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Synthesis and biodistribution of [11C]SN-38

✍ Scribed by Scott M. Apana; Lawrence W. Anderson; Marc S. Berridge

Publisher
John Wiley and Sons
Year
2010
Tongue
French
Weight
222 KB
Volume
53
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

SN‐38 (7‐ethyl‐10‐hydroxy camptothecin) is a topoisomerase I inhibitor that is the active chemotherapeutic agent of irinotecan, indicated for colon cancer. Because the rate of response to irinotecan treatment is low, it is of interest to have a prognostic indicator to identify and more selectively treat those who are likely to respond to treatment. We have therefore prepared SN‐38 labeled with carbon‐11. SN‐38 was prepared by radical oxidation of 3‐[^11^C]propionaldehyde and subsequent radical addition of the ethyl fragment to 10‐hydroxycamptothecin. Labeled propionaldehyde was prepared by reaction of methyl iodide with 2‐lithiomethyl‐1,3‐dioxolane. Overall chemical yield was 34% from carbon dioxide. The murine biodistribution and radiation dosimetry of [^11^C]SN‐38 was measured by PET scanning in preparation for initial human studies. Biodistribution was fairly uniform except for hepatobiliary and urinary excretion. Copyright © 2010 John Wiley & Sons, Ltd.

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