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[Nonpeptide angiotensin II-receptor antagonists]
1Pharmaceutical Research Laboratories I, Takeda Chemical Industries, Ltd., Osaka, Japan.
Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica
|September 1, 1994
Summary
New nonpeptide angiotensin II (A II)-receptor antagonists, like TCV-116, effectively treat hypertension and congestive heart failure (CHF). These drugs show promise for broader cardiovascular disease applications by targeting the renin-angiotensin system (RAS).
Area of Science:
- Pharmacology
- Cardiovascular Medicine
- Nephrology
Context:
- The renin-angiotensin system (RAS) significantly impacts cardiovascular diseases.
- Research is advancing on orally active nonpeptide angiotensin II (A II)-receptor antagonists.
- Early discoveries in the late 1970s paved the way for modern A II antagonists like losartan.
Purpose:
- To review the current state of orally active nonpeptide A II-receptor antagonists.
- To detail the pharmacological characterization of these novel compounds.
- To explore the therapeutic potential of TCV-116 and its active metabolite CV-11974.
Summary:
- TCV-116 is a prodrug converted to CV-11974, demonstrating potent A II-receptor antagonism.
- Both TCV-116 and CV-11974 effectively counter A II-induced cardiovascular effects and reduce blood pressure in hypertensive animal models.
- TCV-116 showed benefits in congestive heart failure (CHF), stroke prevention, renal disease progression, and vascular injury in preclinical studies.
Impact:
- Clinical trials confirm TCV-116's efficacy in treating essential hypertension.
- A II antagonists may offer therapeutic benefits beyond hypertension and CHF, potentially impacting other cardiovascular conditions.
- Further research will elucidate the RAS's role in physiological regulation and cardiovascular pathophysiology.