Sunshine Biopharma Inc., a development stage pharmaceutical company focused on the treatment of various forms of cancer, announced earlier today that it has completed a study in which the ability of Adva-27a, its lead compound, to inhibit the activity of Topoisomerase II was directly measured.
Topoisomerase II (Top2) is an enzyme that enables cancers to grow rapidly. In multi-drug resistant breast cancer, the gene that encodes Top2 has been found to be amplified as much as 1,000%, allowing these cancer cells to make tens of thousands of Top2 molecules. By inhibiting Topoisomerase II activity, Adva-27a would arrest the ability of cancer cells to multiply rapidly and spread to other parts of the body.
The ability of Adva-27a to inhibit Topoisomerase II was measured in a concentration dependent fashion using highly purified, human Topoisomerase II alpha and concatenated plasmid DNA as a substrate. According to today’s press release, Adva-27a was shown to be an excellent inhibitor of Top2 in the study. Inhibition of 50% of Top2 activity (IC50) took place at a concentration of only 13.7 micromolar Adva-27a.
Dr. Steve N. Slilaty, Sunshine’s President and CEO, stated, “An IC50 of 13.7 micromolar indicates that Adva-27a is an excellent inhibitor of Topoisomerase II. Compounds displaying IC50′s in the 75 to 100 micromolar range cannot be developed into effective drugs as the amounts which would have to be administered to patients would be too toxic. We are delighted to find that our compound has such low IC50. This is a significant milestone in our continued development of Adva-27a.”
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