異常な細胞の増殖の診断および治療に有効なコバラミン誘導体

Japanese Patent JP4927560

B2

The invention relates to cobalamin derivatives having no or low binding affinity to the transport protein transcobalamin II (TCII) and retaining activity as a vitamin B12 substitute, optionally carrying a therapeutic and/or diagnostic agent, such as a radioactive metal. These compounds have a much reduced accumulation rate in blood and benign organs, such as kidney and liver, compared to the accumulation rate in neoplastic tissues, and are more rapidly eliminated from blood. The invention further relates to a method of diagnosis and a method of treatment of a neoplastic disease or an infection by microorganisms in a mammal by exposing the mammal to a period of a vitamin B12 free diet, and subsequently applying a cobalamin derivative of the invention carrying a diagnostic and/or therapeutic agent. By selecting cobalamin derivatives acting as vitamin B12 substitutes, the risk of the formation of resistant off-spring in neoplastic tissue is much reduced.

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Trichler, Hans-Jörg
Albert, Roger
Weibel, Robert
Martinez, Cuenzi
Nyaesh, Jacob
Muntwiller, Stephan
Fan star ferren, darf ell

JP2006546174A

May 09, 2012

December 21, 2004

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SOLIDAGO AG
UNIVERSITAET ZUERICH
PAUL SCHERRER INSTITUT

A61K31/714; C07H23/00; A61K51/00; A61P31/00; A61P35/00

JP2233693A
JP2133469A
JP58000997A
JP10502334A
JP8510261A
JP63501015A
JP2000500753A
JP54157600A
JP57058698A

WO2003026674A1
WO2001028595A1
WO2001028592A1
WO2000062808A1
WO1999065930A1

Hajime Tsukuni
Satoko Ito
Keiko Ozawa
Toshio Miyake

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