Novel drugs targeting hypertension: renin inhibitors and beyond.

The idea of renin inhibition is not new, and evidence of attempts to block its activity can be found in the literature as early as the 1950s. Throughout the latter half of the 20th century, development of renin inhibitors encountered many problems. Only recently, after the x-ray crystallography of its active site, new and effective renin inhibitors have been developed. The purpose of this review is to describe the basic evidence to support the efficacy of these agents and to elaborate on new possibilities of their use and combination with other antihypertensive drugs.