FAP-Targeted Radionuclide Therapy of Advanced Radioiodine-Refractory Differentiated Thyroid Cancer With Multiple Cycles of 177Lu-FAPI-46

Fu, Hao; Huang, Jinxiong; Sun, Long; Wang, Hua; Chen, Haojun

doi:10.1097/rlu.0000000000004260

Cited by 27 publications

(19 citation statements)

References 8 publications

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“…The third case report described a radioiodine-refractory thyroid cancer patient with no conventional treatment options. The patient was treated with four cycles of in total 22.3 GBq [ 177 Lu]Lu-FAPI-46 [27]. Uptake was observed 72-h post injection on whole-body scintigraphy.…”

Section: Clinical Datamentioning

confidence: 99%

Fibroblast activation protein-targeted radionuclide therapy: background, opportunities, and challenges of first (pre)clinical studies

Privé

Boussihmad

Timmermans

et al. 2023

Eur J Nucl Med Mol Imaging

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Introduction Fibroblast activation protein (FAP) is highly overexpressed in stromal tissue of various cancers. While FAP has been recognized as a potential diagnostic or therapeutic cancer target for decades, the surge of radiolabeled FAP-targeting molecules has the potential to revolutionize its perspective. It is presently hypothesized that FAP targeted radioligand therapy (TRT) may become a novel treatment for various types of cancer. To date, several preclinical and case series have been reported on FAP TRT using varying compounds and showing effective and tolerant results in advanced cancer patients. Here, we review the current (pre)clinical data on FAP TRT and discuss its perspective towards broader clinical implementation. Methods A PubMed search was performed to identify all FAP tracers used for TRT. Both preclinical and clinical studies were included if they reported on dosimetry, treatment response or adverse events. The last search was performed on July 22 2022. In addition, a database search was performed on clinical trial registries (date 15th of July 2022) to search for prospective trials on FAP TRT. Results In total, 35 papers were identified that were related to FAP TRT. This resulted in the inclusion of the following tracers for review: FAPI-04, FAPI-46, FAP-2286, SA.FAP, ND-bisFAPI, PNT6555, TEFAPI-06/07, FAPI-C12/C16, and FSDD. Conclusion To date, data was reported on more than 100 patients that were treated with different FAP targeted radionuclide therapies such as [177Lu]Lu-FAPI-04, [90Y]Y-FAPI-46, [177Lu]Lu-FAP-2286, [177Lu]Lu-DOTA.SA.FAPI and [177Lu]Lu-DOTAGA.(SA.FAPi)2. In these studies, FAP targeted radionuclide therapy has resulted in objective responses in difficult to treat end stage cancer patients with manageable adverse events. Although no prospective data is yet available, these early data encourages further research.

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Section: Clinical Datamentioning

confidence: 99%

Fibroblast activation protein-targeted radionuclide therapy: background, opportunities, and challenges of first (pre)clinical studies

Privé

Boussihmad

Timmermans

et al. 2023

Eur J Nucl Med Mol Imaging

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“…(a) mRAIR‐TC [Reproduced with permission from Ref. [144]. Copyright]; (b) Nasopharyngeal carcinoma [Reproduced with permission from Ref.…”

Section: Conclusion and Prospectsmentioning

confidence: 99%

Clinical applications of fibroblast activation protein‐targeted theranostics in oncologic and nononcologic disease: Current status and future directions

Fu,

Guo,

Huang

et al. 2023

iRADIOLOGY

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Quinoline‐based fibroblast activation protein (FAP) inhibitor (FAPI)‐based positron emission tomography (PET) imaging and radioligand therapy (RLT) are being investigated for use in a wide variety of diseases, and recent results have been promising. This review summarizes the current status of FAPI radiopharmaceuticals in PET imaging of malignant tumors and benign conditions and compares their diagnostic efficacy with 18F‐fluorodeoxyglucose. In addition, we summarize the previously published FAP‐targeted RLT data and discuss its current clinical use and future potential. Our qualitative summary can inform future research directions, medical guidelines, and optimal clinical decision‐making.

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“…PR was documented in four (26.7%), and SD in three patients (20%); the serum Tg level significantly decreased after treatment. Another recent study reported a RAIR-DTC patient received SD after 4 circles of treatments of FAP-targeted radionuclide 177 Lu-FAPI-46 ( 96 ). The results demonstrated that FAPi-based targeted theranostics might provide a novel treatment option for patients with advanced RAIR-DTC.…”

Section: Landscape Of Treatment In Dedifferentiated Thyroid Cancermentioning

confidence: 99%

Towards an era of precise diagnosis and treatment: Role of novel molecular modification-based imaging and therapy for dedifferentiated thyroid cancer

Zhang

Sun

et al. 2022

Front. Endocrinol.

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Dedifferentiated thyroid cancer is the major cause of mortality in thyroid cancer and is difficult to treat. Hence, the essential molecular mechanisms involved in dedifferentiation should be thoroughly investigated. Several studies have explored the biomolecular modifications of dedifferentiated thyroid cancer such as DNA methylation, protein phosphorylation, acetylation, ubiquitination, and glycosylation and the new targets for radiological imaging and therapy in recent years. Novel radionuclide tracers and drugs have shown attractive potential in the early diagnosis and treatment of dedifferentiated thyroid cancer. We summarized the updated molecular mechanisms of dedifferentiation combined with early detection by molecular modification-based imaging to provide more accurate diagnosis and novel therapeutics in the management of dedifferentiated thyroid cancer.

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FAP-Targeted Radionuclide Therapy of Advanced Radioiodine-Refractory Differentiated Thyroid Cancer With Multiple Cycles of 177Lu-FAPI-46

Cited by 27 publications

References 8 publications

Fibroblast activation protein-targeted radionuclide therapy: background, opportunities, and challenges of first (pre)clinical studies

Fibroblast activation protein-targeted radionuclide therapy: background, opportunities, and challenges of first (pre)clinical studies

Clinical applications of fibroblast activation protein‐targeted theranostics in oncologic and nononcologic disease: Current status and future directions

Towards an era of precise diagnosis and treatment: Role of novel molecular modification-based imaging and therapy for dedifferentiated thyroid cancer

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