Conjugate, combined two-component systems intended for use in a host, compounds or a pharmaceutically acceptable salt thereof, enzyme, polynucleotide and de02 nucleotide sequence, vector, host cell, enzyme and conjugate production processes and treatment of neoplastic cells in a host, pharmaceutical composition and plasmid

摘要

"CONJUGATE, SYSTEM OF TWO COMBINED COMPONENTS INTENDED FOR USE IN A HOST, COMPOUNDS OR A SALT OF THESE PHARMACEUTICALLY ACCEPTABLE, ENZYME, SEQUENCE OF POLINUCLEOTIDS AND NUCLEOTIDES, VECTOR OF A HOSPITAL AND HOSTED CELL, A PROCEDURE FOR HOSTING OF NEOPLASTIC CELLS IN A HOST, PHARMACEUTICAL AND PLASMIDIC COMPOSITION ". Antibody-directed Enzyme Pro-Drug Therapy (ADEPT) systems for use in cancer based on transformed carboxypeptidase B (CPB) enzymes. Enzyme conjugates for ADEPT are substantially non-immunogenic in humans, comprising a targeting moiety (e.g. an antibody) capable of binding with a tumor-associated antigen, the target moiety being linked to a transformed form of a CPB enzyme capable of converting a prodrug in an anti-neoplastic drug, where the prodrug is not significantly convertible into an anti-neoplastic drug in humans by the unprocessed natural enzyme. A preferred enzyme mutant is human pancreatic CPB, comprising a Lys or Arg residue at position 253. Suitable mustard prodrugs are presented in the specification.