A second agent from this program, OSI-817, is currently being evaluated in preclinical toxicology experiments prior to entry into the clinic. Both these drug candidates are potent tyrosine kinase inhibitors that block cellular signaling through the receptor tyrosine kinases, c-kit and vascular epidermal growth factor receptor (VEGFR, also known as KDR).
The agents are designed to target both cancer cell proliferation and blood vessel growth, or angiogenesis. OSI anticipates moving both candidates through early stages of development before selecting one of the two candidates for full clinical development in cancer patients.
This single-center, open-label, vehicle-controlled phase I study is scheduled to enroll up to 35 healthy volunteers in the US, and is designed to determine the safety and tolerability of single oral doses of OSI-930. The study will include extensive pharmacokinetic sampling and pharmacodynamic evaluation and will assist in the design of an optimal clinical program in cancer patients.
“Our research efforts are focused on the development of next-generation targeted therapies designed to supplement and complement a portfolio built around Tarceva, our flagship product,” stated Dr Neil Gibson, vice president of research at OSI. “We believe the kinase inhibitory profile of OSI-930 and OSI-817 offers a unique blend of likely efficacy and side effects that will allow for competitive positioning of this program.”