Oral 5lipoxygenaseactivating protein inhibitors

An oral small molecule inhibitor of 5-lipoxygenase-activating protein (FLAP), DG-031, of unknown structure, is in clinical trials with CHD patients. FLAP inhibitors are anticipated to reduce proinflammatory leukotriene mediators such as the potent chemotactic agent, LTB4 (Figure 6). In a 4-week phase II trial in patients with a previous history of MI, DG-031 (250, 500, and 750 mg day" 1 p.o.) at the highest dose reduced serum LTB4 (26%) and MPO (12%) levels as well as soluble intercellular adhesion molecule. As discussed previously, MPO and LTB4 are inflammatory markers associated with a higher risk of CHD. Plasma CRP levels were also reduced at the highest dose, but the response did not reach statistical significance. Accompanying these changes, LDLc levels increased slightly, by 8% with the highest dose.92 These results represent the first demonstration that two key biomarkers of inflammation were reduced following oral dosing with an anti-inflammatory agent in a CHD patient population. It remains to be seen whether these biomarker results translate to a corresponding benefit in actual clinical events, especially given the absence of any profound changes in LDLc, in phase III trials.

Dealing With Back Pain

Dealing With Back Pain

Deal With Your Pain, Lead A Wonderful Life An Live Like A 'Normal' Person. Before I really start telling you anything about me or finding out anything about you, I want you to know that I sympathize with you. Not only is it one of the most painful experiences to have backpain. Not only is it the number one excuse for employees not coming into work. But perhaps just as significantly, it is something that I suffered from for years.

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