Targeting of the cholecystokinin-2 receptor with the minigastrin analog 177Lu-DOTA-PP-F11N: does the use of protease inhibitors further improve in vivo distribution?

AW Sauter, R Mansi, U Hassiepen… - Journal of Nuclear …, 2019 - Soc Nuclear Med
Patients with metastatic medullary thyroid cancer (MTC) have limited systemic treatment
options. The use of radiolabeled gastrin analogs targeting the cholecystokinin-2 receptor …

Cholecystokinin 2 receptor agonist 177Lu-PP-F11N for radionuclide therapy of medullary thyroid carcinoma: Results of the lumed phase 0a study

C Rottenburger, GP Nicolas, L McDougall… - Journal of nuclear …, 2020 - Soc Nuclear Med
Treatment of patients with advanced medullary thyroid carcinoma (MTC) is still a challenge.
For more than 2 decades, it has been known that the cholecystokinin 2 receptor is a …

[HTML][HTML] From preclinical development to clinical application: Kit formulation for radiolabelling the minigastrin analogue CP04 with In-111 for a first-in-human clinical …

D Pawlak, C Rangger, PK Peitl, P Garnuszek… - European Journal of …, 2016 - Elsevier
Introduction A variety of radiolabelled minigastrin analogues targeting the cholecystokinin 2
(CCK2) receptor were developed and compared in a concerted preclinical testing to select …

DOTA-MGS5, a new cholecystokinin-2 receptor-targeting peptide analog with an optimized targeting profile for theranostic use

M Klingler, D Summer, C Rangger… - Journal of Nuclear …, 2019 - Soc Nuclear Med
Molecular imaging and targeted radiotherapy with radiolabeled cholecystokinin-2 receptor
(CCK2R) targeting peptide probes holds high promise to improve the clinical management …

Preliminary clinical experience with cholecystokinin-2 receptor PET/CT using the 68Ga-labeled minigastrin analog DOTA-MGS5 in patients with medullary thyroid …

E von Guggenberg, C Uprimny, M Klinger… - Journal of Nuclear …, 2023 - Soc Nuclear Med
PET/CT with the new 68Ga-labeled minigastrin analog DOTA-dGlu-Ala-Tyr-Gly-Trp-(N-Me)
Nle-Asp-1-Nal-NH2 (68Ga-DOTA-MGS5) was performed on patients with advanced …

[HTML][HTML] Initial in vitro and in vivo evaluation of a novel CCK2R targeting peptide analog labeled with lutetium-177

AA Hörmann, M Klingler, M Rezaeianpour, N Hörmann… - Molecules, 2020 - mdpi.com
Targeting of cholecystokinin-2 receptor (CCK2R) expressing tumors using radiolabeled
minigastrin (MG) analogs is hampered by rapid digestion of the linear peptide in vivo. In this …

[HTML][HTML] Site-specific stabilization of minigastrin analogs against enzymatic degradation for enhanced cholecystokinin-2 receptor targeting

M Klingler, C Decristoforo, C Rangger, D Summer… - Theranostics, 2018 - ncbi.nlm.nih.gov
Minigastrin (MG) analogs show high affinity to the cholecystokinin-2 receptor (CCK2R) and
have therefore been intensively studied to find a suitable analog for imaging and treatment …

[HTML][HTML] [111In]In-CP04 as a novel cholecystokinin-2 receptor ligand with theranostic potential in patients with progressive or metastatic medullary thyroid cancer: final …

L Lezaic, PA Erba, C Decristoforo, K Zaletel… - European Journal of …, 2023 - Springer
Introduction Medullary thyroid cancer (MTC) is a rare malignant tumour of the parafollicular
C-cells with an unpredictable clinical course and currently suboptimal diagnostic and …

[HTML][HTML] Preclinical pharmacokinetics, biodistribution, radiation dosimetry and toxicity studies required for regulatory approval of a phase I clinical trial with 111In-CP04 …

T Maina, MW Konijnenberg, P KolencPeitl… - European Journal of …, 2016 - Elsevier
Introduction From a series of radiolabelled cholecystokinin (CCK) and gastrin analogues,
111 In-CP04 (111 In-DOTA-(DGlu) 6-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH 2) was selected for …

[HTML][HTML] Pharmacological inhibition of mTORC1 increases CCKBR-specific tumor uptake of radiolabeled minigastrin analogue [177Lu] Lu-PP-F11N

M Grzmil, Y Qin, C Schleuniger, S Frank… - Theranostics, 2020 - ncbi.nlm.nih.gov
Rationale: A high tumor-to-healthy-tissue uptake ratio of radiolabeled ligands is an essential
prerequisite for safe and effective peptide receptor radionuclide therapy (PRRT). In the …