Safety, Biodistribution, and Dosimetry of 99mTc-HYNIC-Annexin V, a Novel Human Recombinant Annexin V for Human Application

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FIGURE 1.
Conjugate views from whole-body scans of 22-y-old male volunteer. Scans were acquired at about 30 min (A) and 24 h (B) after intravenous injection of 263 MBq of ^99mTc-HYNIC-AnxV. In each pair, anterior view is on left and posterior view is on right.
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FIGURE 2.
Decay-corrected ^99mTc uptake vs. time curves for liver (A), left kidney (B), spleen (C), and total body (D) after intravenous injection of ^99mTc-HYNIC-AnxV. Curves representing mean (thick line) and mean ± 1 SD (thin lines) are shown. For comparison, curves representing average uptake for ^99mTc-i-AnxV (dotted line) and ^99mTc-BTAP-AnxV (dashed line) from previous studies are also shown (9,10).
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FIGURE 3.
Cumulative excreted activity in urine (decay corrected). Curves representing mean (thick line) and mean ± 1 SD (thin lines) are shown.

TABLE 2

Dosimetric Data for Intravenously Administered ^99mTc-HYNIC-AnxV

Site	Uptake* (%ID)	Effective half-life^† (h)	Residence time (h)	Absorbed dose (μGy/MBq)	Absorbed dose, Apomate^‡ (μGy/MBq)	Absorbed dose, ^99mTc-i-AnxV^§ (μGy/MBq)
Kidneys	49.7 ± 8.1^‖	5.9 ± 0.1	3.90 ± 0.63	196 ± 31	63 ± 22	93 ± 24
Liver	13.1 ± 1.0^‖	5.9 ± 0.1	1.03 ± 0.10	16.9 ± 1.3	13 ± 3	17 ± 2
Red bone marrow	9.2 ± 1.8	6.0 ± 0.1	0.78 ± 0.15	8.4 ± 0.9	4.0 ± 0.7	5.5 ± 0.8
Spleen	4.6 ± 1.6	5.7 ± 0.4	0.36 ± 0.13	41 ± 12	15 ± 3	22 ± 6
Testes (n = 6)	0.16 ± 0.04	4.6 ± 0.3	0.014 ± 0.003	5.3 ± 0.9	6.3 ± 1.6	15 ± 3
Thyroid	0.14 ± 0.08	4.4 ± 0.7	0.011 ± 0.005	7.1 ± 3.2	5.6 ± 3.6	10 ± 6
Urinary bladder^¶	—	—	0.15 ± 0.01	7.5 ± 0.4	20 ± 6	7.5 ± 2.6
Remainder	—	—	1.58 ± 0.81	—	—	—
Total body	91.6 ± 1.7	5.5 ± 0.1	7.82 ± 0.08	11.0 ± 0.8^#	7.6 ± 0.5^#	9.7 ± 1.0^#

↵* Uptake values are at 3 h after injection and are corrected for physical decay.
↵^† Results are from a fit with a single exponential.
↵^‡ (10).
↵^§ (9).
↵^‖ Including correction for overlap between right kidney and liver; see text.
↵^¶ Dynamic bladder model (20); 4-h voiding interval; biologic half-life of activity in total body from individual measurements (average, 69 ± 7 h); fraction of activity to urine = 1.0.
↵^# Effective dose (ICRP 60) in μSv/MBq.
Data are mean ± SD (n = 6).