Gefitinib, a novel, orally administered agent for the treatment of cancer.

2.50
Hdl Handle:
http://hdl.handle.net/10541/77736
Title:
Gefitinib, a novel, orally administered agent for the treatment of cancer.
Authors:
Ranson, Malcolm R; Wardell, Stephen
Abstract:
Traditional cytotoxic anticancer therapies do not differentiate between tumour and host cells, and research efforts have been focused on finding new agents that target tumour tissue. Gefitinib ('Iressa', ZD1839) is an orally active epidermal growth factor receptor tyrosine kinase inhibitor that blocks signal pathways implicated in solid tumour growth and metastasis. In phase II trials, gefitinib 250 mg/day demonstrated efficacy in the control of advanced non-small-cell lung cancer (NSCLC) in patients who had undergone prior chemotherapy. Response rates were 18.4 and 11.8%, and disease control rates were 54.4 and 42.2%, at 250 mg/day in two multicentre trials - IDEAL 1 and 2. Gefitinib also caused rapid relief from the symptoms of NSCLC in approximately 40% of patients, while displaying a generally good tolerability profile that most commonly included mild, reversible gastrointestinal and skin adverse events. Gefitinib 250 mg/day has been approved for use in advanced, previously treated NSCLC in several countries including the USA, Japan and Australia. As a monotherapy and combination therapy, it is being investigated for the treatment of several common tumour types in addition to NSCLC. The pharmacokinetics of gefitinib have shown it to be suitable for once daily dosing, with a terminal half-life of approximately 48 h in patients with cancer. Steady-state exposure is achieved after 10 days dosing, and exposure is dose proportional up to 250 mg/day. Gefitinib is cleared principally by the biliary route and in part by metabolism. This review summarizes relevant data from studies of gefitinib that inform its clinical administration.
Affiliation:
Department of Medical Oncology, Christie Hospital and Holt Radium Institute, Manchester, UK. malcolm.ransom@man.ac.uk
Citation:
Gefitinib, a novel, orally administered agent for the treatment of cancer. 2004, 29 (2):95-103 J Clin Pharm Ther
Journal:
Journal of Clinical Pharmacy and Therapeutics
Issue Date:
Apr-2004
URI:
http://hdl.handle.net/10541/77736
DOI:
10.1111/j.1365-2710.2004.00543.x
PubMed ID:
15068398
Type:
Article
Language:
en
ISSN:
0269-4727
Appears in Collections:
All Christie Publications

Full metadata record

DC FieldValue Language
dc.contributor.authorRanson, Malcolm R-
dc.contributor.authorWardell, Stephen-
dc.date.accessioned2009-08-18T15:11:30Z-
dc.date.available2009-08-18T15:11:30Z-
dc.date.issued2004-04-
dc.identifier.citationGefitinib, a novel, orally administered agent for the treatment of cancer. 2004, 29 (2):95-103 J Clin Pharm Theren
dc.identifier.issn0269-4727-
dc.identifier.pmid15068398-
dc.identifier.doi10.1111/j.1365-2710.2004.00543.x-
dc.identifier.urihttp://hdl.handle.net/10541/77736-
dc.description.abstractTraditional cytotoxic anticancer therapies do not differentiate between tumour and host cells, and research efforts have been focused on finding new agents that target tumour tissue. Gefitinib ('Iressa', ZD1839) is an orally active epidermal growth factor receptor tyrosine kinase inhibitor that blocks signal pathways implicated in solid tumour growth and metastasis. In phase II trials, gefitinib 250 mg/day demonstrated efficacy in the control of advanced non-small-cell lung cancer (NSCLC) in patients who had undergone prior chemotherapy. Response rates were 18.4 and 11.8%, and disease control rates were 54.4 and 42.2%, at 250 mg/day in two multicentre trials - IDEAL 1 and 2. Gefitinib also caused rapid relief from the symptoms of NSCLC in approximately 40% of patients, while displaying a generally good tolerability profile that most commonly included mild, reversible gastrointestinal and skin adverse events. Gefitinib 250 mg/day has been approved for use in advanced, previously treated NSCLC in several countries including the USA, Japan and Australia. As a monotherapy and combination therapy, it is being investigated for the treatment of several common tumour types in addition to NSCLC. The pharmacokinetics of gefitinib have shown it to be suitable for once daily dosing, with a terminal half-life of approximately 48 h in patients with cancer. Steady-state exposure is achieved after 10 days dosing, and exposure is dose proportional up to 250 mg/day. Gefitinib is cleared principally by the biliary route and in part by metabolism. This review summarizes relevant data from studies of gefitinib that inform its clinical administration.en
dc.language.isoenen
dc.subjectLung Canceren
dc.subject.meshAdministration, Oral-
dc.subject.meshAntineoplastic Agents-
dc.subject.meshArea Under Curve-
dc.subject.meshCarcinoma, Non-Small-Cell Lung-
dc.subject.meshClinical Trials, Phase I as Topic-
dc.subject.meshClinical Trials, Phase II as Topic-
dc.subject.meshEpidermal Growth Factor-
dc.subject.meshHumans-
dc.subject.meshLung Neoplasms-
dc.subject.meshQuinazolines-
dc.subject.meshSurvival Analysis-
dc.subject.meshTreatment Outcome-
dc.titleGefitinib, a novel, orally administered agent for the treatment of cancer.en
dc.typeArticleen
dc.contributor.departmentDepartment of Medical Oncology, Christie Hospital and Holt Radium Institute, Manchester, UK. malcolm.ransom@man.ac.uken
dc.identifier.journalJournal of Clinical Pharmacy and Therapeuticsen
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