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<meta name="robots" content="INDEX,FOLLOW,NOARCHIVE" /><meta name="citation_inbook_title" content="Molecular Imaging and Contrast Agent Database (MICAD) [Internet]" /><meta name="citation_title" content="4-[18F]Fluoropaclitaxel" /><meta name="citation_publisher" content="National Center for Biotechnology Information (US)" /><meta name="citation_date" content="2012/02/14" /><meta name="citation_author" content="Kam Leung" /><meta name="citation_pmid" content="20641916" /><meta name="citation_fulltext_html_url" content="https://www.ncbi.nlm.nih.gov/books/NBK23721/" /><link rel="schema.DC" href="http://purl.org/DC/elements/1.0/" /><meta name="DC.Title" content="4-[18F]Fluoropaclitaxel" /><meta name="DC.Type" content="Text" /><meta name="DC.Publisher" content="National Center for Biotechnology Information (US)" /><meta name="DC.Contributor" content="Kam Leung" /><meta name="DC.Date" content="2012/02/14" /><meta name="DC.Identifier" content="https://www.ncbi.nlm.nih.gov/books/NBK23721/" /><meta name="description" content="One of the mechanisms that tumor cells use to escape the cytotoxic effects of chemotherapeutic agents, such as Adriamycin, Vinca alkaloids, epipodophyllotoxins, actinomycin D, and paclitaxel (PAC), is to limit their presence inside the cells through the actions of P-glycoprotein (P-gp), a protein encoded by the multidrug resistance (MDR-1) gene (1, 2). 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<div class="pre-content"><div><div class="bk_prnt"><p class="small">NCBI Bookshelf. A service of the National Library of Medicine, National Institutes of Health.</p><p>Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013. </p></div><div class="iconblock clearfix whole_rhythm no_top_margin bk_noprnt"><a class="img_link icnblk_img" title="Table of Contents Page" href="/books/n/micad/"><img class="source-thumb" src="/corehtml/pmc/pmcgifs/bookshelf/thumbs/th-micad-lrg.png" alt="Cover of Molecular Imaging and Contrast Agent Database (MICAD)" height="100px" width="80px" /></a><div class="icnblk_cntnt eight_col"><h2>Molecular Imaging and Contrast Agent Database (MICAD) [Internet].</h2><a data-jig="ncbitoggler" href="#__NBK23721_dtls__">Show details</a><div style="display:none" class="ui-widget" id="__NBK23721_dtls__"><div>Bethesda (MD): <a href="https://www.ncbi.nlm.nih.gov/" ref="pagearea=page-banner&targetsite=external&targetcat=link&targettype=publisher">National Center for Biotechnology Information (US)</a>; 2004-2013.</div></div><div class="half_rhythm"><ul class="inline_list"><li style="margin-right:1em"><a class="bk_cntns" href="/books/n/micad/">Contents</a></li></ul></div><div class="bk_noprnt"><form method="get" action="/books/n/micad/" id="bk_srch"><div class="bk_search"><label for="bk_term" class="offscreen_noflow">Search term</label><input type="text" title="Search this book" id="bk_term" name="term" value="" data-jig="ncbiclearbutton" /> <input type="submit" class="jig-ncbibutton" value="Search this book" submit="false" style="padding: 0.1em 0.4em;" /></div></form></div></div><div class="icnblk_cntnt two_col"><div class="pagination bk_noprnt"><a class="active page_link prev" href="/books/n/micad/FITM-18F/" title="Previous page in this title">< Prev</a><a class="active page_link next" href="/books/n/micad/NS10743-18F/" title="Next page in this title">Next ></a></div></div></div></div></div>
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<div class="main-content lit-style" itemscope="itemscope" itemtype="http://schema.org/CreativeWork"><div class="meta-content fm-sec"><h1 id="_NBK23721_"><span class="title" itemprop="name">4-[<sup>18</sup>F]Fluoropaclitaxel</span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm">[<sup>18</sup>F]FPAC</div><p class="contrib-group"><span itemprop="author">Kam Leung</span>, PhD.</p><a data-jig="ncbitoggler" href="#__NBK23721_ai__" style="border:0;text-decoration:none">Author Information and Affiliations</a><div style="display:none" class="ui-widget" id="__NBK23721_ai__"><div class="contrib half_rhythm"><span itemprop="author">Kam Leung</span>, PhD<div class="affiliation small">National Center for Biotechnology Information, NLM, NIH, Bethesda, MD<div><span class="email-label">Email: </span><a href="mailto:dev@null" data-email="vog.hin.mln.ibcn@dacim" class="oemail">vog.hin.mln.ibcn@dacim</a></div></div><div class="small">Corresponding author.</div></div></div><p class="small">Created: <span itemprop="datePublished">January 2, 2006</span>; Last Update: <span itemprop="dateModified">February 14, 2012</span>.</p></div><div class="jig-ncbiinpagenav body-content whole_rhythm" data-jigconfig="allHeadingLevels: ['h2'],smoothScroll: false" itemprop="text"><div id="FPAC18F.T.nc_chemical_name418ffluoropacl" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK23721/table/FPAC18F.T.nc_chemical_name418ffluoropacl/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__FPAC18F.T.nc_chemical_name418ffluoropacl_lrgtbl__"><table><tbody><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Chemical name:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">4-[<sup>18</sup>F]Fluoropaclitaxel</td><td rowspan="9" colspan="1" style="text-align:center;vertical-align:middle;">
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<a href="https://pubchem.ncbi.nlm.nih.gov/substance/8036875" title="View this structure in PubChem" class="img_link" ref="pagearea=body&targetsite=entrez&targetcat=link&targettype=pubchem"><img src="https://pubchem.ncbi.nlm.nih.gov/image/imgsrv.fcgi?t=l&sid=8036875" alt="image 8036875 in the ncbi pubchem database" /></a>
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</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Abbreviated name:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">[<sup>18</sup>F]FPAC</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Synonym:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">[<sup>18</sup>F]Taxol®</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Agent category:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Compound</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Target:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">P-glycoprotein (P-gp) multidrug transporter, MDR-1</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Target category:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Transporter</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Method of detection:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Positron emission tomography (PET)</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Source of signal:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>18</sup>F</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Activation:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">No</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Studies:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<ul class="simple-list"><li class="half_rhythm"><div>
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" />
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<i>In vitro</i>
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</div></li><li class="half_rhythm"><div>
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Rodents
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</div></li><li class="half_rhythm"><div>
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Non-Human Primates
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</div></li><li class="half_rhythm"><div>
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Humans
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</div></li></ul>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Click on the above structure for additional information in <a href="http://pubchem.ncbi.nlm.nih.gov/" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubChem</a>.</td></tr></tbody></table></div></div><div id="FPAC18F.Background"><h2 id="_FPAC18F_Background_">Background</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%2818F%20paclitaxel%20or%20fluoropaclitaxel%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>One of the mechanisms that tumor cells use to escape the cytotoxic effects of chemotherapeutic agents, such as Adriamycin, Vinca alkaloids, epipodophyllotoxins, actinomycin D, and paclitaxel (PAC), is to limit their presence inside the cells through the actions of P-glycoprotein (P-gp), a protein encoded by the multidrug resistance (MDR-1) gene (<a class="bk_pop" href="#FPAC18F.REF.1" data-bk-pop-others="FPAC18F.REF.2">1, 2</a>). P-gp is an ATP-dependent transmembrane multidrug transporter that is capable of actively pumping a variety of agents out of cells. Injection of unlabeled efflux pump substrates increases the retention of radioactivity in tumors rather than lessening the retention, as seen with receptor-binding radiotracers. Overexpression of P-gp in tumor cells (such as renal carcinoma, hepatoma, pheochromocytoma, and colon carcinoma) leads to resistance to anticancer drugs (<a class="bk_pop" href="#FPAC18F.REF.3">3</a>). P-gp is also present in a variety of normal cells, such as intestinal mucosal cells, hepatocytes, renal proximal tubule epithelial cells, and endothelial cells of the blood-brain barrier (<a class="bk_pop" href="#FPAC18F.REF.4" data-bk-pop-others="FPAC18F.REF.5">4, 5</a>). Calcium channel blockers, cyclosporin A, and its non-immunosuppressive analog PSC 833 are MDR modulators that inhibit transport of P-gp substrates out of cells (<a class="bk_pop" href="#FPAC18F.REF.6" data-bk-pop-others="FPAC18F.REF.7">6, 7</a>).</p><p>Sestamibi (MIBI) is a substrate for P-gp. <a href="/books/n/micad/MIBI99mtc/"><sup>99m</sup>Tc-MIBI</a> has been approved by the United States Food and Drug Administration (FDA) as a myocardial perfusion imaging agent for use with single-photon emission computed tomography (SPECT) to assess the risk of future cardiac events. It is also approved as a tumor-imaging agent in breast, lung, thyroid, and brain cancers. PAC is an FDA-approved chemotherapeutic agent exerting its antitumor activity by binding to β-tubulin to inhibit cell division (<a class="bk_pop" href="#FPAC18F.REF.8">8</a>). It is also a transport substrate for P-gp in tumor cells, leading to drug-related resistance to chemotherapy (<a class="bk_pop" href="#FPAC18F.REF.8" data-bk-pop-others="FPAC18F.REF.9">8, 9</a>). Therefore, [<sup>18</sup>F]fluoropaclitaxel ([<sup>18</sup>F]FPAC) is being developed as a positron emission tomography (PET) agent to noninvasively study P-gp function and multidrug resistance in tumors and normal tissues.</p><div id="FPAC18F.Related_Resource_Links"><h3>Related Resource Links:</h3><ul><li class="half_rhythm"><div>Chapters in MICAD (<a href="/sites/entrez?Db=books&Cmd=DetailsSearch&Term=P-glycoprotein%5BAll+Fields%5D+AND+micad%5Bbook%5D" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">P-glycoprotein</a>)</div></li><li class="half_rhythm"><div>Gene information in NCBI (<a href="/gene/5243" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">P-glycoprotein</a>)</div></li><li class="half_rhythm"><div>Articles in OMIM (<a href="/sites/entrez?Db=omim&Cmd=DetailsSearch&Term=P-glycoprotein%5BAll+Fields%5D" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">P-glycoprotein</a>)</div></li><li class="half_rhythm"><div>Clinical trials (<a href="http://www.clinicaltrials.gov/ct2/results?term=P-glycoprotein" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">P-glycoprotein</a>, <a href="http://www.clinicaltrials.gov/ct2/results?term=Sestamibi" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri"><sup>99m</sup>Tc-MIBI</a>, <a href="http://www.clinicaltrials.gov/ct2/results?term=paclitaxel" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Paclitaxel</a>)</div></li><li class="half_rhythm"><div>Drug information in FDA (<a href="http://google2.fda.gov/search?q=99mTc-sestamibi+&client=FDAgov&site=FDAgov&lr=&proxystylesheet=FDAgov&output=xml_no_dtd&getfields=*&x=12&y=16" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri"><sup>9</sup><sup>9</sup><sup>m</sup>Tc-MIBI</a>, <a href="http://google2.fda.gov/search?q=paclitaxel&client=FDAgov&site=FDAgov&lr=&proxystylesheet=FDAgov&output=xml_no_dtd&getfields=*" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Paclitaxel</a>)</div></li></ul></div></div><div id="FPAC18F.Synthesis"><h2 id="_FPAC18F_Synthesis_">Synthesis</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%2818F%20paclitaxel%20or%20fluoropaclitaxel%29%20and%20synthesis" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Kiesewetter et al. (<a class="bk_pop" href="#FPAC18F.REF.10">10</a>) prepared [<sup>18</sup>F]FPAC by incorporating [<sup>18</sup>F]fluoride (Kryptofix 2.2.2 and K<sub>2</sub>CO<sub>3</sub>) into [<sup>18</sup>F]fluorobenzoate ester via nucleophilic displacement of a trimethylammonium moiety. The ester group was removed, and the resulting [<sup>18</sup>F]fluorobenzoic acid was coupled to 3´-debenzoylpaclitaxel (<a class="bk_pop" href="#FPAC18F.REF.10">10</a>).The final product was purified by high-performance liquid chromatography. The radiochemical yield for the syntheses was 18.3 ± 5.5% (not corrected for decay). The specific activity at the end of bombardment was 169-453 GBq/mmol (4.58-12.25 Ci/mmol) for 14 syntheses. The total synthesis time was 80 min.</p></div><div id="FPAC18F.In_Vitro_Studies_Testing_in_Cell"><h2 id="_FPAC18F_In_Vitro_Studies_Testing_in_Cell_"><i>In Vitro</i> Studies: Testing in Cells and Tissues</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%2818F%20fluoropaclitaxel%20%29%20and%20in%20vitro" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>In an <i>in vitro</i> study using human hepatocytes, 50% [<sup>18</sup>F]FPAC was metabolized to produce one major metabolite, 6α-hydroxy-FPAC, after 4 h of incubation (<a class="bk_pop" href="#FPAC18F.REF.10">10</a>). In rat hepatocytes, 3 metabolites were produced from [<sup>18</sup>F]FPAC with a half-life of 194 min.</p></div><div id="FPAC18F.Animal_Studies"><h2 id="_FPAC18F_Animal_Studies_">Animal Studies</h2><div id="FPAC18F.Rodents"><h3>Rodents</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%2818F%20paclitaxel%20or%20fluoropaclitaxel%29%20and%20rodentia" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Biodistribution studies in normal rats showed high accumulation of radioactivity, as measured by differential uptake ratio, in the liver (1.64), followed by the kidney (1.59), heart (1.28), and lung (0.99) at 60 min after injection of [<sup>18</sup>F]FPAC (<a class="bk_pop" href="#FPAC18F.REF.10">10</a>). Levels of the tracer were low in the brain (0.018) and blood (0.08). Pretreatment (20 min) with PAC (200 nmol) increased [<sup>18</sup>F]FPAC accumulation in the blood (33%), heart (32%), lung (38%), liver (30%), kidney (142%), and brain (5%). Increased accumulation is consistent with saturation of the efflux pump, P-gp. There was a significantly greater accumulation of [<sup>18</sup>F]FPAC in the heart (79% increase), lung (143%), muscle (38%), and brain (1300%) in mdr1a/1b(-/-) mice than in wild-type mice. Furthermore, biodistribution studies in both types of mice with pre-injection of PAC or XR9576, an MDR modulator, showed little effect on the accumulation of [<sup>18</sup>F]FPAC in the knockout mice compared with the wild-type mice, which showed significant increases only in the lung and kidney. The kidney contained 42-71% intact [<sup>18</sup>F]FPAC, whereas the liver contained 59-86% at 30 min after injection in both types of mice.</p><p>Biodistributions of [<sup>18</sup>F]FPAC and [<sup>3</sup>H]PAC were very similar in nude mice bearing MCF-7 human breast tumors, with the highest accumulations in the small intestine, the lowest accumulations in the brain, and intermediate accumulations in the tumor (<a class="bk_pop" href="#FPAC18F.REF.11">11</a>). Uptake in these and other tissues was not significantly inhibited or enhanced by the presence of unlabeled PAC (20 mg/kg). Administration of cyclosporin A (10 mg/kg) increased uptake of both [<sup>18</sup>F]FPAC and [<sup>3</sup>H]PAC into the tumor by 1-fold.</p></div><div id="FPAC18F.Other_NonPrimate_Mammals"><h3>Other Non-Primate Mammals</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%2818F%20fluoropaclitaxel%29%20and%20%28dog%20or%20pig%20or%20rabbit%20or%20sheep%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No publications are currently available.</p></div><div id="FPAC18F.NonHuman_Primates"><h3>Non-Human Primates</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%2818F-paclitaxel%20or%20fluoropaclitaxel%29%20and%20%28nonhuman%20primate%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Kurdziel et al. (<a class="bk_pop" href="#FPAC18F.REF.12">12</a>) performed PET imaging in 3 rhesus monkeys after injection of 222-444 MBq (6-12 mCi) of [<sup>18</sup>F]FPAC. Pretreatment with XR9576 (a P-gp blocker) changed the Logan plot slope (distribution volume) for the liver by +104% (<i>P</i> = 0.02), the lung by +87% (<i>P</i> = 0.01), and the kidney by -14% (<i>P</i> = 0.08) (<a class="bk_pop" href="#FPAC18F.REF.12">12</a>). Changes in the mean area under time-activity curve (AUC; plasma metabolite-corrected) were +54% (<i>P</i> = 0.08), +97% (<i>P</i> = 0.04), and -12% (<i>P</i> = 0.02), respectively, for the liver, lung, and kidney. This indicates that accumulation of [<sup>18</sup>F]FPAC in the liver and lung is modulated by the MDR P-gp efflux pump. No significant difference was found in the AUC between the baseline and XR9576 studies.</p><p>Kurdziel et al. (<a class="bk_pop" href="#FPAC18F.REF.12">12</a>) estimated the human dosimetry of [<sup>18</sup>F]FPAC in 3 rhesus monkeys after injection of 222-444 MBq (6-12 mCi) of [<sup>18</sup>F]FPAC. The organs that received the highest absorbed doses were the gallbladder (0.19 mGy/MBq, or 0.69 rad/mCi), the liver (0.14 mGy/MBq, or 0.52 rad/mCi), upper intestine (0.094 mGy/MBq, or 35 rad/mCi), and the kidneys (0.044 mGy/MBq, or 0.163 rad/mCi). The effective dose was 0.022 mSv/MBq (0.083 rem/mCi).</p></div></div><div id="FPAC18F.Human_Studies"><h2 id="_FPAC18F_Human_Studies_">Human Studies</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%2818F-paclitaxel%20or%20fluoropaclitaxel%29%20and%20%28%20human%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Kurdziel et al. (<a class="bk_pop" href="#FPAC18F.REF.13">13</a>) estimated the human dosimetry of [<sup>18</sup>F]FPAC in 3 healthy subjects after injection of 192.4 MBq (5.2 mCi) of [<sup>18</sup>F]FPAC. The organs receiving the highest radiation dose were the gallbladder, large intestine and small intestine at 0.23 mGy/MBq (0.85 rad/mCi), 0.19 mGy/MBq (0.68 rad/mCi), and 0.16 mGy/MBq (0.60 rad/mCi), respectively. The effective dose was 28.79 μSv/MBq (0.107 rem/mCi). [<sup>18</sup>F]FPAC PET studies were performed with dynamic scans for 60 min and static scans for 120 min in 3 breast cancer patients. The tumor uptake was low with an average maximum standard uptake value (SUV<sub>max</sub>) of 1.8 at 80 s after injection decreased slightly over time. When compared with background tissue (contralateral breast), the tumors were visible with an average maximum tumor/background ratio of 7.7 at 20 min. Tumor/blood ratios increased slightly over time to an average maximum of 1.9.</p></div><div id="FPAC18F.NIH_Support"><h2 id="_FPAC18F_NIH_Support_">NIH Support</h2><p>Intramural Research Program, 1R21 CA098334-01A1</p></div><div id="FPAC18F.References"><h2 id="_FPAC18F_References_">References</h2><dl class="temp-labeled-list"><dt>1.</dt><dd><div class="bk_ref" id="FPAC18F.REF.1">Endicott J.A., Ling V.
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<em>The biochemistry of P-glycoprotein-mediated multidrug resistance.</em>
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||
<span><span class="ref-journal">Annu Rev Biochem. </span>1989;<span class="ref-vol">58</span>:137–71.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2570548" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2570548</span></a>]</div></dd><dt>2.</dt><dd><div class="bk_ref" id="FPAC18F.REF.2">Gottesman M.M., Pastan I.
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<em>Biochemistry of multidrug resistance mediated by the multidrug transporter.</em>
|
||
<span><span class="ref-journal">Annu Rev Biochem. </span>1993;<span class="ref-vol">62</span>:385–427.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/8102521" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 8102521</span></a>]</div></dd><dt>3.</dt><dd><div class="bk_ref" id="FPAC18F.REF.3">Fojo A.T., Ueda K., Slamon D.J., Poplack D.G., Gottesman M.M., Pastan I.
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||
<em>Expression of a multidrug-resistance gene in human tumors and tissues.</em>
|
||
<span><span class="ref-journal">Proc Natl Acad Sci U S A. </span>1987;<span class="ref-vol">84</span>(1):265–9.</span> [<a href="/pmc/articles/PMC304184/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC304184</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/2432605" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2432605</span></a>]</div></dd><dt>4.</dt><dd><div class="bk_ref" id="FPAC18F.REF.4">Piwnica-Worms D., Rao V.V., Kronauge J.F., Croop J.M.
|
||
<em>Characterization of multidrug resistance P-glycoprotein transport function with an organotechnetium cation.</em>
|
||
<span><span class="ref-journal">Biochemistry. </span>1995;<span class="ref-vol">34</span>(38):12210–20.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/7547962" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 7547962</span></a>]</div></dd><dt>5.</dt><dd><div class="bk_ref" id="FPAC18F.REF.5">Thiebaut F., Tsuruo T., Hamada H., Gottesman M.M., Pastan I., Willingham M.C.
|
||
<em>Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues.</em>
|
||
<span><span class="ref-journal">Proc Natl Acad Sci U S A. </span>1987;<span class="ref-vol">84</span>(21):7735–8.</span> [<a href="/pmc/articles/PMC299375/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC299375</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/2444983" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2444983</span></a>]</div></dd><dt>6.</dt><dd><div class="bk_ref" id="FPAC18F.REF.6">Hughes C.S., Vaden S.L., Manaugh C.A., Price G.S., Hudson L.C.
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||
<em>Modulation of doxorubicin concentration by cyclosporin A in brain and testicular barrier tissues expressing P-glycoprotein in rats.</em>
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||
<span><span class="ref-journal">J Neurooncol. </span>1998;<span class="ref-vol">37</span>(1):45–54.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/9525837" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 9525837</span></a>]</div></dd><dt>7.</dt><dd><div class="bk_ref" id="FPAC18F.REF.7">Mayer U., Wagenaar E., Dorobek B., Beijnen J.H., Borst P., Schinkel A.H.
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||
<em>Full blockade of intestinal P-glycoprotein and extensive inhibition of blood-brain barrier P-glycoprotein by oral treatment of mice with PSC833.</em>
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||
<span><span class="ref-journal">J Clin Invest. </span>1997;<span class="ref-vol">100</span>(10):2430–6.</span> [<a href="/pmc/articles/PMC508442/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC508442</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/9366556" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 9366556</span></a>]</div></dd><dt>8.</dt><dd><div class="bk_ref" id="FPAC18F.REF.8">Horwitz S.B., Cohen D., Rao S., Ringel I., Shen H.J., Yang C.P.
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||
<em>Taxol: mechanisms of action and resistance.</em>
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||
<span><span class="ref-journal">J Natl Cancer Inst Monogr. </span>1993;(15):55–61.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/7912530" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 7912530</span></a>]</div></dd><dt>9.</dt><dd><div class="bk_ref" id="FPAC18F.REF.9">Huang Y., Ibrado A.M., Reed J.C., Bullock G., Ray S., Tang C., Bhalla K.
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<em>Co-expression of several molecular mechanisms of multidrug resistance and their significance for paclitaxel cytotoxicity in human AML HL-60 cells.</em>
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<span><span class="ref-journal">Leukemia. </span>1997;<span class="ref-vol">11</span>(2):253–7.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/9009089" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 9009089</span></a>]</div></dd><dt>10.</dt><dd><div class="bk_ref" id="FPAC18F.REF.10">Kiesewetter D.O., Jagoda E.M., Kao C.H., Ma Y., Ravasi L., Shimoji K., Szajek L.P., Eckelman W.C.
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<em>Fluoro-, bromo-, and iodopaclitaxel derivatives: synthesis and biological evaluation.</em>
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<span><span class="ref-journal">Nucl Med Biol. </span>2003;<span class="ref-vol">30</span>(1):11–24.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/12493538" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 12493538</span></a>]</div></dd><dt>11.</dt><dd><div class="bk_ref" id="FPAC18F.REF.11">Gangloff A., Hsueh W.A., Kesner A.L., Kiesewetter D.O., Pio B.S., Pegram M.D., Beryt M., Townsend A., Czernin J., Phelps M.E., Silverman D.H.
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<em>Estimation of paclitaxel biodistribution and uptake in human-derived xenografts in vivo with (18)F-fluoropaclitaxel.</em>
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<span><span class="ref-journal">J Nucl Med. </span>2005;<span class="ref-vol">46</span>(11):1866–71.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16269601" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 16269601</span></a>]</div></dd><dt>12.</dt><dd><div class="bk_ref" id="FPAC18F.REF.12">Kurdziel K.A., Kiesewetter D.O., Carson R.E., Eckelman W.C., Herscovitch P.
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<em>Biodistribution, radiation dose estimates, and in vivo Pgp modulation studies of 18F-paclitaxel in nonhuman primates.</em>
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||
<span><span class="ref-journal">J Nucl Med. </span>2003;<span class="ref-vol">44</span>(8):1330–9.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/12902425" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 12902425</span></a>]</div></dd><dt>13.</dt><dd><div class="bk_ref" id="FPAC18F.REF.13">Kurdziel K.A., Kalen J.D., Hirsch J.I., Wilson J.D., Bear H.D., Logan J., McCumisky J., Moorman-Sykes K., Adler S., Choyke P.L.
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<em>Human dosimetry and preliminary tumor distribution of 18F-fluoropaclitaxel in healthy volunteers and newly diagnosed breast cancer patients using PET/CT.</em>
|
||
<span><span class="ref-journal">J Nucl Med. </span>2011;<span class="ref-vol">52</span>(9):1339–45.</span> [<a href="/pmc/articles/PMC3224978/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC3224978</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/21849404" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 21849404</span></a>]</div></dd></dl></div><div id="bk_toc_contnr"></div></div></div>
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<div class="post-content"><div><div class="half_rhythm"><a href="/books/about/copyright/">Copyright Notice</a></div><div class="small"><span class="label">Bookshelf ID: NBK23721</span><span class="label">PMID: <a href="https://pubmed.ncbi.nlm.nih.gov/20641916" title="PubMed record of this page" ref="pagearea=meta&targetsite=entrez&targetcat=link&targettype=pubmed">20641916</a></span></div><div style="margin-top:2em" class="bk_noprnt"><a class="bk_cntns" href="/books/n/micad/">Contents</a><div class="pagination bk_noprnt"><a class="active page_link prev" href="/books/n/micad/FITM-18F/" title="Previous page in this title">< Prev</a><a class="active page_link next" href="/books/n/micad/NS10743-18F/" title="Next page in this title">Next ></a></div></div></div></div>
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<div id="ncbi_share_book"><a href="#" class="ncbi_share" data-ncbi_share_config="popup:false,shorten:true" ref="id=NBK23721&db=books">Share</a></div>
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<div xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance"></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Views</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="PDF_download" id="Shutter"></a></div><div class="portlet_content"><ul xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="simple-list"><li><a href="/books/NBK23721/?report=reader">PubReader</a></li><li><a href="/books/NBK23721/?report=printable">Print View</a></li><li><a data-jig="ncbidialog" href="#_ncbi_dlg_citbx_NBK23721" data-jigconfig="width:400,modal:true">Cite this Page</a><div id="_ncbi_dlg_citbx_NBK23721" style="display:none" title="Cite this Page"><div class="bk_tt">Leung K. 4-[18F]Fluoropaclitaxel. 2006 Jan 2 [Updated 2012 Feb 14]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013. <span class="bk_cite_avail"></span></div></div></li><li><a href="/books/NBK23721/pdf/Bookshelf_NBK23721.pdf">PDF version of this page</a> (148K)</li><li><a href="/books/n/micad/toc/bin/micad.csv">MICAD summary (CSV file)</a></li></ul></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>In this page</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="page-toc" id="Shutter"></a></div><div class="portlet_content"><ul xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="simple-list"><li><a href="#FPAC18F.Background" ref="log$=inpage&link_id=inpage">Background</a></li><li><a href="#FPAC18F.Synthesis" ref="log$=inpage&link_id=inpage">Synthesis</a></li><li><a href="#FPAC18F.In_Vitro_Studies_Testing_in_Cell" ref="log$=inpage&link_id=inpage"><i>In Vitro</i> Studies: Testing in Cells and Tissues</a></li><li><a href="#FPAC18F.Animal_Studies" ref="log$=inpage&link_id=inpage">Animal Studies</a></li><li><a href="#FPAC18F.Human_Studies" ref="log$=inpage&link_id=inpage">Human Studies</a></li><li><a href="#FPAC18F.NIH_Support" ref="log$=inpage&link_id=inpage">NIH Support</a></li><li><a href="#FPAC18F.References" ref="log$=inpage&link_id=inpage">References</a></li></ul></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Search MICAD</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="source-application" id="Shutter"></a></div><div class="portlet_content"><form xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" name="frmSearch" method="get" action="/books/NBK5330/" id="frmSearch"><script type="text/javascript" src="/corehtml/pmc//js/bookshelf/micad.js">/**/</script><label class="offscreen_noflow" for="txtfield">Search term</label><input id="txtfield" type="text" name="f1_term" size="22" onKeyPress="KeyPress('micad',event,'/books/NBK5330/','')" /><button name="f1_search" type="submit">Go</button><button onclick="this.form.reset();" type="reset">Clear</button><p><b>Limit my Search:</b></p><div class="clearfix"><label for="detection">Method of detection:</label><div class="right"><select name="detection" id="detection" style="width:200px"><option value="" selected="selected">Any</option><option value="(MRI OR "Magnetic resonance imaging" OR MRS)">MRI</option><option value="Multimodal">Multimodal imaging</option><option value="Optical">Optical imaging</option><option value="PET">PET</option><option value="Photoacoustic">Photoacoustic imaging</option><option value="(SPECT OR planar)">SPECT</option><option value="Ultrasound">Ultrasound</option><option value="(x-ray OR ct)">X-ray, CT</option></select></div></div><div class="clearfix"><label for="signal">Source of signal/contrast:</label><div class="right"><select name="signal" id="signal" style="width:200px"><option value="" selected="selected">Any</option><optgroup label="MRI agents"><option value="(Copper OR Cu)">Copper</option><option value="(Europium OR Eu3+)">Europium</option><option value="(Fluorine OR 19F)">Fluorine</option><option value="(Gadolinium OR Gd3+)">Gadolinium</option><option value=""Hyperpolarized 13C"">Hyperpolarized 13C</option><option value=""Iron oxide"">Iron oxide</option><option value=""Nitroxide radicals"">Nitroxide radicals</option><option value="(Oxygen OR 17O)">Oxygen</option><option value="Thulium">Thulium</option></optgroup><optgroup label="Multimodal agents"><option value="((Gadolinium OR Gd3+) AND Optical)">Gadolinium and optical</option><option value="((Gadolinium OR Gd3+) AND (Gold OR Au))">Gadolinium and Gold</option><option value="("Iron oxide" AND (64Cu OR 124I OR 111In))">Iron oxide and
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europium</option><option value="(166Ho OR 67Ga OR 68Ga OR 123I OR 124I OR 125I)">Radionuclides</option></optgroup><optgroup label="Optical agents"><option value="("Fluorescent dyes" OR protein)">Fluorescent dyes or proteins</option><option value=""Luminescent agents"">Luminescent agents</option><option value="(Metals OR Metal OR Gold OR Au)">Metals (Au)</option><option value="Nanotubes">Nanotubes</option><option value=""Quantum dots"">Quantum dots</option></optgroup><optgroup label="PET radionuclides"><option value="("Arsenic 74" OR 74As)">Arsenic-74</option><option value="("Bromine 76" OR 76Br)">Bromine-76</option><option value="("Carbon 11" OR 11C)">Carbon-11</option><option value="(Copper-60 OR Copper-61 OR Copper-62 OR Copper-64 OR 60Cu OR 61Cu OR 62Cu OR 64Cu)">Copper-60, 61, 62, 64</option><option value="("Fluorine 18" OR 18F)">Fluorine-18</option><option value="(Gallium-68 OR 68Ga)">Gallium-68</option><option value="("Iodine 124" OR 124I)">Iodine-124</option><option value="("Nitrogen 13" OR 13N)">Nitrogen-13</option><option value="("Yttrium 86" OR 86Y)">Yttrium-86</option><option value="("Zirconium 89" OR 89Zr)">Zirconium-89</option></optgroup><optgroup label="Photoacoustic agents"><option value="(Gold OR Au)">Gold</option><option value="("Indocyanine green" OR ICG)">Indocyanine green</option></optgroup><optgroup label="SPECT radionuclides"><option value="(Gallium-67 OR 67Ga)">Gallium-67</option><option value="("Indium 111" OR 111In)">Indium-111</option><option value="("Iodine 123" OR "Iodine 125" OR "Iodine 131" OR 123I OR 125I OR 131I)">Iodine-123, 125, 131</option><option value="("Lutetium 177" OR 177Lu)">Lutetium-177</option><option value="(Rhenium OR 186Re OR 188Re)">Rhenium</option><option value="("Technetium 99m" OR 99mTc)">Technetium-99m</option><option value="("Tellurium 125m" OR 125mTe)">Tellurium-125m</option></optgroup><optgroup label="Ultrasound agents"><option value="Microbubbles">Microbubbles</option><option value="Nanobubbles">Nanobubbles</option></optgroup><optgroup label="X-ray and CT agents"><option value="(Bismuth OR Bi)">Bismuth</option><option value="(Gold OR Au)">Gold</option><option value="Iodine">Iodine</option></optgroup></select></div></div><div class="clearfix"><label for="agent">Agent Category:</label><div class="right"><select name="agent" id="agent" style="width:200px"><option value="" selected="selected">Any</option><option value="(antibody OR trastuzumab OR immunoglobulin)">Antibodies</option><option value="(bacteria OR bacteriophage OR coli)">Bacteria</option><option value="cell">Cells</option><option value="(compound OR "amino acid" OR "folic acid" OR "cage molecule" OR carbohydrate OR copolymers OR polymer OR "small molecule" OR macromolecule OR triiodobenzoate OR estradiol OR glycosaminoglycan)">Compounds</option><option value="ligand">Ligands</option><option value="(lipid OR liposome OR liposomes">Lipids</option><option value="metal">Metal</option><option value="(nanoparticle OR nanoparticles OR nanotubes OR "iron oxide")">Nanoparticles</option><option value="(siRNA OR "nucleic acid" OR oligonucleotide)">Nucleic acids</option><option value="peptide">Peptides</option><option value="polyeptide">Polyeptides</option><option value="(protein OR albumin OR chemokin OR immunoprotein OR luciferase OR albumin)">Proteins</option><option value="(virus OR adenovirus)">Viruses</option></select></div></div><div class="clearfix"><label for="target">Target Category:</label><div class="right"><select name="target" id="target" style="width:200px"><option value="" selected="selected">Any</option><option value="acceptor">Acceptors</option><option value=""adhesion molecule"">Adhesion molecules</option><option value="(antigen OR antibody-antigen)">Antigens</option><option value="(enzyme OR enzymes OR enzyme-substrate)">Enzymes</option><option value="(lipids OR lipophilic cation)">Lipids</option><option value="(receptor OR receptors OR receptor-ligand OR receptor-antibody OR antibody-receptor)">Receptors</option><option value="transporter">Transporters</option><option value="non-targeted">Non-targeted</option><option value=""nucleic acid"">Nucleic acids</option><option value="(non-targeted OR "unknown binding site")">Others</option></select></div></div><div><input id="__micad_btn_1" type="radio" name="stage" value="vitro" /><label for="__micad_btn_1"><i>In vitro</i></label><input id="__micad_btn_2" type="radio" name="stage" value="rodents" /><label for="__micad_btn_2">Rodents</label><input id="__micad_btn_3" type="radio" name="stage" value="mammals" /><label for="__micad_btn_3">Non-primate non-rodent mammals</label><br /><input id="__micad_btn_4" type="radio" name="stage" value="primates" /><label for="__micad_btn_4">Non-human primates</label><input id="__micad_btn_5" type="radio" name="stage" value="humans" /><label for="__micad_btn_5">Humans</label><input id="__micad_btn_6" type="radio" name="stage" value="any" checked="checked" /><label for="__micad_btn_6">Any</label></div></form><form xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" name="frmGo" method="get" action="javascript:alert('frmGo:_@action_was_not_set')" id="frmGo"><input name="term" value="." type="hidden" /></form></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Related information</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="discovery_db_links" id="Shutter"></a></div><div class="portlet_content"><ul><li class="brieflinkpopper"><a class="brieflinkpopperctrl" href="/books/?Db=pmc&DbFrom=books&Cmd=Link&LinkName=books_pmc_refs&IdsFromResult=1508776" ref="log$=recordlinks">PMC</a><div class="brieflinkpop offscreen_noflow">PubMed Central citations</div></li><li class="brieflinkpopper"><a class="brieflinkpopperctrl" 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|
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</li>
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<li>
|
||
<a class="text-white" href="https://www.hhs.gov/">HHS</a>
|
||
</li>
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||
<li>
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<a class="text-white" href="https://www.usa.gov/">USA.gov</a>
|
||
</li>
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</ul>
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||
</nav>
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</div>
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||
</div>
|
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</div>
|
||
</section>
|
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<script type="text/javascript" src="/portal/portal3rc.fcgi/rlib/js/InstrumentOmnitureBaseJS/InstrumentNCBIConfigJS/InstrumentNCBIBaseJS/InstrumentPageStarterJS.js?v=1"> </script>
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<script type="text/javascript" src="/portal/portal3rc.fcgi/static/js/hfjs2.js"> </script>
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</div><!-- /.twelve_col -->
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<span class="PAFAppResources"></span>
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|
||
<noscript><img alt="statistics" src="/stat?jsdisabled=true&ncbi_db=books&ncbi_pdid=book-part&ncbi_acc=NBK23721&ncbi_domain=micad&ncbi_report=record&ncbi_type=fulltext&ncbi_objectid=&ncbi_pcid=/NBK23721/&ncbi_pagename=4-[18F]Fluoropaclitaxel - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf&ncbi_bookparttype=chapter&ncbi_app=bookshelf" /></noscript>
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<script type="text/javascript" src="//static.pubmed.gov/portal/portal3rc.fcgi/4216699/js/3879255/4121861/3501987/4008961/3893018/3821238/4062932/4209313/4212053/4076480/3921943/3400083/3426610.js" snapshot="books"></script></body>
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