Saturday, February 4, 2017

Drugs in Clinical Pipeline: AZD5718 | 5-Lipoxygenase Activating Protein (FLAP) Inhibitor | Treatment of Cardiovascular Disorders

AZD5178 is an orally available small molecule inhibitor of 5-lipoxygenase activating protein (FLAP) for the treatment of inflammatory diseases. In a 2016 publication, researchers have disclosed novel pyrazoles that inhibit 5 -lipoxygenase activating protein (FLAP) and therefore leukotriene production. The publication further reports the utility of such pyrazoles in treating and/or preventing clinical conditions including cardiovascular diseases (CVD), such as atherosclerosis, coronary artery disease (CAD), coronary heart disease (CHD), heart failure (HF), high risk coronary artery disease (HRCAD), and abdominal aortic aneurysms (AAA). Also, methods for their therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds are disclosed.

AstraZeneca is developing a crystalline and amorphous oral suspension of AZD5718 for the treatment of cardiovascular disorders. It is under Phase-1 trials for coronary artery disease (in UK, USA). 
1. Broddefalk, J. O.; et. al. Pyrazole derivatives useful as 5-lipoxygenase activating protein (flap) inhibitors. WO2016177703A1
2. A Study to Estimate the Effect of AZD5718 on the Pharmacokinetics (What Does the Body Does to the Drug) of Rosuvastatin to Measure the Relative Bioavailability (the Extent to Which a Drug or Other Substance Becomes Available to the Body) of AZD5718 Oral Suspension vs AZD5718 Immediate Release Tablet. NCT02963116
3. A Study to Assess the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of AZD5718 After Single and Multiple Ascending Dose Administration to Healthy Male Subjects. NCT02632526
Note: No article/publication is available for AZD5718. This report is based on in-house searches done for the molecule. It will be updated regularly.
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