Identification

Name
Valsartan
Accession Number
DB00177
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

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 435.5188
Monoisotopic: 435.227039819
Chemical Formula
C24H29N5O3
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

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.23,18

Associated Conditions
Contraindications & Blackbox Warnings
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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.18

TargetActionsOrganism
AType-1 angiotensin II receptor
antagonist
Humans
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]

Hover over products below to view reaction partners

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]

Adverse Effects
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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
AbataceptThe metabolism of Valsartan can be increased when combined with Abatacept.
AbirateroneThe metabolism of Valsartan can be decreased when combined with Abiraterone.
AcebutololThe risk or severity of hyperkalemia can be increased when Valsartan is combined with Acebutolol.
AceclofenacThe risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Valsartan is combined with Aceclofenac.
AcemetacinThe risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Valsartan is combined with Acemetacin.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Valsartan.
AcetohexamideThe metabolism of Acetohexamide can be decreased when combined with Valsartan.
Acetyl sulfisoxazoleThe metabolism of Valsartan can be decreased when combined with Acetyl sulfisoxazole.
AcetylcysteineThe excretion of Valsartan can be decreased when combined with Acetylcysteine.
Acetylsalicylic acidThe risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Valsartan is combined with Acetylsalicylic acid.
Additional Data Available
  • Extended Description
    Extended Description

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

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  • Severity
    Severity

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

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  • Evidence Level
    Evidence Level

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

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  • Action
    Action

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

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Food Interactions
  • Take with or without food. Co-administration with food slightly alters pharmacokinetics, but not to a clinically significant extent.

Products

Product Images
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Act ValsartanTabletOralActavis Pharma Company2011-02-162019-08-14Canada flag
Act ValsartanTabletOralActavis Pharma Company2011-02-162019-08-14Canada flag
Act ValsartanTabletOralActavis Pharma Company2011-02-162019-08-14Canada flag
Act ValsartanTabletOralActavis Pharma Company2011-02-162019-08-14Canada flag
CopaliaTablet, film coatedOralNovartis Europharm Limited2007-01-15Not applicableEU flag
CopaliaTablet, film coatedOralNovartis Europharm Limited2007-01-15Not applicableEU flag
CopaliaTablet, film coatedOralNovartis Europharm Limited2007-01-15Not applicableEU flag
CopaliaTablet, film coatedOralNovartis Europharm Limited2007-01-15Not applicableEU flag
CopaliaTablet, film coatedOralNovartis Europharm Limited2007-01-15Not applicableEU flag
CopaliaTablet, film coatedOralNovartis Europharm Limited2007-01-15Not applicableEU flag
Additional Data Available
  • Application Number
    Application Number

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

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  • Product Code
    Product Code

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

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEU flag
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEU flag
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEU flag
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEU flag
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEU flag
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEU flag
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEU flag
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEU flag
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEU flag
Amlodipine-valsartan MylanTablet, film coatedOralMylan S.A.S.2016-03-22Not applicableEU flag
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 EndRegionImage
Amlodipine and ValsartanValsartan (160 mg/1) + Amlodipine besylate (10 mg/1)Tablet, film coatedOralMylan Pharmaceuticals Inc.2015-03-30Not applicableUS flag
Amlodipine and ValsartanValsartan (160 mg/1) + Amlodipine besylate (5 mg/1)Tablet, film coatedOralAlembic Pharmaceuticals Inc.2016-12-01Not applicableUS flag
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine (5 mg/1)TabletOralAvKARE, Inc.2018-09-11Not applicableUS flag
Amlodipine and ValsartanValsartan (160 mg/1) + Amlodipine besylate (5 mg/1)Tablet, film coatedOralTrigen Laboratories, Inc.2010-12-282017-11-20US flag
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine besylate (10 mg/1)TabletOralLupin Pharmaceuticals2015-03-30Not applicableUS flag
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine (5 mg/1)TabletOralPar Pharmaceutical, Inc.2014-09-30Not applicableUS flag49884 0576 11 nlmimage10 ba3f5d3a
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine besylate (10 mg/1)TabletOralLupin Pharmaceuticals, Inc.2015-03-30Not applicableUS flag
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine besylate (5 mg/1)TabletOralAv Kare, Inc.2015-04-272017-05-01US flag
Amlodipine and ValsartanValsartan (160 mg/1) + Amlodipine besylate (5 mg/1)TabletOralLupin Pharmaceuticals2015-03-30Not applicableUS flag
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine besylate (5 mg/1)TabletOralLupin Pharmaceuticals, Inc.2015-03-31Not applicableUS flag

Categories

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
Drug Categories
Chemical TaxonomyProvided by Classyfire
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
Aromatic heteromonocyclic compound / Azacycle / Azole / Benzenoid / Biphenyl / Carbonyl group / Carboxamide group / Carboxylic acid / Heteroaromatic compound / Hydrocarbon derivative
show 17 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
monocarboxylic acid, monocarboxylic acid amide, biphenylyltetrazole (CHEBI:9927)

Chemical Identifiers

UNII
80M03YXJ7I
CAS number
137862-53-4
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)[[email protected]@H](C(C)C)C(O)=O

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. FDA Approved Drug Products: Diovan (valsartan) oral tablets [Link]
  19. NZ Data Sheet, Valsartan and sacubitril [File]
  20. Valsartan and Sacubitril FDA label [File]
  21. Valsartan and Amlodipine FDA label [File]
  22. Valsartan and Nevibolol FDA label [File]
  23. Health Canada Monograph - Valsartan [File]
Human Metabolome Database
HMDB0014323
KEGG Drug
D00400
PubChem Compound
60846
PubChem Substance
46509000
ChemSpider
54833
BindingDB
50049186
RxNav
69749
ChEBI
9927
ChEMBL
CHEMBL1069
ZINC
ZINC000003875259
Therapeutic Targets Database
DAP000363
PharmGKB
PA451848
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Valsartan
AHFS Codes
  • 24:32.08 — Angiotensin Ii Receptor Antagonists
FDA label
Download (237 KB)
MSDS
Download (24 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingBasic ScienceHypoxia / Obstructive Sleep Apnea (OSA) / Sleep Apnea1
4Active Not RecruitingTreatmentBlood Pressures / Stroke, Ischemic1
4Active Not RecruitingTreatmentHeart Failure1
4CompletedBasic ScienceType 2 Diabetes Mellitus1
4CompletedDiagnosticCongestive Heart Failure (CHF) / 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

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, coatedOral40 MG
TabletOral12.5 mg
Tablet, coatedOral2.5 mg
Tablet, coatedOral320 mg
Tablet, coatedOral1.25 mg
Tablet, coated5 mg
Tablet, film coated160 mg
Tablet, film coated320 mg
Tablet, film coated80 mg
TabletOral160 mg
Tablet, film coatedOral
CapsuleOral160 mg/1
CapsuleOral80 mg/1
TabletOral160 mg/1
TabletOral320 mg
TabletOral320 mg/1
TabletOral40 mg
TabletOral40 mg/1
TabletOral80 mg/1
Tablet, film coatedOral160 mg
Tablet, film coatedOral320 MG
Tablet, film coatedOral40 MG
CapsuleOral
Tablet, film coatedOral80 mg
TabletOral
Tablet, delayed releaseOral320 mg
Tablet, delayed releaseOral100 mg
Tablet, film coatedOral200 mg
Tablet, film coatedOral50 mg
Tablet, film coatedOral10 mg
Tablet, film coatedOral5 mg
TabletOral5 mg
Tablet, film coatedOral
Tablet, coatedOral100 mg
Tablet, coatedOral200 mg
Tablet, coatedOral50 mg
Tablet, coatedOral24 mg
Tablet, coatedOral49 mg
Tablet, coatedOral97 mg
SolutionOral4 mg/1mL
Tablet, coatedOral10 mg
TabletOral80 mg
Tablet, coatedOral5 mg
Capsule160 MG
Capsule80 MG
SolutionOral3 MG/ML
Tablet, coated160 MG
Tablet, coated320 MG
Tablet, coated40 MG
Tablet, coated80 MG
Tablet, film coatedOral160 mg/1
Tablet, film coatedOral320 mg/1
Tablet, film coatedOral40 mg/1
Tablet, film coatedOral80 mg/1
Tablet, coatedOral25 mg
Tablet, coatedOral12.5 mg
Tablet, film coatedOral120 MG
TabletOral
CapsuleOral160 MG
CapsuleOral40 MG
CapsuleOral80 MG
Tablet, coatedOral80 mg
Tablet, coatedOral160 mg
Tablet, film coatedOral12.5 mg
Tablet
Capsule, liquid filledOral160 mg
Capsule, liquid filledOral12.5 mg
Capsule, liquid filledOral80 mg
Tablet, coatedOral13.86857 mg
Tablet, coatedOral6.93429 mg
Capsule, liquid filledOral10 mg
Capsule, liquid filledOral5 mg
Tablet, film coated40 mg
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)Region
US5399578No1995-03-212012-03-21US flag
CA2259148No2009-09-292017-06-18Canada flag
CA2036427No1998-12-292011-02-15Canada flag
US6294197Yes2001-09-252017-12-18US flag
US5559111Yes1996-09-242019-01-21US flag
US6395728No2002-05-282019-07-08US flag
US5972990Yes1999-10-262017-04-26US flag
US8168616No2012-05-012026-07-03US flag
US8101599No2012-01-242023-05-16US flag
US8475839Yes2013-07-022023-11-16US flag
US8796331Yes2014-08-052023-07-14US flag
US8101659Yes2012-01-242023-07-14US flag
US7468390Yes2008-12-232024-05-27US flag
US8404744Yes2013-03-262023-07-14US flag
US8877938Yes2014-11-042027-11-27US flag
US7803838No2010-09-282026-08-29US flag
US7838552No2010-11-232027-10-04US flag
US9388134Yes2016-07-122027-05-08US flag
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

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 September 27, 2020 08:17

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