YL242 + pembrolizumab

YL242 + pembrolizumab is an investigational combination therapy comprising a novel antibody-drug conjugate (ADC) and a programmed cell death protein 1 (PD-1) inhibitor. YL242, developed by MediLink Therapeutics, is a non-internalized ADC targeting vascular endothelial growth factor (VEGF). It utilizes the proprietary TMALIN (Tumor Microenvironment Activable Linker-payload) platform, featuring a protease-cleavable tripeptide linker and a DNA topoisomerase I inhibitor payload (C24). Unlike traditional ADCs that require internalization, YL242 releases its payload extracellularly within the tumor microenvironment upon enzymatic cleavage, potentially overcoming limitations related to target expression heterogeneity and exerting a potent bystander effect. Pembrolizumab (Keytruda) is a humanized monoclonal antibody that blocks the interaction between PD-1 and its ligands (PD-L1 and PD-L2), thereby revitalizing the immune system's ability to detect and destroy cancer cells. This combination is currently being evaluated in Phase 1/2 clinical trials for patients with advanced solid tumors, including non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, and gastric cancers, to leverage the anti-angiogenic and cytotoxic properties of YL242 alongside the immunomodulatory effects of pembrolizumab.

Other names

YL242 + Keytruda