Patent Issued on New Antibiotic Technology

A U.S. patent has issued that covers new technology for killing antibiotic-resistant bacteria by using the pathogen's own resistance enzyme. Called Enzyme Catalyzed Therapeutic Activation (ECTA), the new technology is being applied to drug resistance in infectious diseases, especially hospital-acquired infections.

ECTA exploits the resistance enzyme by mimicking the biologic molecule, or so-called substrate, with which the enzyme normally reacts. The ECTA drug carries a potent toxin hidden within its chemical structure through the walls of the unsuspecting diseased cell. Once inside the cell, the resistance enzyme catalyzes the release and activation of the toxin, causing the cell to self-destruct. Diseased cells are more susceptible to the drug and its payload because they have higher concentrations of the resistance enzyme.

The developer of the technology, NewBiotics Inc. (San Diego, CA, USA), is designing ECTA drugs to overcome antibiotic resistance in bacteria that results when the resistance enzyme beta-lactamase is overproduced in response to penicillin and cephalosporin antibiotics. The company's antibiotic candidate, NB2001, is a new class of cephalosporin that provides a two-pronged attack against drug-resistant and nonresistant bacteria.
Against nonresistant bacteria, NB2001 acts like a typical antibiotic to block bacterial cell-wall synthesis. When NB2001 enters the cell wall of an antibiotic-resistant bacterium containing beta-lactamase, the resistance enzyme recognizes the drug as its normal substrate. Upon reacting with the drug, however, the enzyme inadvertently triggers the release and activation of the bactericide triclosan concealed within NB2001, causing the bacterium to self-destruct.

In laboratory tests, NB2001 was shown to be 30 times more effective than penicillin in nonresistant bacteria and 1,000 times more toxic to resistant bacteria than to nonresistant bacteria. The drug has also exhibited good activity, similar to that of vancomycin, against Staphylococcus aureus. NewBiotics is also using its ECTA technology to develop anticancer drugs.

"Drug-resistant bacterial infections, particularly nosocomial infections, continue to be a major problem throughout the world,” said H. Michael Shepard, president and chief scientific officer of NewBiotics. "We're applying our understanding of enzyme production in antibiotic-resistant bacteria to transform drug resistance into therapeutic advantage.”



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