Rakovina Therapeutics Inc (TSX-V:RKV) revealed new data indicating that its kt-3000 lead candidate could be effective in treating certain tumors resistant to existent therapies.
The data was presented at the American Association of Cancer Research (AACR) annual meeting in Orlando, Florida, in a poster entitled “A novel bi-functional agent targeting PARP and HDAC in Ewing sarcoma."
A class of DNA-damage response inhibitors with dual PARP HDAC inhibitor functionality, Rakovina’s kt-3000 series was developed based on the hypothesis that combining both HDAC and PARP inhibition into a single molecule could give patients both efficacy and limited side effects, according to the company.
Rakovina presented data demonstrating that its kt-3000 prototype lead candidate showed higher PARP-1 versus PARP-2 selectivity when compared to an existing FDA-approved PARP inhibitor.
Data also showed that the dual functional kt-3000 prototype lead candidate is more effective against Ewing sarcoma tumor cells than either a PARP inhibitor or HDAC inhibitor alone, the company told shareholders.
Studies in mice showed that the lead compound effectively reduced lung metastases in mice inoculated with Ewing sarcoma tumor cells.
"The kt-3000 series compounds were designed with an aim of achieving synergistic PARP+HDAC activity against treatment of resistant tumors while improving safety and tolerability of treatment," Rakovina president and chief scientific officer Mads Daugaard said in a statement.
“We believe that this profile offers potential as a new treatment for tumors traditionally resistant to therapy, particularly in the recurrent disease setting for Ewing sarcoma and major cancers such as breast and ovarian cancer that has become resistant to treatment with FDA-approved PARP inhibitors.”
The news is very encouraging for patients – mostly children and young adults – who suffer from the highly aggressive form of cancer known as Ewing sarcoma, which affects the bones and soft tissue.
Previous studies have demonstrated that Ewing sarcoma cells are sensitive to FDA-approved PARP inhibitors, Rakovina noted, but have not been as successful in clinical trials.
Vancouver-based Rakovina develops new cancer treatments based on novel DNA-damage response (DDR) technologies.
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