ARTICLE | Tools & Techniques

Another X-Ception

March 27, 2006 8:00 AM UTC

Antagonizing the mineralocorticoid receptor (MR) is an established method for treating cardiovascular diseases such as hypertension and congestive heart failure, but marketed products have been associated with problems including elevated serum potassium. Last week, Daiichi Sankyo Co. licensed from Exelixis Inc. a preclinical portfolio of MR antagonists that may obviate these problems due to increased specificity and selectivity.

Aldactone spironolactone, which was discovered over a quarter century ago, has long been recognized as an effective but flawed antihypertensive. The drug effectively lowers blood pressure by competitively inhibiting aldosterone from binding to the MR. However, it also hits other nuclear hormone receptors, causing side effects such as menstrual irregularities, male breast enlargement and other sexual side effects. ...