VRC-2

VRC-2 (Velcade Re-sensitizing Compound 2) is a novel small molecule identified through high-throughput screening for its ability to overcome resistance to the proteasome inhibitor bortezomib (Velcade) in multiple myeloma. Developed by researchers at the Penn State Hershey Cancer Institute and the University of Minnesota, VRC-2 was discovered using isogenic pairs of bortezomib-sensitive and -resistant myeloma cells. The compound demonstrates modest single-agent activity against resistant cells but exhibits potent synergistic activity when combined with bortezomib, effectively re-sensitizing refractory cells to treatment. Preclinical studies have indicated a favorable safety profile, with a 100-fold higher IC50 in normal fibroblasts compared to malignant myeloma cells, suggesting a wide therapeutic window.

Other names

Velcade Re-sensitizing Compound 2