Paul Scherrer Institut

University Of Zürich

Solidago Ag

Zurich, Universtitat

Stefan Mundwiler

Roger Alberto

Robert Waibel

Hans-Jörg Treichler

Dave R Van Staveren

Susanne Barbara Kunze

Martin T Küenzi

Hector Knight Castro

Jakob Nüesch

The present invention relates to a metal complex of the general formula M(L), wherein each L is independently selected and represents a ligand and at least one L is vitamin B(cyanocobalamin) or a derivative thereof bound through the nitrogen atom of its cyanide group to M, which is an element selected from the transition metals, thus, forming a M-NC-[Co] moiety with [Co] representing vitamin Bwithout cyanide and wherein n is 1, 2, 3, 4, 5 or 6. The complex can be prepared by mixing a precursor molecule with vitamin B. The metal complexes can be used for radiodiagnostics, chemotherapy and radionuclide therapy. 

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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.

Cobalamine derivatives useful for diagnosis and treatment of abnormal cellular proliferation

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Aarau, Switzerland

Stefan Mundwiler