Table 1 Characteristics of 166Ho-EDTMP and 166Ho-DOTMP. The results are expressed as the means ± standard deviations; n = 3 for each experimental point (M/M: molar/molar ratio, mbq: Megabecquerel, RCP: radiochemical purity, SA: specific activity). (a) 166Ho3+ (mmol) = calculated as ~ 200 Mg Ho2O3 × 87.28% (Ho3+ in Ho2O3)/164.9 g.mol, divided by 4 (volume of 166Ho3+ solution, 4 mL) = 0.264 mM (b) concentration: determined as the activity of 166HoCl3 (MBq)/mL (collected range: 74,275–82,880 MBq/4.0 mL). *Radiochemical purity of 166Ho-EDTMP/166Ho-DOTMP was determined by a PC (using 20 × 200 mm strips). **Specific activity (MBq/mg) of 166Ho: calculated as 166Ho activity/200 Mg 165Ho2O3 × 0.8728 Ho3+ content) = 451.44 ± 33.53. **Specific activity (MBq/mg) of 166Ho-EDTMP: Range = 8.11–9.00. **Specific activity (MBq/mg) of 166Ho-DOTMP: Range = 4.30–4.77. #166Ho/EDTMP molar ratio: calculated as = 0.0132 mmol Ho3+/0.264 mmol EDTMP × 99.10% (efficiency) = 0.0495. #166Ho/DOTMP molar ratio: calculated as 0.0132 mmol Ho3+/0.264 mmol DOTMP × 99.35% (efficiency) = 0.0331. The stability of 166Ho-EDTMP and 166DOTMP was evaluated under various conditions (Fig. S1a,b). A radiochemical purity exceeding 95% was observed at 4 °C and 24 °C in 0.9% NaCl and 0.2 M PBS and at 37 °C in 0.05% HSA after 3 days of storage.

From: Acute radiotoxicity studies and safety assessment of 166Ho-EDTMP and 166Ho-DOTMP for the palliative treatment of bone metastases

Agents

mMa (M/M)

Conc.b (MBq/mL)

RCP* (%)

SA** (MBq/mg)

166Ho/Ligand#

Stability

(%)

166HoCl3

0.264

19,701 ± 1,442

99.62 ± 0.34

451.44 ± 33.53

-

> 99.9

166Ho-EDTMP

20:1

372.3 ± 2.3

99.10 ± 0.55

8.55 ± 0.62

0.0495

> 95.0

166Ho-DOTMP

30:1

374.6 ± 3.7

99.35 ± 0.35

4.53 ± 0.33

0.0331

> 96.0