Valsartan

Generic Name
Valsartan
Brand Names
Dafiro, Diovan, Diovan Hct, Entresto, Exforge, Exforge Hct
Drug Type
Small Molecule
Chemical Formula
C24H29N5O3
CAS Number
137862-53-4
Unique Ingredient Identifier
80M03YXJ7I
Background

Valsartan belongs to the angiotensin II receptor blocker (ARB) family of drugs, which also includes telmisartan, candesartan, losartan, olmesartan, and irbesartan. ARBs selectively bind to angiotensin receptor 1 (AT1) and prevent the protein angiotensin II from binding and exerting its hypertensive effects, which include vasoconstriction, stimulation and synthesis of aldosterone and ADH, cardiac stimulation, and renal reabsorption of sodium, among others. Overall, valsartan's physiologic effects lead to reduced blood pressure, lower aldosterone levels, reduced cardiac activity, and increased excretion of sodium.

Valsartan also affects the renin-angiotensin aldosterone system (RAAS), which plays an important role in hemostasis and regulation of kidney, vascular, and cardiac functions. Pharmacological blockade of RAAS via AT1 receptor blockade inhibits negative regulatory feedback within RAAS, which is a contributing factor to the pathogenesis and progression of cardiovascular disease, heart failure, and renal disease. In particular, heart failure is associated with chronic activation of RAAS, leading to inappropriate fluid retention, vasoconstriction, and ultimately a further decline in left ventricular function. ARBs have been shown to have a protective effect on the heart by improving cardiac function, reducing afterload, increasing cardiac output and preventing ventricular hypertrophy and remodelling.

By comparison, the angiotensin-converting enzyme inhibitor (ACEI) class of medications (which includes drugs such as ramipril, lisinopril, and perindopril) inhibit the conversion of angiotensin I to angiotensin II through inhibition of the ACE enzyme. However, this does not prevent the formation of all angiotensin II within the body. The angiotensin II receptor blocker (ARB) family of drugs unique in that it blocks all angiotensin II activity, regardless of where or how it was synthesized.

Valsartan is commonly used for the management of hypertension, heart failure, and Type 2 Diabetes-associated nephropathy, particularly in patients who are unable to tolerate ACE inhibitors. ARBs such as valsartan have been shown in a number of large-scale clinical outcomes trials to improve cardiovascular outcomes including reducing risk of myocardial infarction, stroke, the progression of heart failure, and hospitalization. Valsartan also slows the progression of diabetic nephropathy due to its renoprotective effects. Improvements in chronic kidney disease with valsartan include both clinically and statistically significant decreases in urinary albumin and protein excretion in patients diagnosed with type 2 diabetes and in nondiabetic patients diagnosed with chronic kidney disease.

Valsartan was initially approved in 1996 in Europe for the treatment of hypertension in adults. Shortly after, in 1997, this drug was approved in the United States. Valsartan is generally well-tolerated with a side-effect profile superior to that of other antihypertensive drugs.

Indication

Valsartan is indicated for the treatment of hypertension to reduce the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. It is also indicated for the treatment of heart failure (NYHA class II-IV) and for left ventricular dysfunction or failure after myocardial infarction when the use of an angiotensin-converting enzyme inhibitor (ACEI) is not appropriate.

It is also used in combination with sacubitril.

Associated Conditions
Cardiovascular Mortality, Diabetic Nephropathy, Heart Failure, Hypertension, Moderate Essential Hypertension, Chronic heart failure with reduced ejection fraction (NYHA Class II), Chronic heart failure with reduced ejection fraction (NYHA Class III), Chronic heart failure with reduced ejection fraction (NYHA Class IV), Hospitalization due to cardiac failure
Associated Therapies
-

To Assess the Effects of Valsartan on Albuminuria/Proteinuria in Hypertensive Patients With Type 2 Diabetes Mellitus

Phase 4
Completed
Conditions
Interventions
First Posted Date
2007-10-26
Last Posted Date
2017-02-23
Lead Sponsor
Novartis
Target Recruit Count
509
Registration Number
NCT00550095
Locations
🇪🇬

Novartis Investigative Site ,, Cairo, Egypt

Efficacy and Safety of LCZ696A in Patients With Essential Hypertension

First Posted Date
2007-10-26
Last Posted Date
2015-08-25
Lead Sponsor
Novartis Pharmaceuticals
Target Recruit Count
1334
Registration Number
NCT00549770
Locations
🇨🇳

Novartis Investigative Site, Taipei, Taiwan

The Effects of Systolic Blood Pressure Lowering on Diastolic Function Using Valsartan + Amlodipine in Patients With Hypertension and Diastolic Dysfunction

First Posted Date
2007-08-31
Last Posted Date
2012-04-23
Lead Sponsor
Novartis Pharmaceuticals
Target Recruit Count
229
Registration Number
NCT00523549
Locations
🇺🇸

Novartis Investigative Sites, USA, New Jersey, United States

Preventing Microalbuminuria in Type 2 Diabetes

First Posted Date
2007-07-18
Last Posted Date
2019-09-06
Lead Sponsor
Mario Negri Institute for Pharmacological Research
Target Recruit Count
612
Registration Number
NCT00503152
Locations
🇮🇹

Hospital "Casa Sollievo della Sofferenza" - Division of Endocrinology, San Giovanni Rotondo, Foggia, Italy

🇮🇹

Azienda USL 2, Olbia, Italy

🇮🇹

Hospital "Azienda Ospedaliera di Treviglio e Caravaggio" - Diabetologic Ambulatory of Ponte San Pietro, Ponte San Pietro, Bergamo, Italy

and more 6 locations

Preventing ESRD in Overt Nephropathy of Type 2 Diabetes

First Posted Date
2007-07-02
Last Posted Date
2016-06-01
Lead Sponsor
Mario Negri Institute for Pharmacological Research
Target Recruit Count
102
Registration Number
NCT00494715
Locations
🇮🇹

Clinical Research Center for Rare Diseases "Aldo e Cele Daccò", Ranica, Bergamo, Italy

🇮🇹

Hospital " Casa Sollievo della Sofferenza" - Unit of Nephrology, San Giovanni Rotondo, Foggia, Italy

🇮🇹

University - AUSL 1 - Institute of Medical Pathology, Sassari, Italy

and more 12 locations

A Study to Evaluate the Long-term Use of Valsartan in Children 6 Months to 5 Years Old With Hypertension

Phase 3
Completed
Conditions
Interventions
First Posted Date
2007-04-06
Last Posted Date
2021-09-05
Lead Sponsor
Novartis Pharmaceuticals
Target Recruit Count
66
Registration Number
NCT00457626
Locations
🇹🇷

Novartis Investigative Site, Izmir, Turkey

Extension Study to Assess Long Term Safety, Tolerability, and Efficacy of Valsartan and Enalapril Combined and Alone in Children With Hypertension

First Posted Date
2007-03-13
Last Posted Date
2011-07-12
Lead Sponsor
Novartis Pharmaceuticals
Target Recruit Count
250
Registration Number
NCT00446511
Locations
🇫🇷

Sites in France, France, France

🇮🇳

Sites in India, India, India

🇵🇱

Sites in Poland, Poland, Poland

and more 6 locations

Efficacy and Safety of Valsartan in Combination With Amlodipine Compared to Losartan Plus Hydrochlorothiazide in Patients With Hypertension and Left Ventricular Hypertrophy

First Posted Date
2007-03-13
Last Posted Date
2011-05-11
Lead Sponsor
Novartis
Target Recruit Count
90
Registration Number
NCT00446563
Locations
🇩🇪

25 centers in Germany, Ludwigshafen, Germany

Effect of Valsartan Compared to Enalapril on Sitting Systolic Blood Pressure in Children With High Blood Pressure

Phase 3
Completed
Conditions
Interventions
First Posted Date
2007-02-12
Last Posted Date
2011-05-19
Lead Sponsor
Novartis Pharmaceuticals
Target Recruit Count
300
Registration Number
NCT00433836
Locations
🇮🇹

Sites in Italy, Sites in Italy, Italy

🇫🇷

Sites in France, Sites in France, France

🇸🇪

Sites in Sweden, Sites in Sweden, Sweden

and more 8 locations

A Study of the Antioxidant Probucol Combined With Valsartan in Patients With IgA Nephropathy

First Posted Date
2007-01-24
Last Posted Date
2013-08-28
Lead Sponsor
Guangdong Provincial People's Hospital
Target Recruit Count
75
Registration Number
NCT00426348
Locations
🇨🇳

Guangdong General Hospital, Guangzhou, Guangdong, China

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