The anti-cancer drug candidate NOV202 is a small-molecule microtubule-targeting agent for both intravenous and oral administration. NOV202 was identified from Noviga’s compound library as one of the most potent anti-proliferative compound in a large panel of cancer cell lines, including both solid and hematological malignancies. It is of particular interest to note that NOV202 is as effective in cancer cells overexpressing the P-glycoprotein transporters which confer multidrug resistance, and is therefore an interesting candidate for second line treatment of P-glycoprotein mediated multidrug resistant tumors. Notably, the clinically used chemotherapeutic drugs vincristine and paclitaxel were found to be significantly less potent in the resistant cells as compared to the parental cells.
In-vivo efficacy studies in human ovarian cancer xenograft models show that NOV202 potently suppresses tumor growth, and in-vivo efficacy studies in mice have shown that NOV202 was well tolerated when dosed p.o. over a period of up to 26 days, suggesting little off-target toxicity.
Characterization of NOV202, both in cell free systems and in live cells, showed that NOV202 potently destabilized microtubules. Furthermore, NOV202 has also been shown to be a potent vascular disrupting agent, causing both inhibition of cord formation, as well as disruption of established cord structures, at low nanomolar concentrations.
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