Chemical compounds

Details Chemical compounds Chemical compounds

C - Chemistry, Metallurgy

12

N

C12N 15/57 (2006.01) A61K 38/48 (2006.01) A61K 47/48 (2006.01) C07C 237/36 (2006.01) C07K 5/062 (2006.01) C07K 16/30 (2006.01) C12N 9/48 (2006.01) C12N 9/96 (2006.01)

Patent

CA 2227040

Antibody Directed Enzyme Prodrug Therapy (ADEPT) systems for use in cancer based on mutated carboxypeptidase B (CPB) enzymes. Enzyme conjugates for ADEPT are substantially non-immunogenic in humans comprising a targeting moiety (for example an antibody) capable of binding with a tumour associated antigen, the targeting moiety being linked to a mutated form of a CPB enzyme capable of converting a prodrug into an antineoplastic drug wherein the prodrug is not significantly convertible into antineoplastic drug in humans by natural unmutated enzyme. A preferred enzyme mutant is human pancreatic CPB comprising a Lys or Arg residue at position 253. Suitable mustard prodrugs are disclosed in the specification.

Cette invention se rapporte à des systèmes de thérapie par promédicaments contenant des enzymes ayant une action sur des anticorps (systèmes ADEPT), lesdits systèmes servant à traiter les cancers liés aux enzymes carboxypeptidases B (CPB) ayant subi une mutation. Les conjugués d'enzymes destinés aux systèmes ADEPT sont sensiblement non immunogènes chez les humains comportant une fraction ciblante (par exemple un anticorps) pouvant se lier à un antigène associé à une tumeur, la fraction ciblante étant liée à une forme résultant d'une mutation d'un enzyme CPB capable de transformer un promédicament en un médicament antinéoplasique, ce promédicament n'étant pas transformable de façon significative en médicament antinéoplasique chez les humains par l'enzyme naturel n'ayant pas subi de mutation. Un enzyme mutant préféré est le CPB pancréatique d'origine humaine qui comporte un résidu de lysine et d'arginine en position 253. L'invention concerne également des promédicaments adaptés à base d'ypérite.

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