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Activation of prodrugs by antibody‐enzyme conjugates: a new approach to cancer therapy
Author(s) -
Senter Peter D.
Publication year - 1990
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.4.2.2404820
Subject(s) - prodrug , monoclonal antibody , enzyme , adept , chemistry , conjugate , in vivo , antibody , drug , cancer cell , pharmacology , cancer , biochemistry , cancer research , biology , immunology , mathematical analysis , genetics , mathematics , microbiology and biotechnology
A new strategy for the delivery of cytotoxic agents to solid tumors is described in which monoclonal antibodies are used as carriers for enzymes to tumor cell surfaces. The enzymes are chosen for their abilities to convert relatively noncytotoxic drug precursors (prodrugs) into active anticancer drugs. The drugs thus formed can then penetrate into nearby tumor cells, resulting in cell death. A number of prodrugs have been developed that can be transformed into active anticancer drugs by enzymes of both mammalian and non‐mammalian origin. The enzymes have been shown to localize into tumors when linked to monoclonal antibodies that bind to tumor‐associated antigens. In vivo studies indicate that MAb‐enzyme/prodrug combinations can result in antitumor activities significantly greater than those of the prodrugs or drugs given alone. This is most likely due to the generation of large amounts of active drug at the tumor site.— S enter , P. D. The activation of prodrugs by antibody‐enzyme conjugates: a new approach to cancer therapy. FASEB J. 4: 188‐193; 1990.