Table 1.

Pharmacokinetics of [⁶⁸Ga]Ga-DK223 in mice with MDAMB231 xenografts and predicted residence times in human organs with respective absorbed doses.

	%ID/g [68Ga]Ga-DK223 time (minutes)
Tissues	5	30	60	60 (block)	90	180	Residence time (h)	Organ dose (rem/mCi)
Blood	28.67 ± 8.65	7.63 ± 0.87	3.05 ± 0.11	1.09 ± 0.18	2.14 ± 0.08	1.72 ± 0.04	0.17533	n/a
Muscle	2.29 ± 0.09	0.85 ± 0.09	0.36 ± 0.04	0.85 ± 0.07	0.17 ± 0.01	0.08 ± 0.02	0.06168	0.0083
Tumor	8.62 ± 0.29	14.26 ± 1.54	15.21 ± 1.43	0.04 ± 0.01	12.15 ± 0.32	11.59 ± 0.79	n/a	n/a
Lung	14.83 ± 0.4	11.03 ± 2.29	4.7 ± 0.42	0.57 ± 0.1	5.3 ± 1.68	2.98 ± 0.71	0.03245	0.0705
Thymus	9.96 ± 0.82	7.02 ± 1.06	3.53 ± 0.27	2.76 ± 0.16	1.26 ± 0.47	1.52 ± 0.75	0.00047	0.0434
Heart	6.39 ± 0.35	2.49 ± 0.3	0.95 ± 0.07	2.42 ± 0.4	0.73 ± 0.03	0.46 ± 0.03	0.0151	0.0558
Liver	5.63 ± 0.29	2.85 ± 0.41	1.31 ± 0.08	0.99 ± 0.14	0.91 ± 0.11	0.82 ± 0.09	0.01633	0.0252
Stomach (with contents)	2.2 ± 0.16	1.39 ± 0.31	0.65 ± 0.09	0.35 ± 0.07	0.46 ± 0.09	0.37 ± 0.04	0.00072	0.0061
Pancreas	3.04 ± 0.11	2.01 ± 0.54	0.45 ± 0.05	0.41 ± 0.02	0.39 ± 0.01	0.24 ± 0.03	0.00052	0.015
Spleen	3.69 ± 0.13	2.45 ± 0.51	1.05 ± 0.07	0.91 ± 0.07	0.71 ± 0.06	0.58 ± 0.03	0.00129	0.0196
Small intestine (with contents)	3.41 ± 0.37	1.64 ± 0.32	0.65 ± 0.2	0.44 ± 0.04	0.96 ± 0.09	0.74 ± 0.17	0.00453	0.013
Large intestine (with contents)	2.01 ± 0.16	0.79 ± 0.1	0.52 ± 0.09	0.29 ± 0.06	0.42 ± 0.1	1.74 ± 0.37	0.00099	0.0084
Adrenals	4.18 ± 0.26	2.22 ± 0.19	4.74 ± 3.64	1.32 ± 0.09	0.18 ± 0.03	0.16 ± 0.11	0.00014	0.0181
Kidney	28.59 ± 2.4	24.4 ± 1.5	22.99 ± 2.01	26.34 ± 0.19	16.23 ± 0.8	19.14 ± 1.32	0.0337	0.21
Ovaries	6.1 ± 0.55	2.69 ± 0.34	0.93 ± 0.08	2.92 ± 0.79	0.47 ± 0.09	0.27 ± 0.18	0.00011	0.017
Uterus	7.48 ± 1.37	3.82 ± 0.57	1.52 ± 0.26	1.03 ± 0.06	1.13 ± 0.09	0.47 ± 0.03	0.00114	0.0253
Bladder	5.74 ± 0.71	4.09 ± 0.49	1.42 ± 0.12	2.69 ± 1.82	0.78 ± 0.07	1.28 ± 0.32	0.00187	0.0081
Femur	10.58 ± 5.79	1.74 ± 0.14	0.89 ± 0.06	0.34 ± 0.03	0.59 ± 0.04	0.64 ± 0.07	0.03956	0.0333
Brain	0.65 ± 0.08	0.22 ± 0.05	0.08 ± 0.01	0.44 ± 0.09	0.05 ± 0.01	0.04 ± 0.01	0.00118	0.0029

Note: Ex vivo biodistribution studies in NSG mice bearing MDAMB231 tumors. Mice were injected with ∼740 kBq (∼50 μCi) [⁶⁸Ga]Ga-DK223 and sacrificed after corresponding time point (n = 4–5). Blocking was performed by treating mice with nonradioactive 50 μg DK223. Residence time and equivalent human organ dose was calculated using OLINDA/XEM software.