Anthera's first-in-class heart drug ahead of schedule

By Mike Nagle

- Last updated on GMT

Related tags: Atherosclerosis

The mid-stage trial of a drug that tackles atherosclerosis in a
totally new way is months ahead of schedule, according to its
developers Anthera.

The California-based private biopharmaceutical firm has revealed that the Phase II clinical study of A-002, its lead cardiovascular product, has completed enrolment months ahead of schedule and preliminary results are expected later this year. The drug is the first in a new class of compounds that aim to suppress the activity of secretory phospholipase A2 (sPLA2), a family of proteins that contribute to the inflammation seen in atherosclerosis, which characterises this artery-hardening disease. As this target is upstream of other inflammatory mediators, it could prove a more powerful therapeutic option. A-002 is therefore also thought to reduce other "well established markers of inflammation and cardiovascular risk in patients with stable coronary artery disease"​, said Anthera. sPLA2 is a calcium-dependent enzyme which breaks phospholipids at the sn-2 position to generate non-esterified fatty acids and lysophospholipids (LPL). It is secreted by many cells within the body as a reaction to inflammatory signals such as tumour necrosis factor (TNF) and interleukin-1 (IL-1). Of the ten different forms of sPLA2 known, groups IIA, V and X appear to be involved in the development of atherosclerosis. This is due to their ability to modify low density lipoprotein (LDL, or 'bad' cholesterol) to increase its retention on blood vessel walls, thus making it more susceptible to oxidation and uptake by macrophages and thus promoting foam cell formation. They also decrease the ability of high density lipoprotein (HDL, or 'good' cholesterol) to help the body to get rid of cholesterol. Anthera recently showed some of the animal data for the drug at the Congress on Inflammation in Copenhagen, Denmark. Treatment with A-002 resulted in statistically significant reductions in atherosclerosis and cholesterol by 50% and 25% respectively, when compared with the untreated group. The Phospholipase Levels And Serological Markers of Atherosclerosis (PLASMA) trial will initially test 200 patients although the company said it is also contemplating using the unexpected extra time to expanding the trial. At the same time, it is also sponsoring an academic trial at the University of Toronto, Canada. During this study, 164 patients undergoing percutaneous coronary intervention (PCI) will be given A-002 - a protocol that has just been ratified by Health Canada. An assay to measure sPLA2 is available from Cayman Chemical.

Related topics: Upstream Processing

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