Product Pipeline > Background

One of the most exciting new cancer targets to be discovered in recent years is the proteasome. The proteasome controls the turnover of proteins in all cells, but cancer cells are more susceptible to cell death when the proteasome is inhibited. The proteasome was validated as a clinical target for the treatment of cancer in 2003, when Velcade® (bortezomib), the first proteasome inhibitor to be tested in clinical trials, was approved for the treatment of multiple myeloma, and subsequently, mantle cell lymphoma. The development of resistance to standard therapies, including Velcade®, in multiple myeloma patients underlines the need for new therapies with improved efficacy and reduced toxicity. Although blocking proteasome activity induces cell death in a wide variety of cancer cells, the clinical success of proteasome inhibitors to date has been primarily in multiple myeloma and mantle cell lymphoma. Proteolix is working to develop more efficacious inhibitors that have the potential to expand treatment to other cancers.

Proteasome inhibitors also work to block immune responses. A distinct form of the proteasome, called the immunoproteasome, is the predominant form found in immune cells. Selective inhibitors that modulate the immunoproteasome may be useful for treating immune disorders and have fewer side effects than conventional proteasome inhibitors.

Proteolix is dedicated to developing proteasome inhibitors for multiple therapeutic uses. The company is developing several second generation proteasome inhibitors, including an oral proteasome inhibitor and a selective immunoproteasome inhibitor, to expand the therapeutic potential of this new target class.