On April 18, 2018 Verseon, a technology-based pharmaceutical company employing a computer-driven platform to develop a diverse drug pipeline, reported new preclinical data on its anticancer drug candidates at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) annual meeting yesterday (Press release, Verseon, APR 18, 2018, View Source [SID1234525513]). Dr. Mohan Sivaraja, Associate Director of Discovery Biology, presented studies showing that Verseon’s drug candidates are potent against a range of cancer cell lines, including those that exhibit multidrug resistance.
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While chemotherapy remains the first line of treatment against most cancers, many tumors 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 transport proteins (efflux pumps) that expel many chemicals, including chemotherapeutics. In addition, cells can become resistant to tubulin-targeting chemotherapy drugs by overexpression of β-III tubulin.
The preclinical studies presented at the AACR (Free AACR Whitepaper) conference demonstrate that 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 the major MDR1, MRP1, and BCRP efflux pumps, Verseon’s drug candidates are only weakly affected by these transporters (typically less than 2-fold). The Company’s drug candidates also appear unaffected by the overexpression of β-III tubulin. Dr. Sivaraja also presented pharmacokinetic data for one of Verseon’s tubulin inhibitors, which shows good exposure suitable for infusion. The candidate was also well tolerated in a preclinical repeat-dosing study.
"We are very encouraged by these preclinical results," said Dr. Sivaraja. "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."
About Verseon’s oncology program
Verseon plans to use its promising class of tubulin inhibitors to target multidrug resistant cancers. Several drug candidates show potency in functional and cellular assays. Furthermore, Verseon’s inhibitors maintain their efficacy across multiple chemotherapy-resistant cancer cell lines and are either unaffected or only weakly affected by the overexpression of common transporters, a primary source of multidrug resistance.