Research Pipeline
Microtable Inhibitor for Solid Tumors: Genistein Analogs
Oncolin Therapeutics recently announced that it agreed to terms for an exclusive worldwide right to option patents covering the composition and use of Genistein analogs for cancer treatment. The technology was discovered and patented by the Pharmaceutical Research Institute of Warsaw Poland and involves compounds that appear to be novel antimicrotubule agents.
Given the widespread success of antimicrotubule therapies in curative and palliative cancer treatment, the microtubule is perhaps the single best cancer target identified to date and continues to be recognized as a strategic target against which to direct new development efforts.
The approved drugs from this mechanistic class include the Vinca Alkaloids such as vincristine, the taxanes with paclitaxel and docetaxel and the epothilones with its first drug recently approved by Bristol Myers. Each of these different types of compounds classes appear to interact at different parts of the microtubule and have different spectrums of activity and show effectiveness against resistant disease. This technology provides the opportunity to develop what may be yet another unique antimicrotubule class of compounds. This specific mechanism continues to be of great interest to the cancer research community as it may provide yet another different spectrum of activity in the clinic.
Enzyme Inhibitor of Glycolysis
It has recently been published that a key enzyme in the glycolytic pathway 6 – phosphofrutose -2 – kinase/Fructose 2, 6 bis phosphotase (PFKFB3) is highly upregulated in tumor cells with especially high levels in gliomas (brain tumor).
The three dimensional structural of the active site of this enzyme has been elucidated providing the platform to identify and modify inhibitors with potent selective antitumor activity. Lead compounds with some activity have been identified which will be the basis of future research to design and test novel drug like analogs for clinical testing. Much of this research is funded by an R01 National Institute of Health grant for four years starting March 1, 2008.
Heat Activated Cytotoxic Drugs
A long term goal of Cancer research is to overcome the inherent tumor resistance and toxicity to antineoplastic agents. One strategy to achieve this result is to develop locally targeted therapies that would have the potential for increased specificity and decreased toxicity.
This research program has developed thermally responsive polypeptide � conjugates of chemotherapeutic drugs. These conjugates can be targeted to the tumor site by applying local hyperthermia. Initial in vitro studies have demonstrated that these conjugates work in cell culture.
These continuing research studies will provide the basis for a new technology for targeted delivery of chemotherapeutics. The research is supported by an SBIR grant for $179,980 which also began March 1, 2008.