Iprotics

Multiple Myeloma (MM) is a devastating blood cancer for which no satisfactory solution exists. The current first-in-line therapeutics are proteasome inhibitors, that however feature dose-limiting toxicity that make MM patients experience such severe side effects, that many abandon treatment. The Overkleeft group at Leiden University, who previously developed lead compounds currently in clinical development for inherited metabolic disorders (www.azafaros.com), now discovered superior proteasome inhibitors, and it is the aim of iProtics to develop these leads to become the first-in-line treatment for MM patients. The unique compounds, for which IP protection is sought for and to which iProtics will obtain an exclusive license, inhibit with exquisite selectivity immunoproteasomes while leaving constitutive proteasomes intact. MM cells uniquely rely on immunoproteasomes for protein turnover and survival, whereas healthy tissue express constitutive proteasomes mostly. We have proof of concept in cell lines and primary patient tumour cells showing that our compounds efficiently and at low concentrations kill MM cells, but not healthy cells. Our leads are expected to give less side effects and a considerably enlarged therapeutic window, and potentially increase patient lifespan and quality of life. Current clinical proteasome inhibitors having blockbuster status; and immunoproteasome activities being hallmarks of other (blood) cancers as well as various autoimmune diseases, successful implementation of the iProtics therapeutics will have great societal impact and generate substantial revenues. We have defined steps up to and including phase IIA clinical trials and look for financial support of up to four million Euros to tackle the first stage: preclinical studies.