Preclinical and clinical profile of valsartan, a selective angiotensin II type-1 receptor blocker.

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  • KIMURA Masaaki
    Research Division, Tsukuba Research Institute, Novartis Pharma K.K.
  • MITANI Hironobu
    Research Division, Tsukuba Research Institute, Novartis Pharma K.K.
  • ISOMURA Yasuo
    Research Division, Tsukuba Research Institute, Novartis Pharma K.K.

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  • アンジオテンシンＩＩ受容体きっ抗薬，バルサルタン（ディオバン）の薬理学的特性および臨床効果
  • 新薬紹介総説 アンジオテンシン2受容体拮抗薬,バルサルタン(ディオバン)の薬理学的特性および臨床効果
  • シンヤク ショウカイ ソウセツ アンジオテンシン 2 ジュヨウタイ キッコウヤク バルサルタン ディオバン ノ ヤクリガクテキ トクセイ オヨビ リンショウ コウカ

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Abstract

Valsartan (Diovan®) is a potent, orally active, specific, and highly selective blocker for the AT1-receptor subtype. The antihypertensive effects of oral treatment with valsartan were preclinically demonstrated in the sodium-depleted marmosets, renal hypertensive rats (2K1C), spontaneous hypertensive rats (SHR) and stroke-prone SHR. Moreover, valsartan had protective effects against hypertensive end-organ damage such as cardiac hypertrophy and renal disease. In an investigation of pharmacokinetics and pharmacodynamics in normotensive male volunteers, valsartan was rapidly absorbed with the maximal plasma concentration occurring 2-3 h after oral administration. The elimination half-life was about 4-6 h, valsartan was poorly metabolized, and most of the drug was excreted via feces. Valsartan produced persistent reductions of blood pressure in patients with mild to moderate essential hypertension and had a good safety profile with a wide therapeutic window between the effective pharmacological doses and the toxic doses. Therefore, valsartan is expected to be a safe and effective antihypertensive agent for the treatment of essential and severe hypertension.<br>

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