When linezolid (Zyvox) received federal approval in early 2000, it was the first completely new antibiotic compound to reach the pharmaceutical market in 35 years. The synthetic compound even proved effective against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VRE) bacteria, for which no other line of defense existed. Its creator, New Jersey-based Pharmacia, sounded confident that few people would become resistant to the drug. It was not to be. Within months, patients infected with MRSA and VRE were not responding to linezolid.1,2

Such quick resistance epitomizes the dilemma of antibiotics development: Drugs cost hundreds of millions of dollars and take at least a decade to develop, and then become increasingly less effective. (see 'Renewing the Fight Against Bacteria,').

In the past, a classic screening approach, which tests in vitro the inhibitory effect of synthetic and natural compounds or extracts, led to the discovery of many...

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