Long-acting Leukotriene Receptor Antagonist Shows Promise In RA

NEW YORK (Reuters Health) - In patients with moderately severe rheumatoid arthritis, BIIL 284, an experimental oral long-acting leukotriene B4 (LTB4) receptor antagonist effectively inhibits LTB4-induced expression of the adhesion molecule Mac-1 (CD11b/CD18), results indicate.

Noting that LTB4 plays a key role in the pathophysiology of rheumatoid arthritis, investigators speculate that "longer treatment with BIIL 284 may result in clinical benefit for patients with rheumatoid arthritis," something this study was not designed to address.

Researchers from Boehringer-Ingelheim Pharma KG in Biberach an der Riss, the drug's developer, and elsewhere studied the pharmacokinetics and inhibition of LTB4-induced Mac-1 expression in leukocytes by BIIL 284 (25 or 150 mg once daily) or placebo in 26 adult rheumatoid arthritis patients.

Dr. Gerhard Steinmann and colleagues report in the February issue of that Annals of the Rheumatic Diseases, that both doses of BIIL 284 "considerably to completely" inhibited LTB4-induced Mac-1 expression starting at day 1 and the effect lasted for at least 6 hours after the last treatment on day 14.

The difference between BIIL 284 and placebo in this primary efficacy (pharmacodynamic) parameter was statistically significant with a p value of <0.005.

Based on these early results, "it is expected that BIIL 284 may be a potent inhibitor" of LTB4-mediated processes in the pathophysiology of rheumatoid arthritis, the researchers write.

Secondary clinical efficacy endpoints, including tender and swollen joint counts, pain, disease activity, erythrocyte sedimentation rate, and C-reactive protein, remained unchanged probably due to the short study duration, the researchers contend.

Over the course of 14 days, BIIL 284 was generally well tolerated, with "no specific safety risks which have to be considered in further studies," the investigators say, noting, however, long term data and exposure are needed to fully evaluate the safety of BIIIL 284.

Source: Ann Rheum Dis 2004;63:170-176. [ Google search on this article ]

MeSH Headings: Drugs, Investigational

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