Tdp inhibitors are a new class of anticancer drugs. The project implements a platform solution using various inhibitors of DNA repair enzymes and analysis of genes controlling the activity of DNA replication and repair enzymes. The 1st drug currently in development is a Tdp1 inhibitor that:
– selectively inhibits Tdp1 activity (IC50 – 26 nM) and significantly (by several times) enhances the cytotoxic effect of Top1 inhibitors on tumor cells in vitro;
– significantly enhances the anticancer effect of Top1 inhibitors – inhibits primary tumor growth and suppresses metastasis in vivo (in lung cancer models).
Main advantages:
– allows to overcome tumor resistance and enhance the effectiveness of anticancer therapy;
– reduces the severity of dangerous side effects of cytostatic drugs.
Indications for use: combined chemotherapy (with Top1 and Top2 inhibitors) of lung, colon, ovarian cancer and certain other types of cancer.