Verseon presents anticancer drug candidates targeting multidrug resistant cancers

20180515ep06

Verseon’s drug candidates target cancer cells by inhibiting the protein tubulin, which leads to cell cycle arrest

Verseon presented new preclinical studies on its anticancer drug candidates at the American Association for Cancer Research (AACR) annual meeting. The data show that Verseon’s drug candidates are potent against a range of cancer cell lines, including those that exhibit multidrug resistance. While chemotherapy remains the first line of treatment against most cancers, many tumours develop resistance to chemotherapy agents over time, limiting their efficacy. A common way for cancer cells to render drugs ineffective is by triggering an overproduction of transporter proteins (efflux pumps) that expel many chemicals, including chemotherapeutics. Verseon’s drug candidates target cancer cells by inhibiting the protein tubulin, which leads to cell cycle arrest. While marketed chemotherapies such as doxorubicin, paclitaxel, and vincristine show up to 2,000-fold reduced potency in cell lines overexpressing major efflux pumps (MDR1, MRP1, and BCRP), Verseon’s drug candidates are only weakly affected by these transporters (typically less than 2-fold). In addition, cells can become resistant to tubulin-targeting chemotherapy drugs by overexpression of ß-III tubulin, but again Verseon’s drug candidates are unaffected. Verseon also presented pharmacokinetic data for one of its tubulin inhibitors, which show that the candidate is suitable for infusion, a standard mode of administration for chemotherapeutics. The candidate was also well tolerated in a preclinical repeat-dosing study. “We are very encouraged by these preclinical results,” said Dr Sivaraja, who presented the results at the AACR. “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 ß-III tubulin may help us address the need for a more effective, precise therapy.” Verseon uses a computer-driven drug discovery platform embedded in a comprehensive chemistry and biology workflow to design new drug candidates for a wide range of diseases. In addition to the oncology programme, the company currently has drug programmes in anticoagulation, diabetic macular edema, and hereditary angioedema.