Cudarolimab (IBI-101) is a fully human anti-OX40 antibody with potential immune checkpoint inhibitory and anti-tumor activity for the study of cancer.

OX40-dependent NF-κB reporter:4.432 nM (EC50)

Cudarolimab bound to CHO-S cells overexpressing OX40 at concentrations of 0.01, 1, 100, or 10,000 nM, partially blocking the binding of OX40 to its ligand OX40L. In Jurkat-OX40 reporter cells co-cultured with Raji cells, Cudarolimab activated the OX40-dependent NF-κB reporter with an EC50 of 4.432 nM.Cudarolimab binds in a dose-dependent manner at concentrations of 0.01, 0.1, 1, 10, 100 or 1000 nM to activated human CD4+ T cells and activated crab-eating monkey CD4+ T cells. Also, Cudarolimab increases IL-2 secretion from human CD4+ T cells at concentrations of 0.4, 4.0 and 40.4 nM. [1]

Cudarolimab at a dose of 10 mg/kg via intraperitoneal injection significantly reduced tumor volume in human-derived NOG mice bearing LoVo tumors. Cudarolimab at doses of 0.1, 1, and 10 mg/kg via intraperitoneal injection significantly reduced tumor volume and enhanced CD8+ T cell expression of IFN-γ and IFN-α in tumors and spleen in OX40 knock-in mice harboring MC38 tumors after a single dose on days 6, 9, 12, and 16. In addition, at doses of 0.1, 1, and 10 mg/kg by intraperitoneal injection, Cudarolimab significantly reduced the expression of CD3+CD8+, CD3+CD4+, and CD4+CD25highFoxP3+ cells in the tumors and spleens of OX40 knock-in mice harboring MC38 tumors after a single administration on days 10 and 14. [1]