PaperEnhanced tumour uptake and in vitro radiotoxicity of no-carrier-added [131i] metaiodobenzylguanidine: Implications for the targeted radiotherapy of neuroblastoma
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I-131 Metaiodobenzylguanidine Therapy of Pheochromocytoma and Paraganglioma
2016, Seminars in Nuclear MedicineCitation Excerpt :The theoretical advantages in using a high specific activity preparation are improved targeting, greater tumor concentration, and decreased potential for pharmacologic effects. The former has been demonstrated in animal models.40,42 At present, limited clinical studies with this reagent have reported it to be safe43 with a lower incidence of nausea, vomiting, and hypertension,44 although a clear advantage of higher tumor targeting has yet to be established.45
Opportunities and challenges for use of tumor spheroids as models to test drug delivery and efficacy
2012, Journal of Controlled ReleaseCitation Excerpt :Thus, glucosylated PEPE dendrimers can serve as potential delivery system for the treatment of gliomas. To assess in vivo tumor targeting and therapeutic efficacy, neuroblastoma spheroids and nude mice xenografted with human neuroblastoma cells were treated with radioisotope iodine-131-metaiodobenzylguanidine ([130] MIBG) without any added carrier [120]. The drug was uptaken successfully in the tumor in vivo, where it reduced tumor burden, and prevented regrowth of spheroid in vitro, suggesting that the spheroid results correlate well with those in the animal model.
Preclinical assessment of strategies for enhancement of metaiodobenzylguanidine therapy of neuroendocrine tumors
2011, Seminars in Nuclear MedicineCitation Excerpt :The absorbed doses in the NET-rich heart and adrenal were also greater by a similar factor. Doses to the liver and lung were higher by 30%-45%, whereas those to the remaining organs were 65%-95% less than those resulting from the administration of ca [131I]MIBG.23 The increased accumulation of activity in tumor achieved by the administration of nca [131I]MIBG corresponded to its greater efficacy.24
Radioiodinated metaiodobenzylguanidine (MIBG): Radiochemistry, biology, and pharmacology
2011, Seminars in Nuclear MedicineCitation Excerpt :Furthermore, nonradiolabeled molecules can compete with radiolabeled MIBG for NET binding, resulting in reduced tumor cell uptake of [131I]MIBG.58 Therefore, the higher SA and lower concentration of cold carrier in the final drug product enables administration of a more potent (in terms of radioactivity) therapeutic dose that has less potential to saturate the uptake process in tumor cells, thereby maximizing tumoricidal activity for the n.c.a. form of the [131I]MIBG.57 For example, to treat a patient with 800 mCi of [131I]MIBG (SA, 50 mCi/mg) prepared on the basis of isotope exchange method might contain a total MIBG mass of 16 mg (57 μmol).
A convenient solution-phase method for the preparation of meta-iodobenzylguanidine in high effective specific activity
2008, Nuclear Medicine and BiologyOptimizing MIBG therapy of neuroendocrine tumors: preclinical evidence of dose maximization and synergy
2008, Nuclear Medicine and Biology