid tumors. This design enables the selective release of the cytotoxic payload within the tumor while sparing normal tissues, potentially improving the therapeutic index compared to conventional exatecan. FAP-exatecan is designed for sustained tumor drug exposure and has demonstrated a bystander effect on FAP-negative cancer cells in preclinical models. It is currently being evaluated in Phase 1 clinical trials for the treatment of various solid tumors, including pancreatic, cervical, gastric, and small cell lung cancers.
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