Identification

Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Logo pink
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.
#DrugBankUpdates
Name
Valsartan
Accession Number
DB00177  (APRD00133)
Type
Small Molecule
Groups
Approved, Investigational
Description

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.5

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.1,9,10,11,12,13,14,15 Valsartan also slows the progression of diabetic nephropathy due to its renoprotective effects.6,7,8 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.1,10

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.1 Valsartan is generally well-tolerated with a side-effect profile superior to that of other antihypertensive drugs.3,4

Structure
Thumb
Synonyms
  • (S)-N-Valeryl-N-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]-methyl}-valine
  • N-(P-(O-1H-Tetrazol-5-ylphenyl)benzyl)-N-valeryl-L-valine
  • N-pentanoyl-N-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-L-valine
  • Valsartan
External IDs
CGP 48933 / CGP-48933
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act ValsartanTabletOralActavis Pharma Company2011-02-162019-08-14Canada
Act ValsartanTabletOralActavis Pharma Company2011-02-162019-08-14Canada
Act ValsartanTabletOralActavis Pharma Company2011-02-162019-08-14Canada
Act ValsartanTabletOralActavis Pharma Company2011-02-162019-08-14Canada
CopaliaTablet, film coatedOralNovartis Europharm Limited2007-01-15Not applicableEu
CopaliaTablet, film coatedOralNovartis Europharm Limited2007-01-15Not applicableEu
CopaliaTablet, film coatedOralNovartis Europharm Limited2007-01-15Not applicableEu
CopaliaTablet, film coatedOralNovartis Europharm Limited2007-01-15Not applicableEu
CopaliaTablet, film coatedOralNovartis Europharm Limited2007-01-15Not applicableEu
CopaliaTablet, film coatedOralNovartis Europharm Limited2007-01-15Not applicableEu
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEu
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEu
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEu
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEu
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEu
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEu
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEu
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEu
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEu
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEu
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine besylate (5 mg/1)Tablet, film coatedOralAlembic Pharmaceuticals Inc.2016-12-01Not applicableUs
Amlodipine and ValsartanValsartan (160 mg/1) + Amlodipine besylate (10 mg/1)Tablet, film coatedOralMylan Pharmaceuticals Inc.2015-03-30Not applicableUs
Amlodipine and ValsartanValsartan (160 mg/1) + Amlodipine besylate (5 mg/1)Tablet, film coatedOralTrigen Laboratories, Inc.2010-12-282017-11-20Us
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine besylate (10 mg/1)TabletOralLupin Pharmaceuticals, Inc.2015-03-31Not applicableUs
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine besylate (10 mg/1)Tablet, film coatedOralAlembic Pharmaceuticals Limited2016-12-01Not applicableUs
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine (5 mg/1)TabletOralPar Pharmaceutical, Inc.2014-09-30Not applicableUs49884 0576 11 nlmimage10 ba3f5d3a
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine besylate (10 mg/1)TabletOralmedsource pharmaceuticals2015-03-30Not applicableUs
Amlodipine and ValsartanValsartan (160 mg/1) + Amlodipine besylate (10 mg/1)TabletOralTorrent Pharmaceuticals Limited2015-03-302019-10-31Us
Amlodipine and valsartanValsartan (160 mg/1) + Amlodipine besylate (10 mg/1)Tablet, film coatedOralAurobindo Pharma Limited2016-04-22Not applicableUs
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine besylate (5 mg/1)Tablet, film coatedOralSandoz Inc2015-03-302022-09-30Us
Categories
UNII
80M03YXJ7I
CAS number
137862-53-4
Weight
Average: 435.5188
Monoisotopic: 435.227039819
Chemical Formula
C24H29N5O3
InChI Key
ACWBQPMHZXGDFX-QFIPXVFZSA-N
InChI
InChI=1S/C24H29N5O3/c1-4-5-10-21(30)29(22(16(2)3)24(31)32)15-17-11-13-18(14-12-17)19-8-6-7-9-20(19)23-25-27-28-26-23/h6-9,11-14,16,22H,4-5,10,15H2,1-3H3,(H,31,32)(H,25,26,27,28)/t22-/m0/s1
IUPAC Name
(2S)-3-methyl-2-[N-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)pentanamido]butanoic acid
SMILES
CCCCC(=O)N(CC1=CC=C(C=C1)C1=CC=CC=C1C1=NNN=N1)[C@@H](C(C)C)C(O)=O

Pharmacology

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.22,23

Associated Conditions
Pharmacodynamics

Valsartan inhibits the pressor effects of angiotensin II with oral doses of 80 mg inhibiting the pressor effect by about 80% at peak with approximately 30% inhibition persisting for 24 hours. Removal of the negative feedback of angiotensin II causes a 2- to 3-fold rise in plasma renin and consequent rise in angiotensin II plasma concentration in hypertensive patients. Minimal decreases in plasma aldosterone were observed after administration of valsartan.

In multiple-dose studies in hypertensive patients, valsartan had no notable effects on total cholesterol, fasting triglycerides, fasting serum glucose, or uric acid.[F4607]

Hypotension

Excessive hypotension was rarely seen (0.1%) in patients with uncomplicated hypertension treated with valsartan alone. In patients with an activated renin-angiotensin system, such as volume- and/or salt-depleted patients receiving high doses of diuretics, symptomatic hypotension may occur. This condition should be corrected prior to administration of valsartan, or the treatment should start under close medical supervision.

Caution should be observed when initiating therapy in patients with heart failure. Patients with heart failure given valsartan commonly have some reduction in blood pressure, but discontinuation of therapy because of continuing symptomatic hypotension usually is not necessary when dosing instructions are followed. In controlled trials in heart failure patients, the incidence of hypotension in valsartan-treated patients was 5.5% compared to 1.8% in placebo-treated patients.

If excessive hypotension occurs, the patient should be placed in the supine position and, if necessary, given an intravenous infusion of normal saline. A transient hypotensive response is not a contraindication to further treatment, which usually can be continued without difficulty once the blood pressure has stabilized.[F4607]

Impaired Renal Function

Changes in renal function including acute renal failure can be caused by drugs that inhibit the renin-angiotensin system and by diuretics. Patients whose renal function may depend in part on the activity of the renin-angiotensin system (e.g., patients with renal artery stenosis, chronic kidney disease, severe congestive heart failure, or volume depletion) may be at particular risk of developing acute renal failure on valsartan. Monitor renal function periodically in these patients. Consider withholding or discontinuing therapy in patients who develop a clinically significant decrease in renal function on valsartan.[F4607]

Hyperkalemia

Some patients with heart failure have developed increases in potassium. These effects are usually minor and transient, and they are more likely to occur in patients with pre-existing renal impairment. Dosage reduction and/or discontinuation of valsartan may be required.[F4607]

Mechanism of action

Valsartan belongs to the angiotensin II receptor blocker (ARB) family of drugs, which selectively bind to angiotensin receptor 1 (AT1) and prevent angiotensin II from binding and exerting its hypertensive effects. These 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 prevent ventricular hypertrophy.5

The angiotensin-converting enzyme inhibitor (ACEI) class of medications (which includes drugs such as ramipril, lisinopril, and perindopril) inhibits the conversion of angiotensin I to angiotensin II by inhibiting the ACE enzyme but does not prevent the formation of all angiotensin II. ARB activity is 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.1,9,10,11,12,13,14,15 Valsartan also slows the progression of diabetic nephropathy due to its renoprotective effects.6,7,8 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.1,10

Valsartan also binds to the AT2 receptor, however AT2 is not known to be associated with cardiovascular homeostasis like AT1. Valsartan has about 20,000-fold higher affinity for the AT1 receptor than for the AT2 receptor. The increased plasma levels of angiotensin II following AT1 receptor blockade with valsartan may stimulate the unblocked AT2 receptor.23

TargetActionsOrganism
AType-1 angiotensin II receptor
antagonist
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

Learn more
Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

Learn more
Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

Learn more
Absorption

After one oral dose, the antihypertensive activity of valsartan begins within approximately 2 hours and peaks within 4-6 hours in most patients.[F3139] Food decreases the exposure to orally administered valsartan by approximately 40% and peak plasma concentration by approximately 50%. AUC and Cmax values of valsartan genereally increase linearly with increasing dose over the therapeutic dose range. Valsartan does not accumulate appreciably in plasma following repetitive administration.[F4607]

Volume of distribution

The steady state volume of distribution of valsartan after intravenous administration is small (17 L), indicating that valsartan does not distribute into tissues extensively.[F3139,F3607]

Protein binding

Valsartan is highly bound to serum proteins (95%), mainly serum albumin.[F4607]

Metabolism

Valsartan undergoes minimal liver metabolism and is not biotransformed to a high degree, as only approximately 20% of a single dose is recovered as metabolites.1 The primary metabolite, accounting for about 9% of dose, is valeryl 4-hydroxy valsartan. In vitro metabolism studies involving recombinant CYP 450 enzymes indicated that the CYP 2C9 isoenzyme is responsible for the formation of valeryl-4-hydroxy valsartan. Valsartan does not inhibit CYP 450 isozymes at clinically relevant concentrations. CYP 450 mediated drug interaction between valsartan and coadministered drugs are unlikely because of the low extent of metabolism.[F4607]

Route of elimination

Valsartan, when administered as an oral solution, is primarily recovered in feces (about 83% of dose) and urine (about 13% of dose). The recovery is mainly as unchanged drug, with only about 20% of dose recovered as metabolites.[F4607]

Half life

After intravenous (IV) administration, valsartan demonstrates bi-exponential decay kinetics, with an average elimination half-life of about 6 hours.[F4607]

Clearance

Following intravenous administration, plasma clearance of valsartan is approximately 2 L/hour and its renal clearance is 0.62 L/hour (about 30% of total clearance).[F4607]

Toxicity

Approximate LD50 >2000 mg/kg (Gavage, rat) [F3139]

Reproductive Toxicology Studies

No teratogenic effects were seen when valsartan was given to pregnant mice and rats at oral doses up to 600 mg/kg/day and to pregnant rabbits at oral doses reaching up to 10 mg/kg/day. Despite this, marked decreases in fetal weight, pup birth weight, pup survival rate, and delays in developmental milestones were noted in studies in which parental rats were treated with valsartan at oral, maternally toxic doses of 600 mg/kg/day during the organogenesis period or during late gestation and lactation.[F4607]

Pregnancy

When used in pregnancy, drugs that act directly on the renin-angiotensin system (RAAS) can cause injury and death to the developing fetus. When pregnancy is detected, valsartan should be discontinued as soon as possible.[F4607]

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Valsartan Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Valsartan.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Valsartan.
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid may decrease the antihypertensive activities of Valsartan.
1-benzylimidazole1-benzylimidazole may decrease the antihypertensive activities of Valsartan.
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Valsartan.
2,5-Dimethoxy-4-ethylthioamphetamine2,5-Dimethoxy-4-ethylthioamphetamine may decrease the antihypertensive activities of Valsartan.
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Valsartan.
4-Methoxyamphetamine4-Methoxyamphetamine may decrease the antihypertensive activities of Valsartan.
5-methoxy-N,N-dimethyltryptamine5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Valsartan.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Valsartan.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

    Learn more
  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
Not Available

References

Synthesis Reference

Zvi Harel, Igor Rukhman, "Process for the preparation of valsartan." U.S. Patent US20050010053, issued January 13, 2005.

US20050010053
General References
  1. Black HR, Bailey J, Zappe D, Samuel R: Valsartan: more than a decade of experience. Drugs. 2009;69(17):2393-414. doi: 10.2165/11319460-000000000-00000. [PubMed:19911855]
  2. Fogari R, Zoppi A: A drug safety evaluation of valsartan. Expert Opin Drug Saf. 2011 Mar;10(2):295-303. doi: 10.1517/14740338.2011.543416. Epub 2010 Dec 11. [PubMed:21142805]
  3. McInnes GT: Clinical advantage of valsartan. Cardiology. 1999;91 Suppl 1:14-8. doi: 10.1159/000047283. [PubMed:10449890]
  4. Chiolero A, Burnier M: Pharmacology of valsartan, an angiotensin II receptor antagonist. Expert Opin Investig Drugs. 1998 Nov;7(11):1915-25. doi: 10.1517/13543784.7.11.1915 . [PubMed:15991938]
  5. Akazawa H, Yabumoto C, Yano M, Kudo-Sakamoto Y, Komuro I: ARB and cardioprotection. Cardiovasc Drugs Ther. 2013 Apr;27(2):155-60. doi: 10.1007/s10557-012-6392-2. [PubMed:22538956]
  6. Zhou G, Cheung AK, Liu X, Huang Y: Valsartan slows the progression of diabetic nephropathy in db/db mice via a reduction in podocyte injury, and renal oxidative stress and inflammation. Clin Sci (Lond). 2014 May;126(10):707-20. doi: 10.1042/CS20130223. [PubMed:24195695]
  7. Suzuki K, Souda S, Ikarashi T, Kaneko S, Nakagawa O, Aizawa Y: Renoprotective effects of low-dose valsartan in type 2 diabetic patients with diabetic nephropathy. Diabetes Res Clin Pract. 2002 Sep;57(3):179-83. [PubMed:12126767]
  8. Currie G, Bethel MA, Holzhauer B, Haffner SM, Holman RR, McMurray JJV: Effect of valsartan on kidney outcomes in people with impaired glucose tolerance. Diabetes Obes Metab. 2017 Jun;19(6):791-799. doi: 10.1111/dom.12877. Epub 2017 Mar 17. [PubMed:28093841]
  9. Ezekowitz JA, O'Meara E, McDonald MA, Abrams H, Chan M, Ducharme A, Giannetti N, Grzeslo A, Hamilton PG, Heckman GA, Howlett JG, Koshman SL, Lepage S, McKelvie RS, Moe GW, Rajda M, Swiggum E, Virani SA, Zieroth S, Al-Hesayen A, Cohen-Solal A, D'Astous M, De S, Estrella-Holder E, Fremes S, Green L, Haddad H, Harkness K, Hernandez AF, Kouz S, LeBlanc MH, Masoudi FA, Ross HJ, Roussin A, Sussex B: 2017 Comprehensive Update of the Canadian Cardiovascular Society Guidelines for the Management of Heart Failure. Can J Cardiol. 2017 Nov;33(11):1342-1433. doi: 10.1016/j.cjca.2017.08.022. Epub 2017 Sep 6. [PubMed:29111106]
  10. Leung AA, Daskalopoulou SS, Dasgupta K, McBrien K, Butalia S, Zarnke KB, Nerenberg K, Harris KC, Nakhla M, Cloutier L, Gelfer M, Lamarre-Cliche M, Milot A, Bolli P, Tremblay G, McLean D, Tran KC, Tobe SW, Ruzicka M, Burns KD, Vallee M, Prasad GVR, Gryn SE, Feldman RD, Selby P, Pipe A, Schiffrin EL, McFarlane PA, Oh P, Hegele RA, Khara M, Wilson TW, Penner SB, Burgess E, Sivapalan P, Herman RJ, Bacon SL, Rabkin SW, Gilbert RE, Campbell TS, Grover S, Honos G, Lindsay P, Hill MD, Coutts SB, Gubitz G, Campbell NRC, Moe GW, Howlett JG, Boulanger JM, Prebtani A, Kline G, Leiter LA, Jones C, Cote AM, Woo V, Kaczorowski J, Trudeau L, Tsuyuki RT, Hiremath S, Drouin D, Lavoie KL, Hamet P, Gregoire JC, Lewanczuk R, Dresser GK, Sharma M, Reid D, Lear SA, Moullec G, Gupta M, Magee LA, Logan AG, Dionne J, Fournier A, Benoit G, Feber J, Poirier L, Padwal RS, Rabi DM: Hypertension Canada's 2017 Guidelines for Diagnosis, Risk Assessment, Prevention, and Treatment of Hypertension in Adults. Can J Cardiol. 2017 May;33(5):557-576. doi: 10.1016/j.cjca.2017.03.005. Epub 2017 Mar 10. [PubMed:28449828]
  11. Lee VC, Rhew DC, Dylan M, Badamgarav E, Braunstein GD, Weingarten SR: Meta-analysis: angiotensin-receptor blockers in chronic heart failure and high-risk acute myocardial infarction. Ann Intern Med. 2004 Nov 2;141(9):693-704. doi: 10.7326/0003-4819-141-9-200411020-00011. [PubMed:15520426]
  12. Brenner BM, Cooper ME, de Zeeuw D, Keane WF, Mitch WE, Parving HH, Remuzzi G, Snapinn SM, Zhang Z, Shahinfar S: Effects of losartan on renal and cardiovascular outcomes in patients with type 2 diabetes and nephropathy. N Engl J Med. 2001 Sep 20;345(12):861-9. doi: 10.1056/NEJMoa011161. [PubMed:11565518]
  13. Yusuf S, Teo KK, Pogue J, Dyal L, Copland I, Schumacher H, Dagenais G, Sleight P, Anderson C: Telmisartan, ramipril, or both in patients at high risk for vascular events. N Engl J Med. 2008 Apr 10;358(15):1547-59. doi: 10.1056/NEJMoa0801317. Epub 2008 Mar 31. [PubMed:18378520]
  14. Pfeffer MA, McMurray JJ, Velazquez EJ, Rouleau JL, Kober L, Maggioni AP, Solomon SD, Swedberg K, Van de Werf F, White H, Leimberger JD, Henis M, Edwards S, Zelenkofske S, Sellers MA, Califf RM: Valsartan, captopril, or both in myocardial infarction complicated by heart failure, left ventricular dysfunction, or both. N Engl J Med. 2003 Nov 13;349(20):1893-906. doi: 10.1056/NEJMoa032292. Epub 2003 Nov 10. [PubMed:14610160]
  15. O'Gara PT, Kushner FG, Ascheim DD, Casey DE Jr, Chung MK, de Lemos JA, Ettinger SM, Fang JC, Fesmire FM, Franklin BA, Granger CB, Krumholz HM, Linderbaum JA, Morrow DA, Newby LK, Ornato JP, Ou N, Radford MJ, Tamis-Holland JE, Tommaso CL, Tracy CM, Woo YJ, Zhao DX: 2013 ACCF/AHA guideline for the management of ST-elevation myocardial infarction: a report of the American College of Cardiology Foundation/American Heart Association Task Force on Practice Guidelines. J Am Coll Cardiol. 2013 Jan 29;61(4):e78-e140. doi: 10.1016/j.jacc.2012.11.019. Epub 2012 Dec 17. [PubMed:23256914]
  16. Nakashima A, Kawashita H, Masuda N, Saxer C, Niina M, Nagae Y, Iwasaki K: Identification of cytochrome P450 forms involved in the 4-hydroxylation of valsartan, a potent and specific angiotensin II receptor antagonist, in human liver microsomes. Xenobiotica. 2005 Jun;35(6):589-602. [PubMed:16192110]
  17. Bader, M. (2004). Renin-angiotensin-aldosterone system. In Encyclopedic reference of molecular pharmacology (pp. 810-814). Berlin: Springer. [ISBN:9783540298328]
  18. NZ Data Sheet, Valsartan and sacubitril [File]
  19. Valsartan and Sacubitril FDA label [File]
  20. Valsartan and Amlodipine FDA label [File]
  21. Valsartan and Nevibolol FDA label [File]
  22. Health Canada Monograph - Valsartan [File]
  23. FDA Label - Valsartan [File]
External Links
Human Metabolome Database
HMDB0014323
KEGG Drug
D00400
PubChem Compound
60846
PubChem Substance
46509000
ChemSpider
54833
BindingDB
50049186
ChEBI
9927
ChEMBL
CHEMBL1069
Therapeutic Targets Database
DAP000363
PharmGKB
PA451848
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Valsartan
ATC Codes
C09DX05 — Valsartan and nebivololC10BX10 — Rosuvastatin and valsartanC09DA03 — Valsartan and diureticsC09CA03 — ValsartanC09DX02 — Valsartan and aliskirenC09DX01 — Valsartan, amlodipine and hydrochlorothiazideC09DB08 — Valsartan and lercanidipineC09DB01 — Valsartan and amlodipineC09DX04 — Valsartan and sacubitril
AHFS Codes
  • 24:32.08 — Angiotensin Ii Receptor Antagonists
FDA label
Download (237 KB)
MSDS
Download (24 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Not Yet RecruitingTreatmentCKD1
0RecruitingBasic ScienceThyroid Cancer, Medullary1
1Active Not RecruitingOtherHealthy Volunteers1
1CompletedNot AvailableHealthy Male Subjects1
1CompletedNot AvailableHealthy Volunteers1
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of Valsartan1
1CompletedNot AvailableHigh Blood Pressure (Hypertension) / Hyperlipidemias1
1CompletedNot AvailableType 2 Diabetes Mellitus1
1CompletedBasic ScienceAdministration, Oral / Magnetic Resonance Imaging (MRI) / Pharmacokinetics1
1CompletedBasic ScienceChronic Kidney Disease (CKD) / High Blood Pressure (Hypertension) / Nephrotic Syndrome1
1CompletedBasic ScienceHealthy Male Subjects2
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceHigh Blood Pressure (Hypertension) / Hyperlipidemias1
1CompletedOtherHigh Blood Pressure (Hypertension) / Hyperlipidemias1
1CompletedSupportive CareHealthy Volunteers1
1CompletedTreatmentHealthy Male Subjects1
1CompletedTreatmentHealthy Male Volunteers2
1CompletedTreatmentHealthy Normotensive Volunteers1
1CompletedTreatmentHealthy Volunteers6
1CompletedTreatmentHigh Blood Pressure (Hypertension)2
1CompletedTreatmentHigh Blood Pressure (Hypertension) / Hyperlipidemias3
1CompletedTreatmentHypertension, Hyperlipidemia1
1CompletedTreatmentType 2 Diabetes Mellitus1
1Not Yet RecruitingBasic ScienceHealthy Volunteers1
1RecruitingTreatmentType 2 Diabetes Mellitus1
1Unknown StatusTreatmentHealthy Volunteers1
1WithdrawnTreatmentHigh Blood Pressure (Hypertension) / Metabolic Syndromes1
1, 2Not Yet RecruitingTreatmentArthritis / BMI >30 kg/m2 / High Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
2Active Not RecruitingTreatmentHypertrophic Cardiomyopathy (HCM)1
2CompletedNot AvailableSalt-sensitive Hypertension1
2CompletedBasic ScienceHigh Blood Pressure (Hypertension)1
2CompletedTreatmentAlport Syndrome1
2CompletedTreatmentAtherosclerosis / Carotid Artery Diseases1
2CompletedTreatmentChronic Heart Failure (CHF)2
2CompletedTreatmentComplication of Hemodialysis / End Stage Renal Failure on Dialysis1
2CompletedTreatmentHigh Blood Pressure (Hypertension)5
2CompletedTreatmentHypertension,Essential3
2CompletedTreatmentMyocardial Ischemia / Post Acute Coronary Syndrome1
2CompletedTreatmentSystolic Hypertension1
2Not Yet RecruitingOtherCardiovascular Heart Disease / Diabetes Mellitus (DM) / Energy Expenditure / Insulin Sensitivity/Resistance / Metabolic Diseases / Metabolism / Natriuretic Peptides1
2Not Yet RecruitingTreatmentHeart Failure With Preserved Ejection Fraction (HFpEF) / Human Immunodeficiency Virus Infection(HIV)/Acquired Immunodeficiency Syndrome (AIDS)1
2Not Yet RecruitingTreatmentHypertrophic Cardiomyopathy (HCM)1
2RecruitingPreventionHeart Failure / Malignant Neoplasm of Female Breast1
2RecruitingTreatmentDiastolic Dysfunction1
2RecruitingTreatmentDiastolic Dysfunction / Myocardial Infarction1
2RecruitingTreatmentDiastolic Dysfunction / Type 2 Diabetes Mellitus1
2RecruitingTreatmentHypertrophic Cardiomyopathy (HCM)1
2RecruitingTreatmentPeripheral Arterial Disease (PAD)1
2WithdrawnBasic ScienceHeart Failure1
2WithdrawnBasic ScienceChronic heart failure with reduced ejection fraction (NYHA Class II) / Chronic heart failure with reduced ejection fraction (NYHA Class III) / NYHA Class I Congestive heart failure1
2, 3CompletedTreatmentHypertension,Essential1
2, 3Not Yet RecruitingTreatmentAngiotensin Receptor Antagonists / Aortic Valve Stenosis / Heart Valve Prosthesis Implantation / Left Ventricular Hypertrophy / Transcatheter Aortic Valve Replacement / Valsartan1
3Active Not RecruitingTreatmentChronic Heart Failure (CHF) / Heart Failure1
3Active Not RecruitingTreatmentHeart Failure1
3Active Not RecruitingTreatmentHeart Failure With Preserved Ejection Fraction (HFpEF)2
3CompletedPreventionAtherosclerosis / Cardiovascular Heart Disease / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / High Blood Pressure (Hypertension) / High Cholesterol / Type 2 Diabetes Mellitus1
3CompletedPreventionDe Novo Renal Transplantation1
3CompletedPreventionType 2 Diabetes Mellitus1
3CompletedTreatmentAtrial Fibrillation (AF)1
3CompletedTreatmentChronic Heart Failure With Reduced Ejection Fraction (HFrEF)1
3CompletedTreatmentChronic Kidney Disease (CKD) / High Blood Pressure (Hypertension)1
3CompletedTreatmentDiabetes Mellitus (DM)2
3CompletedTreatmentDyslipidemias / High Blood Pressure (Hypertension)1
3CompletedTreatmentDyslipidemias / High Blood Pressure (Hypertension) / High Cholesterol1
3CompletedTreatmentHigh Blood Pressure (Hypertension)48
3CompletedTreatmentHigh Blood Pressure (Hypertension) / High Cholesterol1
3CompletedTreatmentHigh Blood Pressure (Hypertension) / Hyperlipidemias1
3CompletedTreatmentHigh Blood Pressure (Hypertension) / Metabolic Syndromes1
3CompletedTreatmentHigh Cholesterol / Hypertension,Essential1
3CompletedTreatmentHypertension,Essential3
3CompletedTreatmentHypertension; Hypertrophy, Left Ventricular1
3CompletedTreatmentPediatric Hypertension With or Without CKD1
3CompletedTreatmentStage 1 Hypertension / Stage 2 Hypertension1
3Enrolling by InvitationTreatmentHigh Blood Pressure (Hypertension) / Hyperlipidemias1
3Enrolling by InvitationTreatmentHypertension With Hyperlipidemia1
3Not Yet RecruitingTreatmentAcute Coronary Syndromes (ACS) / Ischemic Heart Disease / Revascularization1
3Not Yet RecruitingTreatmentDyslipidemias / High Blood Pressure (Hypertension)1
3Not Yet RecruitingTreatmentHeart Failure With Preserved Ejection Fraction (HFpEF)2
3Not Yet RecruitingTreatmentHypertensive Heart Disease1
3RecruitingTreatmentAcute Myocardial Infarction (AMI)1
3RecruitingTreatmentHeart Failure1
3SuspendedOtherElevated Blood Pressure / High Blood Pressure (Hypertension) / Pre-Diabetic / Type 2 Diabetes Mellitus1
3TerminatedHealth Services ResearchEndothelial Dysfunction / Oxidative Stress1
3TerminatedTreatmentHigh Blood Pressure (Hypertension)1
3WithdrawnTreatmentHuman Immunodeficiency Virus (HIV) Infections / Kidney Diseases1
4Active Not RecruitingBasic ScienceArterial hypoxia / OSAS (Obstructive Sleep Apneas Syndrome) / Sleep Apnea1
4Active Not RecruitingTreatmentBlood Pressures / Stroke, Ischemic1
4Active Not RecruitingTreatmentHigh Blood Pressure (Hypertension)1
4CompletedBasic ScienceType 2 Diabetes Mellitus1
4CompletedDiagnosticCongestive Heart Failure / High Blood Pressure (Hypertension) / Ischemic Heart Disease / Stroke1
4CompletedDiagnosticHypertension,Essential1
4CompletedOtherHeart Failure1
4CompletedOtherHeart Failure With Reduced Ejection Fraction (HFrEF)1
4CompletedPreventionBlood Pressures / Hypertension Complicated / Left Ventricular Hypertrophy1
4CompletedPreventionHigh Blood Pressure (Hypertension)1
4CompletedPreventionHigh Blood Pressure (Hypertension) / Metabolic Syndromes / Pre-Hypertension1
4CompletedPreventionHigh Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
4CompletedPreventionNon-Hodgkin's Lymphoma (NHL)1
4CompletedSupportive CareAcute Heart Failure (AHF)1
4CompletedSupportive CareHearth Failure With Reduced Ejection Fraction (HFrEF)1
4CompletedTreatmentAlbuminuria / High Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
4CompletedTreatmentBlood Pressures1
4CompletedTreatmentCardiovascular Heart Disease / Chronic Kidney Disease (CKD) / Hypertension,Essential / Stroke1
4CompletedTreatmentCardiovascular Heart Disease / Deficiency, Vitamin D / Osteoporosis / Secondary Hyp1
4CompletedTreatmentChronic Kidney Disease (CKD) / High Blood Pressure (Hypertension)1
4CompletedTreatmentCongestive Cardiomyopathy1
4CompletedTreatmentCongestive Heart Failure / High Blood Pressure (Hypertension)1
4CompletedTreatmentCoronary Artery Disease1
4CompletedTreatmentCoronary Artery Disease / Diabetes Mellitus (DM) / High Blood Pressure (Hypertension)1
4CompletedTreatmentCoronary Artery Disease / High Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus (DM) / Heart Failure1
4CompletedTreatmentDiabetes Mellitus (DM) / High Blood Pressure (Hypertension) / Proteinuria1
4CompletedTreatmentDiabetic Nephropathies / High Blood Pressure (Hypertension)2
4CompletedTreatmentDiastolic Dysfunction, Symptomatic Heart Failure1
4CompletedTreatmentDiastolic Dysfunction / High Blood Pressure (Hypertension)2
4CompletedTreatmentDyslipidemias / High Blood Pressure (Hypertension)1
4CompletedTreatmentErectile Dysfunction / High Blood Pressure (Hypertension) / Ventricular Remodelling1
4CompletedTreatmentEssential,Hypertension1
4CompletedTreatmentGlomerulonephritis / IgA Nephropathy1
4CompletedTreatmentHealthy Volunteers1
4CompletedTreatmentHeart Failure With Reduced Ejection Fraction (HFrEF)1
4CompletedTreatmentHeart Failure / Left Ventricular Dysfunction1
4CompletedTreatmentHigh Blood Pressure (Hypertension)42
4CompletedTreatmentHigh Blood Pressure (Hypertension) / High Cholesterol1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Impaired Glucose Tolerance1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Left Ventricular Hypertrophy1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Metabolic Syndromes1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Proteinuria / Type 2 Diabetes Mellitus1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
4CompletedTreatmentHypertension, Dyslypidaemia1
4CompletedTreatmentHypertension,Essential3
4CompletedTreatmentIgA Nephropathy1
4CompletedTreatmentLeft Ventricular Dysfunction / Mitral Valve Insufficiency1
4CompletedTreatmentMicroalbuminuria / Proteinuria1
4CompletedTreatmentMyocardial Infarction1
4CompletedTreatmentSmall Abdominal Aortic Aneurysm1
4CompletedTreatmentStage 2 Hypertension1
4CompletedTreatmentStage 2 Systolic Hypertension1
4Not Yet RecruitingBasic ScienceHigh Blood Pressure (Hypertension)1
4Not Yet RecruitingPreventionBlood Pressures / BMI >30 kg/m2 / Impaired Glucose Tolerance / Pre-Diabetic1
4Not Yet RecruitingTreatmentBMI >30 kg/m2 / High Blood Pressure (Hypertension)1
4Not Yet RecruitingTreatmentChagas Disease / Heart Failure1
4Not Yet RecruitingTreatmentHeart Failure1
4Not Yet RecruitingTreatmentHypertension;Nephropathy1
4RecruitingBasic ScienceHeart Failure1
4RecruitingPreventionBlood Pressures / High Blood Pressure (Hypertension) / Stroke1
4RecruitingPreventionFirst Time Dual Chamber Pacemaker Implantation1
4RecruitingTreatmentHeart Diseases / Type 2 Diabetes Mellitus1
4RecruitingTreatmentHeart Failure4
4RecruitingTreatmentHeart Failure With Preserved Ejection Fraction (HFpEF)1
4RecruitingTreatmentHeart Failure, Systolic1
4RecruitingTreatmentPrimary IgA Nephropathy1
4RecruitingTreatmentType2 Diabetes1
4TerminatedNot AvailableHeavy Proteinuria1
4TerminatedPreventionHigh Blood Pressure (Hypertension)1
4TerminatedTreatmentAtrial Fibrillation (AF)1
4TerminatedTreatmentCongestive Heart Failure1
4TerminatedTreatmentDiabetes Mellitus (DM) / High Blood Pressure (Hypertension) / Stage 2 Hypertension1
4TerminatedTreatmentDiabetic Nephropathies / Glomerulonephritis, Membranous / Glomerulopathy (Obesity-associated) / Glomerulosclerosis, Focal Segmental / Hypertensive Nephrosclerosis / IgA Nephropathy / Proteinuric Kidney Disease1
4TerminatedTreatmentDiabetic Nephropathies / High Blood Pressure (Hypertension)1
4TerminatedTreatmentEarly Diabetic Nephropathy / High Blood Pressure (Hypertension)1
4TerminatedTreatmentHeart Failure1
4Unknown StatusDiagnosticChronic Kidney Disease (CKD) / Proteinuria1
4Unknown StatusPreventionBMI >30 kg/m2 / High Blood Pressure (Hypertension)1
4Unknown StatusTreatmentAcute Ischemic Stroke (AIS)1
4Unknown StatusTreatmentAlbuminuria / Diabetes Mellitus (DM) / High Blood Pressure (Hypertension)1
4Unknown StatusTreatmentChronic Kidney Disease (CKD)1
4Unknown StatusTreatmentCongestive Heart Failure / High Blood Pressure (Hypertension) / Ischemic Heart Disease1
4Unknown StatusTreatmentDiabetes Mellitus (DM)1
4Unknown StatusTreatmentHigh Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentHypertension,Essential1
4Unknown StatusTreatmentMajor Depressive Disorder (MDD)1
4WithdrawnTreatmentCongestive Heart Failure / High Blood Pressure (Hypertension)1
4WithdrawnTreatmentHeart Failure With Reduced Ejection Fraction (HFrEF)1
4WithdrawnTreatmentLipotoxicity / Metabolic Syndromes1
4WithdrawnTreatmentStroke, Acute1
Not AvailableActive Not RecruitingNot AvailableHeart Failure1
Not AvailableActive Not RecruitingOtherChronic Heart Failure (CHF) / Sleep Apnea1
Not AvailableActive Not RecruitingTreatmentHeart Failure1
Not AvailableActive Not RecruitingTreatmentRenal Dysfunction / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableHealthy Normotensive Participants2
Not AvailableCompletedNot AvailableHealthy Volunteers2
Not AvailableCompletedNot AvailableHypertension,Essential1
Not AvailableCompletedPreventionAtherosclerosis1
Not AvailableCompletedPreventionMyocardial Infarction1
Not AvailableCompletedTreatmentCardiovascular Heart Disease1
Not AvailableCompletedTreatmentHealthy Volunteers1
Not AvailableCompletedTreatmentHigh Blood Pressure (Hypertension) / Left Ventricular Hypertrophy1
Not AvailableCompletedTreatmentRenal Function Disorder1
Not AvailableNot Yet RecruitingNot AvailableHeart Failure With Reduced Ejection Fraction (HFrEF)1
Not AvailableNot Yet RecruitingTreatmentAtrial Fibrillation (AF) / Cardiac Remodeling, Atrial / Sacubitril/Valsartan1
Not AvailableNot Yet RecruitingTreatmentHigh Blood Pressure (Hypertension)1
Not AvailableRecruitingNot AvailableHeart Failure1
Not AvailableRecruitingNot AvailableHeart Failure, Systolic1
Not AvailableRecruitingNot AvailableLower Leg Edema / Orthostatic Hypertension1
Not AvailableRecruitingNot AvailableObesity, Morbid1
Not AvailableRecruitingPreventionCardiotoxicity / Hematopoietic Stem Cell Transplantation (HSCT)1
Not AvailableRecruitingTreatmentAcute Myocardial Infarction (AMI)1
Not AvailableRecruitingTreatmentChronic Heart Failure (CHF)1
Not AvailableTerminatedPreventionAging / Angiotensin Receptor Antagonists / Human Immunodeficiency Virus (HIV) / Sarcopenia1
Not AvailableTerminatedTreatmentAortic Compliance / Diastolic Function / Insulin Sensitivity1
Not AvailableTerminatedTreatmentHigh Blood Pressure (Hypertension) / Microvascular Angina1
Not AvailableUnknown StatusNot AvailableHigh Blood Pressure (Hypertension)1
Not AvailableWithdrawnTreatmentCerebrovascular Accident1

Pharmacoeconomics

Manufacturers
  • Novartis pharmaceuticals corp
  • Novartis Corporation
Packagers
  • Advanced Pharmaceutical Services Inc.
  • AQ Pharmaceuticals Inc.
  • A-S Medication Solutions LLC
  • Bryant Ranch Prepack
  • Cardinal Health
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Doctor Reddys Laboratories Ltd.
  • Heartland Repack Services LLC
  • Lake Erie Medical and Surgical Supply
  • Murfreesboro Pharmaceutical Nursing Supply
  • Novartis AG
  • Nucare Pharmaceuticals Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Promex Medical Inc.
  • Resource Optimization and Innovation LLC
  • Southwood Pharmaceuticals
  • Stat Rx Usa
  • Vangard Labs Inc.
Dosage forms
FormRouteStrength
Tablet, film coatedOral
CapsuleOral160 mg/1
CapsuleOral80 mg/1
TabletOral160 mg/1
TabletOral320 mg/1
TabletOral320 mg
TabletOral40 mg
TabletOral40 mg/1
TabletOral80 mg/1
CapsuleOral
TabletOral
Tablet, film coatedOral
SolutionOral4 mg/1mL
TabletOral160 mg
TabletOral80 mg
Tablet, film coatedOral160 mg/1
Tablet, film coatedOral320 mg/1
Tablet, film coatedOral40 mg/1
Tablet, film coatedOral80 mg/1
TabletOral
Prices
Unit descriptionCostUnit
Diovan hct 320-25 mg tablet4.63USD tablet
Diovan hct 320-12.5 mg tablet4.1USD tablet
Diovan hct 160-25 mg tablet3.66USD tablet
Diovan hct 160-12.5 mg tablet3.27USD tablet
Diovan 320 mg tablet3.17USD tablet
Diovan hct 80-12.5 mg tablet3.0USD tablet
Diovan 160 mg tablet2.42USD tablet
Diovan 80 mg tablet2.33USD tablet
Diovan 40 mg tablet2.32USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5399578No1995-03-212012-03-21Us
CA2259148No2009-09-292017-06-18Canada
CA2036427No1998-12-292011-02-15Canada
US6294197Yes2001-09-252017-12-18Us
US5559111Yes1996-09-242019-01-21Us
US6395728No2002-05-282019-07-08Us
US5972990Yes1999-10-262017-04-26Us
US8168616No2012-05-012026-07-03Us
US8101599No2012-01-242023-05-16Us
US8475839Yes2013-07-022023-11-16Us
US8796331No2014-08-052023-01-14Us
US8101659No2012-01-242023-01-14Us
US7468390No2008-12-232023-11-27Us
US8404744No2013-03-262023-01-14Us
US8877938No2014-11-042027-05-27Us
US7803838No2010-09-282026-08-29Us
US7838552No2010-11-232027-10-04Us
US9388134No2016-07-122026-11-08Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)116-117 °Chttps://www.chemicalbook.com/ChemicalProductProperty_US_CB6182539.aspx
boiling point (°C)83-88https://www.trc-canada.com/product-detail/?V095750
water solubilitysoluble in ethanol, DMSO, and dimethyl formamide at 30 mg/mLhttps://www.caymanchem.com/pdfs/14178.pdf
logP1.499http://www.japsonline.com/admin/php/uploads/54_pdf.pdf
pKa4.73http://www.japsonline.com/admin/php/uploads/54_pdf.pdf
Predicted Properties
PropertyValueSource
Water Solubility0.0234 mg/mLALOGPS
logP3.68ALOGPS
logP5.27ChemAxon
logS-4.3ALOGPS
pKa (Strongest Acidic)4.37ChemAxon
pKa (Strongest Basic)-0.11ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area112.07 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity134.77 m3·mol-1ChemAxon
Polarizability47.27 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9956
Blood Brain Barrier-0.8032
Caco-2 permeable-0.6912
P-glycoprotein substrateSubstrate0.685
P-glycoprotein inhibitor INon-inhibitor0.5548
P-glycoprotein inhibitor IINon-inhibitor0.5966
Renal organic cation transporterNon-inhibitor0.8646
CYP450 2C9 substrateNon-substrate0.7722
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.5073
CYP450 1A2 substrateNon-inhibitor0.8707
CYP450 2C9 inhibitorNon-inhibitor0.5398
CYP450 2D6 inhibitorNon-inhibitor0.8816
CYP450 2C19 inhibitorInhibitor0.5539
CYP450 3A4 inhibitorNon-inhibitor0.5521
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5618
Ames testNon AMES toxic0.6384
CarcinogenicityNon-carcinogens0.645
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6518 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9766
hERG inhibition (predictor II)Non-inhibitor0.7388
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-001i-0000900000-45397dbc5403f1111d85
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-003r-0303900000-1056988fef13dc9becc8
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-004i-0900000000-65d8dfbf9280fcea77fb
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-004i-0900000000-77a9588a3e936c9d2e28
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0udi-0009000000-160f82ad0952fc9b3350
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-001i-0000900000-d7bf9d8976f47e44ab4a
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0fb9-0915000000-1f5a4e134cd8450810e7
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0900000000-19095db3835430e9fe16
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0900000000-00e9b9924b37c4db7a8d
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0900000000-fb8741bb91ee87d8245e
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-001i-0000900000-be5ab1c8cde8851235e3
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0fb9-0915000000-08501c181e1066f2aa0a
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0900000000-6cabcfa5948837eddb2e
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0900000000-d0aedd0bab06b374571a
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0901000000-a4572421f0a393f299a1
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0udi-0009000000-0f743f9e78dce83f2414
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-003r-0912600000-feeef5a05d8ef569460d
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-000i-0022900000-07c84eac301d580a8bea
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0a4u-0190000000-8a48f701b19b54e7ebf9
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0a4u-0190000000-34257438319cae238dcb
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0a4i-0590000000-403ef14fce06289de8e7
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0a59-0960000000-d4e79af5b474f613f6e9
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-052u-0093000000-ee050d1727838e542ce7
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-066r-0013900000-27f31e9591de9c0d036b
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4u-0096600000-2c9e5fef1cb7e2e64e67
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4u-0091000000-0bff344a92ee0cc41b8f
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0390000000-fa2f74ef15c1a6b93838
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a59-0960000000-ca847cc390cd0e68c6b6
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0pec-0920000000-5c29e64b37c8cde1c7ba
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0ziu-0910000000-08f3eecf83a71f4fb485
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4u-0096600000-598ea56da3433ecd4bab
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4u-0091000000-0aaf7a6567cb3745cb23
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0490000000-4b8d8ce6d0a486599b71
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a59-0950000000-6cd1be141d3f05844a75
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0pec-0920000000-053a50818908a33699b3
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0ziu-0910000000-c10b0879c877503826c5
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-066r-0013900000-af025bf00303b40b6d48
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-0122900000-e2d5ae1b4433254a8ebe
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4u-1492000000-bc19c44b1bd382b3180f
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-0012900000-1b87098801f65211057a
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4u-0392000000-5823d4f7c41e4fd6208b
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4u-0391100000-8997765a9ed3c9424c07

Taxonomy

Description
This compound belongs to the class of organic compounds known as valine and derivatives. These are compounds containing valine or a derivative thereof resulting from reaction of valine at the amino group or the carboxy group, or from the replacement of any hydrogen of glycine by a heteroatom.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Valine and derivatives
Alternative Parents
N-acyl-L-alpha-amino acids / Biphenyls and derivatives / Phenyltetrazoles and derivatives / N-acyl amines / Tertiary carboxylic acid amides / Heteroaromatic compounds / Monocarboxylic acids and derivatives / Carboxylic acids / Azacyclic compounds / Organopnictogen compounds
show 4 more
Substituents
N-acyl-alpha-amino acid / Valine or derivatives / N-acyl-alpha amino acid or derivatives / N-acyl-l-alpha-amino acid / Biphenyl / Phenyltetrazole / Monocyclic benzene moiety / N-acyl-amine / Benzenoid / Azole
show 17 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
monocarboxylic acid, monocarboxylic acid amide, biphenylyltetrazole (CHEBI:9927)

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
Receptor for angiotensin II. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
Gene Name
AGTR1
Uniprot ID
P30556
Uniprot Name
Type-1 angiotensin II receptor
Molecular Weight
41060.53 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Azizi M, Menard J, Bissery A, Guyenne TT, Bura-Riviere A, Vaidyanathan S, Camisasca RP: Pharmacologic demonstration of the synergistic effects of a combination of the renin inhibitor aliskiren and the AT1 receptor antagonist valsartan on the angiotensin II-renin feedback interruption. J Am Soc Nephrol. 2004 Dec;15(12):3126-33. [PubMed:15579516]
  3. Criscione L, de Gasparo M, Buhlmayer P, Whitebread S, Ramjoue HP, Wood J: Pharmacological profile of valsartan: a potent, orally active, nonpeptide antagonist of the angiotensin II AT1-receptor subtype. Br J Pharmacol. 1993 Oct;110(2):761-71. [PubMed:8242249]
  4. Shargorodsky M, Leibovitz E, Lubimov L, Gavish D, Zimlichman R: Prolonged treatment with the AT1 receptor blocker, valsartan, increases small and large artery compliance in uncomplicated essential hypertension. Am J Hypertens. 2002 Dec;15(12):1087-91. [PubMed:12460705]
  5. de Gasparo M, Whitebread S: Binding of valsartan to mammalian angiotensin AT1 receptors. Regul Pept. 1995 Nov 10;59(3):303-11. [PubMed:8577935]
  6. Siragy HM, El-Kersh MA, De Gasparo M, Webb RL, Carey RM: Differences in AT2 -receptor stimulation between AT1 -receptor blockers valsartan and losartan quantified by renal interstitial fluid cGMP. J Hypertens. 2002 Jun;20(6):1157-63. [PubMed:12023686]
  7. Stanfield, Cindy L.;Germann, William J. (2009). Principles of Human Physiology (3rd ed.). Benjamin-Cummings Publishing Company. [ISBN:978-0321556660]
  8. Valsartan HCT monograph [File]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Nakashima A, Kawashita H, Masuda N, Saxer C, Niina M, Nagae Y, Iwasaki K: Identification of cytochrome P450 forms involved in the 4-hydroxylation of valsartan, a potent and specific angiotensin II receptor antagonist, in human liver microsomes. Xenobiotica. 2005 Jun;35(6):589-602. [PubMed:16192110]
  2. Kamiyama E, Yoshigae Y, Kasuya A, Takei M, Kurihara A, Ikeda T: Inhibitory effects of angiotensin receptor blockers on CYP2C9 activity in human liver microsomes. Drug Metab Pharmacokinet. 2007 Aug;22(4):267-75. [PubMed:17827781]
  3. Cabaleiro T, Roman M, Ochoa D, Talegon M, Prieto-Perez R, Wojnicz A, Lopez-Rodriguez R, Novalbos J, Abad-Santos F: Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers. Drug Metab Dispos. 2013 Jan;41(1):224-9. doi: 10.1124/dmd.112.046292. Epub 2012 Nov 1. [PubMed:23118328]
  4. Guo G, Zhao Y, Chai J, Hao D, Song F: Effectiveness evaluation of cardiovascular drugs based on CYP2C9 target protein. Pak J Pharm Sci. 2015 Jul;28(4 Suppl):1545-9. [PubMed:26431654]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. Poirier A, Cascais AC, Funk C, Lave T: Prediction of pharmacokinetic profile of valsartan in human based on in vitro uptake transport data. J Pharmacokinet Pharmacodyn. 2009 Dec;36(6):585-611. doi: 10.1007/s10928-009-9139-3. Epub 2009 Nov 20. [PubMed:19936896]
  2. Poirier A, Cascais AC, Funk C, Lave T: Prediction of pharmacokinetic profile of valsartan in humans based on in vitro uptake-transport data. Chem Biodivers. 2009 Nov;6(11):1975-87. doi: 10.1002/cbdv.200900116. [PubMed:19937834]
  3. Hanna I, Alexander N, Crouthamel MH, Davis J, Natrillo A, Tran P, Vapurcuyan A, Zhu B: Transport properties of valsartan, sacubitril and its active metabolite (LBQ657) as determinants of disposition. Xenobiotica. 2018 Mar;48(3):300-313. doi: 10.1080/00498254.2017.1295171. Epub 2017 Mar 10. [PubMed:28281384]
  4. Alam K, Crowe A, Wang X, Zhang P, Ding K, Li L, Yue W: Regulation of Organic Anion Transporting Polypeptides (OATP) 1B1- and OATP1B3-Mediated Transport: An Updated Review in the Context of OATP-Mediated Drug-Drug Interactions. Int J Mol Sci. 2018 Mar 14;19(3). pii: ijms19030855. doi: 10.3390/ijms19030855. [PubMed:29538325]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. Poirier A, Cascais AC, Funk C, Lave T: Prediction of pharmacokinetic profile of valsartan in human based on in vitro uptake transport data. J Pharmacokinet Pharmacodyn. 2009 Dec;36(6):585-611. doi: 10.1007/s10928-009-9139-3. Epub 2009 Nov 20. [PubMed:19936896]
  2. Poirier A, Cascais AC, Funk C, Lave T: Prediction of pharmacokinetic profile of valsartan in humans based on in vitro uptake-transport data. Chem Biodivers. 2009 Nov;6(11):1975-87. doi: 10.1002/cbdv.200900116. [PubMed:19937834]
  3. Karlgren M, Ahlin G, Bergstrom CA, Svensson R, Palm J, Artursson P: In vitro and in silico strategies to identify OATP1B1 inhibitors and predict clinical drug-drug interactions. Pharm Res. 2012 Feb;29(2):411-26. doi: 10.1007/s11095-011-0564-9. Epub 2011 Aug 23. [PubMed:21861202]
  4. Alam K, Crowe A, Wang X, Zhang P, Ding K, Li L, Yue W: Regulation of Organic Anion Transporting Polypeptides (OATP) 1B1- and OATP1B3-Mediated Transport: An Updated Review in the Context of OATP-Mediated Drug-Drug Interactions. Int J Mol Sci. 2018 Mar 14;19(3). pii: ijms19030855. doi: 10.3390/ijms19030855. [PubMed:29538325]
  5. Hanna I, Alexander N, Crouthamel MH, Davis J, Natrillo A, Tran P, Vapurcuyan A, Zhu B: Transport properties of valsartan, sacubitril and its active metabolite (LBQ657) as determinants of disposition. Xenobiotica. 2018 Mar;48(3):300-313. doi: 10.1080/00498254.2017.1295171. Epub 2017 Mar 10. [PubMed:28281384]
  6. Valsartan Canadian Monograph [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
References
  1. Yamashiro W, Maeda K, Hirouchi M, Adachi Y, Hu Z, Sugiyama Y: Involvement of transporters in the hepatic uptake and biliary excretion of valsartan, a selective antagonist of the angiotensin II AT1-receptor, in humans. Drug Metab Dispos. 2006 Jul;34(7):1247-54. doi: 10.1124/dmd.105.008938. Epub 2006 Apr 19. [PubMed:16624871]
  2. Hanna I, Alexander N, Crouthamel MH, Davis J, Natrillo A, Tran P, Vapurcuyan A, Zhu B: Transport properties of valsartan, sacubitril and its active metabolite (LBQ657) as determinants of disposition. Xenobiotica. 2018 Mar;48(3):300-313. doi: 10.1080/00498254.2017.1295171. Epub 2017 Mar 10. [PubMed:28281384]
  3. Valsartan HCT Canadian Monograph [File]

Drug created on June 13, 2005 07:24 / Updated on December 07, 2019 14:16