The University of British Columbia

Provincial Health Services Authority

Hsiou-Ting Kuo

François Bénard

Kuo-Shyan Lin

Zhengxing Zhang

David Perrin

Helen Merkens

This application relates to compounds of Formula I. R, Rand Ris —COH, —SOH, —SOH, —SOH, —POH, —POH or —POH. Ris a linker, e.g. butylene. Ris a linkage, e.g. —O—, —S—, —S(O)—, S(O)—, —NHC(O)—, —C(O)NH—, or 1,2,3-triazole. R4 is —(CH)CH(R)(CH)— wherein Ris —(CH)CHor certain aromatic fused-ring systems. Rand Rare hydrogen or methyl. Each Xaa(if present) is an amino acid. Ris a radiolabeling group, e.g.: a radiometal chelator optionally bound by a radiometal; an aryl substituted with a radioisotope; a prosthetic group containing a trifluoroborate; or a prosthetic group containing a silicon-fluorine-acceptor moiety. The compounds may be useful for imaging prostate-specific membrane antigen (PSMA)-expressing tissues or for treating PSMA-expressing diseases (e.g. cancer).

Radiolabelled compounds for diagnosis or treatment of prostate-specific membrane antigen- expressing cancer

A compound comprising a prostate specific membrane antigen (PSMA)-targeting moiety of the following formula or of a salt or a solvate thereof. Ris O or S. Each of R, Rand Rmay be &#x2014;COH, &#x2014;SOH, &#x2014;SOH, &#x2014;POH, or &#x2014;POH, for example. Rmay be methylene or a derivative thereof, propylene or a derivative thereof, or a derivative of ethylene, optionally substituted. Ris a linker. When the PSMA-targeting moiety is linked to a radiolabeling group, the compound may be used as an imaging agent or therapeutic agent for PSMA-expressing diseases/conditions. 

Radiolabeled compounds targeting the prostate-specific membrane antigen

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Sherbrooke, Canada

Hsiou-Ting Kuo