Tarceva.net

The recommended daily dose of Tarceva is 150 mg ^[1]

• For the treatment of NSCLC, Tarceva is available in strengths of 150 mg, 100 mg and 25 mg.*^[1]

*25-mg tablet not available in all countries.

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Multiple tablet strengths allow for dose reduction

• In the pivotal trial, most patients tolerated the 150-mg dose. ^[1,2]
  
• If patients experience intolerable adverse events, such as intolerable skin reactions, intolerable diarrhea that is unresponsive to loperamide or that causes dehydration, or severe liver function test abnormalities, consider dose reduction or interruption of Tarceva. ^[1]
  
• The pivotal Phase III protocol specified the following dose modification guidelines for Grade ≥ 3 rash or diarrhea that could not be medically managed: ^[1,2]
  
• withhold therapy until symptom severity is returned to Grade ≤ 1 ^[2]
  
• then resume therapy at a 50-mg step lower than original dose ^[1]
  
• Six percent and 1% of patients needed dose reduction for rash and diarrhea, respectively. ^[1]
  
• Treatment should continue unless a patient experiences unacceptable toxicity, disease progression or Interstitial Lung Disease (ILD). ^[1]
  
• There is no evidence that treatment beyond disease progression is beneficial. ^[4]
  
• Tarceva therapy should be suspended if ILD is suspected and discontinued if confirmed. ^[1]

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Precautions with Tarceva

• Women of childbearing potential must be advised to avoid pregnancy while on Tarceva. ^[1]
  
• Current smokers should be advised to stop smoking, as plasma concentrations in smokers are reduced compared to nonsmokers. ^[1]
  

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Established safety profile for NSCLC

• In the pivotal Phase III clinical trial, Tarceva was not shown to be associated with myelosuppression, neutropenia or neuropathy. ^[1,2]
  
• The most common adverse drug reactions in patients receiving Tarceva were rash and diarrhea. In the pivotal trial, Grade 3/4 rash and diarrhea occurred in 9% and 6%, respectively, of Tarceva-treated patients. ^[1]
  
• The most common side effects, rash and diarrhea, were mild to moderate; each resulted in treatment discontinuation in 1% of Tarceva-treated patients. ^[1,2]

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Concomitant use with CYP3A4 inhibitors and inducers

• Co-treatment with the CYP3A4 inducer rifampicin decreased erlotinib AUC by 69%. Alternate treatments lacking CYP3A4 inducing activity should be considered. ^[1]
  
• Co-treatment with the potent CYP3A4 inhibitor ketoconazole increases erlotinib AUC by 86%. Caution should be used when administering or taking Tarceva with ketoconazole or other strong CYP3A4 inhibitors. ^[1]
  
• Concomitant use of CYP3A4 substrates and modulators may require dose adjustment. ^[1]

Download a copy of the summary of product characteristics.

References:

1. Tarceva® (erlotinib) summary of product characteristics, F. Hoffmann-La Roche Ltd., 2007.
2. Data on file, OSI Pharmaceuticals, Inc.
3. Hidalgo M, Sui LL, Nemunaitis J, et al. Phase I and pharmacologic study of OSI-774, an epidermal growth factor receptor tyrosine kinase inhibitor, in patients with advanced solid malignancies. J Clin Oncol. 2001;19:3267-3279.
4. Tarceva® (erlotinib) full prescribing information, OSI Pharmaceuticals, Inc., 2005.