W5

Novel chalcone derivative for cancer treatment

Dr Katrina Vanura, Medical University Vienna;  Prof. Ulrich Jäger, Medical University Vienna;  Prof. Thomas Erker, University Vienna;  Dr Gerda Brunhofer-Bolzer, University Vienna

Austria Wirtschaftsservice


Challenge

Globally, 0.0188% of men and 0.01% of all women suffer from leukemia. The number of new cases of chronic lymphocytic leukemia (CLL) are 0,006% (men) and 0,003% (women) per year. The number of deaths was 1.3 per 100,000 men and women per year. These rates are age-adjusted and based on 2009-2013 cases and deaths.

Market growth by 2020 is expected to be 18.5%. For example Celera / Janssen reported sales of $ 700 million for Ibrutinib in 2014 and projected to reach US $ 6127 million by 2020 and for Obinutuzumab sales of $ 54 million and projected sales of $ 2011 million by 2020.

The low rates of healing in lymphomas, severe side effects, and frequent recurrences in specific patient groups are indications that the search for new potential drugs for monotherapy and combination therapy is still ongoing.


Technology

Researchers of the Medical University of Vienna and the University of Vienna have identified highly active synthetic chalcones derived from the chalcone scaffold. These cytotoxic compounds were found and developed by modifying the chalcone lead structure concurrent with in vitro tests to evaluate their cytotoxic potential in different cancer cell lines. Compounds were thoroughly tested regarding their efficacy in inhibiting proliferation and viability in cancer cell lines of the hematopoietic system.


Commercial Opportunity

Partnership - all-size biotech and pharmaceutical partners with a complementary expertise in oncology drug development, in order to support the preclinical development of the anti-cancer small molecule via a co-development agreement and/or license agreement, or purchase


Development Status

The combination of the new chalcone compound with the targeting agents, Idelalisib and Ibrutinib, which are novel compounds in the treatment of hematological malignancies, displayed higher cytotoxicity on CLL cells than Idelalisib and Ibrutinib alone.
Ongoing:

  • Determination of cytotoxity in a pre-clinical experimental system
  • In depth analysis regarding the mode of action (microarrays)

Patent Situation

Priority application 8/2014


Further Reading

WO 2016/030510
Lin et al. 2010 J Clin Oncol, Blum et al. 2011 Leukemia, Stephens et al. 2012 Haematologica, Woyach et al. 2012 Leukemia, Karp et al. 2012 Haematologica


 

Novel chalcone derivative for cancer treatment
Novel chalcone derivative for cancer treatment

Impact of APG38 on the viability of primary cells from CLL patients (N=10) and healthy donors (N=2), and the mouse fibroblast cell line M210B4. Cells were incubated in triplicates for 48h before viability was determined. Mean values and standard deviations are shown. Since the x-axis has a logarithmic scale, the vehicle only incubation (= origin - „0“) with the 100% viability reference point is not depicted.