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OtherBASIC SCIENCE INVESTIGATIONS

Pharmacokinetics of [18F]FETNIM: A Potential Hypoxia Marker for PET

Tove Grönroos, Olli Eskola, Kaisa Lehtiö, Heikki Minn, Päivi Marjamäki, Jörgen Bergman, Merja Haaparanta, Sarita Forsback and Olof Solin
Journal of Nuclear Medicine September 2001, 42 (9) 1397-1404;
Tove Grönroos
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Olli Eskola
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Kaisa Lehtiö
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Heikki Minn
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Päivi Marjamäki
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Jörgen Bergman
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Merja Haaparanta
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Sarita Forsback
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Olof Solin
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  • FIGURE 1.
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    FIGURE 1.

    Radiochemical synthesis of [18F]FETNIM from 1-(2′-nitro-1′-imidazolyl)-2,3-O-isopropylidene-4-tosyloxybutane.

  • FIGURE 2.
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    FIGURE 2.

    Typical chromatograms of rat and human tissues as detected by radio-TLC and digital autoradiography. Human plasma sample was analyzed at 30 min after injection of [18F]FETNIM, whereas rat tumor and liver samples were analyzed at 60 min. Radiochromatograms of rat and human plasma were qualitatively and quantitatively similar. arb. = arbitrary.

  • FIGURE 3.
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    FIGURE 3.

    Relationship between percentage of unchanged [18F]FETNIM and uptake in DMBA-induced rat tumors. Poor correlation was observed at early times (A and B), but, at later time, significant inverse correlation was found (C).

Tables

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    TABLE 1

    Biodistribution of [18F]FETNIM in Rats Bearing DMBA-Induced Mammary Tumors

    Tissue15 min (n = 3)30 min (n = 3)60 min (n = 4)120 min (n = 7)240 min (n = 3)
    Blood0.325 ± 0.0560.333 ± 0.0560.206 ± 0.0040.099 ± 0.0240.053 ± 0.009
    Plasma0.313 ± 0.0640.310 ± 0.0470.155 ± 0.015*0.080 ± 0.003†0.030 ± 0.007
    Heart0.338 ± 0.0840.359 ± 0.0570.246 ± 0.0110.134 ± 0.0320.071 ± 0.010
    Lung0.357 ± 0.0560.360 ± 0.0530.246 ± 0.0140.113 ± 0.0280.057 ± 0.008
    Liver0.400 ± 0.1000.478 ± 0.0910.322 ± 0.0110.168 ± 0.0460.142 ± 0.043
    Spleen0.329 ± 0.0880.338 ± 0.0610.213 ± 0.0070.102 ± 0.0230.054 ± 0.010
    Kidney0.737 ± 0.0691.200 ± 0.4500.504 ± 0.0240.397 ± 0.0920.231 ± 0.041
    Bladder2.10 ± 1.701.67 ± 0.890.90 ± 0.290.73 ± 0.71NA
    Urine35 ± 11‡NANA14 ± 5§18 ± 9
    Adrenal gland0.379 ± 0.0740.480 ± 0.1300.386 ± 0.0940.177 ± 0.0540.080 ± 0.002
    Pancreas0.246 ± 0.0970.336 ± 0.0590.186 ± 0.0150.103 ± 0.0220.063 ± 0.012
    Intestine0.330 ± 0.1100.370 ± 0.0650.360 ± 0.1000.230 ± 0.1500.129 ± 0.018
    Stomach0.320 ± 0.1300.328 ± 0.0380.370 ± 0.1800.146 ± 0.036NA
    Fat (subcutaneous)0.045 ± 0.0120.043 ± 0.0150.035 ± 0.0100.013 ± 0.0040.010 ± 0.006
    Muscle0.263 ± 0.0650.345 ± 0.0480.242 ± 0.0090.116 ± 0.0230.061 ± 0.011
    Ovary0.400 ± 0.1200.418 ± 0.0850.255 ± 0.0230.123 ± 0.021NA
    Bone (skull)0.054 ± 0.0160.071 ± 0.0090.058 ± 0.0070.087 ± 0.0520.025 ± 0.003
    Marrow0.480 ± 0.1500.630 ± 0.2700.372 ± 0.0670.119 ± 0.038NA
    Cerebellum0.069 ± 0.0290.103 ± 0.0240.094 ± 0.0160.063 ± 0.0090.045 ± 0.004
    Tumor0.480 ± 0.10*0.383 ± 0.096‡0.239 ± 0.037§0.178 ± 0.046∥0.087 ± 0.043¶
    • ↵* n = 2.

    • ↵† n = 3.

    • ↵‡ n = 5.

    • ↵§ n = 6.

    • ↵∥ n = 23.

    • ↵¶ n = 21.

    • NA = not available.

    • Data are mean ± SD %ID/g.

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    TABLE 2

    Ratios of [18F]FETNIM in Rats Bearing DMBA-Induced Mammary Tumors

    Ratio15 min (n = 3)30 min (n = 3)60 min (n = 4)120 min (n = 7)240 min (n = 3)
    Tumor-to-blood1.49 ± 0.401.15 ± 0.351.16 ± 0.181.79 ± 0.641.65 ± 0.87
    Liver-to-blood1.23 ± 0.371.44 ± 0.371.56 ± 0.061.69 ± 0.622.70 ± 0.94
    Muscle-to-blood0.81 ± 0.241.04 ± 0.231.17 ± 0.051.17 ± 0.371.16 ± 0.30
    Tumor-to-muscle1.84 ± 0.591.11 ± 0.320.99 ± 0.161.53 ± 0.501.42 ± 0.76
    • Data are mean ± SD.

    • View popup
    TABLE 3

    Percentage of Unchanged [18F]FETNIM in Rat Tissues

    Time (min)PlasmaLiverTumor
    %n%n%n
    1572  (66–78)65.01161
    3087  (85–88)31.5  (0.6–2.3)321  (3–45)4
    6084  (83–86)21.5  (0.6–2.3)224  (9–49)3
    12080  (77–84)30.2  (0.0–1.0)423  (6–71)5
    24071  (69–74)21.4  (0.0–2.3)310  (5–14)6
    • Data are mean (range).

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Journal of Nuclear Medicine
Vol. 42, Issue 9
September 1, 2001
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Pharmacokinetics of [18F]FETNIM: A Potential Hypoxia Marker for PET
Tove Grönroos, Olli Eskola, Kaisa Lehtiö, Heikki Minn, Päivi Marjamäki, Jörgen Bergman, Merja Haaparanta, Sarita Forsback, Olof Solin
Journal of Nuclear Medicine Sep 2001, 42 (9) 1397-1404;

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Pharmacokinetics of [18F]FETNIM: A Potential Hypoxia Marker for PET
Tove Grönroos, Olli Eskola, Kaisa Lehtiö, Heikki Minn, Päivi Marjamäki, Jörgen Bergman, Merja Haaparanta, Sarita Forsback, Olof Solin
Journal of Nuclear Medicine Sep 2001, 42 (9) 1397-1404;
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