Tarceva^® (erlotinib) is a small molecule human epidermal growth factor type 1/epidermal growth factor receptor (HER1/EGFR) inhibitor which is currently marketed for the treatment of non-small cell lung cancer and pancreatic cancer. In November 2004, the U.S. Food and Drug Administration (FDA) approved Tarceva for the treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) after failure of at least one prior chemotherapy regimen. Tarceva demonstrated, in a Phase III clinical trial, an increase in overall survival in advanced NSCLC patients.

In November 2005 the FDA-approved Tarceva in combination with gemcitabine chemotherapy for the treatment of advanced pancreatic cancer in patients who have not received previous chemotherapy. In a Phase III trial, Tarceva showed an improvement in overall survival when added to gemcitabine chemotherapy as initial treatment for pancreatic cancer.

OSI, together with our partners Genentech and Roche, continues to invest in the future development of Tarceva. Our longer-term strategy for Tarceva is to elevate its efficacy and safety in the front-line and adjuvant settings in NSCLC, other cancers, and in combination with other targeted therapies.

For more information on Tarceva clinical trials, please go to www.clinicaltrials.gov*.

Safety Information

Tarceva has a well-established safety profile. The most common side effects in patients with NSCLC receiving Tarceva monotherapy 150 mg were mild-to-moderate rash and diarrhea. Grade 3/4 rash and diarrhea occurred in 9 and 6 percent of Tarceva-treated patients, respectively, with each resulting in 1 percent of patients discontinuing the single-agent Phase III trial.

There have been infrequent reports of serious Interstitial Lung Disease (ILD)-like events, including fatalities, in patients receiving Tarceva for treatment of NSCLC, pancreatic cancer or other advanced solid tumors. In the NSCLC single-agent trial, the incidence of ILD-like events were infrequent (0.8 percent) and were equally distributed between treatment arms. The overall incidence of ILD in Tarceva-treated patients from all studies was approximately 0.7 percent.

There are no adequate and well-controlled studies in pregnant women using Tarceva. Women of childbearing potential should be advised to avoid pregnancy and breastfeeding while on Tarceva. Tarceva is pregnancy category D.

In the Phase III study in pancreatic cancer, the most common adverse events reported were fatigue, rash, nausea, anorexia and diarrhea. Rash was reported in 69 percent of patients who received Tarceva plus gemcitabine and in 30 percent of patients who received gemcitabine plus placebo. Diarrhea was reported in 48 percent of patients who received Tarceva plus gemcitabine and in 36 percent of patients who received gemcitabine plus placebo. Rash and diarrhea each resulted in dose reductions in two percent of patients, and resulted in study discontinuation in up to one percent of patients who received Tarceva plus gemcitabine. In addition, severe and potential fatal adverse events included interstitial lung disease-like complications, myocardial infarction or ischemia, cerebrovascular accident, and microangiopathic hemolytic anemia with thrombocytopenia of patients who received Tarceva plus gemcitabine.

Mechanism of Action

Tarceva is a small molecule designed to target the human epidermal growth factor receptor (HER1) pathway, which is one of the factors critical to cell growth in numerous cancers, including non-small cell lung and pancreatic. HER1, also known as EGFR, is a component of the HER signaling pathway, which plays a role in the formation and growth of non-small cell lung and pancreatic cancers. Tarceva is designed to inhibit the tyrosine kinase activity of the HER1 signaling pathway inside the cell.

The clinical anti-tumor action of erlotinib is not fully characterized.

Non-Small Cell Lung Cancer

It is estimated that more than 185,600 people will be diagnosed with lung cancer in the United States in 2007. According to the American Cancer Society, lung cancer is the single largest cause of cancer deaths in the United States, and is responsible for nearly 28 percent of cancer deaths in this country. NSCLC is the most common form of the disease and accounts for almost 80 percent of all lung cancers.

Pancreatic Cancer

The American Cancer Society predicts that in 2007 about 37,1170 people in the United States will be diagnosed with pancreatic cancer and about 33,370 will die of the disease. Although pancreatic cancer accounts for two percent of new cancer cases in the United States, it is the fourth leading cause of all cancer deaths. Most pancreatic tumors originate in the exocrine duct cells or in the cells that produce digestive enzymes (acinar cells). Called adenocarcinomas, these tumors account for nearly 95 percent of pancreatic cancers.

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