<sup>203</sup>Pb-Labeled α-Melanocyte–Stimulating Hormone Peptide as an Imaging Probe for Melanoma Detection

Miao, Yubin; Figueroa, Said Daibes; Fisher, Darrell R.; Moore, Herbert; Testa, R.; Hoffman, Timothy J.; Quinn, Thomas P.

doi:10.2967/jnumed.107.048553

Cited by 64 publications

(64 citation statements)

References 18 publications

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“…Micro-SPECT scans of 60 frames for each animal were acquired and total counts acquisitions of 524,672 and 278,242 counts (2 h acquisition) were achieved for both SPECT scans, respectively. The micro-SPECT images were obtained using the Micro-CAT II CT/SPECT (Siemens) unit equipped with high resolution 2 mm pinhole collimators (22). Reconstructed data from SPECT and CT were visualized and co-registered using Amira 3.1 (Ascent Media System & Technology Service, Northvale, NJ).…”

Section: Imaging Melanoma With 111 In-dota-cycmsh and 111 In-dota-glymentioning

confidence: 99%

¹¹¹In-Labeled Lactam Bridge-Cyclized α-Melanocyte Stimulating Hormone Peptide Analogues for Melanoma Imaging

et al. 2008

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The purpose of this study was to examine the influence of the lactam bridge cyclization on melanoma targeting and biodistribution properties of the radiolabeled conjugates. Two novel lactam bridge-cyclized α-MSH peptide analogues, 4,7,4,7, In-DOTAGlyGlu-CycMSH by SPECT/CT images at 2 h post-injection. Whole-body clearance of the peptides was fast, with greater than 90% of the radioactivities cleared through urinary system by 2 h post-injection. There was low radioactivity (<0.8 %ID/g) accumulated in blood and normal organs except kidneys at all time points investigated. Introduction of a negatively-charged linker (-Gly-Glu-) into the peptide sequence decreased the renal uptake by 44% without affecting the tumor uptake at 4 h post-injection. High receptor-mediated melanoma uptakes coupled with fast whole-body clearance in B16/F1 melanoma-bearing C57 mice demonstrated the feasibility of using 111 In-labeled lactam bridge-cyclized α-MSH peptide analogues as a novel class of imaging probes for receptor-targeting melanoma imaging.

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Section: Imaging Melanoma With 111 In-dota-cycmsh and 111 In-dota-glymentioning

confidence: 99%

¹¹¹In-Labeled Lactam Bridge-Cyclized α-Melanocyte Stimulating Hormone Peptide Analogues for Melanoma Imaging

et al. 2008

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“…In recent years, several other radiolabeled imaging probes have been evaluated for melanoma imaging, including methylene blue dye (10), monoclonal antibodies against melanoma-associated antigens (11,12), iodoamphetamine (13), a-melanocyte-stimulating hormone ana-logs (14,15), and benzamide (BZA)-based compounds (16,17). To date, iodinated BZA analogs have been among the most promising of the newer melanoma radiotracers for both diagnosis and therapeutic applications.…”

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confidence: 99%

High-Contrast PET of Melanoma Using ¹⁸F-MEL050, a Selective Probe for Melanin with Predominantly Renal Clearance

Denoyer¹,

Greguric²,

Roselt³

et al. 2010

J Nucl Med

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The aim of this study was to evaluate the novel probe 18 F-6-fluoro-N-[2-(diethylamino)ethyl] pyridine-3-carboxamide ( 18 F-MEL050) for the imaging of primary and metastatic melanoma. Methods: PET using 18 F-MEL050 was performed in murine models of melanoma. The specificity of 18 F-MEL050 was studied by comparing its accumulation in pigmented B16-F0 allograft tumors with that of human amelanotic A375 xenografts using PET and high-resolution autoradiography. 18 F-MEL050 PET results were compared with 18 F-FDG PET, the current standard in melanoma molecular imaging. To test the ability of 18 F-MEL050 to assess the metastatic spread of melanoma, a murine model of lung metastasis was imaged by PET/CT, and results correlated with physical assessment of tumor burden in the lungs. Results: In pigmented B16-F0 grafts, 18 F-MEL050 PET yielded a tumor-to-background ratio of approximately 20:1 at 1 h and greater than 50:1 at 2 and 3 h. In the B16-F0 melanoma allograft model, tumor-to-background ratio was more than 9-fold higher for 18 F-MEL050 than for 18 F-FDG (50.9 6 6.9 vs. 5.8 6 0.5). No uptake was observed in the amelanotic melanoma xenografts. Intense uptake of 18 F-MEL050 was evident in metastatic lesions in the lungs of B16-BL6 tumor-bearing mice on PET at 2 h after tracer injection, with high concordance between 18 F-MEL050 accumulation on PET/CT and tumor burden determined at necroscopy. Conclusion: 18 F-MEL050 has a rapid tumor uptake and high retention with specificity for melanin, suggesting great potential for noninvasive clinical evaluation of suspected metastatic melanoma.

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“…4) in B16/F1 tumor-bearing mice highlight their potential to be used at lower doses for patient-specific dosimetry to support melanoma peptide-targeted radionuclide therapy. Likewise, 203 Pb-DOTA-Re(Arg 11 )CCMSH was shown to yield high quality SPECT images in B16/F1 tumor-bearing mice [86], demonstrating its ability as a matched-pair imaging agent for 212 Pb-DOTA-Re(Arg 11 )CCMSH. While no imaging data was reported for 188 Re-HYNIC-4B4, it is likely that lower doses of the 188 Re-labeled peptide will serve as an imaging agent in support of therapy.…”

Section: Prospects and Challenges Of Peptide-targeted Melanoma Therapymentioning

confidence: 97%

Peptide-targeted radionuclide therapy for melanoma

Miao

Quinn

2008

Critical Reviews in Oncology/Hematology

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Melanocortin-1 receptor (MC1-R) and melanin are two attractive melanoma-specific targets for peptide-targeted radionuclide therapy for melanoma. Radiolabeled peptides targeting MC1-R/melanin can selectively and specifically target cytotoxic radiation generated from therapeutic radionuclides to melanoma cells for cell killing, while sparing the normal tissues and organs. This review highlights the recent advances of peptide-targeted radionuclide therapy of melanoma targeting MC1-R and melanin. The promising therapeutic efficacies of 188Re-(Arg(11))CCMSH (188Re-[Cys(3,4,10), D-Phe(7),Arg(11)]-alpha-MSH(3-13)), 177Lu- and 212Pb-labeled DOTA-Re(Arg(11))CCMSH (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-[ReO-(Cys(3,4,10), D-Phe(7), Arg(11))]-alpha-MSH(3-13)) and 188Re-HYNIC-4B4 (188Re-hydrazinonicotinamide-Tyr-Glu-Arg-Lys-Phe-Trp-His-Gly-Arg-His) in preclinical melanoma-bearing models demonstrate an optimistic outlook for peptide-targeted radionuclide therapy for melanoma. Peptide-targeted radionuclide therapy for melanoma will likely contribute in an adjuvant setting, once the primary tumor has been surgically removed, to treat metastatic deposits and for treatment of end-stage disease. The lack of effective treatments for metastatic melanoma and end-stage disease underscores the necessity to develop and implement new treatment strategies, such as peptide-targeted radionuclide therapy.

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²⁰³Pb-Labeled α-Melanocyte–Stimulating Hormone Peptide as an Imaging Probe for Melanoma Detection

Cited by 64 publications

References 18 publications

¹¹¹In-Labeled Lactam Bridge-Cyclized α-Melanocyte Stimulating Hormone Peptide Analogues for Melanoma Imaging

¹¹¹In-Labeled Lactam Bridge-Cyclized α-Melanocyte Stimulating Hormone Peptide Analogues for Melanoma Imaging

High-Contrast PET of Melanoma Using ¹⁸F-MEL050, a Selective Probe for Melanin with Predominantly Renal Clearance

Peptide-targeted radionuclide therapy for melanoma

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203Pb-Labeled α-Melanocyte–Stimulating Hormone Peptide as an Imaging Probe for Melanoma Detection

Cited by 64 publications

References 18 publications

111In-Labeled Lactam Bridge-Cyclized α-Melanocyte Stimulating Hormone Peptide Analogues for Melanoma Imaging

111In-Labeled Lactam Bridge-Cyclized α-Melanocyte Stimulating Hormone Peptide Analogues for Melanoma Imaging

High-Contrast PET of Melanoma Using 18F-MEL050, a Selective Probe for Melanin with Predominantly Renal Clearance

Peptide-targeted radionuclide therapy for melanoma

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²⁰³Pb-Labeled α-Melanocyte–Stimulating Hormone Peptide as an Imaging Probe for Melanoma Detection

¹¹¹In-Labeled Lactam Bridge-Cyclized α-Melanocyte Stimulating Hormone Peptide Analogues for Melanoma Imaging

¹¹¹In-Labeled Lactam Bridge-Cyclized α-Melanocyte Stimulating Hormone Peptide Analogues for Melanoma Imaging

High-Contrast PET of Melanoma Using ¹⁸F-MEL050, a Selective Probe for Melanin with Predominantly Renal Clearance