OSI Pharmaceuticals, Inc., a biotechnology company, announced that it has initiated a Phase II dose-escalation study of Tarceva (erlotinib HCl) in patients with advanced non-small cell lung cancer (NSCLC) who have failed prior chemotherapy. Tarceva, OSI's leading drug candidate, is designed to block tumor cell growth by inhibiting the tyrosine kinase activity of the HER1/EGFR receptor thereby blocking the HER1/EGFR signaling pathway inside the cell. Tarceva is being developed in a global alliance between OSI, Genentech and Roche.

This open-label study is designed to evaluate the feasibility of dose escalation of Tarceva to induce tolerable rash with no other undue toxicities and to assess whether there is evidence of enhanced activity in patients who have developed rash. The study is designed to explore the previously reported observation that survival of patients who developed rash in the completed Phase II studies of Tarceva was longer than in those without rash, generating the hypothesis that rash might be a surrogate for patient's benefit.

"The observed correlation between rash and survival previously reported with Tarceva and some other agents targeting the HER1/EGFR pathway is intriguing and of particular interest to the oncology community," stated Dr. Eric Rowinsky, principal investigator and director of Clinical Research, Institute for Drug Development. "More importantly, this potential opportunity to maximize the clinical benefit of Tarceva to cancer patients warrants further exploration."

Tarceva is a small molecule designed to target the human epidermal growth factor receptor 1 (HER1) pathway, which is critical to cell growth in many cancers. HER1, also known as EGFR, is a key component of the HER signaling pathway, which often is involved in the formation and growth of numerous cancers. Tarceva is designed to inhibit the tyrosine kinase activity of the HER1 signaling pathway inside the cell, which blocks tumor cell growth. Tarceva currently is being studied as an oral dosage tablet.