Temposartan Treatment for Oxidative Stress and Hypertension

As many as 60 million Americans have hypertension, the medical term for high blood pressure. Uncontrolled hypertension is a major factor in many cases of death and disability resulting from heart attack, stroke, and kidney failure. Current guidelines for the treatment of hypertension recommend an angiotensin receptor blocker (ARB) or an angiotensin-converting enzyme inhibitor (ACEI) as first-or second-line therapy. The limits of benefit by the renin system intervention may have been reached with current ACEIs and ARBs because combination therapy does not appear to provide further protection against heart attacks and was achieved at the cost of increased adverse events. Georgetown University researchers have developed novel compound adducts that combine an antioxidant, tempol, with ARBs such as telmisartan. It was found that the combination of tempol with an ARB (i.e. telmisartan) either given as two agents together or as a novel, ester-linked compound (tempol/telmisartan adduct) is more effective than either compound alone in reducing vascular superoxide concentrations in smooth muscle cells cultured from hypertensive rats, and in reducing blood pressure in conscious, hypertensive rats. The tempol/telmisartan adduct both retained the full effect of either drug on angiotensin receptor binding and showed a 100-fold to 1,000- fold enhanced sensitivity as a cellular antioxidant.

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