Chiron initiates Ph I trial of cancer drug CHIR-265

US biotechnology major Chiron Corp has inititated a Phase I clinical trial of its selective Raf kinase inhibitor, CHIR-265, in patients with malignant melanoma. Stephen Dilly, the firm's chief medical officer, noted that this is a promising indication for the agent, given "the high percentage of Raf mutations associated with the disease and the need for effective new treatments."

The single-agent, open-label Phase I evaluation is designed to assess its safety, dose-tolerability and pharmacokinetic profile. A translational medicine approach will be used to monitor biomarkers in order to evaluate the biological activity and define the optimal dose. The study is expected to enroll up to 60 patients at three cancer centers in the USA.

According to Chiron, preclinical data sugests that the novel, orally-bioavailable small-molecule inhibitor of the Raf kinases, including mutant B-Raf (V600E), also inhibits VEGFR-2. It adds that it has both direct anti-proliferative and pro-apoptotic activity on tumor cells, as well as anti-angiogenic activity that targets the tumor blood supply.