&lt;SUP&gt;99m&lt;/SUP&gt;Tc-Tetrofosmin for Functional Imaging of P-glycoprotein Modulation In Vivo

Ballinger, J.R.

doi:10.1177/00912700122013246

Cited by 4 publications

(3 citation statements)

References 41 publications

(112 reference statements)

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“…Effects of MDR1 modulators can also be detected by TF [25,28,37]. The behavior of TF is similar to that of MIBI in functional imaging of Pgp modulation in drugresistant human cancer lines [38]. Addition of 1.0 μM PSC833 resulted in a 9-fold-enhanced accumulation in a rat breast carcinoma cell line with Pgp overexpression but no significant change in the wild-type cell line [28].…”

Section: Discussionmentioning

confidence: 99%

Imaging recognition of inhibition of multidrug resistance in human breast cancer xenografts using 99mTc-labeled sestamibi and tetrofosmin

Liu

Stevenson

Barrett

et al. 2005

Nuclear Medicine and Biology

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Background-99m Tc-sestamibi (MIBI) and 99m Tc-tetrofosmin (TF) are avid transport substrates recognized by the multidrug resistance (MDR) P-glycoprotein (Pgp). This study was designed to compare the properties of MIBI and TF in assessing the inhibition of Pgp by PSC833 in severe combined immunodeficient mice bearing MCF7 human breast tumors using SPECT imaging.Methods-Animals with drug-sensitive (MCF/WT) and drug-resistant (MCF7/AdrR) tumors were treated by PSC833 and by carrier vehicle 1 h before imaging, respectively. Dynamic images were acquired for 30 min after intravenous injection of MIBI/TF using a SPECT system, FastSPECT. The biodistribution of MIBI and TF was determined at the end of the imaging session.Results-MCF7/WT in the absence and presence of PSC833 could be visualized by MIBI and TF imaging within 5 min and remained detectable for 30 min postinjection. MCF7/AdrR could be visualized only 2-5 min without PSC833 treatment but could be detected for 30 min with PSC833, very similar to MCF7/WT. MCF7/AdrR without PSC833 showed significantly greater radioactive washout than MCF7/WT and MCF7/AdrR with PSC833 treatment. PSC833 increased the accumulation (%ID/g) in MCF7/AdrR 3.0-fold (1.62 ± 0.15 vs. 0.55 ± 0.05, P <.05) for TF and 1.9-fold (1.21 ± 0.04 vs. 0.64 ± 0.05, P <.05) for MIBI but did not affect MCF7/WT.Conclusions-The feasibility of MIBI and TF for assessment of MDR expression and inhibition was demonstrated in mice through FastSPECT imaging. The results indicate that TF may be at least comparable with MIBI in recognizing Pgp expression and modulation.

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Section: Discussionmentioning

confidence: 99%

Imaging recognition of inhibition of multidrug resistance in human breast cancer xenografts using 99mTc-labeled sestamibi and tetrofosmin

Liu

Stevenson

Barrett

et al. 2005

Nuclear Medicine and Biology

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“…The properties of tetrofosmin are similar but not identical to those of MIBI. The available data suggest that clinical studies involving imaging of MDR function and in vivo modulation of MDR function can be performed with both tetrofosmin and MIBI, but the 2 should probably not be used interchangeably [ 18 ] . Recent experiments with the positron-emitter [ 94m Tc]MIBI parallel previous studies with [ 99m Tc]MIBI, showing essentially identical performance and thereby providing biological validation for the use of micro-positron emission tomography (PET) [ 19 ] .…”

Section: In Vivo Imaging Of Abc Transporters In Multidrug Resistancementioning

confidence: 99%

Imaging of multidrug resistance in cancer

Dizdarevic

Peters

2011

Cancer Imaging

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Primary intrinsic and/or acquired multidrug resistance (MDR) is the main obstacle to successful cancer treatment. Functional molecular imaging of MDR in cancer using single photon or positron emitters may be helpful to identify multidrug-resistant tumours and predict not only those patients who are resistant to treatment, with a clinically unfavourable prognosis, but also those who are susceptible to the development of drug toxicity or even certain tumours . Variations in the mdr1 gene product may directly affect the therapeutic effectiveness, and single nucleotide polymorphisms for the mdr1 gene may be associated with altered oral bioavailability of MDR1 substrates, drug resistance, and a susceptibility to some human diseases. The challenge of translating the concept of MDR modulation in vivo involves a complex cellular interplay between both malignant and normal cells. Integration and correlation of functional single photon emission tomography or positron emission tomography imaging findings with mdr1 genotype and clinical data may contribute to efficient management by selecting cancer patients with the appropriate molecular phenotype for maximal individual therapeutic benefit, as well as those who are non-responders. This review describes a role for functional imaging of classical mechanisms of MDR with an emphasis on readily available [99mTc]MIBI scintigraphy. MIBI scintigraphy has been shown to be a non-invasive cost-effective in vivo assay of ATP-binding cassette transporters associated with MDR in cancer, including P-glycoprotein, multidrug-resistant protein 1 and breast cancer resistant protein. New imaging agents for molecular targets such as vascular endothelial growth factor and HER2 receptors, may potentially be combined with MDR imaging substrates to more accurately predict the therapeutic response to anticancer drugs, guiding individualised treatment while minimising the economic health costs of ineffective therapy in an era of personalised medicine.

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“…Moreover, it is notable that resistance to chemotherapy is more commonly encountered in lung cancers of smokers compared with nonsmokers (79 vs. 50% according to Volm et al [7]), and that 58% of the malignant tissue from smokers displayed immunohistochemical expression of P-gp compared with only 9% of the malignant tissue from nonsmokers [7]. 99m Tc-tetrofosmin is also a substrate for P-gp [18,19]. We reasoned, therefore, that if P-gp was involved in 99m Tc-sestamibi clearance from the lung, then the clearance kinetics from the lungs following inhalation of 99m Tc-tetrofosmin would be similar to those of 99m Tcsestamibi.…”

Section: Introductionmentioning

confidence: 99%

Does P-glycoprotein have a role in the lung clearances of inhaled 99mTc-sestamibi and 99mTc-tetrofosmin?

Cheow¹,

Ruparelia²,

Shankar

et al. 2009

Nuclear Medicine Communications

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<SUP>99m</SUP>Tc-Tetrofosmin for Functional Imaging of P-glycoprotein Modulation In Vivo

Cited by 4 publications

References 41 publications

Imaging recognition of inhibition of multidrug resistance in human breast cancer xenografts using 99mTc-labeled sestamibi and tetrofosmin

Imaging recognition of inhibition of multidrug resistance in human breast cancer xenografts using 99mTc-labeled sestamibi and tetrofosmin

Imaging of multidrug resistance in cancer

Does P-glycoprotein have a role in the lung clearances of inhaled 99mTc-sestamibi and 99mTc-tetrofosmin?

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