The Current Situation: Erlotinib (Tarceva®) and Gefitinib (Iressa®) in Non-Small Cell Lung Cancer

Comis, Robert L.

doi:10.1634/theoncologist.10-7-467

Cited by 65 publications

(47 citation statements)

References 19 publications

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“…At the end of the study, 15 of the 54 patients were still alive (27.77%). The median follow-up was 8 months (range [3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18][19][20]. The median survival time was 6 months (95% CI 1.7-10.3).…”

Section: Resultsmentioning

confidence: 99%

“…EGFR is associated with cellular processes leading to tumorigenesis (2,3). Data exist concerning erlotinib administration for malignant tumors, mainly pancreatic cancer, in combination with another cytotoxic agent, as well as for non-small cell lung cancer (NSCLC) in a large number of patients as a second-line treatment (4). Erlotinib has provided a survival benefit for advanced NSCLC patients (5,6).…”

Section: Introductionmentioning

confidence: 99%

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Erlotinib treatment in pretreated patients with non-small cell lung cancer: A Phase II study

Stathopoulos

Trafalis²,

Dimitroulis³

et al. 2010

Oncology Letters

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Abstract. Erlotinib is an oral, small-molecule targeting therapy that inhibits epidermal growth factor tyrosine kinase receptors. Erlotinib has been administered for the treatment of advanced pancreatic cancer and non-small cell lung cancer. In the present trial, erlotinib was administered as second-line monotherapy in pretreated patients with advanced non-small cell lung cancer. Our objectives were to determine response, survival and toxicity. Fifty-four patients pretreated with cisplatin or its analogue-based combinations were evaluated. The disease stage of the patients was IIIB and IV. Thirty-eight patients were male, 16 were female, the median age was 65 years, and the WHO performance status was 0-2. Twenty-five cases were adenocarcinomas, 19 squamous cell carcinomas and 10 were undifferentiated. Erlotinib was administered at a dose of 150 mg daily. In case of intolerable adverse reactions, the dose was either reduced to 100 mg daily or treatment was interrupted for a maximum of two weeks. A partial response was observed in 10 (18.52%) and stable disease in 40 (74.07%) patients. The median time to disease progression was 3 months (95% CI 1.7-10.3), and the median survival was 6 months. Concerning toxicity, 53 patients (98.15%) developed a grade 1-2 skin rash, and 1 (1.85%) grade 3. Diarrhea occurred in 9 (16.67%) patients, nausea and vomiting in 4 (7.41%) and gastritis in 2 (3.70%). The majority of patients tolerated the erlotinib treatment. Of note were the 18.52% response rate and 74.07% stable disease.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Erlotinib treatment in pretreated patients with non-small cell lung cancer: A Phase II study

Stathopoulos

Trafalis²,

Dimitroulis³

et al. 2010

Oncology Letters

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“…However, the clinical dose of erlotinib is set at 150 mg, which is the maximum tolerated dose [9]. There is no report in the literature comparing the transfer of gefi tinib and elotinib into the CSF but dose-dependency has been confi rmed for both.…”

Section: Discussionmentioning

confidence: 99%

Erlotinib May be More Effective for Central Nervous Metastasis of Lung Adenocarcinoma Than Gefitinib Because of the Difference in the Clinical Regimes

Imahashi

2011

J Med Cases

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A 54-year-old woman with lung adenocarcinoma which has EGFR point mutation at exon 21 initially improved by administration of gefi tinib. Lung lesions responded to gefi tinib at 250 mg, but central nervous system lesions, such as carcinomatous meningitis and brain metastasis occurred. The therapy was changed from gefi tinib to erlotinib at 150 mg, resulting in remarkable improvement of carcinomatous meningitis and brain metastasis improved dramatically. We hypothesized that the effective concentration of the clinical dose of erlotinib in the CSF is higher than that of gefi tinib.

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“…The FDA approved gefitinib through a new accelerated process at May-15, 2003(Comis 2005) as a mono therapy for the treatment of patients with locally advanced or metastatic NSCLC after failure of both platinum-based and docetaxel chemotherapies (Chang, Chang et al 2013). As a condition of accelerated approval, the FDA required demonstration of a survival benefit in a subsequent clinical trial.…”

Section: Gefitinibmentioning

confidence: 99%

EGFR Signaling and its inhibition by EGFR inhibitors in NSCLC

Patel

2014

Int J Appl Sci Biotechnol

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Lung cancer is the third most cancer among the population. The American society's estimation for lung cancer in the United States for 2014 states that about 2,24,210 people are suffering from the lung cancer and 1,59,260 deaths are occur from lung cancer. Among all the types of lung cancer, NSCLC (Non-Small cell Lung Cancer) represents 85% of the lung cancer. The estimated spread of NSCLC is 2, 26,160 and 1, 60, 340 cases are of death in 2012. One of the risk factor for NSCLC is over expression of epidermal growth factor receptor (EGFR) and its intracellular signaling pathways. EGFR is over expressed in 40 -80 % cases of NSCLC. EGFR belongs to the ErbB family of receptor tyrosine kinases (RTK) having molecular weight 170 to 185 kDa. Epidermal Growth Factor (EGF) binds to the EGFR at its extracellular domain and this binding leads to the homo or hetero dimerization and autophosphorylation of EGFR which initiates the several intracellular pathways. Several mutations in EGFR or in any of the proteins of the pathway leads to the growth and survival of the tumor cells.so in order to inhibit the growth of tumor cell, several EGFR inhibitors and targeted therapies are found to target the particular mutations.

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The Current Situation: Erlotinib (Tarceva®) and Gefitinib (Iressa®) in Non-Small Cell Lung Cancer

Cited by 65 publications

References 19 publications

Erlotinib treatment in pretreated patients with non-small cell lung cancer: A Phase II study

Erlotinib treatment in pretreated patients with non-small cell lung cancer: A Phase II study

Erlotinib May be More Effective for Central Nervous Metastasis of Lung Adenocarcinoma Than Gefitinib Because of the Difference in the Clinical Regimes

EGFR Signaling and its inhibition by EGFR inhibitors in NSCLC

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