Faropenem daloxate - antibiotic
The overuse and misuse of antibiotics are contributing to an alarming growth in the resistance of bacteria to many or even all available antibiotic agents. They mutate into forms that are unaffected by the drugs, usually because they produce b-lactamase that destroys the drug molecules. A particular problem exists in treatments for respiratory infections. Several penem antibiotics have been developed that have stability to β-lactamase, as well as high potency and a broad spectrum of activity, such as imipenem, ertapenem and meropenem, but none of these is orally available.
Launched in Japan in 1997, faropenem has a similarly broad spread of activity, being effective against many different Gram positive and Gram negative bacteria, including those that produce extended spectrum β-lactamases.1
Now an orally available pro-drug, faropenem daloxate, has been developed; it is converted to the active moiety faropenem by hydrolysis in the plasma.
In a randomised, double blind, placebo controlled Phase I study in 48 male and female subjects aged from 18 to 86, doses of 300mg were given after an overnight fast. The agent was shown to be well tolerated and safe, with no serious adverse events being observed, and the only minor side-effect being a headache.2 A further non-blinded, randomised, two-way crossover trial in 12 healthy males looked at the effect of food consumption on the effectiveness of the drug. The subjects were given a 300mg dose either after fasting or a high fast breakfast, and it had no effects on the effectiveness of the drug.3
The pro-drug was discovered by Suntory, of Japan, and has been licensed to Bayer. It is currently undergoing Phase III trials for the treatment of respiratory tract infections in the US and Europe. Bayer hopes it will be on the market by 2004.