Experimental drug drop exceeds current medications
Researchers have presented interesting results for the European League Against Rheumatism 2011 (EULAR) Congress. A medicine for gout research lesinurad was able to get a rapid and sustained reduction in urate levels in gout patients who did not receive the desired results with uric acid-lowering drugs used.
“Lesinurad, an inhibitor of the URAT1 increases urinary excretion of uric acid, is a potential treatment option for patients with gout,” said Dr. Fernando Perez-Ruiz, Spanish researchers from the Hospital de Cruces, Barakaldo Vizcaya.
Lenisurad activity has shown a significant reduction of urate is used both alone and in combination with prescription Allopurinal (brand name Zyloprim) or febuxostat (Uloric). The Spanish study involved 208 patients with gout who had high levels of urate in the blood for at least 6 months, even while taking the drug allopurinol gout. Patients continued with allopurinol and were randomly assigned to receive placebo or lesinurad at 200 mg, 400 mg or 600 mg for four weeks.
The three groups that received lesinurad showed significantly lower levels of uric acid at the end of the month. The percentage of patients achieving target levels of uric acid after treatment was 28% in the placebo group, 71% in the 200 mg, 76% in the 400 mg group and 87% in the 600 mg.
After the first 4 weeks of treatment, 115 patients entered an extension phase in which most of them continued treatment with 200 mg of lesinurad. At week 28, 83% of the first 30 evaluable patients were in the target serum urate levels without serious adverse effects.
This is supposed to decrease uric acid levels have a significant impact on the dissolution and resorption of gout tophi (deposits of crystallized uric acid) in the body.
New drugs for gout are few and far between, but today there are at least eight medicines drop “in the pipeline.” Drop the first drug approved in 40 years, febuxostat (Uloric brand name) in 2009. In 2010 the FDA approved Krystexxa, an intravenous drug for chronic and severe gout who are unresponsive to other treatments. Due to the stringent approval process by FDA, may be some time before patients can purchase Lenisurad U.S. drop.
Lesinurad The mechanism of action is different from that of allopurinol and febuxostat. Both allopurinol and febuxostat are xanthine oxidase inhibitors that decrease the production of uric acid. Is a uricosuric drug Lesinurad increasing the excretion of uric acid by the kidneys.
Initial studies show that lesinurad can have significant advantages over other existing uricosuric drugs, probenecid (Benemid), including less interaction with other drugs and more effective in patients taking diuretics. This additional benefit is that lesinurad is also active against another important regulator of the secretion of uric acid, OAT4. OAT4 is believed to be responsible for high levels of uric acid in gouty arthritis patients whose condition is caused or aggravated by diuretics.
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