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<script type="text/javascript" src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.boots.min.js"> </script><title>4-[18F]Fluoropaclitaxel - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf</title>
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<meta name="citation_inbook_title" content="Molecular Imaging and Contrast Agent Database (MICAD) [Internet]">
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<meta name="citation_title" content="4-[18F]Fluoropaclitaxel">
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<meta name="citation_date" content="2012/02/14">
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<meta name="citation_author" content="Kam Leung">
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<meta name="DC.Title" content="4-[18F]Fluoropaclitaxel">
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<meta name="og: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). 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 (3). 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 (4, 5). 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 (6, 7).">
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yet</button><a id="jr-fip-next" class="wsprkl btn" title="Jump to next match">▶</a></nav></nav></div><div id="jr-epub-interstitial" class="hidden"></div><div id="jr-content"><article data-type="main"><div class="main-content lit-style" itemscope="itemscope" itemtype="http://schema.org/CreativeWork"><div class="meta-content fm-sec"><div class="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="contribs">Leung K.</p><p class="fm-aai"><a href="#_NBK23721_pubdet_">Publication Details</a></p></div></div><div class="jig-ncbiinpagenav body-content whole_rhythm" data-jigconfig="allHeadingLevels: ['h2'],smoothScroll: false" itemprop="text"><div class="iconblock whole_rhythm clearfix ten_col table-wrap" id="figFPAC18FTncchemicalname418ffluoropacl"><a href="/books/NBK23721/table/FPAC18F.T.nc_chemical_name418ffluoropacl/?report=objectonly" target="object" title="Table" class="img_link icnblk_img figpopup" rid-figpopup="figFPAC18FTncchemicalname418ffluoropacl" rid-ob="figobFPAC18FTncchemicalname418ffluoropacl"><img class="small-thumb" src="/books/NBK23721/table/FPAC18F.T.nc_chemical_name418ffluoropacl/?report=thumb" src-large="/books/NBK23721/table/FPAC18F.T.nc_chemical_name418ffluoropacl/?report=previmg" alt="Image " /></a><div class="icnblk_cntnt"><h4 id="FPAC18F.T.nc_chemical_name418ffluoropacl"><a href="/books/NBK23721/table/FPAC18F.T.nc_chemical_name418ffluoropacl/?report=objectonly" target="object" rid-ob="figobFPAC18FTncchemicalname418ffluoropacl">Table</a></h4><p class="float-caption no_bottom_margin">
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<i>In vitro</i>
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Rodents
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</p></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="bibr" href="#FPAC18F.REF.1" rid="FPAC18F.REF.1 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="bibr" href="#FPAC18F.REF.3" rid="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="bibr" href="#FPAC18F.REF.4" rid="FPAC18F.REF.4 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="bibr" href="#FPAC18F.REF.6" rid="FPAC18F.REF.6 FPAC18F.REF.7">6, 7</a>).</p><p>Sestamibi (MIBI) is a substrate for P-gp. <a href="/books/n/micad/MIBI99mtc/?report=reader"><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="bibr" href="#FPAC18F.REF.8" rid="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="bibr" href="#FPAC18F.REF.8" rid="FPAC18F.REF.8 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="bibr" href="#FPAC18F.REF.10" rid="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="bibr" href="#FPAC18F.REF.10" rid="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="bibr" href="#FPAC18F.REF.10" rid="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="bibr" href="#FPAC18F.REF.10" rid="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="bibr" href="#FPAC18F.REF.11" rid="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="bibr" href="#FPAC18F.REF.12" rid="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="bibr" href="#FPAC18F.REF.12" rid="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="bibr" href="#FPAC18F.REF.12" rid="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="bibr" href="#FPAC18F.REF.13" rid="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"><dl class="bkr_refwrap"><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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<em>Biochemistry of multidrug resistance mediated by the multidrug transporter.</em>
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<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></dl><dl class="bkr_refwrap"><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>
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<em>Characterization of multidrug resistance P-glycoprotein transport function with an organotechnetium cation.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues.</em>
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<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></dl><dl class="bkr_refwrap"><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></dl><dl class="bkr_refwrap"><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></dl><dl class="bkr_refwrap"><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></dl><dl class="bkr_refwrap"><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></dl><dl class="bkr_refwrap"><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></dl><dl class="bkr_refwrap"><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></dl><dl class="bkr_refwrap"><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></dl><dl class="bkr_refwrap"><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>
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<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></dl></div><div id="bk_toc_contnr"></div></div></div><div class="fm-sec"><h2 id="_NBK23721_pubdet_">Publication Details</h2><h3>Author Information and Affiliations</h3><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><h3>Publication History</h3><p class="small">Created: <span itemprop="datePublished">January 2, 2006</span>; Last Update: <span itemprop="dateModified">February 14, 2012</span>.</p><h3>Copyright</h3><div><div class="half_rhythm"><a href="/books/about/copyright/">Copyright Notice</a></div></div><h3>Publisher</h3><p><a href="http://www.ncbi.nlm.nih.gov/" ref="pagearea=page-banner&targetsite=external&targetcat=link&targettype=publisher">National Center for Biotechnology Information (US)</a>, Bethesda (MD)</p><h3>NLM Citation</h3><p>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></p></div><div class="small-screen-prev"><a href="/books/n/micad/FITM-18F/?report=reader"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><path d="M75,30 c-80,60 -80,0 0,60 c-30,-60 -30,0 0,-60"></path><text x="20" y="28" textLength="60" style="font-size:25px">Prev</text></svg></a></div><div class="small-screen-next"><a href="/books/n/micad/NS10743-18F/?report=reader"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><path d="M25,30c80,60 80,0 0,60 c30,-60 30,0 0,-60"></path><text x="20" y="28" textLength="60" style="font-size:25px">Next</text></svg></a></div></article><article data-type="table-wrap" id="figobFPAC18FTncchemicalname418ffluoropacl"><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></article></div><div id="jr-scripts"><script src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/libs.min.js"> </script><script src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.min.js"> </script></div></div>
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