Copper-64-diacetyl-bis(N(4)-methylthiosemicarbazone): An agent for radiotherapy

Systemic administration of hypoxia-selective (64)Cu-diacetyl-bis(N(4)-methylthiosemicarbazone) ((64)Cu-ATSM) has increased significantly the survival time of hamsters bearing human GW39 colon cancer tumors. Radiotherapy experiments were performed in animals bearing either 7-day-old (0.5–1.0 g) or 15...

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Main Authors: Lewis, Jason S., Laforest, Richard, Buettner, Thomas L., Song, Sheng-Kwei, Fujibayashi, Yasuhisa, Connett, Judith M., Welch, Michael J.
Formato: Artigo
Idioma:en
Publicado em: The National Academy of Sciences 2001
Assuntos:
Biological Sciences
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC14733/
https://ncbi.nlm.nih.gov/pubmed/11158618
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spelling pubmed-147332001-03-07 Copper-64-diacetyl-bis(N(4)-methylthiosemicarbazone): An agent for radiotherapy Lewis, Jason S. Laforest, Richard Buettner, Thomas L. Song, Sheng-Kwei Fujibayashi, Yasuhisa Connett, Judith M. Welch, Michael J. Proc Natl Acad Sci U S A Biological Sciences Systemic administration of hypoxia-selective (64)Cu-diacetyl-bis(N(4)-methylthiosemicarbazone) ((64)Cu-ATSM) has increased significantly the survival time of hamsters bearing human GW39 colon cancer tumors. Radiotherapy experiments were performed in animals bearing either 7-day-old (0.5–1.0 g) or 15-day-old (1.5–2.0 g) tumors. Studies compared animals treated with a single dose of 0, 4, 6, 7, 8, or 10 mCi of (64)Cu-ATSM (1 Ci = 37 GBq) with or without the vasodilator hydralazine. A multiple dose regimen of 3 × 4 mCi at 72-h intervals was studied also. Single doses of >6 mCi of (64)Cu-ATSM and the dose-fractionation protocol significantly increased the survival time of the hamsters compared with controls. The highest dose, 10 mCi of (64)Cu-ATSM, increased survival to 135 days in 50% of animals bearing 7-day-old tumors, 6-fold longer than control animals' survival (20 days), with only transient leucopenia and thrombocytopenia but no overt toxicity. Human absorbed doses were calculated from hamster biodistribution; the dose-critical organs were the lower large intestine (1.43 ± 0.19 rad/mCi) and upper large intestine (1.20 ± 0.38 rad/mCi). High-resolution MRI and positron-emission tomography using a therapeutic administration of 10 mCi were used to monitor tumor volume and morphology and to assess tumor dosimetry accurately, giving a tumor dose of 81 ± 7.5 rad/mCi. (64)Cu-ATSM has increased the survival time of tumor-bearing animals significantly with no acute toxicity and thus is a promising agent for radiotherapy. The National Academy of Sciences 2001-01-30 /pmc/articles/PMC14733/ /pubmed/11158618 Text en Copyright © 2001, The National Academy of Sciences
institution US National Library of Medicine
collection PubMed Central
language en
format Article
topic Biological Sciences
spellingShingle Biological Sciences
Lewis, Jason S.
Laforest, Richard
Buettner, Thomas L.
Song, Sheng-Kwei
Fujibayashi, Yasuhisa
Connett, Judith M.
Welch, Michael J.
Copper-64-diacetyl-bis(N(4)-methylthiosemicarbazone): An agent for radiotherapy
description Systemic administration of hypoxia-selective (64)Cu-diacetyl-bis(N(4)-methylthiosemicarbazone) ((64)Cu-ATSM) has increased significantly the survival time of hamsters bearing human GW39 colon cancer tumors. Radiotherapy experiments were performed in animals bearing either 7-day-old (0.5–1.0 g) or 15-day-old (1.5–2.0 g) tumors. Studies compared animals treated with a single dose of 0, 4, 6, 7, 8, or 10 mCi of (64)Cu-ATSM (1 Ci = 37 GBq) with or without the vasodilator hydralazine. A multiple dose regimen of 3 × 4 mCi at 72-h intervals was studied also. Single doses of >6 mCi of (64)Cu-ATSM and the dose-fractionation protocol significantly increased the survival time of the hamsters compared with controls. The highest dose, 10 mCi of (64)Cu-ATSM, increased survival to 135 days in 50% of animals bearing 7-day-old tumors, 6-fold longer than control animals' survival (20 days), with only transient leucopenia and thrombocytopenia but no overt toxicity. Human absorbed doses were calculated from hamster biodistribution; the dose-critical organs were the lower large intestine (1.43 ± 0.19 rad/mCi) and upper large intestine (1.20 ± 0.38 rad/mCi). High-resolution MRI and positron-emission tomography using a therapeutic administration of 10 mCi were used to monitor tumor volume and morphology and to assess tumor dosimetry accurately, giving a tumor dose of 81 ± 7.5 rad/mCi. (64)Cu-ATSM has increased the survival time of tumor-bearing animals significantly with no acute toxicity and thus is a promising agent for radiotherapy.
author Lewis, Jason S.
Laforest, Richard
Buettner, Thomas L.
Song, Sheng-Kwei
Fujibayashi, Yasuhisa
Connett, Judith M.
Welch, Michael J.
author_facet Lewis, Jason S.
Laforest, Richard
Buettner, Thomas L.
Song, Sheng-Kwei
Fujibayashi, Yasuhisa
Connett, Judith M.
Welch, Michael J.
author_sort Lewis, Jason S.
title Copper-64-diacetyl-bis(N(4)-methylthiosemicarbazone): An agent for radiotherapy
title_short Copper-64-diacetyl-bis(N(4)-methylthiosemicarbazone): An agent for radiotherapy
title_full Copper-64-diacetyl-bis(N(4)-methylthiosemicarbazone): An agent for radiotherapy
title_fullStr Copper-64-diacetyl-bis(N(4)-methylthiosemicarbazone): An agent for radiotherapy
title_full_unstemmed Copper-64-diacetyl-bis(N(4)-methylthiosemicarbazone): An agent for radiotherapy
title_sort copper-64-diacetyl-bis(n(4)-methylthiosemicarbazone): an agent for radiotherapy
publisher The National Academy of Sciences
publisher_facet The National Academy of Sciences
publishDate 2001
url https://ncbi.nlm.nih.gov/pmc/articles/PMC14733/
https://ncbi.nlm.nih.gov/pubmed/11158618
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