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Ready-to-use 177Lu-Rituximab injection for Non-Hodgkin’s Lymphoma: Formulation and preliminary clinical study

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Abstract

This study was aimed at the preparation of 177Lu-CHX-A″-DTPA-Rituximab injection at the hospital pharmacy for non-Hodgkin lymphoma. Rituximab was conjugated with CHX-A″-DTPA-NCS and the CHX-A″-DTPA-Rituximab conjugate was radiolabeled with 177Lu in > 95% purity. The product exhibited excellent in vitro stability up to 5 days at 37 °C. In vitro cell binding studies in Raji cells confirmed the specificity of 177Lu-CHX-A″-DTPA-Rituximab to CD20 antigen. The radioimmunoconjugate exhibited predominantly hepatobiliary clearance and low bone uptake in Swiss mice. Preliminary clinical studies corroborated the usefulness of 177Lu-CHX-A″-DTPA-Rituximab for therapy of non-Hodgkin lymphoma.

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Acknowledgements

Authors gratefully acknowledge staff of Radiochemicals Section, RPhD, BARC for the supply of 177LuCl3 and the staff of Kovai Medical Centre and Hospital, Coimbatore for their help during the clinical studies.

Funding

Research at the Bhabha Atomic Research Centre is fully funded by the Government of India.

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Author notes

  1. Mythili Kameswaran and Usha Pandey have contributed equally to this work.

Authors and Affiliations

  1. Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400 085, India

    Mythili Kameswaran, Usha Pandey, Naresh Gamre, Suresh Subramanian & Ashutosh Dash

  2. Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400 085, India

    Haladhar Dev Sarma

  3. Department of Nuclear Medicine and PET/CT, Kovai Medical Center and Hospital Limited, Coimbatore, Tamil Nadu, India

    Ajit Shinto & K. K. Kamleshwaran

  4. Homi Bhabha National Institute, Anushakti Nagar, Mumbai, 400 094, India

    Usha Pandey & Ashutosh Dash

Authors
  1. Mythili Kameswaran
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  2. Usha Pandey
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  3. Naresh Gamre
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  4. Ajit Shinto
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  5. Suresh Subramanian
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  6. Haladhar Dev Sarma
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  7. K. K. Kamleshwaran
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  8. Ashutosh Dash
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Corresponding author

Correspondence to Mythili Kameswaran.

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Kameswaran, M., Pandey, U., Gamre, N. et al. Ready-to-use 177Lu-Rituximab injection for Non-Hodgkin’s Lymphoma: Formulation and preliminary clinical study. J Radioanal Nucl Chem 318, 849–856 (2018). https://doi.org/10.1007/s10967-018-6042-7

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  • DOI: https://doi.org/10.1007/s10967-018-6042-7

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