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news.Critical Therapeutics has initiated a Phase I clinical trial to assess the safety and tolerability of an oral single dose of the R(+) isomer of experimental asthma treatment zileuton in healthy subjects.
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Twelve subjects will be randomly assigned to one of two groups of R(+) isomer zileuton (100mg or 300mg). The trial is designed to confirm that the R(+) isomer of zileuton when dosed alone for the first time has the expected prolonged pharmacokinetic and potent pharmacodynamic profile.
R(+) zileuton combined in equal proportion with its mirror image isomer, S(-) zileuton, comprise racemic zileuton, which is the pharmaceutical ingredient in Zyflo (zileuton tablets) and Zyflo CR (zileuton) extended-release tablets.
Roger Rush, vice president, preclinical development, said: “We have generated preclinical data indicating that the R(+) isomer of zileuton could be a more potent leukotriene synthesis inhibitor with a more prolonged pharmacokinetic profile than the S(-) isomer. We believe these characteristics may allow for the development of the R(+) isomer as a next generation leukotriene synthesis inhibitor that offers a reduced dosing and/or a smaller tablet size compared with Zyflo CR.”
“In addition to asthma, the successful development of the R(+) isomer may also allow for possible development opportunities in other diseases, such as chronic obstructive pulmonary disease, atherosclerosis and nasal polyps, in which the inhibition of the leukotriene pathway could provide benefit,” Rush concluded.