A101-GP-MMAE

A101-GP-MMAE is a mesothelin-targeted nanobody-drug conjugate (NDC) developed for the treatment of pancreatic ductal adenocarcinoma (PDAC). It is composed of a camelid-derived VHH nanobody (A101) that specifically binds to mesothelin (MSLN), a cell-surface protein highly expressed in pancreatic cancer. The nanobody is conjugated to the cytotoxic payload monomethyl auristatin E (MMAE), a microtubule inhibitor, via a glycine-proline (GP) linker. The NDC format utilizes the small size of the nanobody to enhance penetration through the dense stroma of the pancreatic tumor microenvironment, which often limits the efficacy of traditional monoclonal antibody-based therapies. In preclinical studies, A101-GP-MMAE demonstrated MSLN-specific internalization and potent cytotoxicity against PDAC cell lines, although it was noted to have lower in vivo efficacy compared to variants utilizing novel intracellularly cleavable linkers.

Other names

A101-glycine-proline-MMAEA-101-glycine-proline-MMAEA 101-glycine-proline-MMAEA101-glycine-proline-monomethyl auristatin EA-101-glycine-proline-monomethyl auristatin EA 101-glycine-proline-monomethyl auristatin E