Exelixis Initiates PI anticancer trial
Exelixis, from south San Francisco, CA, has initiated a Phase I clinical trial to evaluate the safety, tolerability and pharmacokinetic profile of XL647, a novel, orally available, proprietary anticancer com-pound that targets multiple receptor tyrosine kinases (RTKs).
Exelixis, from south San Francisco, CA, has initiated a Phase I clinical trial to evaluate the safety, tolerability and pharmacokinetic profile of XL647, a novel, orally available, proprietary anticancer com-pound that targets multiple receptor tyrosine kinases (RTKs).
RTKs are implicated in tumour proliferation and vascularisation (angiogenesis). The Phase I clinical trial is designed as an open-label, single and repeat dose-escalation study and will be conducted in patients with solid tumours for whom there is no alternative therapy. Dr Branimir Sikic, professor of medicine, division of oncology and director, General Clinical Research Center at Stanford University Medical Center said: 'We are intrigued by the selected spectrum of gene targets inhibited by XL647. This novel approach could represent a promising avenue for intervening in influential genetic pathways implicated in cancer and deserves to be studied in a clinical setting.'
XL647 is the first of several Spectrum Selective Kinase Inhibitors (SSKI) that Exelixis intends to advance into clinical testing. Each SSKI has a different RTK inhibition spectrum, and each has the potential to achieve efficacy through simultaneous inhibition of multiple RTKs. XL647 simultaneously inhibits the EGFR, HER2, VEGFR and EphB4 RTKs with high potency and demonstrates excellent activity in target-specific cellular functional assays. In preclinical models of major tumor types, including human breast, lung, colon and prostate cancer, XL647 demonstrates potent inhibition of tumour growth and has been shown to cause tumour regression.
'The initiation of the Phase I clinical trial of XL647 is an important milestone for Exelixis, as it is the first of what we believe is an exciting portfolio of novel and highly potent Spectrum Selective Kinase Inhibitors to advance into clinical development,' said Dr George Scangos, president and chief executive officer. 'We have made rapid progress in the last year in expanding our development pipeline with novel, differentiated compounds that we believe have the potential to represent new approaches to treating cancer and other proliferative diseases. We believe that the strategy of generating a multiplicity of high quality product oppor-tunities will be key to our success in building a sustainable pharmaceutical business.'