On January 27, 2016 Kancera reported the approval of their patent covering small molecule inhibitors of PFKFB3 in the United States (Press release, Kancera, JAN 27, 2016, View Source;releaseID=1097861 [SID:1234508869]). Further, a patent application covering new chemical series in the HDAC6 project has been filed according to plan. In the ROR project, the company intends in the near future to further strengthen the patent portfolio with new highly potent ROR inhibitors.

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The PFKFB3 project: To complement the patent approved in the United States (patent number US9233946), Kancera intends during the spring to file a divisional application for the use of anti-cancer PFKFB3 inhibitors by counteracting the ability of cancer cells to repair their DNA.

The HDAC6 project: As previously reported, Kancera filed a patent application in 2014 covering new inhibitors which in laboratory studies kill both cancer cells and helper cells in tumors. In December 2014, Kancera reported that the HDAC6 inhibitors also act by an additional unique mechanism ("Target 2"), which may contribute to decrease the survival of cancer cells. Kancera has now filed a patent application (EP15201841.2) covering new potent series of compounds that only inhibit HDAC6. In order to facilitate the filing of the new patent application Kancera has, as previously announced, decided to use the opportunity to postpone the publication of the first patent application for one year.

The ROR project: In February 2015, Kancera reported that a patent application (EP15153394.0) was filed which included ca 100 examples of small-molecule ROR inhibitors, including the drug candidate KAN0439834. This patent application is now entering the international phase and Kancera will now strengthen the application by adding examples of ca 300 substances. The application will then cover substances showing more than 20 times higher potency than KAN0439834 against cancer cells from CLL patients.

About the PFKFB3 project
By blocking mechanisms which enable the cancer cells to adapt to periods of oxygen deprivation, possibilities open for new treatment strategies. Kancera’s project is based on a specific inhibition of the enzyme PFKFB3 resulting in a decreased metabolism in cancer cells, and decreased cell growth. In addition, research shows that PFKFB3 is involved in the regulation of both angiogenesis and division of cells, two critical processes that contribute to tumor growth. PFKFB3 is more common in oxygen-deficient tumor tissue compared to healthy tissue, which makes a targeted effect therapy with fewer side effects than traditional chemotherapy possible. Inhibition of PFKFB3 is expected to starve and weaken the tumor cells by reducing their glycolysis and cell division. This is a way to overcome the current problems of tumor resistance to radiation and chemotherapy. Kancera’s PFKFB3 inhibitors have also been shown to prevent DNA repair in cancer cells following e.g. radiation treatment.

About the HDAC6 project
Histone deacetylases (HDACs) are primarily involved in removing acetyl groups from the so-called histones and thereby affect how our genes are stored and activated in the cell nucleus. Some HDACs also affect the cell function outside the cell nucleus. HDAC6 belongs to this group of HDACs with a major biological role in the regulation of the cancer cell´s ability to migrate and to form metastases. The use of HDAC inhibitors in the treatment of cancer patients has so far yielded promising results, but has been limited due to severe side effects. For this reason, the pharmaceutical industry is now looking for more selective inhibitors of individual HDAC enzymes. Kancera´s discovery of selective HDAC6 inhibitors may provide a solution on how health care could take advantage of the anti-cancer effects of HDAC inhibitors without causing the patient severe side effects.

About the ROR project
ROR is a family of receptors, ROR1 and ROR2. The ROR receptors mediate signals for growth and survival. Originally ROR was linked to fetal development, but it is now known that they also contribute to cancer cell development and proliferation. Professor Håkan Mellstedt, Kancera´s co-founder and professor at the Karolinska Institute, and his colleagues have shown that Kancera´s ROR inhibitors have the ability to kill cells from tumors in pancreas and leukemia cells. Professor Mellstedt and his colleagues as well as independent researchers have shown that ROR is also active as a target in prostate, breast, skin and lung cancer.

Because ROR primarily generates a survival and growth signal to tumor cells but is inactive in healthy cells in adults, there are good prospects that a drug directed against ROR hit the tumor much harder than the surrounding healthy cells. Kancera and Professor Mellstedt have shown that inhibition of ROR leads to that cancer