SG3299

SG3299 is an integrin αvβ6-targeted peptide-drug conjugate (PDC) developed for the treatment of pancreatic ductal adenocarcinoma (PDAC). It consists of the αvβ6-specific peptide A20FMDV2 conjugated to tesirine, a potent DNA-binding pyrrolobenzodiazepine (PBD) dimer payload. Integrin αvβ6 is highly expressed in over 80% of human PDAC tumors and their metastases but is absent in healthy pancreatic tissue, providing a high degree of tumor selectivity. Upon binding to the αvβ6 receptor, the conjugate is internalized, and the PBD payload is released to induce DNA cross-linking and subsequent apoptosis. Preclinical studies in immunocompetent murine models have demonstrated that SG3299 significantly reduces primary tumor growth and metastatic burden in the liver, peritoneum, and lungs, leading to improved survival compared to non-targeting controls.

Other names

A20FMDV2-tesirineA-20FMDV2-tesirineA 20FMDV2-tesirinealpha-v-beta-6-targeting peptide-drug conjugatealpha-v-beta6-targeting peptide-drug conjugatealpha-v-beta 6-targeting peptide-drug conjugate