certepetide

Certepetide is an investigational cyclic peptide drug designed to enhance the delivery and uptake of anti-cancer drugs into solid tumors. It operates via the C-end rule (CendR) pathway, selectively targeting alpha-v integrins that are upregulated on tumor endothelial and tumor cells but not on healthy tissue. Upon binding, certepetide is cleaved by proteases in the tumor microenvironment, generating a fragment that binds to neuropilin-1 (NRP-1), activating a novel uptake pathway for more efficient and selective transport of co-administered or tethered anti-cancer agents into tumors. This mechanism also modifies the tumor microenvironment, making it less immunosuppressive and more susceptible to immunotherapies while inhibiting metastasis. Certepetide has demonstrated favorable safety, tolerability, and clinical activity in combination with standard-of-care chemotherapy for metastatic pancreatic ductal adenocarcinoma (mPDAC) as well as other advanced solid tumors. The drug has received multiple orphan drug designations—including for pancreatic cancer, glioma, osteosarcoma, and cholangiocarcinoma—and fast track designation in the US[1][2][3][4][5][6].

Brand names

certepetide

Other names

Internalised-arginylglycylaspartic Acid Cyclic Peptide