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Molecules 2008, 13(2), 391-404; doi:10.3390/molecules13020391

Novel Prodrugs for Targeting Diagnostic and Therapeutic Radionuclides to Solid Tumors

* , , ,  and
Department of Radiology, Harvard Medical School, Armenise Building, Room D2-137, 200 Longwood Avenue, Boston, Massachusetts 02115, USA
* Author to whom correspondence should be addressed.
Received: 6 February 2008 / Revised: 15 February 2008 / Accepted: 15 February 2008 / Published: 18 February 2008
(This article belongs to the collection Prodrugs)
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Most cancer therapeutics (chemo, radiation, antibody-based, anti-angiogenic)are at best partially and/or temporarily effective. In general, the causes for failure can besummarized as: (i) poor diffusion and/or nonuniform distribution of drug/prodrugmolecules in solid tumors; (ii) high drug concentration and retention in normal tissues(leading to side effects); (iii) requirement for plasma-membrane permeability and/orinternalization of drug/prodrug molecules; (iv) low uptake of drug by tumor; (v) lack ofretention of drug within tumor (most have gradient-driven reversible binding); and (vi)multidrug resistance. We are developing an innovative technology that aims to surmountthese problems by actively concentrating and permanently entrapping radioimaging andradiotherapeutic prodrugs specifically within solid tumors. The approach will enablenoninvasive sensing (imaging) and effective therapy of solid tumors, allowing tumordetection, diagnosis, and treatment to be closely coupled (personalized medicine).
Keywords: Prodrug; solid tumors; radioiodine; radioimaging; radiotherapy Prodrug; solid tumors; radioiodine; radioimaging; radiotherapy
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Kassis, A.I.; Korideck, H.; Wang, K.; Pospisil, P.; Adelstein, S.J. Novel Prodrugs for Targeting Diagnostic and Therapeutic Radionuclides to Solid Tumors. Molecules 2008, 13, 391-404.

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