Gefitinib in Non Small Cell Lung Cancer
Gefitinib is an oral, reversible, tyrosine kinase inhibitor of epidermal growth factor receptor (EGFR) that plays a key role in the biology of non small cell lung cancer (NSCLC). Phase I studies indicated that the recommended dose of gefitinib was 250 mg/day. Rash, diarrhea, and nausea were the most...
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| Veröffentlicht in: | BioMed research international 2011-01, Vol.2011 (2011), p.1-14 |
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| creator | Sandomenico, Claudia Piccirillo, Maria Carmela Costanzo, Raffaele Carillio, Guido Montanino, Agnese Daniele, Gennaro Giordano, Pasqualina Bryce, Jane De Feo, Gianfranco Di Maio, Massimo Rocco, Gaetano Normanno, Nicola Perrone, Francesco Morabito, Alessandro |
| description | Gefitinib is an oral, reversible, tyrosine kinase inhibitor of epidermal growth factor receptor (EGFR) that plays a key role in the biology of non small cell lung cancer (NSCLC). Phase I studies indicated that the recommended dose of gefitinib was 250 mg/day. Rash, diarrhea, and nausea were the most common adverse events. The positive results obtained in early phase 2 clinical trials with gefitinib were not confirmed in large phase 3 trials in unselected patients with advanced NSCLC. The subsequent discovery that the presence of somatic mutations in the kinase domain of EGFR strongly correlates with increased responsiveness to EGFR tyrosine kinase inhibitors prompted phase 2 and 3 trials with gefitinib in the first line-treatment of EGFR-mutated NSCLC. The results of these trials have demonstrated the efficacy of gefitinib that can be now considered as the standard first-line treatment of patients with advanced NSCLC harbouring activating EGFR mutations. |
| doi_str_mv | 10.1155/2011/815269 |
| format | Article |
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Phase I studies indicated that the recommended dose of gefitinib was 250 mg/day. Rash, diarrhea, and nausea were the most common adverse events. The positive results obtained in early phase 2 clinical trials with gefitinib were not confirmed in large phase 3 trials in unselected patients with advanced NSCLC. The subsequent discovery that the presence of somatic mutations in the kinase domain of EGFR strongly correlates with increased responsiveness to EGFR tyrosine kinase inhibitors prompted phase 2 and 3 trials with gefitinib in the first line-treatment of EGFR-mutated NSCLC. The results of these trials have demonstrated the efficacy of gefitinib that can be now considered as the standard first-line treatment of patients with advanced NSCLC harbouring activating EGFR mutations.</description><identifier>ISSN: 1110-7243</identifier><identifier>ISSN: 2314-6133</identifier><identifier>EISSN: 1110-7251</identifier><identifier>EISSN: 2314-6141</identifier><identifier>DOI: 10.1155/2011/815269</identifier><identifier>PMID: 21660144</identifier><language>eng</language><publisher>Cairo, Egypt: Hindawi Puplishing Corporation</publisher><subject>Acne ; Antineoplastic Agents - adverse effects ; Antineoplastic Agents - therapeutic use ; Cancer ; Cancer therapies ; Carcinoma, Non-Small-Cell Lung - drug therapy ; Care and treatment ; Chemotherapy ; Clinical medicine ; Clinical trials ; Development and progression ; Diarrhea ; Drug therapy ; ErbB Receptors - antagonists & inhibitors ; ErbB Receptors - genetics ; ErbB Receptors - therapeutic use ; Feasibility studies ; Gefitinib ; Health aspects ; Humans ; Lung cancer ; Lung cancer, Non-small cell ; Lung Neoplasms - drug therapy ; Mutation ; Physiological aspects ; Protein Kinase Inhibitors - adverse effects ; Protein Kinase Inhibitors - therapeutic use ; Proteins ; Quinazolines - adverse effects ; Quinazolines - therapeutic use ; Radiation therapy ; Review ; Thoracic surgery ; Tumors</subject><ispartof>BioMed research international, 2011-01, Vol.2011 (2011), p.1-14</ispartof><rights>Copyright © 2011 Raffaele Costanzo et al.</rights><rights>COPYRIGHT 2011 John Wiley & Sons, Inc.</rights><rights>Copyright © 2011 Raffaele Costanzo et al. Raffaele Costanzo et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.</rights><rights>Copyright © 2011 Raffaele Costanzo et al. 2011</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c601t-d6146d7fc50b48f1fefd098e488e35acf086558f3d6ec693487e0ca35f1191a73</citedby><cites>FETCH-LOGICAL-c601t-d6146d7fc50b48f1fefd098e488e35acf086558f3d6ec693487e0ca35f1191a73</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC3110340/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC3110340/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,314,727,780,784,885,27924,27925,53791,53793</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/21660144$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><contributor>Gridelli, Cesare</contributor><creatorcontrib>Sandomenico, Claudia</creatorcontrib><creatorcontrib>Piccirillo, Maria Carmela</creatorcontrib><creatorcontrib>Costanzo, Raffaele</creatorcontrib><creatorcontrib>Carillio, Guido</creatorcontrib><creatorcontrib>Montanino, Agnese</creatorcontrib><creatorcontrib>Daniele, Gennaro</creatorcontrib><creatorcontrib>Giordano, Pasqualina</creatorcontrib><creatorcontrib>Bryce, Jane</creatorcontrib><creatorcontrib>De Feo, Gianfranco</creatorcontrib><creatorcontrib>Di Maio, Massimo</creatorcontrib><creatorcontrib>Rocco, Gaetano</creatorcontrib><creatorcontrib>Normanno, Nicola</creatorcontrib><creatorcontrib>Perrone, Francesco</creatorcontrib><creatorcontrib>Morabito, Alessandro</creatorcontrib><title>Gefitinib in Non Small Cell Lung Cancer</title><title>BioMed research international</title><addtitle>J Biomed Biotechnol</addtitle><description>Gefitinib is an oral, reversible, tyrosine kinase inhibitor of epidermal growth factor receptor (EGFR) that plays a key role in the biology of non small cell lung cancer (NSCLC). Phase I studies indicated that the recommended dose of gefitinib was 250 mg/day. Rash, diarrhea, and nausea were the most common adverse events. The positive results obtained in early phase 2 clinical trials with gefitinib were not confirmed in large phase 3 trials in unselected patients with advanced NSCLC. The subsequent discovery that the presence of somatic mutations in the kinase domain of EGFR strongly correlates with increased responsiveness to EGFR tyrosine kinase inhibitors prompted phase 2 and 3 trials with gefitinib in the first line-treatment of EGFR-mutated NSCLC. The results of these trials have demonstrated the efficacy of gefitinib that can be now considered as the standard first-line treatment of patients with advanced NSCLC harbouring activating EGFR mutations.</description><subject>Acne</subject><subject>Antineoplastic Agents - adverse effects</subject><subject>Antineoplastic Agents - therapeutic use</subject><subject>Cancer</subject><subject>Cancer therapies</subject><subject>Carcinoma, Non-Small-Cell Lung - drug therapy</subject><subject>Care and treatment</subject><subject>Chemotherapy</subject><subject>Clinical medicine</subject><subject>Clinical trials</subject><subject>Development and progression</subject><subject>Diarrhea</subject><subject>Drug therapy</subject><subject>ErbB Receptors - antagonists & inhibitors</subject><subject>ErbB Receptors - genetics</subject><subject>ErbB Receptors - therapeutic use</subject><subject>Feasibility studies</subject><subject>Gefitinib</subject><subject>Health aspects</subject><subject>Humans</subject><subject>Lung cancer</subject><subject>Lung cancer, Non-small cell</subject><subject>Lung Neoplasms - drug therapy</subject><subject>Mutation</subject><subject>Physiological aspects</subject><subject>Protein Kinase Inhibitors - adverse effects</subject><subject>Protein Kinase Inhibitors - therapeutic use</subject><subject>Proteins</subject><subject>Quinazolines - adverse effects</subject><subject>Quinazolines - therapeutic use</subject><subject>Radiation therapy</subject><subject>Review</subject><subject>Thoracic surgery</subject><subject>Tumors</subject><issn>1110-7243</issn><issn>2314-6133</issn><issn>1110-7251</issn><issn>2314-6141</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>RHX</sourceid><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><recordid>eNqFks9rFDEUgINYbK2ePCuDHgqVafMmvy9CWbQVFj2o55DNvGxTZpI6s6P435t12sXKggSSkHz5kvfyCHkB9AxAiPOGApxrEI00j8gRANBaNQIe7-acHZKn43hDKSgtzRNy2ICUFDg_IieXGOImpriqYqo-5VR96V3XVQss3XJK62rhksfhGTkIrhvx-d14TL59eP91cVUvP19-XFwsa1-Em7qVwGWrghd0xXWAgKGlRiPXGplwPlAthdCBtRK9NIxrhdQ7JgKAAafYMXk3e2-nVY-tx7QZXGdvh9i74ZfNLtqHOyle23X-YVmJlXFaBCd3giF_n3Dc2D6OvkTjEuZptIYqkEYrXsjX_5A3eRpSic5qJRsl6R_dmxlauw5tTCGXW_1WaS8aKWVjNIdC1XuoNSYsT8yppLgsP-DP9vCltdhHv_fA2_mAH_I4Dhh2GQFqt1Vgt1Vg5yoo9Ku_k7hj77-9AKczcB1T637G_9hezjAWBIPbwYLSxkj2Gyo_vpM</recordid><startdate>20110101</startdate><enddate>20110101</enddate><creator>Sandomenico, Claudia</creator><creator>Piccirillo, Maria Carmela</creator><creator>Costanzo, Raffaele</creator><creator>Carillio, Guido</creator><creator>Montanino, Agnese</creator><creator>Daniele, Gennaro</creator><creator>Giordano, Pasqualina</creator><creator>Bryce, Jane</creator><creator>De Feo, Gianfranco</creator><creator>Di Maio, Massimo</creator><creator>Rocco, Gaetano</creator><creator>Normanno, Nicola</creator><creator>Perrone, Francesco</creator><creator>Morabito, Alessandro</creator><general>Hindawi Puplishing Corporation</general><general>Hindawi Publishing Corporation</general><general>John Wiley & Sons, Inc</general><general>Hindawi Limited</general><scope>ADJCN</scope><scope>AHFXO</scope><scope>RHU</scope><scope>RHW</scope><scope>RHX</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>7QL</scope><scope>7QO</scope><scope>7T7</scope><scope>7TK</scope><scope>7U7</scope><scope>7U9</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8FD</scope><scope>8FE</scope><scope>8FG</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>ARAPS</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BGLVJ</scope><scope>BHPHI</scope><scope>C1K</scope><scope>CCPQU</scope><scope>CWDGH</scope><scope>DWQXO</scope><scope>FR3</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>H94</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>LK8</scope><scope>M0S</scope><scope>M1P</scope><scope>M7N</scope><scope>M7P</scope><scope>P5Z</scope><scope>P62</scope><scope>P64</scope><scope>PIMPY</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>5PM</scope></search><sort><creationdate>20110101</creationdate><title>Gefitinib in Non Small Cell Lung Cancer</title><author>Sandomenico, Claudia ; Piccirillo, Maria Carmela ; Costanzo, Raffaele ; Carillio, Guido ; Montanino, Agnese ; Daniele, Gennaro ; Giordano, Pasqualina ; Bryce, Jane ; De Feo, Gianfranco ; Di Maio, Massimo ; Rocco, Gaetano ; Normanno, Nicola ; Perrone, Francesco ; Morabito, Alessandro</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c601t-d6146d7fc50b48f1fefd098e488e35acf086558f3d6ec693487e0ca35f1191a73</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2011</creationdate><topic>Acne</topic><topic>Antineoplastic Agents - 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| subjects | Acne Antineoplastic Agents - adverse effects Antineoplastic Agents - therapeutic use Cancer Cancer therapies Carcinoma, Non-Small-Cell Lung - drug therapy Care and treatment Chemotherapy Clinical medicine Clinical trials Development and progression Diarrhea Drug therapy ErbB Receptors - antagonists & inhibitors ErbB Receptors - genetics ErbB Receptors - therapeutic use Feasibility studies Gefitinib Health aspects Humans Lung cancer Lung cancer, Non-small cell Lung Neoplasms - drug therapy Mutation Physiological aspects Protein Kinase Inhibitors - adverse effects Protein Kinase Inhibitors - therapeutic use Proteins Quinazolines - adverse effects Quinazolines - therapeutic use Radiation therapy Review Thoracic surgery Tumors |
| title | Gefitinib in Non Small Cell Lung Cancer |
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