muzastotug + pembrolizumab

Muzastotug + pembrolizumab is an investigational combination immunotherapy consisting of muzastotug (ADG126), a masked, tumor-activated, fully human monoclonal antibody targeting cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4), and pembrolizumab, a humanized monoclonal antibody targeting programmed cell death protein 1 (PD-1). Muzastotug utilizes Adagene's proprietary SAFEbody technology, featuring cleavable masking peptides that are preferentially cleaved by proteases in the tumor microenvironment. This selective activation restricts CTLA-4 blockade and regulatory T-cell (Treg) depletion to the tumor site, significantly widening the therapeutic index compared to legacy CTLA-4 inhibitors. Pembrolizumab blocks the interaction between PD-1 and its ligands (PD-L1 and PD-L2), restoring T-cell-mediated anti-tumor immune responses. By combining localized CTLA-4 inhibition and Treg depletion with systemic PD-1 blockade, the regimen aims to overcome immune resistance in 'cold' tumors. The combination is primarily being developed for the treatment of advanced or metastatic solid tumors, with a particular focus on microsatellite stable metastatic colorectal cancer (MSS mCRC) without liver metastases, for which it has received FDA Fast Track designation.

Other names

ADG126 + KeytrudaADG126 + pembrolizumabmuzastotug + Keytruda