Systemic Radioligand Therapy with
            <sup>177</sup>
            Lu Labeled Prostate Specific Membrane Antigen Ligand for Imaging and Therapy in Patients with Metastatic Castration Resistant Prostate Cancer

Heck, Matthias; Retz, Margitta; D’Alessandria, Calogero; Rauscher, Isabel; Scheidhauer, Klemens; Maurer, Tobias; Storz, Enno; Janssen, F.; Schottelius, Margret; Wester, Hans‐Jürgen; Gschwend, Jürgen E.; Schwaiger, Markus; Tauber, Robert; Eiber, Matthias

doi:10.1016/j.juro.2016.02.2969

Cited by 174 publications

(149 citation statements)

References 21 publications

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“…In an initial study in mice, it has a highly efficient internalisation into prostate cancer cells with approximately 75% of the peptide bound to the cell internalised after 3 h of incubation 22. A similar small molecule PSMA peptide ending with a different chemical conjugation ( 177 Lu PSMA‐I&T) also appears effective as a therapeutic agent in a number of published studies 3, 2118, 23 …”

Section: Labelling Of Lu 177 With Psma Peptides: Different Available mentioning

confidence: 99%

Lutetium ¹⁷⁷ PSMA radionuclide therapy for men with prostate cancer: a review of the current literature and discussion of practical aspects of therapy

Emmett

Willowson

Violet

et al. 2017

J of Medical Radiation Sci

247

233

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Prostate‐specific membrane antigen (PSMA) is a receptor on the surface of prostate cancer cells that is revolutionising the way we image and treat men with prostate cancer. New small molecule peptides with high‐binding affinity for the PSMA receptor have allowed high quality, highly specific PET imaging, in addition to the development of targeted radionuclide therapy for men with prostate cancer. This targeted therapy for prostate cancer has, to date, predominately used Lutetium 177 (Lu) labelled PSMA peptides. Early clinical studies evaluating the safety and efficacy of Lu PSMA therapy have demonstrated promising results with a significant proportion of men with metastatic prostate cancer, who have already failed other therapies, responding clinically to Lu PSMA. This review discusses the practical issues of administering Lu PSMA, and gives an overview of the findings from currently published trials in regards to treatment response rates, expected toxicities and safety.

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Section: Labelling Of Lu 177 With Psma Peptides: Different Available mentioning

confidence: 99%

Lutetium ¹⁷⁷ PSMA radionuclide therapy for men with prostate cancer: a review of the current literature and discussion of practical aspects of therapy

Emmett

Willowson

Violet

et al. 2017

J of Medical Radiation Sci

247

233

View full text Add to dashboard Cite

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“…PSMA ligand PET/CT has an evolving role in PSMA-targeting treatments (e.g., radioligand therapy), evaluating target expression and therefore potentially predicting response (62)(63)(64). A rare but potential limitation is absent or low PSMA expression (e.g., in visceral metastases) in advanced disease, which may be related to therapy-induced specific biologic subtypes (e.g., neuroendocrine differentiated PC) (65,66).…”

Section: Advanced Diseasementioning

confidence: 99%

PSMA Ligands for PET Imaging of Prostate Cancer

et al. 2017

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“…A variety of PSMA ligands for radioligand therapy (RLT) have been developed in recent years (5). Several studies using 131 I-or 177 Lu-labeled PSMA ligands for RLT reported reductions in tumor volume and serum prostate-specific antigen (PSA) levels (3,(6)(7)(8)(9)(10). For the assessment of a new radiopharmaceutical, dosimetry is essential to aim for the optimal therapeutic response with limited side effects.…”

mentioning

confidence: 99%

Radiation Dosimetry for¹⁷⁷Lu-PSMA I&T in Metastatic Castration-Resistant Prostate Cancer: Absorbed Dose in Normal Organs and Tumor Lesions

et al. 2016

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Prostate-specific membrane antigen (PSMA)-targeted radioligand therapy is increasingly used in metastatic castration-resistant prostate cancer. We aimed to estimate the absorbed doses for normal organs and tumor lesions using 177 Lu-PSMA I&T (I&T is imaging and therapy) in patients undergoing up to 4 cycles of radioligand therapy. Results were compared with pretherapeutic Glu-NH-CO-NH-Lys-(Ahx)-[ 68 Ga(HBEDCC)] ( 68 Ga-PSMA-HBED-CC) PET. Methods: A total of 34 cycles in 18 patients were analyzed retrospectively. In 15 patients the first, in 9 the second, in 5 the third, and in 5 the fourth cycle was analyzed, respectively. Whole-body scintigraphy was performed at least between 30-120 min, 24 h, and 6-8 d after administration. Regions of interest covering the whole body, organs, and up to 4 tumor lesions were drawn. Organ and tumor masses were derived from pretherapeutic 68 Ga-PSMA-HBED-CC PET/CT. Absorbed doses for individual cycles were calculated using OLINDA/EXM. SUVs from pretherapeutic PET were compared with absorbed doses and with change of SUV. Results: The mean whole-body effective dose for all cycles was 0.06 6 0.03 Sv/GBq. The mean absorbed organ doses were 0.72 6 0.21 Gy/GBq for the kidneys; 0.12 6 0.06 Gy/GBq for the liver; and 0.55 6 0.14 Gy/GBq for the parotid, 0.64 6 0.40 Gy/ GBq for the submandibular, and 3.8 6 1.4 Gy/GBq for the lacrimal glands. Absorbed organ doses were relatively constant among the 4 different cycles. Tumor lesions received a mean absorbed dose per cycle of 3.2 6 2.6 Gy/GBq (range, 0.22-12 Gy/GBq). Doses to tumor lesions gradually decreased, with 3.5 6 2.9 Gy/GBq for the first, 3.3 6 2.5 Gy/GBq for the second, 2.7 6 2.3 Gy/GBq for the third, and 2.4 6 2.2 Gy/GBq for the fourth cycle. SUVs of pretherapeutic PET moderately correlated with absorbed dose (r 5 0.44, P , 0.001 for SUV max ; r 5 0.43, P , 0.001 for SUV mean ) and moderately correlated with the change of SUV (r 5 0.478, P , 0.001 for SUV max , and r 5 0.50, P , 0.001 for SUV mean ). Conclusion: Organ-and tumorabsorbed doses for 177 Lu-PSMA I&T are comparable to recent reports and complement these with information on an excellent correlation between the 4 therapy cycles. With the kidneys representing the critical organ, a cumulative activity of 40 GBq of 177 Lu-PSMA I&T appears to be safe and justifiable. The correlation between pretherapeutic SUV and absorbed tumor dose emphasizes the need for PSMA-ligand PET imaging for patient selection.

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Systemic Radioligand Therapy with ¹⁷⁷ Lu Labeled Prostate Specific Membrane Antigen Ligand for Imaging and Therapy in Patients with Metastatic Castration Resistant Prostate Cancer

Abstract: Radioligand therapy with (177)Lu-PSMA-I&T appears to be safe and active in heavily pretreated patients with metastatic castration resistant prostate cancer.

Cited by 174 publications

References 21 publications

Lutetium ¹⁷⁷ PSMA radionuclide therapy for men with prostate cancer: a review of the current literature and discussion of practical aspects of therapy

Lutetium ¹⁷⁷ PSMA radionuclide therapy for men with prostate cancer: a review of the current literature and discussion of practical aspects of therapy

PSMA Ligands for PET Imaging of Prostate Cancer

Radiation Dosimetry for¹⁷⁷Lu-PSMA I&T in Metastatic Castration-Resistant Prostate Cancer: Absorbed Dose in Normal Organs and Tumor Lesions

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Systemic Radioligand Therapy with 177 Lu Labeled Prostate Specific Membrane Antigen Ligand for Imaging and Therapy in Patients with Metastatic Castration Resistant Prostate Cancer

Abstract: Radioligand therapy with (177)Lu-PSMA-I&T appears to be safe and active in heavily pretreated patients with metastatic castration resistant prostate cancer.

Cited by 174 publications

References 21 publications

Lutetium 177 PSMA radionuclide therapy for men with prostate cancer: a review of the current literature and discussion of practical aspects of therapy

Lutetium 177 PSMA radionuclide therapy for men with prostate cancer: a review of the current literature and discussion of practical aspects of therapy

PSMA Ligands for PET Imaging of Prostate Cancer

Radiation Dosimetry for177Lu-PSMA I&T in Metastatic Castration-Resistant Prostate Cancer: Absorbed Dose in Normal Organs and Tumor Lesions

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Systemic Radioligand Therapy with ¹⁷⁷ Lu Labeled Prostate Specific Membrane Antigen Ligand for Imaging and Therapy in Patients with Metastatic Castration Resistant Prostate Cancer

Lutetium ¹⁷⁷ PSMA radionuclide therapy for men with prostate cancer: a review of the current literature and discussion of practical aspects of therapy

Lutetium ¹⁷⁷ PSMA radionuclide therapy for men with prostate cancer: a review of the current literature and discussion of practical aspects of therapy

Radiation Dosimetry for¹⁷⁷Lu-PSMA I&T in Metastatic Castration-Resistant Prostate Cancer: Absorbed Dose in Normal Organs and Tumor Lesions