The purpose of this study is to determine the use of 177Lu-PP-F11N for imaging and therapy of patients with advanced medullary thyroid carcinoma (MTC). 177Lu-PP-F11N is a gastrin analogon, binding to cholecystokinin-2 receptors. This receptors show an overexpression on more than 90 % of medullary thyroid carcinomas.

Start Date13 Dec 2018

Sponsor / Collaborator

Universitätsspital Basel

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100 Clinical Results associated with 177Lu-PP-F11N

100 Translational Medicine associated with 177Lu-PP-F11N

100 Patents (Medical) associated with 177Lu-PP-F11N

Literatures (Medical) associated with 177Lu-PP-F11N

01 Apr 2020·Journal of Nuclear MedicineQ1 · MEDICINE

Cholecystokinin 2 Receptor Agonist ¹⁷⁷Lu-PP-F11N for Radionuclide Therapy of Medullary Thyroid Carcinoma: Results of the Lumed Phase 0a Study

Q1 · MEDICINE

Article

Author: Geistlich, Susanne ; Schibli, Roger ; Kaul, Felix ; McDougall, Lisa ; Nicolas, Guillaume P ; Schumann, Anne ; Glatz, Katharina ; Cachovan, Michal ; Behe, Martin ; Vija, A Hans ; Rau, Tilman ; Rottenburger, Christof ; Christ, Emanuel R ; Wild, Damian

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 promising target for the treatment of MTC with radiolabeled minigastrin analogs. Unfortunately, kidney toxicity has precluded their therapeutic application so far. In 6 consecutive patients, we evaluated with advanced 3-dimensional dosimetry whether improved minigastrin analog ¹⁷⁷Lu-DOTA-(d-Glu)₆-Ala-Tyr-Gly-Trp-Nle-Asp-PheNH₂ (¹⁷⁷Lu-PP-F11N) is a suitable agent for the treatment of MTC. Methods: Patients received 2 injections of about 1 GBq (∼80 μg) of ¹⁷⁷Lu-PP-F11N with and without a solution of succinylated gelatin (SG, a plasma expander used for nephroprotection) in a random crossover sequence to evaluate biodistribution, pharmacokinetics, and tumor and organ dosimetry. An electrocardiogram was obtained and blood count and blood chemistry were measured up to 12 wk after the administration of ¹⁷⁷Lu-PP-F11N to assess safety. Results: In all patients, ¹⁷⁷Lu-PP-F11N accumulation was visible in tumor tissue, stomach, and kidneys. Altogether, 13 tumors were eligible for dosimetry. The median absorbed doses for tumors, stomach, kidneys, and bone marrow were 0.88 (interquartile range [IQR]: 0.85-1.04), 0.42 (IQR: 0.25-1.01), 0.11 (IQR: 0.07-0.13), and 0.028 (IQR: 0.026-0.034) Gy/GBq, respectively. These doses resulted in median tumor-to-kidney dose ratios of 11.6 (IQR: 8.11-14.4) without SG and 13.0 (IQR: 10.2-18.6) with SG; these values were not significantly different (P = 1.0). The median tumor-to-stomach dose ratio was 3.34 (IQR: 1.14-4.70). Adverse reactions (mainly hypotension, flushing, and hypokalemia) were self-limiting and not higher than grade 1. Conclusion: ¹⁷⁷Lu-PP-F11N accumulates specifically in MTC at a dose that is sufficient for a therapeutic approach. With a low kidney and bone marrow radiation dose, ¹⁷⁷Lu-PP-F11N shows a promising biodistribution. The dose-limiting organ is most likely the stomach. Further clinical studies are necessary to evaluate the maximum tolerated dose and the efficacy of ¹⁷⁷Lu-PP-F11N.

100 Deals associated with 177Lu-PP-F11N

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Thyroid Cancer, Medullary	Phase 1	-	Universitätsspital Basel	-
Thyroid cancer metastatic	Preclinical	CH	Universitätsspital Basel	13 Dec 2018

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


SNMMI2019	Not Applicable	Thyroid Cancer, Medullary	-	177Lu-PP-F11N with Physiogel	rbmkymusbu(tsfdjjmlyd) = Adverse reactions (mainly hypotension, flushing and hypokalemia) were self-limiting and not higher than grade 1 ngnemaocqj (iqkwdljysi ) View more	-	21 May 2019
				177Lu-PP-F11N without Physiogel

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