The Story of ZYVOX | What ZYVOX’s Discovery Means
Would ZYVOX ever have been discovered in a world without superbugs? Indeed, necessity is the mother of invention, an adage apropos for another reason. Just as the wisdom it conveys has stood the test of time – experts now trace its origin back to Plato’s Republic, the new science, knowledge and medical gains produced by this year’s winners will too stand the test of time.
Of the many important aspects of their achievement, three stand out.
First are the historic dimensions of ZYVOX’s discovery. When it was approved in 2000, its active ingredient linezolid was the first member of any entirely new class of antibacterial agents to reach the market in more than 35 years – specifically, the first new antibiotic with a novel mechanism of action since the first quinolone was approved in 1963.
To this day, linezolid remains the only oxazolidinone on the market.
"The approval of ZYVOX [for pediatric use] is a tremendous advance for the medical community, providing a new, effective and well-tolerated option for infants and children with certain serious infections."
- Sheldon Kaplan, M.D.,
Baylor College of Medicine
Second is its major scientific distinction, namely, its novel mechanism of action. Linezolid works by inhibiting the first step of bacterial protein synthesis, thereby also inhibiting the production of bacterial toxins. Even toxin production in MRSAs that spew up to 40 different toxins is suppressed, Brickner said.
What exactly makes linezolid’s mechanism of action so novel and so effective against multi-resistant bacterial agents?
Antibiotics kill bacteria or prevent their growth by a variety of mechanisms. The most common involve blocking bacterial cell wall synthesis or inhibiting bacterial protein synthesis. … [Being a protein synthesis inhibitor] linezolid binds to the 50S ribosomal subunit, where it blocks the formation of the initiation complex. Without this critical initiation complex, protein synthesis cannot occur, so the bacterial cell cannot carry out essential functions and dies. Most other antibiotics that inhibit protein synthesis act at a much later step … in protein synthesis than does linezolid. This explains why linezolid is unaffected by resistance mechanisms to other protein synthesis inhibitors or bacterial resistance mechanisms in general. 6
In other words, linezolid does not demonstrate cross-resistance with any known antibiotics – including vancomycin; it also has the double benefit of inducing resistance at a very slow rate. (In fact, there have been less than ten cases of MRSA resistance to linezolid.) Specifically, it explains why linezolid is effective against resistant strains of Gram-positive pathogens.
Of the many important aspects of their achievement, three stand out.
First are the historic dimensions of ZYVOX’s discovery. When it was approved in 2000, its active ingredient linezolid was the first member of any entirely new class of antibacterial agents to reach the market in more than 35 years – specifically, the first new antibiotic with a novel mechanism of action since the first quinolone was approved in 1963.
To this day, linezolid remains the only oxazolidinone on the market.
"The approval of ZYVOX [for pediatric use] is a tremendous advance for the medical community, providing a new, effective and well-tolerated option for infants and children with certain serious infections."
- Sheldon Kaplan, M.D.,
Baylor College of Medicine
Second is its major scientific distinction, namely, its novel mechanism of action. Linezolid works by inhibiting the first step of bacterial protein synthesis, thereby also inhibiting the production of bacterial toxins. Even toxin production in MRSAs that spew up to 40 different toxins is suppressed, Brickner said.
What exactly makes linezolid’s mechanism of action so novel and so effective against multi-resistant bacterial agents?
Antibiotics kill bacteria or prevent their growth by a variety of mechanisms. The most common involve blocking bacterial cell wall synthesis or inhibiting bacterial protein synthesis. … [Being a protein synthesis inhibitor] linezolid binds to the 50S ribosomal subunit, where it blocks the formation of the initiation complex. Without this critical initiation complex, protein synthesis cannot occur, so the bacterial cell cannot carry out essential functions and dies. Most other antibiotics that inhibit protein synthesis act at a much later step … in protein synthesis than does linezolid. This explains why linezolid is unaffected by resistance mechanisms to other protein synthesis inhibitors or bacterial resistance mechanisms in general. 6
In other words, linezolid does not demonstrate cross-resistance with any known antibiotics – including vancomycin; it also has the double benefit of inducing resistance at a very slow rate. (In fact, there have been less than ten cases of MRSA resistance to linezolid.) Specifically, it explains why linezolid is effective against resistant strains of Gram-positive pathogens.