Olmesartan medoxomil (CS-866) - An angiotensin II receptor blocker for treatment of hypertension

Olmesartan medoxomil (CS-866) is an angiotensin II receptor blocker under F DA review for treatment of hypertension. It is a tetrazolylbiphenyl-substit uted imidazole derivative that undergoes de-esterification to form its acti ve metabolite, olmesartan, The steady-state AUC and peak plasma concentrati on of olmesartan increase linearly with dose. The drug's absolute bioavaila bility is 26%, which falls in the middle of the range seen with the six FDA -approved ARBs (Iosartan, valsartan, irbesartan, candesartan, eprosartan, a nd telmisartan), Like the six other ARBs, olmesartan medoxomil can be taken once daily without regard to meals. Placebo-controlled trials have establi shed its safety and efficacy at doses from 2.5 to 80 mg once daily in patie nts with mild to moderate hypertension. In addition, a comparative trial ha s shown olmesartan medoxomil to have a more potent antihypertensive effect than Iosartan and valsartan. Its dose-response curve plateaus at 20 to 40 m g. Because this agent does not undergo P-450-mediated biotransformation, it s likelihood of drug interactions is minimal.