nuzefatide pevedotin

Nuzefatide pevedotin (BT5528) is a first-in-class Bicycle Drug Conjugate (BDC) targeting the Ephrin type A receptor 2 (EphA2), a receptor tyrosine kinase frequently overexpressed in various solid tumors and associated with poor prognosis. Developed by Bicycle Therapeutics, the molecule consists of a bicyclic peptide ligand (nuzefatide) conjugated to the cytotoxic payload monomethyl auristatin E (MMAE) via a cleavable linker (the linker-payload complex is known as pevedotin). Unlike traditional antibody-drug conjugates (ADCs), BDCs utilize a fully synthetic, constrained peptide scaffold to achieve high affinity and selectivity for the target while facilitating rapid tumor penetration and fast systemic clearance. Nuzefatide pevedotin is currently being evaluated in Phase I/II clinical trials for the treatment of advanced solid tumors, including non-small cell lung cancer, ovarian cancer, and urothelial carcinoma, as well as in Phase II trials for recurrent metastatic pancreatic ductal adenocarcinoma.

Other names

nuzefatide + pevedotin