Oncology R&D

Tarceva, while our first breakthrough product, is far from our only oncology compound to hold promise for patients. While the entire oncology drug discovery and development process can take more than a decade and is thus subject to significant risk and attrition, we are confident in the potential of our programs, in particular: OSI-930 and its back-up OSI-817 and our IGF-1R program, where OSI-906 is the lead development candidate.

OSI-930 is a tyrosine kinase inhibitor designed to target both cancer cell proliferation and blood vessel growth (angiogenesis) in selected tumors. OSI-930 is the first de novo development candidate to emerge from our oncology discovery research operation since we concluded our long-term cancer discovery alliance with Pfizer in 2001. In 2005, we initiated Phase I dose-escalation studies in healthy volunteers and we anticipate Phase I dose-escalation studies in cancer patients in the second quarter of 2006.

While OSI-906, for which we anticipate filing an IND (investigational new drug application) in the fourth quarter of 2006, is also designed as a tryosine kinase inhibitor, the receptor target is, in this case, the IGF-1R receptor, which stimulates proliferation, enables oncogenic transformation, and suppresses apoptosis. Inhibitors of IGF-1R are expected to have broad utility in oncology; the over-expression of IGF-1R and/or its ligands, or the down-regulation of ligand binding proteins, occurs in numerous human malignancies, including lung, colon, breast, prostate, brain and skin cancers. OSI-906 could be useful both as a single agent and in the potentiation of other molecular targeted therapies such as Tarceva.