Tarceva (originally coded ZD1839) is a drug used in the treatment of certain types of cancer. Acting in a similar manner to erlotinib (marketed as Tarceva), gefitinib selectively targets the mutant proteins in malignant cells. It is marketed by AstraZeneca under the trade name Iressa. .

Medicinal name:
  • Erlotinib 25 MG Oral Tablet [Tarceva]
  • Erlotinib 100 MG Oral Tablet [Tarceva]
  • Erlotinib 150 MG Oral Tablet [Tarceva]

Tarceva - Pharmacology:

Tarceva inhibits the epidermal growth factor receptor (EGFR) tyrosine kinase by binding to the adenosine triphosphate (ATP)-binding site of the enzyme. Thus the function of the EGFR tyrosine kinase in activating the Ras signal transduction cascade is inhibited; and malignant cells are inhibited. Tarceva is the first selective inhibitor of the EGFR tyrosine kinase which is also referred to as Her1 or ErbB-1. EGFR is overexpressed in the cells of certain types of human carcinomas - for example in lung and breast cancers. Overexpression leads to inappropriate activation of the apoptotic Ras signal transduction cascade, eventually leading to uncontrolled cell proliferation.

Tarceva mini report

Tarceva NDA
NDA - A product marketed under an approved New Drug Application
Tarceva global name
erlotinib hydrochloride
Start - Stop data
Start - Stop data
not occurred

Tarceva for patients

Patients should be advised to seek medical advice promptly if they develop 1) severe or persistent diarrhea, nausea, anorexia, or vomiting, as these have sometimes been associated with dehydration; 2) an onset or worsening of pulmonary symptoms, ie, shortness of breath or cough; 3) an eye irritation; or, 4) any other new symptom.

Women of childbearing potential must be advised to avoid becoming pregnant.

Tarceva Interactions

Substances that are inducers of CYP3A4 activity increase the metabolism of gefitinib and decrease its plasma concentrations. In patients receiving a potent CYP3A4 inducer such as rifampicin or phenytoin, a dose increase to 500 mg daily should be considered in the absence of severe adverse drug reaction, and clinical response and adverse events should be carefully monitored (see CLINICAL PHARMACOLOGY-Pharmacokinetics-Drug-Drug Interactions and DOSAGE AND ADMINISTRATION-Dosage Adjustment sections).

International Normalized Ratio (INR) elevations and/or bleeding events have been reported in some patients taking warfarin while on IRESSA therapy. Patients taking warfarin should be monitored regularly for changes in prothrombin time or INR.

Substances that are potent inhibitors of CYP3A4 activity (eg, ketoconazole and itraconazole) decrease gefitinib metabolism and increase gefitinib plasma concentrations. This increase may be clinically relevant as adverse experiences are related to dose and exposure; therefore, caution should be used when administering CYP3A4 inhibitors with IRESSA.

Drugs that cause significant sustained elevation in gastric pH (histamine H2-receptor antagonists such as ranitidine or cimetidine) may reduce plasma concentrations of IRESSA and therefore potentially may reduce efficacy.

Phase II clinical trial data, where IRESSA and vinorelbine have been used concomitantly, indicate that IRESSA may exacerbate the neutropenic effect of vinorelbine.

Tarceva Contraindications

IRESSA is contraindicated in patients with severe hypersensitivity to gefitinib or to any other component of IRESSA.

Manufacturers name:

  • Physicians Total Care, Inc
  • Genentech, Inc

Tarceva tags categories:

Generic name, Overdose, Half Life Tarceva, Food Interactions, Chemical, etc..

Tarceva see also FDA report

Brand Names containing Gefitinib