Pharmos Corporation announced the dosing of the first patients in the US using its compound levotofisopam (S-tofisopam) to treat patients with hyperuricemia and gout. This phase 2a proof-of-concept trial is being conducted at the Duke Clinical Research Unit of Duke University and the principal investigator is John Sundy, MD, PhD an expert in the treatment of gout. The trial is designed to assess the safety and efficacy of levotofisopam as a uric acid lowering agent in patients with gout.
This trial follows two phase 1 clinical studies that were completed by Vela Pharmaceuticals (merged with Pharmos in October 2006). In these studies, conducted in healthy volunteers in the United Kingdom and The Netherlands, levotofisopam treatment was generally well tolerated and was associated with a large and rapid reduction in serum uric acid values.
Levotofisopam is the S-entantiomer of the racemic mixture RS-tofisopam, a well tolerated, effective, nonsedating agent used for the treatment of a variety of disorders associated with stress or autonomic instability. Racemic tofisopam is not approved in the US but has been approved since 1974 and marketed in more than 20 other countries around the world. Dextofisopam, the R-enantiomer, is being developed for the treatment of irritable bowel syndrome (IBS) and has completed testing through phase 2b in the US.
Pharmos owns the rights to both R- and S-tofisopam, the two enantiomers of racemic tofisopam, through two US issued composition-of-matter patents.
Unlike allopurinol, a generic medication commonly used to treat gout patients, levotofisopam does not inhibit xanthine oxidase. Although the precise mechanism by which it lowers uric acid has not been fully elucidated, available data in healthy volunteers indicate that levotofisopam has a uricosuric effect, lowering serum uric acid by increasing the excretion of uric acid by the kidneys. Thus levotofisopam could offer a mechanism of action complimentary to that of xanthine oxidase inhibitors, and may have the potential to be used as a single agent or in combination with xanthine oxidase inhibitors in gout patients who fail to adequately respond to allopurinol.
Pharmos’ strategy is to seek a partner to further develop levotofisopam for the treatment of gout after completion of this proof-of-concept clinical trial. The Company believes levotofisopam has the potential to address a poorly served population of gout patients who respond inadequately to first-line treatment, and that this population represents a substantial global market.
Date: January 10, 2012
Source: Pharmos Corporation