Vasopeptidase inhibitors: a double whammy on heart disease by Mark Greener

The cardiovascular market is one of the most competitive and crowded,although it continues to grow at around 10% per annum. In recent years, the trend in cardiovascular pharmacological innovation has been towards ever-more targeted therapies - the angiotensin II receptor antagonists, for example. However, a number of new agents currently in late-stage clinical trials buck this trend by targeting two enzymes at once. This delivers a double whammy to the renin-angiotensin system, which might translate into clinical benefits over existing cardiovascular medications in both hypertension and heart failure.

In March, a review in Trends in Pharmacological Sciences (2001;22:106-109) examined the therapeutic potential offered by the new drugs, known collectively as vasopeptidase inhibitors. In contrast to the prevailing tendency to target a single enzyme, VPIs block the action of both ACE and neutral endopeptidase (also known as neprilysin). ACE and NEP are members of the metallopeptidase group of enzymes, and their specificity for both substrates and inhibitors partly overlaps.

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