Carvedilol Phosphate, CAS number 72956-09-3, is known as the blockbuster medication Coreg CR. GlaxoSmithKline holds the patent for Coreg CR until February 7, 2016. Useful for treating patients with hypertension and mild-to-severe chronic heart failure of ischemic or cardiomyopathic origin, carvedilol phosphate is available for research and development from LGM Pharma.
In the group of drugs called beta-blockers, carvedilol phosphate works by affecting the heart and circulation, creating better blood flow through arteries and veins. One remarkable study, coined COPERNICUS was actually stopped early due to phenomenal results! This double blind study involved 2,289 patients with heart failure at rest or with minimal exertion and a left ventricular ejection fraction average of 20%. All patients in this study had received prior and unsuccessful treatment with the medications digitalis, diuretics and ACE inhibitors. These patients were then randomized to a placebo or carvedilol. The dose of carvedilol phosphate was titrated from a starting dose of 3.125 milligrams twice daily to the maximum tolerated dose or up to 25 milligrams, two times daily. There was a minimum of 6 weeks of treatment for study participants, and most patients achieved the target dose of 25 milligrams. This study was conducted in the United States, Eastern and Western Europe, Israel, and Canada. The primary end point of this trial was all-cause mortality, however, cause-specific mortality and the risk of death or hospitalization were also examined. The developing trial data was monitored by a data monitoring committee, and mortality analyses were adjusted for these multiple looks. However, this trial was stopped after a median follow-up of 10 months due to an observed 35% reduction in mortality.
With side effects including nausea, vomiting, diarrhea, dry eyes, joint pain, tiredness, and weakness, the carvedilol phosphate capsules are tolerable and efficacious for many patients. The capsules are available in dosages of 10, 20, 40 and 80 milligrams each. Flamel and GlaxoSmithKline (GSK) reported total revenues for the first quarter in 2012 of $7.3 million, with an uptick in growth from the first quarter in 2011 due to an increased production of Coreg CR microparticles.
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