Purification of cyclotron-produced 203Pb for labeling Herceptin

Garmestani, Kayhan; Milenic, Diane E.; Brady, Erik D.; Plascjak, P.; Brechbiel, Martin W.

doi:10.1016/j.nucmedbio.2004.11.004

Cited by 23 publications

(21 citation statements)

References 20 publications

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“…The treatment of 7.4 MBq of 212 Pb-DOTA-Re(Arg 11 )CCMSH cured 45% of B16/F1 murine melanoma-bearing C57 mice in a 120-d study and highlighted its potential as a novel agent for targeted radionuclide therapy of melanoma. 203 Pb and 212 Pb are 2 isotopes with diagnostic and therapeutic properties (11,12). The favorable decay and imaging properties of 203 Pb make it an ideal matched-pair radioisotope for 212 Pb for targeted radionuclide therapy (11,12).…”

Section: Tablementioning

confidence: 99%

“…On decay, 203 Pb (half-life, 51.9 h) emits a 279-keV g-ray (81% abundance) suitable for SPECT. 203 Pb can be produced via the 203 Tl(d,2n) 203 Pb reaction by irradiating natural Tl 2 O 3 or an enriched Tl 2 O 3 ( 203 Tl) target with 13.7-MeV deuterons (11). A simple and rapid procedure was reported for purifying cyclotron-produced 203 Pb via the 203 Tl(d,2n) 203 Pb reaction (11).…”

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confidence: 99%

“…203 Pb can be produced via the 203 Tl(d,2n) 203 Pb reaction by irradiating natural Tl 2 O 3 or an enriched Tl 2 O 3 ( 203 Tl) target with 13.7-MeV deuterons (11). A simple and rapid procedure was reported for purifying cyclotron-produced 203 Pb via the 203 Tl(d,2n) 203 Pb reaction (11). High specific activity and radiochemical purity of 203 Pb are essential for radiolabeling peptides that target lower-copy-number cellular receptors.…”

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confidence: 99%

“…Likewise, low specific activity of 203 Pb preparations may result in the saturation of the targeted receptors with nonradioactively labeled peptides. Purified 203 Pb was used to label the monoclonal antibody trastuzumab (Herceptin; Genentech), which was shown to be immunoreactive and displayed favorable biodistribution properties in vivo, demonstrating the suitability and feasibility of 203 Pb-labeled biomolecules to target cellular antigens (11).…”

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confidence: 99%

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

Miao¹,

Figueroa²,

Fisher³

et al. 2008

J Nucl Med

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Peptide-targeted a-therapy with 7.4 MBq of 212 Pb-[1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid]-ReO-[Cys 3,4,10 , D-Phe 7 ,Arg 11 ]a-MSH 3-13 ( 212 Pb-DOTA-Re(Arg 11 )CCMSH) cured 45% of B16/F1 murine melanoma-bearing C57 mice in a 120-d study, highlighting its melanoma treatment potential. However, there is a need to develop an imaging surrogate for patientspecific dosimetry and to monitor the tumor response to 212 Pb-DOTA-Re(Arg 11 )CCMSH therapy. The purpose of this study was to evaluate the potential of 203 Pb-DOTA-Re(Arg 11 )CCMSH as a matched-pair SPECT agent for 212 Pb-DOTA-Re(Arg 11 ) CCMSH. Methods: DOTA-Re(Arg 11 )CCMSH was labeled with 203 Pb in 0.5 M NH 4 OAc buffer at pH 5.4. The internalization and efflux of 203 Pb-DOTA-Re(Arg 11 )CCMSH were determined in B16/F1 melanoma cells. The pharmacokinetics of 203 Pb-DOTARe(Arg 11 )CCMSH was examined in B16/F1 melanoma-bearing C57 mice. A micro-SPECT/CT study was performed with 203 Pb-DOTA-Re(Arg 11 )CCMSH in a B16/F1 melanoma-bearing C57 mouse at 2 h after injection. Results: 203 Pb-DOTARe(Arg 11 )CCMSH was easily prepared in NH 4 OAc buffer and completely separated from the excess nonradiolabeled peptide by reversed-phase high-performance liquid chromatography (RP-HPLC). 203 Pb-DOTA-Re(Arg 11 )CCMSH displayed fast internalization and extended retention in B16/F1 cells. Approximately 73% of 203 Pb-DOTA-Re(Arg 11 )CCMSH activity internalized after a 20-min incubation at 25°C. After incubation of the cells in culture medium for 20 min, 78% of internalized activity remained in the cells. 203 Pb-DOTA-Re(Arg 11 )CCMSH exhibited a biodistribution pattern similar to that of 212 Pb-DOTA-Re(Arg 11 )CCMSH in B16/ F1 melanoma-bearing mice. 203 Pb-DOTA-Re(Arg 11 )CCMSH exhibited a peak tumor uptake of 12.00 6 3.20 percentage injected dose per gram (%ID/g) at 1 h after injection. The tumor uptake gradually decreased to 3.43 6 1.12 %ID/g at 48 h after injection. 203 Pb-DOTA-Re(Arg 11 )CCMSH exhibited a peak tumor-to-kidney uptake ratio of 1.53 at 2 h after injection. The absorbed doses to the tumor and kidneys were 4.32 and 4.35 Gy, respectively, per 37 MBq. Whole-body clearance of 203 Pb-DOTA-Re(Arg 11 )CCMSH was fast, with approximately 89% of the injected activity cleared through the urinary system by 2 h after injection. 203 Pb showed 1.6-mm SPECT resolution, which was comparable to 99m Tc. Melanoma lesions were visualized through SPECT/CT images of 203 Pb-DOTA-Re(Arg 11 )CCMSH at 2 h after injection. Conclusion: 203 Pb-DOTA-Re(Arg 11 )CCMSH exhibited favorable pharmacokinetic and tumor imaging properties, highlighting its potential as a matched-pair SPECT agent for 212 Pb-DOTA-Re(Arg 11 )CCMSH melanoma treatment.

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Section: Tablementioning

confidence: 99%

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

Miao¹,

Figueroa²,

Fisher³

et al. 2008

J Nucl Med

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“…The new recommended data from point of view of production of 201 T l and the 200 T l and 202 T l impurities didn't differ significantly from recommended data in the IAEA medical library. compounds and antibodies (Chappell et al, 2000;Garmestania et al, 2005) . Preparation of 203 Pb compounds for studies on pathway and effects of lead pollution (Girardi et al, 1975) .…”

Section: The Evaluation Processmentioning

confidence: 99%

Investigation of activation cross-sections of proton induced nuclear reactions on natTl up to 42MeV: Review, new data and evaluation

Tárkányi

Ditrói

Hermanne

et al. 2013

Applied Radiation and Isotopes

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Cross-sections of proton induced nuclear reactions on natural thallium have been studied for investigation of the production of the medical important 201 T l diagnostic radioisotope. The excitation functions of 204m Pb, 203 Pb, 202m Pb, 201 Pb, 200 Pb, 199 Pb, 202 T l (direct, cumulative), 201 T l (direct, cumulative), 200 T l(direct), and 203 Hg were measured up to 42 MeV proton energy by stacked foil technique and activation method. The experimental data were compared with the critically analyzed experimental data in the literature, with the IAEA recommended data and with the results of model calculations by using the ALICE-IPPE, EMPIRE-II and TALYS codes.

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Emerging Therapeutic Radiopharmaceuticals and Their Theranostic Pairs

Carbo-Bague

Ramogida

2021

Encyclopedia of Inorganic and Bioinorganic Chemistry

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Nuclear medicine is a rapidly evolving multidisciplinary research field that has been intensively investigated in the past decades. The successful clinical application of various metal‐based radiopharmaceuticals for cancer imaging and therapy is based on the modular assembly of the drug complex through the popular bifunctional chelate (BFC) strategy. In targeted radionuclide therapy (TRT), potent radiation is selectively delivered to the cancer cells using radiopharmaceuticals that incorporate therapeutic radiometals which emit α ‐particles, β − ‐particles, or Meitner–Auger electrons (MAEs). Radiotheranostics is an emerging concept that connects nuclear imaging (via positron emission tomography (PET) or single‐photon emission computed tomography (SPECT)) and therapy for personalized cancer diagnosis and treatment. This article outlines the fundamentals of radiopharmaceutical design and radiotheranostics and presents a general description of the therapeutic emissions accompanied by literature examples of the most promising radionuclides; 212 Pb, 213 Bi, 225 Ac, 227 Th, and 149 Tb for α therapy; 47 Sc, 67 Cu, 77 As, and 161 Tb for β − therapy; and 119 Sb, 135 La, and 197m/g Hg for MAE therapy. A comparison of the currently used or proposed theranostic pairs of each radiometal is presented.

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Purification of cyclotron-produced 203Pb for labeling Herceptin

Cited by 23 publications

References 20 publications

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

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

Investigation of activation cross-sections of proton induced nuclear reactions on natTl up to 42MeV: Review, new data and evaluation

Emerging Therapeutic Radiopharmaceuticals and Their Theranostic Pairs

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Purification of cyclotron-produced 203Pb for labeling Herceptin

Cited by 23 publications

References 20 publications

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

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

Investigation of activation cross-sections of proton induced nuclear reactions on natTl up to 42MeV: Review, new data and evaluation

Emerging Therapeutic Radiopharmaceuticals and Their Theranostic Pairs

Contact Info

Product

Resources

About

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

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