Radiolabeling of rituximab with 188Re and 99mTc using the tricarbonyl technology

Dias, Carla Roberta; Jeger, Simone; Osso, João Alberto; Müller, Cristina; Pasquale, Christine de; Höhn, Alexander; Waibel, Robert; Schibli, Roger

doi:10.1016/j.nucmedbio.2010.05.010

Cited by 28 publications

(31 citation statements)

References 31 publications

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“…Our results are similar to those described in the literature, indicating that radiolabeling with other isotopes besides 99m Tc does not alter epitope recognition [20]. For the A20 cell line, no differences in binding were observed.…”

Section: Discussionsupporting

confidence: 91%

“…To radiolabel rituximab with 99m Tc, we used NHS-HYNIC-Tfa as a bifunctional chelating agent due to our expertise in radiolabeling antibodies with it [27,28,29,30], highlighting the time it takes to complete the labeling (30 min) compared to other methods [17,18,20,21]. Abrams et al [37] were the first to describe the synthesis and in vivo evaluation of HYNIC bioconjugates.…”

Section: Discussionmentioning

confidence: 99%

“…In the last years, several methods for radiolabeling rituximab with 99m Tc have been described [17,18,19,20,21]. All of them include 2 reduction steps - the first step dedicated to the reduction of 99m Tc, and the second step specifically targeting the antibody, either with photoactivation [18] or 2-mercaptoethanol [19,20]. This last step creates thiol residues that facilitate technetium binding, but could modify the protein structure and decrease antigen recognition.…”

Section: Introductionmentioning

confidence: 99%

“…This last step creates thiol residues that facilitate technetium binding, but could modify the protein structure and decrease antigen recognition. Labeling of rituximab using 99m Tc-carbonyl core ([ 99m Tc(CO) 3 ] + ) has also been performed with interesting results, although heating is required in order to achieve quantitative labeling at micromolar concentrations [17,20,21]. …”

Section: Introductionmentioning

confidence: 99%

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Technetium-99m- or Cy7-Labeled Rituximab as an Imaging Agent for Non-Hodgkin Lymphoma

et al. 2017

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Introduction: Rituximab was the first monoclonal antibody approved for the treatment of B-cell non-Hodgkin lymphoma (NHL) expressing CD20 antigen. This antibody has also the potential to be used as a specific fluorescent and radiolabel agent for targeting NHL. Objective: To radiolabel rituximab with technetium-99m (^99mTc) or Cy7 and evaluate both probes as potential imaging agents for NHL. Methods: Rituximab was derivatized with the trifluoroacetyl hydrazino protected form of succinimidyl ester of HYNIC and radiolabeled with ^99mTc. Radiochemical stability and in vitro cell assays were evaluated. Biodistribution and single-photon emission computed tomography/computed tomography (SPECT/CT) were performed. Raji cells were transfected with luciferase for bioluminescent NHL imaging up to 21 days. Rituximab was labeled with Cy7 for in vivo noninvasive fluorescence imaging up to 96 h. Results: Radiolabeling was carried out in a fast, reproducible, easy, and stable way with high radiochemical purity and did not interfere with epitope recognition. Biodistribution and SPECT/CT studies showed high liver and discrete tumor uptake. Bioluminescence and fluorescence studies helped us evaluate rituximab-Cy7 in Raji subcutaneous engraftment in BALB/c nude mice. Conclusions: Our results support the potential use of rituximab labeled either with ^99mTc or Cy7 as a molecular imaging tool for staging, restaging, and guiding surgical excision of tumors, which merits further evaluation.

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Section: Discussionsupporting

confidence: 91%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Technetium-99m- or Cy7-Labeled Rituximab as an Imaging Agent for Non-Hodgkin Lymphoma

et al. 2017

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“…A captação tumoral do 188 Re(CO) 3-RTXred foi de 2,5% DI/g e 0,8% DI/g para 99m Tc(CO)3-RTXred 48 h após injeção. Os valores para outros órgãos e tecidos foram similares para ambos os compostos [DIAS, 2010;DIAS et. al, 2011].…”

Section: Lu-anti-cd20unclassified

Estudo compartimental e dosimétrico do anti-CD20 marcado com <sup>188</sup>Re

Kuramoto¹

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Radiolabelling rituximab with ^99mTc in three steps procedure

Fontan

Bezombes

Salabert

et al. 2015

Labelled Comp Radiopharmac

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Lymphomas are the most frequent haematological malignancy. In non-Hodgkin's lymphomas (NHL), more than 90% of tumor cells express the cluster of differentiation (CD) 20 antigen. At the end of frontline therapy, the evaluation of remission is based on computed tomography (CT) and positron emission tomography coupled with computer tomography (PET/CT) with [(18)F]-fluorodeoxyglucose ([(18)F]FDG). Unfortunately, these techniques are not specific and cannot distinguish residual active tumor from inflammation. The aim of this study was to develop a specific radiotracer of NHL CD 20+ cells for clinical applications. The radiolabelling technique presented, based on the use of tricarbonyl compound, does not include an antibody reduction because this step could damage the protein. Actually, rituximab, an anti-CD 20 chimeric antibody used for the treatment of these NHL, was radiolabelled with Isolink® (99m)Tc-tricarbonyl compound in a three-step procedure without using a specific antibody reducer. Radiolabelling yield was greater than 97%. In vitro experiments showed a conservation of antibody integrity. In vivo experiments using Single-photon emission computed tomography/CT showed significant tumor targeting 24 h after injection of the radiotracer. It was consequently possible to develop an immunoradiolabelling method to specifically detect the residual disease. As this procedure is fast, reproducible and gentle, it will be possible to comply with Good Manufacturing Practices.

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Radiolabeling of rituximab with 188Re and 99mTc using the tricarbonyl technology

Cited by 28 publications

References 31 publications

Technetium-99m- or Cy7-Labeled Rituximab as an Imaging Agent for Non-Hodgkin Lymphoma

Technetium-99m- or Cy7-Labeled Rituximab as an Imaging Agent for Non-Hodgkin Lymphoma

Estudo compartimental e dosimétrico do anti-CD20 marcado com <sup>188</sup>Re

Radiolabelling rituximab with ^99mTc in three steps procedure

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Radiolabeling of rituximab with 188Re and 99mTc using the tricarbonyl technology

Cited by 28 publications

References 31 publications

Technetium-99m- or Cy7-Labeled Rituximab as an Imaging Agent for Non-Hodgkin Lymphoma

Technetium-99m- or Cy7-Labeled Rituximab as an Imaging Agent for Non-Hodgkin Lymphoma

Estudo compartimental e dosimétrico do anti-CD20 marcado com <sup>188</sup>Re

Radiolabelling rituximab with 99mTc in three steps procedure

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Radiolabelling rituximab with ^99mTc in three steps procedure