gefitinib, Iressa (Discontinued in the US)
Omudhome Ogbru, PharmD
Omudhome Ogbru, PharmD
Dr. Ogbru received his Doctorate in Pharmacy from the University of the Pacific School of Pharmacy in 1995. He completed a Pharmacy Practice Residency at the University of Arizona/University Medical Center in 1996. He was a Professor of Pharmacy Practice and a Regional Clerkship Coordinator for the University of the Pacific School of Pharmacy from 1996-99.
Medical and Pharmacy Editor:
GENERIC NAME: gefitinib
BRAND NAME: Iressa (Discontinued in USA)
On September 9, 2011 Astrazeneca announced that Iressa will no longer be available in the United States. It had received an expedited approval by the U.S. Food and Drug Administration; however, subsequent clinical trials did not confirm Iressa's clinical benefits. Patients may still obtain Iressa via clinical trials. For more information contact Astrazeneca's information center at 1-800-601-8933.
DRUG CLASS AND MECHANISM: Gefitinib is a drug that is used to treat several types of lung cancer. It works by preventing lung cancer cells from growing and multiplying. Many cells, including cancer cells, have receptors on their surfaces for epidermal growth factor (EGF), a protein that is normally produced by the body and that promotes the growth and multiplication of cells. When EGF attaches to epidermal growth factor receptors (EGFRs), it causes an enzyme called tyrosine kinase to become active within the cells. Tyrosine kinase triggers chemical processes that cause the cells, including cancer cells, to grow, multiply, and spread. Gefitinib attaches to EGFRs and thereby blocks the attachment of EGF and the activation of tyrosine kinase. This mechanism for stopping cancer cells from growing and multiplying is very different from the mechanisms of chemotherapy and hormonal therapy. Gefitinib was approved by the FDA in May 2003.
GENERIC AVAILABLE: No.
PREPARATIONS: Clear capsules of 50 mg.
STORAGE: Capsules should be stored at room temperature, 15-30 C (59-86 F).
PRESCRIBED FOR: Gefitinib is used alone (monotherapy) for the treatment of patients with a certain type of lung cancer (non-small cell lung cancer or NSCLC) that has not responded to chemotherapy. Lung cancer is the second most common cancer in both men and women and is the leading cause of deaths from cancer in the US. Lung cancer is divided into two major types: small cell lung cancer and nonsmall cell lung cancer (NSCLC). NSCLC is the most common type, accounting for almost 80% of lung cancers. There are five subtypes of NSCLC, each of which is made up of different kinds of cancer cells. The cancer cells of each type differ in size, shape, and chemical make-up, and grow and spread in different ways. The three most common types of NSCLC are squamous cell carcinoma, adenocarcinoma, and large cell carcinoma. About one in ten people with NSCLC who receive gefitinib will have a substantial reduction in the size of their cancers, even after other drugs have failed; however, the cancer is not cured.
DOSING: Gefitinib is taken by mouth. The dose is 250 mg once daily. The dose is the same for men or women of any age or weight, and gefitinib can be taken with or without food.
DRUG INTERACTIONS: Gefitinib may increase the blood-thinning effects of warfarin (Coumadin) and increase the risk of bleeding. Therefore, patients receiving gefitinib and warfarin at the same time should have more frequent testing of the "thinness" of their blood.
Patients who receive drugs that increase an enzyme in the liver called CYP 3A4 that destroys gefitinib (for example, rifampin or phenytoin (Dilantin) may need a higher dose of gefitinib to maintain the effectiveness of gefitinib.
Similarly, patients who receive drugs that reduce CYP 3A4, for example, ketoconazole (Nizoral), itraconazole (Sporanox), fluconazole (Diflucan), erythromycin, clarithromycin (Biaxin), ritonavir (Norvir), nelfinavir (Viracept), indinavir (Crixivan), nefazodone (Serzone), as well as grapefruit juice, may need a lower dose of gefitinib to prevent side effects from increased levels of gefitinib.
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