Abstract
The optimization of DOTA-NHS-ester conjugation to Rituximab using different Ab:DOTA molar ratios (1:10, 1:20, 1:50 and 1:100) was studied. High radiochemical yield, in vitro stability and immunoreactive fraction were obtained for the Rituximab conjugated at 1:50 molar ratio, resulting in the incorporation of an average number of 4.9 ± 1.1 DOTA per Rituximab molecule. Labeling with 177Lu was performed in high specific activity with great in vitro stability. Biodistribution in healthy and xenographed mice showed tumor uptake and high in vivo stability as evidenced by low uptake in bone. The properties of 177Lu-DOTA-Rituximab prepared from DOTA-NHS-ester suggest the potential for the application of the 177Lu-labeled antibody in preliminary clinical studies.
Keywords: Anti-CD-20, DOTA-NHS-ester, immunoconjugation, Non-Hodgking‘s Limphoma, radioimmunotherapy, Rituximab.
Current Radiopharmaceuticals
Title:Development and biological studies of 177Lu-DOTA-rituximab for the treatment of Non-Hodgkin’s lymphoma
Volume: 9 Issue: 1
Author(s): Adriana V.F. Massicano, Priscilla B. Pujatti, Lais F. Alcarde, Miriam F. Suzuki, Patrick J. Spencer and Elaine B. Araújo
Affiliation:
Keywords: Anti-CD-20, DOTA-NHS-ester, immunoconjugation, Non-Hodgking‘s Limphoma, radioimmunotherapy, Rituximab.
Abstract: The optimization of DOTA-NHS-ester conjugation to Rituximab using different Ab:DOTA molar ratios (1:10, 1:20, 1:50 and 1:100) was studied. High radiochemical yield, in vitro stability and immunoreactive fraction were obtained for the Rituximab conjugated at 1:50 molar ratio, resulting in the incorporation of an average number of 4.9 ± 1.1 DOTA per Rituximab molecule. Labeling with 177Lu was performed in high specific activity with great in vitro stability. Biodistribution in healthy and xenographed mice showed tumor uptake and high in vivo stability as evidenced by low uptake in bone. The properties of 177Lu-DOTA-Rituximab prepared from DOTA-NHS-ester suggest the potential for the application of the 177Lu-labeled antibody in preliminary clinical studies.
Export Options
About this article
Cite this article as:
Massicano V.F. Adriana, Pujatti B. Priscilla, Alcarde F. Lais, Suzuki F. Miriam, Spencer J. Patrick and Araújo B. Elaine, Development and biological studies of 177Lu-DOTA-rituximab for the treatment of Non-Hodgkin’s lymphoma, Current Radiopharmaceuticals 2016; 9 (1) . https://dx.doi.org/10.2174/1874471008666150313103849
DOI https://dx.doi.org/10.2174/1874471008666150313103849 |
Print ISSN 1874-4710 |
Publisher Name Bentham Science Publisher |
Online ISSN 1874-4729 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
B Cells: Programmers of CD4 T Cell Responses
Infectious Disorders - Drug Targets Novel Agents, Combinations and Sequences for the Treatment of Advanced Renal Cell Carcinoma: When is the Revolution Coming?
Current Cancer Drug Targets Novel Drug Therapies for Fertility Preservation in Men Undergoing Chemotherapy: Clinical Relevance of Protector Agents
Current Medicinal Chemistry DNMT Inhibitors in Cancer, Current Treatments and Future Promising Approach: Inhibition of Specific DNMT-Including Complexes
Epigenetic Diagnosis & Therapy (Discontinued) Natural Killer Cells Preferentially Target Cancer Stem Cells; Role of Monocytes in Protection Against NK Cell Mediated Lysis of Cancer Stem Cells
Current Drug Delivery DNA Polymerases and Oxidative Damage: Friends or Foes?
Current Molecular Pharmacology HIV-1 Nef Protein Visits B-Cells via Macrophage Nanotubes: A Mechanism for AIDS-Related Lymphoma Pathogenesis?
Current HIV Research Recent Patents Relating To HCV Molecules Like Putative Targets For Therapeutic Intervention
Recent Patents on DNA & Gene Sequences Targeted Radiotherapy of Bone Malignancies
Current Drug Discovery Technologies Multifunctional Anti-Cancer Nano-Platforms are Moving to Clinical Trials
Current Drug Metabolism Human Immunodeficiency Virus-Induced Apoptosis of Human Breast Cancer Cells Via CXCR4 is Mediated by the Viral Envelope Protein But Does Not Require CD4
Current HIV Research γ δ T Cell Modulation in Anticancer Treatment
Current Cancer Drug Targets Therapeutic Immunoconjugates. Which Cytotoxic Payload: Chemotherapeutic Drug (ADC) or Radionuclide (ARC) ?
Current Cancer Therapy Reviews Interaction Between DNA/histone Methyltransferases and their Inhibitors
Current Medicinal Chemistry The Effects of 5-Aza-2`-Deoxycytidine on DLC-1 Gene Expression, Methylation Level and Expression of Downstream Signaling Molecules Cdc42 in Multiple Myeloma
Current Signal Transduction Therapy STAT3: A Molecular Target for Cancer Whose Time Has Come
Current Signal Transduction Therapy Synergistic Interplay of Medicinal Chemistry and Formulation Strategies in Nanotechnology – From Drug Discovery to Nanocarrier Design and Development
Current Topics in Medicinal Chemistry Endocrine and Antineoplastic Actions of Growth Hormone-Releasing Hormone Antagonists
Current Medicinal Chemistry Radioimmunotherapy of Solid Tumors: Searching for the Right Target
Current Drug Delivery Third Generation Radiopharmaceuticals for Imaging and Targeted Therapy
Current Pharmaceutical Analysis