Fap-activated anti-tumor compounds

Details Fap-activated anti-tumor compounds Fap-activated anti-tumor compounds

C - Chemistry, Metallurgy

07

K

C07K 5/06 (2006.01) A61K 47/48 (2006.01) C07K 5/103 (2006.01) C07K 5/117 (2006.01) C07K 9/00 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2472296

The invention relates to a prodrug that is capable of being converted into a drug by the catalytic action of human fibroblast activation protein (FAP.alpha.), said prodrug is chemically stable under physiological conditions and can be used for the manufacture of physically stable aqueous formulations. It has a cleavage site which is recognised by FAP.alpha., and the drug released by the enzymatic activity of FAP.alpha. is cytotoxic or cytostatic under physiological conditions.

L'invention concerne un promédicament pouvant être transformé en un médicament par l'action catalytique de la protéine d'activation des fibroblastes humains (FAP.alpha.), ledit promédicament étant chimiquement stable dans des conditions physiologiques et pouvant être utilisé dans la fabrication de formulations aqueuses physiquement stables. Ce promédicament présente un site de clivage qui est reconnu par la protéine FAP.alpha., et le médicament libéré par l'activité enzymatique de la protéine FAP.alpha. est cytotoxique ou cytostatique dans des conditions physiologiques.

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