Carotuximab (DE-122) is a novel endocholine antibody with strong antiangiogenic and anti-inflammatory activity. Carotuximab blocks endothelial glycoprotein (CD105) and its downstream Smad signaling pathway. Carotuximab has immunomodulatory and antitumor effects to prevent human endothelial dysfunction induced by hypercholesterolemia and hyperglycemia.

In human aortic endothelial cells, pretreatment with Carotuximab (TRC105) at a concentration of 300 μg/mL for 1 hour, followed by co-culture for 12 hours, resulted in the reduction of 7-ketocholesterol-induced endothelial glycoprotein (Eng) protein levels. Additionally, Carotuximab inhibited the pSmad1/5 and pSmad2/3 signaling pathways. The blockade of Eng by Carotuximab prevented 7-ketocholesterol-induced monocyte adhesion and migration through endothelial monolayer cells [1].

In acute myeloid leukemia (AML) xenografts, the combination of Carotuximab (TRC105) and Decitabine, administered intravenously at a dose of 2 mg/kg once every 3 days for 8 weeks, produces a more durable anti-leukemia effect. Additionally, this combination enhances reactive oxygen species (ROS) activity [2].