Valsartan

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Cat Number

API391230936

CAS Number

137862-53-4

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CAS Number

137862-53-4

EINECS

604-045-2

Storage

Store at room temperature

Synonyms

CGP-48933; Prexxartan; (2S)-3-methyl-2-[pentanoyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]butanoic acid; N-(p-(o-1H-Tetrazol-5-ylphenyl)benzyl)-N-valeryl-L-valine; NSC-758927; 80M03YXJ7I

Molecular Formula

C24H29N5O3

Molecular Weight

435.5

Smiles

CCCCC(=O)N(CC1=CC=C(C=C1)C2=CC=CC=C2C3=NNN=N3)[C@@H](C(C)C)C(=O)O

Appearance

White to off-white powder

Melting Point

116-117℃

Boiling Point

684.9℃

Relative Density

1.212

General Description

Valsartan is a potent, selective angiotensin II receptor blocker (ARB) that specifically antagonizes the angiotensin type 1 (AT1) receptor. It is available in oral tablet form, often in combination with other antihypertensive agents such as amlodipine or hydrochlorothiazide. This agent is characterized by its high oral bioavailability and a duration of action that supports once-daily dosing without the need for hepatic bioactivation.

Mechanism of Action

Valsartan competitively blocks the binding of angiotensin II to AT1 receptors located on vascular smooth muscle, the adrenal gland, and the kidney. This antagonism inhibits the potent vasoconstrictor and aldosterone-secreting effects of angiotensin II, leading to systemic vasodilation, reduced sodium reabsorption, and decreased blood pressure. Unlike ACE inhibitors, valsartan does not inhibit the breakdown of bradykinin, which accounts for its significantly lower incidence of angioedema and dry cough.

Application

It is indicated for the treatment of hypertension, either as monotherapy or in combination regimens, and for the management of heart failure with reduced ejection fraction to reduce hospitalizations. It is also approved to improve survival following myocardial infarction in clinically stable patients with left ventricular dysfunction. The drug has demonstrated renal protective effects in patients with type 2 diabetes and hypertension, slowing the progression of diabetic nephropathy.

This review discusses the role of sacubitril/valsartan, a first‑in‑class angiotensin receptor–neprilysin inhibitor, in patients with heart failure with reduced ejection fraction (HFrEF) and concomitant chronic kidney disease (CKD). While the landmark PARADIGM‑HF trial demonstrated superior cardiovascular mortality reduction compared with enalapril, it largely excluded patients with advanced CKD. Emerging clinical trial and real‑world data suggest that sacubitril/valsartan remains effective and well tolerated across a broader range of kidney impairment, including stages not represented in the pivotal study. Importantly, the drug appears to confer both cardiac and renal benefits, supporting its use in this challenging population where traditional heart failure therapies are often suboptimal.

Fig. 1 Renal mechanisms of sacubitril/valsartan. ANP, atrial natriuretic peptide. (Pontremoli R, et al., 2021)

References

Pontremoli R, et al. Renal protection in chronic heart failure: focus on sacubitril/valsartan. Eur Heart J Cardiovasc Pharmacother. 2021; 7(5):445-452.

In a phase 2, double‑blind, placebo‑controlled trial (178 patients with early‑stage sarcomeric hypertrophic cardiomyopathy), valsartan (up to 320 mg daily in adults, lower in children) given for 2 years significantly improved a composite z‑score of cardiac structure and function compared to placebo (between‑group difference +0.231, 95% CI +0.098 to +0.364, P=0.001). The treatment was well tolerated. This is the first demonstration that an angiotensin receptor blocker can attenuate disease progression in early HCM, offering an accessible and safe therapy.

Fig. 2 Participant enrollment, allocation and follow-up. (Ho CY, et al., 2021)

References

Ho CY, et al. Valsartan in early-stage hypertrophic cardiomyopathy: a randomized phase 2 trial. Nat Med. 2021; 27(10):1818-1824.

Does Valsartan require protection from moisture during storage?

Yes, it is slightly hygroscopic and can absorb moisture, leading to hydrolysis of the tetrazole ring. Store in tightly sealed, moisture-proof containers with desiccant.

What is the recommended storage temperature for Valsartan?

Store at controlled room temperature (15-25°C). Avoid elevated temperatures above 30°C, which can accelerate oxidative degradation and impurity formation.

Is Valsartan stable in combination tablet formulations with amlodipine or hydrochlorothiazide?

Yes, it shows good compatibility. We provide stability data for fixed-dose combinations, including protection against moisture and light in blister packaging.

How is the nitrosamine impurity (NDMA) controlled in Valsartan?

We employ a highly sensitive LC-MS/MS method to monitor NDMA and other nitrosamines, ensuring levels are below regulatory limits (e.g., EMA/FDA acceptable intake).