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. Author manuscript; available in PMC: 2020 Dec 17.
Published in final edited form as: Curr Med Chem. 2020 Jan 1;27(41):7112–7132. doi: 10.2174/0929867327666200625143035

Table 3. Clinical studies with radiolabeled CCK2R targeting peptide derivatives in patients with MTC or other CCK2R expressing tumors.

Peptide derivative Radionuclide Radiopeptide Injected activity (MBq) Injected peptide amount (µg) Tumor type Number of patients Reference
gastrin-I iodine-131 131I-gastrin-I 370 0.5/kg BW metastatic MTC 1 [34,43]
[DTPA0]minigastrin indium-111 111In-DTPA-MG 130-170 0.5/kg BW metastatic MTC occult MTC 2
1		 [43,75]
[DTPA0,DAsp1,Nle 3,6]CCK8 indium-111 111In-DTPA-CCK 158-211 7.2-8.5
1 x 18.7		 metastatic MTC occult MTC 2
5		 [37,76]
[DTPA0DGlu1minigastrin indium-111 111In-DTPA-MG0 185-259 5-10 metastatic MTC occult MTC metastatic carinoid astrocytoma (grade III) 23
22
1
1		 [77,78]
150-200 5.5-7.3 metastatic MTC occult MTC 22
5		 [79]
150-200 5.5-7.3 neuroendocrine tumors 61 [80]
yttrium-90 90Y-DTPA-MG0 1110-1850* Not stated advanced metastatic MTC 8 [77,78,81]
[DTPA0,DAsp1,Nle3,6]CCK8
[DOTA0,DGlu1,DesGlu2-6]minigastrin
[N4-Gly0,DGlu1]minigastrin		 indium-111
indium-111
technetium-99m		 111In-DOTA-CCK
111In-DOTA-MG11
99mTc-Demogastrin-2		 216±19
186±34
773±97		 11.1±0.6
10.8±1.7
9.5±1.5		 metastatic MTC 6 [82]
[HYNIC0,DGlu1,DesGlu2-6]minigastrin technetium-99m 99mTc-HYNIC-MG11 500-700 7-9 presurgical MTC
postsurgical MTC		 7
23		 [83,84]
[DOTA0,DGln1-6]minigastrin gallium-68 68Ga-DOTA-PP-F10 347 MBq ~20 metastatic MTC 1 [58]
[DOTA0,DGlu1-6]minigastrin gallium-68 68Ga-DOTA-PP-F11 Not stated Not stated presurgical MTC 1 [85]
[DOTA0,DGlu1-6]minigastrin indium-111 111In-DOTA-PP-F11 200±20 10 or 50 advanced MTC 6 [86]
[DOTA0,DGlu1-6,Nle11]minigastrin lutetium-177 177Lu-DOTA-PP-F11N 1000§ <100 histologically proven MTC 16 [87]
*

Up to 4 injections in intervals of 4-6 weeks (MBq/m2);

§

two injections with/without Gelofusine within 4 weeks