NDLI: H6phospa-trastuzumab: bifunctional methylenephosphonate-based chelator with 89Zr, 111In and 177Lu.

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H6phospa-trastuzumab: bifunctional methylenephosphonate-based chelator with 89Zr, 111In and 177Lu.

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H6phospa-trastuzumab: bifunctional methylenephosphonate-based chelator with 89Zr, 111In and 177Lu.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Price, Eric W. Adam, Michael J. Zeglis, Brian M. Lewis, Jason S. Orvig, Chris
Description	Author Affiliation: Price EW ( Medicinal Inorganic Chemistry Group, Department of Chemistry, University of British Columbia, 2036 Main Mall, Vancouver, British Columbia, CanadaV6T 1Z1. orvig@chem.ubc.ca.)
Abstract	The acyclic chelator H6phospa and the bifunctional derivative p-SCN-Bn-H6phospa have been synthesized using nosyl protection chemistry and evaluated with (89)Zr, (111)In, and (177)Lu. The p-SCN-Bn-H6phospa derivative was successfully conjugated to trastuzumab with isotopic dilution assays indicating 3.3 ± 0.1 chelates per antibody and in vitro cellular binding assays indicating an immunoreactivity value of 97.9 ± 2.6%. Radiolabeling of the H6phospa-trastuzumab immunoconjugate was achieved with (111)In in 70-90% yields at room temperature in 30 minutes, while (177)Lu under the same conditions produced more inconsistent yields of 40-80%. Stability experiments in human serum revealed the (111)In-phospa-trastuzumab complex to be 52.0 ± 5.3% intact after 5 days at 37 °C, while the (177)Lu-phospa-trastuzumab to be only 2.0 ± 0.3% intact. Small animal SPECT/CT imaging using mice bearing subcutaneous SKOV-3 ovarian cancer xenografts was performed, and it was found that (111)In-phospa-trastuzumab successfully identified and delineated small (~2 mm in diameter) tumors from surrounding tissues, despite visible uptake in the kidneys and bone due to moderate chelate instability. As predicted from stability assays in serum, the (177)Lu-phospa-trastuzumab conjugate served as a negative control and displayed no tumor uptake, with high uptake in bones indicating rapid and complete radiometal dissociation and suggesting a potential application of H6phospa in transient lanthanide chelation for bone-delivery. Radiolabeling with (89)Zr was attempted, but even with elevated temperatures of 37 °C, the maximum observed radiometal incorporation over 18 hours was 12%. It can be concluded from this work that H6phospa is not superior to the previously studied H4octapa for use with (111)In and (177)Lu, but improvements in (89)Zr radiolabeling were observed over H4octapa, suggesting H6phospa to be an excellent starting point for elaboration of (89)Zr-based radiopharmaceutical development. To our knowledge, H6phospa is the best desferrioxamine alternative for (89)Zr radiolabeling to be studied to date.
ISSN	14779226
e-ISSN	13645447
Journal	Dalton Trans.
Issue Number	1
Volume Number	43
Language	English
Publisher	Royal Society of Chemistry
Publisher Date	2014-01-07
Publisher Place	Great Britain (UK)
Access Restriction	Open
Subject Keyword	Antibodies, Monoclonal, Humanized Chemistry Chelating Agents Organophosphorus Compounds Ovarian Neoplasms Animals Pharmacokinetics Cell Line, Tumor Indium Isotope Labeling Lutetium Mice Mice, Nude Diagnosis Ovary Pathology Positron-Emission Tomography Radioisotopes Trastuzumab Zirconium Research Support, N.I.H., Extramural Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, Non-P.H.S.
Content Type	Text
Resource Type	Article
Subject	Inorganic Chemistry

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