BRP-020063

BRP-020063 is a first-in-class peptide-based radionuclide drug conjugate (RDC) developed by Boomray Pharmaceuticals for the treatment of Nectin-4-positive solid tumors. It consists of a high-affinity peptide binder specific to Nectin-4, conjugated to the therapeutic beta-emitting radionuclide Lutetium-177 ($^{177}$Lu). Nectin-4 is a cell surface adhesion molecule that is aberrantly overexpressed in multiple solid tumors, including bladder, breast, and non-small cell lung cancers, while showing limited expression in normal tissues. Preclinical evaluations have demonstrated that BRP-020063 exhibits picomolar to nanomolar binding affinity to Nectin-4 across several species (human, mouse, rat, and cynomolgus monkey) and high selectivity over other Nectin family members. In xenograft models, the drug shows robust tumor uptake, long-term retention, and significant antitumor efficacy, leading to sustained tumor regression and prolonged survival.

Other names

177Lu-DOTA-AC-SPLutetium (177Lu) DOTA-AC-SP