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British Journal of Radiology (2003) 76, 553-560
© 2003 British Institute of Radiology
doi: 10.1259/bjr/30385847

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Comparison between human pharmacokinetics and imaging properties of two conjugation methods for 99mTc-Annexin A5

H H Boersma, PharmD 1,2 I H Liem, MD 1 G J Kemerink, PhD 1 P W L Thimister, MD, PhD 1 L Hofstra, MD, PhD 3 L M L Stolk, PharmD, PhD 2 W L van Heerde, PhD 4 M-T W Pakbiers, BSc 2 D Janssen, BSc 1 A J Beysens, PharmD 2 C P M Reutelingsperger, PhD 5 and G A K Heidendal, MD, PhD 1

Departments of 1 Nuclear Medicine, 2 Clinical Pharmacy and Toxicology and 3 Cardiology, University Hospital Maastricht, P.O. Box 5800, NL-6202 AZ Maastricht, 4 Central Hematology Laboratory, University Medical Center St. Radboud, P.O. Box 9201, 6500 HB Nijmegen and 5 Department of Biochemistry, Cardiovascular Research Institute, University of Maastricht, P.O. Box 616, NL-6200 MD Maastricht, The Netherlands



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Figure 1. Concentration-time curves of I-AnxA5 ({blacklozenge}) and B-AnxA5 ({blacksquare}) of (a) 99mTc-radioactivity in plasma and (b) AnxA5 concentration in plasma. For I-AnxA5, data for 8 individuals are presented, whereas for B-AnxA5 values for 10 (radioactivity) and 12 (plasma concentration AnxA5) patients are given. Radioactivity data were normalized with the administered activity by dividing the obtained plasma radioactivity levels by the administered dose in GBq. All values are depicted as means±standard deviation.

 


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Figure 2. Views of whole-body scan of a male volunteer (35 years, left) and a male patient (53 years, right), taken between 4 h and 5 h after administration of 440 MBq I-AnxA5 and 566 MBq B-AnxA5, respectively. A, anterior view; P, posterior view.

 


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Figure 3. Decay corrected 99mTc-uptake in the total body after (a) injection of I-AnxA5 and (b) B-AnxA5, obtained with the gamma-camera. Curves with mean and (mean±1 standard deviation) are shown. ID, injected dose.

 


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Figure 4. Transverse tomographic image obtained with I-AnxA5 in a patient suffering from acute anteroseptal myocardial infarction. The arrow indicates increased I-AnxA5 uptake in the anteroseptal region 22 h after reperfusion.

 


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Figure 5. Planar images of a patient with leg sarcoma, 16 h after the injection of B-AnxA5. There is increased uptake of B-AnxA5 in a major part of the upper right leg, with a central zone of decreased activity. Almost no uptake is seen in the left leg.

 


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Figure 6. SPECT (5 h post injection of B-AnxA5) images of a patient with mastitis carcinomatosa. The increased uptake, of B-AnxA5, indicated by arrows, can be seen in the anterior part of the left mamma.

 


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Figure 7. Coronal SPECT image of a patient with non-Hodgkin's lymphoma. Increased B-AnxA5 accumulation is seen in the neck region, corresponding to a large mass on a CT image.

 





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