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Research ArticleDrug Discovery and Translational Medicine

Monitoring Tumor Response to Linifanib Therapy with SPECT/CT Using the Integrin αvβ3–Targeted Radiotracer 99mTc-3P-RGD2

Shundong Ji, Yang Zhou, Martin J. Voorbach, Guoqiang Shao, Yumin Zhang, Gerard B. Fox, Daniel H. Albert, Yanping Luo, Shuang Liu and Sarah R. Mudd
Journal of Pharmacology and Experimental Therapeutics August 2013, 346 (2) 251-258; DOI: https://doi.org/10.1124/jpet.112.202622
Shundong Ji
School of Health Sciences, Purdue University, West Lafayette, Indiana (S.J., Ya.Z., G.S., S.L.); and Translational Sciences (M.J.V., Yu.Z., G.B.F., Y.L., S.R.M.) and In Vivo Pharmacology (D.H.A.), AbbVie Inc., North Chicago, Illinois
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Yang Zhou
School of Health Sciences, Purdue University, West Lafayette, Indiana (S.J., Ya.Z., G.S., S.L.); and Translational Sciences (M.J.V., Yu.Z., G.B.F., Y.L., S.R.M.) and In Vivo Pharmacology (D.H.A.), AbbVie Inc., North Chicago, Illinois
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Martin J. Voorbach
School of Health Sciences, Purdue University, West Lafayette, Indiana (S.J., Ya.Z., G.S., S.L.); and Translational Sciences (M.J.V., Yu.Z., G.B.F., Y.L., S.R.M.) and In Vivo Pharmacology (D.H.A.), AbbVie Inc., North Chicago, Illinois
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Guoqiang Shao
School of Health Sciences, Purdue University, West Lafayette, Indiana (S.J., Ya.Z., G.S., S.L.); and Translational Sciences (M.J.V., Yu.Z., G.B.F., Y.L., S.R.M.) and In Vivo Pharmacology (D.H.A.), AbbVie Inc., North Chicago, Illinois
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Yumin Zhang
School of Health Sciences, Purdue University, West Lafayette, Indiana (S.J., Ya.Z., G.S., S.L.); and Translational Sciences (M.J.V., Yu.Z., G.B.F., Y.L., S.R.M.) and In Vivo Pharmacology (D.H.A.), AbbVie Inc., North Chicago, Illinois
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Gerard B. Fox
School of Health Sciences, Purdue University, West Lafayette, Indiana (S.J., Ya.Z., G.S., S.L.); and Translational Sciences (M.J.V., Yu.Z., G.B.F., Y.L., S.R.M.) and In Vivo Pharmacology (D.H.A.), AbbVie Inc., North Chicago, Illinois
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Daniel H. Albert
School of Health Sciences, Purdue University, West Lafayette, Indiana (S.J., Ya.Z., G.S., S.L.); and Translational Sciences (M.J.V., Yu.Z., G.B.F., Y.L., S.R.M.) and In Vivo Pharmacology (D.H.A.), AbbVie Inc., North Chicago, Illinois
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Yanping Luo
School of Health Sciences, Purdue University, West Lafayette, Indiana (S.J., Ya.Z., G.S., S.L.); and Translational Sciences (M.J.V., Yu.Z., G.B.F., Y.L., S.R.M.) and In Vivo Pharmacology (D.H.A.), AbbVie Inc., North Chicago, Illinois
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Shuang Liu
School of Health Sciences, Purdue University, West Lafayette, Indiana (S.J., Ya.Z., G.S., S.L.); and Translational Sciences (M.J.V., Yu.Z., G.B.F., Y.L., S.R.M.) and In Vivo Pharmacology (D.H.A.), AbbVie Inc., North Chicago, Illinois
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Sarah R. Mudd
School of Health Sciences, Purdue University, West Lafayette, Indiana (S.J., Ya.Z., G.S., S.L.); and Translational Sciences (M.J.V., Yu.Z., G.B.F., Y.L., S.R.M.) and In Vivo Pharmacology (D.H.A.), AbbVie Inc., North Chicago, Illinois
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Abstract

The objective of this study was to determine the utility of 99mTc-3P-Arg-Gly-Asp (RGD2) single photon emission computed tomography (SPECT)/computed tomography (CT) for noninvasive monitoring of integrin αvβ3-expression response to antiangiogenic treatment with linifanib. Linifanib or vehicle therapy was carried out in female athymic nu/nu mice bearing U87MG glioma (high αvβ3 expression) or PC-3 prostate (low αvβ3 expression) tumors at 12.5 mg/kg twice daily. The average tumor volume was 180 ± 90 mm3 the day prior to baseline SPECT/CT. Longitudinal 99mTc-3P-RGD2 SPECT/CT imaging was performed at baseline (–1 day) and days 1, 4, 11, and 18. Tumors were harvested at all imaging time points for histopathological analysis with H&E and immunohistochemistry. A significant difference in tumor volumes between vehicle- and linifanib-treated groups was observed after 4 days of linifanib therapy in the U87MG model. The percent injected dose (%ID) tumor uptake of 99mTc-3P-RGD2 peaked in the vehicle-treated group at day 11, while the %ID/cm3 tumor uptake decreased slowly over the whole study period. During the first 2 days of linifanib treatment, a rapid decrease in both %ID/cm3 tumor uptake and tumor/muscle ratios of 99mTc-3P-RGD2 was observed, followed by a slow decrease until day 18. No decrease in tumor uptake of 99mTc-3P-RGD2 or tumor volume was observed for either treatment group in the PC-3 model. Changes in tumor vasculature were confirmed by histopathological H&E analysis and immunohistochemistry. Longitudinal imaging using 99mTc-3P-RGD2 SPECT/CT may be a useful tool for monitoring the downstream biologic effects of linifanib therapy.

Footnotes

    • Received December 18, 2012.
    • Accepted May 21, 2013.
  • This work was supported in part by Purdue University; research grants from the National Institutes of Health National Cancer Institute [Grant R01 CA115883] and from the Susan G. Komen Breast Cancer Foundation [KG111333] (to Ya.Z. and S.L.).

  • This work was funded in part by AbbVie Inc. AbbVie Inc. and Purdue University contributed to the study design, interpretation of data, writing, review, and approval for publication.

  • dx.doi.org/10.1124/jpet.112.202622.

  • Copyright © 2013 by The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 346 (2)
Journal of Pharmacology and Experimental Therapeutics
Vol. 346, Issue 2
1 Aug 2013
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Research ArticleDrug Discovery and Translational Medicine

99mTc-3P-RGD2: An Integrin αvβ3–Targeted Radiotracer to Monitor Linifanib Therapy

Shundong Ji, Yang Zhou, Martin J. Voorbach, Guoqiang Shao, Yumin Zhang, Gerard B. Fox, Daniel H. Albert, Yanping Luo, Shuang Liu and Sarah R. Mudd
Journal of Pharmacology and Experimental Therapeutics August 1, 2013, 346 (2) 251-258; DOI: https://doi.org/10.1124/jpet.112.202622

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Research ArticleDrug Discovery and Translational Medicine

99mTc-3P-RGD2: An Integrin αvβ3–Targeted Radiotracer to Monitor Linifanib Therapy

Shundong Ji, Yang Zhou, Martin J. Voorbach, Guoqiang Shao, Yumin Zhang, Gerard B. Fox, Daniel H. Albert, Yanping Luo, Shuang Liu and Sarah R. Mudd
Journal of Pharmacology and Experimental Therapeutics August 1, 2013, 346 (2) 251-258; DOI: https://doi.org/10.1124/jpet.112.202622
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