Anticancer drug candidates appear to be potent against numerous cancer cell lines including some that exhibit multidrug resistance.

At the recent American Association for Cancer Research (AACR) annual meeting, Verseon presented results from preclinical studies for several of its anticancer drug candidates. The company is targeting treatments for cancers that develop resistance to chemotherapy agents over time, often by triggering the overproduction of transporter proteins that expel chemicals, including active drug compounds, from their cells. 

The drug candidates under development by Verseon inhibit the protein tubulin within cancer cells, which causes cell cycle arrest. The result: these drugs are only minimally affected by the transporter proteins overexpressed by efflux pumps such as MDR1, MRP1, and BCRP. Compared to current treatments such as doxorubicin, paclitaxel, and vincristine, which can experience up to a 2000-fold decrease in potency, the Verseon candidates typically see less than a 2-fold reduction. Importantly, these candidates are also not inhibited by β-III tubulin, which can lead to resistance for tubulin-targeting chemotherapy drugs. 

“Multidrug resistance is one of the main reasons why chemotherapies fail. The insensitivity of our compounds to the major transporters and to the overexpression of β-III tubulin may help us address the need for a more effective, precise therapy,” said Dr. Sivaraja, who presented the results at the meeting.