Pharmacokinetics of iodine-123-IMBA for melanoma imaging
<p>The development of an effective radiopharmaceutical with affinity for malignant melanoma has been a research goal for some time. The early detection of melanoma metastases would greatly improve the therapy outcome for this disease. This article describes the synthesis of radioiodinated IMBA...
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| Hauptverfasser: | , , , , |
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| Dokumenttyp: | Article (Journal) |
| Sprache: | Englisch |
| Veröffentlicht: |
January 1997
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| In: |
Journal of nuclear medicine
Year: 1997, Jahrgang: 38, Heft: 1, Pages: 127-133 |
| ISSN: | 2159-662X |
| Online-Zugang: | Verlag, lizenzpflichtig, Volltext: https://jnm.snmjournals.org/content/38/1/127
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| Verfasserangaben: | Ciaran Nicholl, Ashour Mohammed, William E. Hull, Bernd Bubeck, Michael Eisenhut |
| Zusammenfassung: | <p>The development of an effective radiopharmaceutical with affinity for malignant melanoma has been a research goal for some time. The early detection of melanoma metastases would greatly improve the therapy outcome for this disease. This article describes the synthesis of radioiodinated IMBA, N-(2-diethylaminoethyl)-3-[<sup>123</sup>I/<sup>131</sup>I]iodo- 4-methoxybenzamide 8, its organ distribution, its comparison with BZA and other benzamides, and demonstrates the scintigraphic efficacy of the title compound with three melanoma patients. <b>Methods:</b> The syntheses and radioiodination of eight benzamide derivatives are described. After intravenous injection into C57BI 6-mice subcutaneously transplanted with B16 melanoma, the organ distribution of the respective benzamides were investigated at 1 and 6 hr. n-octanol/phosphate buffer partition coefficients. The whole-body retention, erythrocyte and serum protein bound fractions of radioiodinated benzamides were measured. <b>Results:</b> While structural changes in the amide substituents of N-(2-dialkylaminoalkyl)- 4-iodobenzamides 2-7 resulted in no improvement in organ distribution compared with BZA, the 3-iodo-4-methoxyphenyl form of IMBA showed high melanoma uptake with significantly higher melanoma/nontarget tissue ratios. Compared with BZA the average ratio improved after 1 hr by a factor of eight and was still four times better after 6 hr. BZA and IMBA exhibit almost identical n-octanol/phosphate buffer partition coefficients, however, IMBA has a faster urinary excretion facilitated by a lower affinity to erythrocytes and serum proteins; this could explain the improved tissue partinioning observed. Scintigraphy of patients with melanoma metastases confirmed the promising characteristics derived from the animal studies <b>Conclusion:</b> Due to rapid background clearance and high melanoma affinity, IMBA showed high tumor contrast already at 4 hr after injection which makes it a promising new radiopharmaceutical for the scintigraphic detection of melanoma metastases.</p> |
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| Beschreibung: | Gesehen am 09.122024 |
| Beschreibung: | Online Resource |
| ISSN: | 2159-662X |