Pazopanib and anti-VEGF therapy
Identifieur interne : 005E99 ( Ncbi/Merge ); précédent : 005E98; suivant : 005F00Pazopanib and anti-VEGF therapy
Auteurs : Harry A. Drabkin [États-Unis]Source :
- Open Access Journal of Urology [ 1179-1551 ] ; 2010.
Abstract
Pazopanib (Votrient™, GlaxoSmithKline), a multi-kinase inhibitor with activity against VEGFR and other receptors, was recently approved by the FDA for the treatment of advanced renal cell carcinoma (RCC). Here, we review the history of its development, together with an overview of VEGF and its receptors and co-receptors. Results from selected clinical trial data in RCC and other malignant diseases are presented. Based on available evidence, pazopanib is an effective VEGFR inhibitor with demonstrable clinical activity in metastatic RCC and promising activity in other diseases. Like most kinase inhibitors, its activity is not restricted to VEGF receptors, which is reflected in its side-effect profile.
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PubMed: 24198612
PubMed Central: 3818876
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Drabkin</name><affiliation wicri:level="1"><nlm:aff id="af1-oaju-2-035">Medical University of South Carolina and Hollings Cancer Center, Charleston, SC, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>Medical University of South Carolina and Hollings Cancer Center, Charleston, SC</wicri:regionArea><wicri:noRegion>SC</wicri:noRegion></affiliation></author></titleStmt><publicationStmt><idno type="wicri:source">PMC</idno><idno type="pmid">24198612</idno><idno type="pmc">3818876</idno><idno type="url">http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3818876</idno><idno type="RBID">PMC:3818876</idno><date when="2010">2010</date><idno type="wicri:Area/Pmc/Corpus">004B50</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Corpus" wicri:corpus="PMC">004B50</idno><idno type="wicri:Area/Pmc/Curation">004B49</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Curation">004B49</idno><idno type="wicri:Area/Pmc/Checkpoint">003290</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Checkpoint">003290</idno><idno type="wicri:Area/Ncbi/Merge">005E99</idno></publicationStmt><sourceDesc><biblStruct><analytic><title xml:lang="en" level="a" type="main">Pazopanib and anti-VEGF therapy</title><author><name sortKey="Drabkin, Harry A" sort="Drabkin, Harry A" uniqKey="Drabkin H" first="Harry A" last="Drabkin">Harry A. Drabkin</name><affiliation wicri:level="1"><nlm:aff id="af1-oaju-2-035">Medical University of South Carolina and Hollings Cancer Center, Charleston, SC, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>Medical University of South Carolina and Hollings Cancer Center, Charleston, SC</wicri:regionArea><wicri:noRegion>SC</wicri:noRegion></affiliation></author></analytic><series><title level="j">Open Access Journal of Urology</title><idno type="eISSN">1179-1551</idno><imprint><date when="2010">2010</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en"><p>Pazopanib (Votrient™, GlaxoSmithKline), a multi-kinase inhibitor with activity against VEGFR and other receptors, was recently approved by the FDA for the treatment of advanced renal cell carcinoma (RCC). Here, we review the history of its development, together with an overview of VEGF and its receptors and co-receptors. Results from selected clinical trial data in RCC and other malignant diseases are presented. Based on available evidence, pazopanib is an effective VEGFR inhibitor with demonstrable clinical activity in metastatic RCC and promising activity in other diseases. 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Yau</name></author><author><name sortKey="Chen, Pj" uniqKey="Chen P">PJ Chen</name></author><author><name sortKey="Curtis, Cm" uniqKey="Curtis C">CM Curtis</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Brady, J" uniqKey="Brady J">J Brady</name></author><author><name sortKey="Middleton, M" uniqKey="Middleton M">M Middleton</name></author><author><name sortKey="Midgley, Rs" uniqKey="Midgley R">RS Midgley</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Paez Ribes, M" uniqKey="Paez Ribes M">M Paez-Ribes</name></author><author><name sortKey="Allen, E" uniqKey="Allen E">E Allen</name></author><author><name sortKey="Hudock, J" uniqKey="Hudock J">J Hudock</name></author></analytic></biblStruct></listBibl></div1></back></TEI><pmc article-type="review-article"><pmc-dir>properties open_access</pmc-dir>
<front><journal-meta><journal-id journal-id-type="nlm-ta">Open Access J Urol</journal-id><journal-id journal-id-type="iso-abbrev">Open Access J Urol</journal-id><journal-title-group><journal-title>Open Access Journal of Urology</journal-title></journal-title-group><issn pub-type="epub">1179-1551</issn><publisher><publisher-name>Dove Medical Press</publisher-name></publisher></journal-meta><article-meta><article-id pub-id-type="pmid">24198612</article-id><article-id pub-id-type="pmc">3818876</article-id><article-id pub-id-type="publisher-id">oaju-2-035</article-id><article-categories><subj-group subj-group-type="heading"><subject>Review</subject></subj-group></article-categories><title-group><article-title>Pazopanib and anti-VEGF therapy</article-title></title-group><contrib-group><contrib contrib-type="author"><name><surname>Drabkin</surname><given-names>Harry A</given-names></name><xref ref-type="aff" rid="af1-oaju-2-035"></xref><xref ref-type="corresp" rid="c1-oaju-2-035"></xref></contrib></contrib-group><aff id="af1-oaju-2-035">Medical University of South Carolina and Hollings Cancer Center, Charleston, SC, USA</aff><author-notes><corresp id="c1-oaju-2-035">Correspondence: Harry A Drabkin, Division of Hematology-Oncology, Medical University of South Carolina, Charleston, SC 20425, USA, Tel +1 843-792-4271, Fax +1 843-792-0644, Email <email>drabkin@musc.edu</email></corresp></author-notes><pub-date pub-type="collection"><year>2010</year></pub-date><pub-date pub-type="epub"><day>12</day><month>3</month><year>2010</year></pub-date><volume>2</volume><fpage>35</fpage><lpage>40</lpage><permissions><copyright-statement>© 2010 Drabkin, publisher and licensee Dove Medical Press Ltd</copyright-statement><copyright-year>2010</copyright-year><license><license-p>This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited.</license-p></license></permissions><abstract><p>Pazopanib (Votrient™, GlaxoSmithKline), a multi-kinase inhibitor with activity against VEGFR and other receptors, was recently approved by the FDA for the treatment of advanced renal cell carcinoma (RCC). Here, we review the history of its development, together with an overview of VEGF and its receptors and co-receptors. Results from selected clinical trial data in RCC and other malignant diseases are presented. Based on available evidence, pazopanib is an effective VEGFR inhibitor with demonstrable clinical activity in metastatic RCC and promising activity in other diseases. Like most kinase inhibitors, its activity is not restricted to VEGF receptors, which is reflected in its side-effect profile.</p></abstract><kwd-group><title>Keywords</title><kwd>pazopanib</kwd><kwd>VEGFR</kwd><kwd>renal cell carcinoma</kwd></kwd-group></article-meta></front><floats-group><fig id="f1-oaju-2-035" position="float"><label>Figure 1</label><caption><p>Schematic showing neuropilin1/2, VEGFR1/2 and plexin A receptors/co-receptors and their various ligands. The neuropilins function as co-receptors for various VEGF ligands, whereas the plexins are co-receptors for Sema3s.</p><p><bold>Abbreviations:</bold> FGR, fibroblast growth factor; HGF, hepatocyte growth factor.</p></caption><graphic xlink:href="oaju-2-035Fig1"></graphic></fig><fig id="f2-oaju-2-035" position="float"><label>Figure 2</label><caption><p>The structure of pazopanib (cmpd 13).</p></caption><graphic xlink:href="oaju-2-035Fig2"></graphic></fig></floats-group></pmc><affiliations><list><country><li>États-Unis</li></country></list><tree><country name="États-Unis"><noRegion><name sortKey="Drabkin, Harry A" sort="Drabkin, Harry A" uniqKey="Drabkin H" first="Harry A" last="Drabkin">Harry A. Drabkin</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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