Identification

Name
Valsartan
Accession Number
DB00177  (APRD00133)
Type
Small Molecule
Groups
Approved, Investigational
Description

Valsartan is an angiotensin-receptor blocker (ARB) that may be used to treat a variety of cardiac conditions including hypertension, diabetic nephropathy and heart failure. Valsartan lowers blood pressure by antagonizing the renin-angiotensin-aldosterone system (RAAS); it competes with angiotensin II for binding to the type-1 angiotensin II receptor (AT1) subtype and prevents the blood pressure increasing effects of angiotensin II. Unlike angiotensin-converting enzyme (ACE) inhibitors, ARBs do not have the adverse effect of dry cough. Valsartan may be used to treat hypertension, isolated systolic hypertension, left ventricular hypertrophy and diabetic nephropathy. It may also be used as an alternative agent for the treatment of heart failure, systolic dysfunction, myocardial infarction and coronary artery disease.

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
External IDs
CGP 48933 / CGP-48933
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act ValsartanTablet160 mgOralActavis Pharma Company2011-02-16Not applicableCanada
Act ValsartanTablet80 mgOralActavis Pharma Company2011-02-16Not applicableCanada
Act ValsartanTablet320 mgOralActavis Pharma Company2011-02-16Not applicableCanada
Act ValsartanTablet40 mgOralActavis Pharma Company2011-02-16Not applicableCanada
DiovanTablet320 mg/1OralRebel Distributors2001-07-01Not applicableUs00078 0360 34 nlmimage10 f015780b
DiovanTablet40 mg/1OralCarilion Materials Management2001-07-01Not applicableUs00078 0423 15 nlmimage10 9d3b4eca
DiovanTablet160 mg/1OralCardinal Health2001-07-012015-05-31Us55154 965720180913 8702 fi8r66
DiovanTablet320 mg/1OralA-S Medication Solutions2001-07-01Not applicableUs54569 566620180907 15195 ncwo17
DiovanTablet80 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-02-282014-12-31Us
DiovanTablet320 mg/1OralPd Rx Pharmaceuticals, Inc.2001-07-01Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-valsartanTablet80 mgOralApotex Corporation2012-07-12Not applicableCanada
Apo-valsartanTablet320 mgOralApotex Corporation2012-07-12Not applicableCanada
Apo-valsartanTablet40 mgOralApotex Corporation2012-07-12Not applicableCanada
Apo-valsartanTablet160 mgOralApotex Corporation2012-07-12Not applicableCanada
Auro-valsartanTablet320 mgOralAuro Pharma Inc2014-02-06Not applicableCanada
Auro-valsartanTablet160 mgOralAuro Pharma Inc2014-02-06Not applicableCanada
Auro-valsartanTablet40 mgOralAuro Pharma Inc2014-02-06Not applicableCanada
Auro-valsartanTablet80 mgOralAuro Pharma Inc2014-02-06Not applicableCanada
Ava-valsartanTablet40 mgOralAvanstra Inc2011-08-182014-08-21Canada
Ava-valsartanTablet160 mgOralAvanstra Inc2011-08-182014-08-21Canada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Amlodipine and ValsartanValsartan (160 mg/1) + Amlodipine besylate (5 mg/1)Tablet, film coatedOralMylan Pharmaceuticals Inc.2015-03-30Not applicableUs00378 1721 93 nlmimage10 db48ed97
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine besylate (10 mg/1)TabletOralNovel Laboratories, Inc.2015-03-30Not applicableUs
Amlodipine and ValsartanValsartan (160 mg/1) + Amlodipine besylate (5 mg/1)Tablet, film coatedOralAlembic Pharmaceuticals Inc.2016-12-01Not applicableUs
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine besylate (10 mg/1)Tablet, film coatedOralTrigen Laboratories, Inc.2010-12-282017-11-20Us
Amlodipine and ValsartanValsartan (160 mg/1) + Amlodipine besylate (5 mg/1)TabletOralLupin Pharmaceuticals2015-03-30Not applicableUs
AMLODIPINE and VALSARTANValsartan (160 mg/1) + Amlodipine besylate (5 mg/1)TabletOralNovel Laboratories, Inc.2015-03-30Not applicableUs
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine besylate (10 mg/1)TabletOralLupin Pharmaceuticals2015-03-30Not applicableUs
Amlodipine and ValsartanValsartan (320 mg/1) + Amlodipine besylate (10 mg/1)Tablet, film coatedOralAlembic Pharmaceuticals Limited2016-12-01Not 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 (160 mg/1) + Amlodipine besylate (10 mg/1)Tablet, film coatedOralAurobindo Pharma Limited2016-04-22Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
ImpridaValsartan (160 mg) + Amlodipine (5 mg)Tablet, film coatedOralNovartis Europharm Limited2007-01-172017-05-11Eu
ImpridaValsartan (160 mg) + Amlodipine (10 mg)Tablet, film coatedOralNovartis Europharm Limited2007-01-172017-05-11Eu
ImpridaValsartan (160 mg) + Amlodipine (5 mg)Tablet, film coatedOralNovartis Europharm Limited2007-01-172017-05-11Eu
ImpridaValsartan (160 mg) + Amlodipine (10 mg)Tablet, film coatedOralNovartis Europharm Limited2007-01-172017-05-11Eu
ImpridaValsartan (80 mg) + Amlodipine (5 mg)Tablet, film coatedOralNovartis Europharm Limited2007-01-172017-05-11Eu
ImpridaValsartan (160 mg) + Amlodipine (10 mg)Tablet, film coatedOralNovartis Europharm Limited2007-01-172017-05-11Eu
ImpridaValsartan (160 mg) + Amlodipine (10 mg)Tablet, film coatedOralNovartis Europharm Limited2007-01-172017-05-11Eu
ImpridaValsartan (160 mg) + Amlodipine (5 mg)Tablet, film coatedOralNovartis Europharm Limited2007-01-172017-05-11Eu
ImpridaValsartan (80 mg) + Amlodipine (5 mg)Tablet, film coatedOralNovartis Europharm Limited2007-01-172017-05-11Eu
ImpridaValsartan (80 mg) + Amlodipine (5 mg)Tablet, film coatedOralNovartis Europharm Limited2007-01-172017-05-11Eu
International/Other Brands
Diovan
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

May be used as a first line agent to treat uncomplicated hypertension, isolated systolic hypertension and left ventricular hypertrophy. May be used as a first line agent to delay progression of diabetic nephropathy. Losartan may be also used as a second line agent in the treatment of congestive heart failure, systolic dysfunction, myocardial infarction and coronary artery disease in those intolerant of ACE inhibitors.

Associated Conditions
Pharmacodynamics

Valsartan belongs to a class of antihypertensive agents called angiotensin II receptor blockers (ARBs). Valsartan is a specific and selective type-1 angiotensin II receptor (AT1) antagonist which blocks the blood pressure increasing effects angiotensin II via the renin-angiotensin-aldosterone system (RAAS). RAAS is a homeostatic mechanism for regulating hemodynamics, water and electrolyte balance. During sympathetic stimulation or when renal blood pressure or blood flow is reduced, renin is released from granular cells of the juxtaglomerular apparatus in the kidneys. Renin cleaves circulating angiotensinogen to angiotensin I, which is cleaved by angiotensin converting enzyme (ACE) to angiotensin II. Angiotensin II increases blood pressure by increasing total peripheral resistance, increasing sodium and water reabsorption in the kidneys via aldosterone secretion, and altering cardiovascular structure. Angiotensin II binds to two receptors: AT1 and type-2 angiotensin II receptor (AT2). AT1 is a G-protein coupled receptor (GPCR) that mediates the vasoconstrictive and aldosterone-secreting effects of angiotensin II. Studies performed in recent years suggest that AT2 antagonizes AT1-mediated effects and directly affects long-term blood pressure control by inducing vasorelaxation and increasing urinary sodium excretion. Angiotensin receptor blockers (ARBs) are non-peptide competitive inhibitors of AT1. ARBs block the ability of angiotensin II to stimulate pressor and cell proliferative effects. Unlike ACE inhibitors, ARBs do not affect bradykinin-induced vasodilation. The overall effect of ARBs is a decrease in blood pressure.

Mechanism of action

Valsartan is an ARB that selectively inhibits the binding of angiotensin II to AT1, which is found in many tissues such as vascular smooth muscle and the adrenal glands. This effectively inhibits the AT1-mediated vasoconstrictive and aldosterone-secreting effects of angiotensin II and results in a decrease in vascular resistance and blood pressure. Valsartan is selective for AT1 and has virtually no affinity for AT2. Inhibition of aldosterone secretion may inhibit sodium and water reabsorption in the kidneys while decreasing potassium excretion. The primary metabolite of valsartan, valeryl 4-hydroxy valsartan, has no pharmacological activity.

TargetActionsOrganism
AType-1 angiotensin II receptor
antagonist
Human
Absorption

Absolute bioavailability = 23% with high variability.

Volume of distribution
  • 17 L (low tissue distribution)
Protein binding

94 - 97% bound to serum proteins, primarily serum albumin

Metabolism

Valsartan is excreted largely as unchanged drug (80%) and is minimally metabolized in humans. The primary circulating metabolite, 4-OH-valsartan, is pharmacologically inactive and produced CYP2C9. 4-OH-valsartan accounts for approximately 9% of the circulating dose of valsartan. Although valsartan is metabolized by CYP2C9, CYP-mediated drug-drug interactions between valsartan and other drugs is unlikely.

Route of elimination

83% of absorbed valsartan is excreted in feces and 13% is excreted in urine, primarily as unchanged drug

Half life

The initial phase t1/2 α is < 1 hour while the terminal phase t1/2 β is 5-9 hours.

Clearance
  • 2 L/h [IV administration]
  • 4.5 L/h [heart Failure patients receiving oral administration 40 to 160 mg twice a day]
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Valsartan Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Valsartan.
AbirateroneThe metabolism of Valsartan can be decreased when combined with Abiraterone.
AcebutololThe risk or severity of adverse effects 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.
AcetaminophenThe metabolism of Acetaminophen 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.
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. Bader, M. (2004). Renin-angiotensin-aldosterone system. In Encyclopedic reference of molecular pharmacology (pp. 810-814). Berlin: Springer. [ISBN:9783540298328]
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
IUPHAR
3937
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Valsartan
ATC Codes
C09DX02 — Valsartan and aliskirenC09DB08 — Valsartan and lercanidipineC10BX10 — Rosuvastatin and valsartanC09DB01 — Valsartan and amlodipineC09DX01 — Valsartan, amlodipine and hydrochlorothiazideC09DA03 — Valsartan and diureticsC09CA03 — ValsartanC09DX04 — Valsartan and sacubitril
AHFS Codes
  • 24:32.08 — Angiotensin Ii Receptor Antagonists
FDA label
Download (237 KB)
MSDS
Download (36.2 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Not Yet RecruitingBasic ScienceThyroid Cancer, Medullary1
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) / Glomerulonephritis minimal lesion / High Blood Pressure (Hypertension)1
1CompletedBasic ScienceHealthy Male Subjects1
1CompletedOtherHigh Blood Pressure (Hypertension) / Hyperlipidemias1
1CompletedSupportive CareHealthy Volunteers1
1CompletedTreatmentHealthy Male Volunteers1
1CompletedTreatmentHealthy Normotensive Volunteers1
1CompletedTreatmentHealthy Volunteers4
1CompletedTreatmentHigh Blood Pressure (Hypertension)1
1CompletedTreatmentHigh Blood Pressure (Hypertension) / Hyperlipidemias2
1CompletedTreatmentType 2 Diabetes Mellitus1
1Not Yet RecruitingTreatmentBladder Small Cell Neuroendocrine Carcinoma / Castration-Resistant Prostate Carcinoma / Metastatic Bladder Urothelial Carcinoma / Metastatic Urethral Urothelial Carcinoma / Prostate Carcinoma Metastatic in the Bone / Prostate Neuroendocrine Neoplasm / Prostate Small Cell Carcinoma / Stage III Bladder Cancer AJCC v8 / Stage III Prostate Cancer AJCC v8 / Stage III Urethral Cancer AJCC v8 / Stage IV Bladder Cancer AJCC v8 / Stage IV Prostate Cancer AJCC v8 / Stage IV Urethral Cancer AJCC v8 / Stage IVA Bladder Cancer AJCC v8 / Stage IVB Bladder Cancer AJCC v8 / Transitional Cell Carcinoma / Ureter Small Cell Carcinoma1
1Not Yet RecruitingTreatmentHealthy Male 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 Cardiomyopathy1
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
2RecruitingTreatmentDiastolic Dysfunction1
2RecruitingTreatmentPeripheral Arterial Disease (PAD)1
2WithdrawnBasic ScienceHeart Failure, Unspecified1
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 RecruitingTreatmentHeart Failure With Preserved Ejection Fraction (HFpEF)1
3CompletedPreventionAtherosclerosis / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / High Blood Pressure (Hypertension) / High Cholesterol / Type 2 Diabetes Mellitus1
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)37
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
3CompletedTreatmentNonvalvular Atrial Fibrillation1
3CompletedTreatmentPediatric Hypertension With or Without CKD1
3CompletedTreatmentStage 1 Hypertension / Stage 2 Hypertension1
3Not Yet RecruitingTreatmentHeart Failure, Unspecified1
3Not Yet RecruitingTreatmentHypertensive Heart Disease1
3RecruitingOtherElevated Blood Pressure / High Blood Pressure (Hypertension) / Pre-Diabetic / Type 2 Diabetes Mellitus1
3RecruitingTreatmentAcute Myocardial Infarction (AMI)1
3RecruitingTreatmentChronic Heart Failure (CHF) / Heart Failure, Unspecified1
3RecruitingTreatmentHeart Failure With Preserved Ejection Fraction (HFpEF)1
3TerminatedHealth Services ResearchEndothelial Dysfunction / Oxidative Stress1
3TerminatedTreatmentHigh Blood Pressure (Hypertension)1
3WithdrawnTreatmentHuman Immunodeficiency Virus (HIV) Infections / Kidney Diseases1
4Active Not RecruitingBasic ScienceArterial hypoxia / Obstructive Sleep Apnea (OSA) / Sleep Apnea Syndrome1
4Active Not RecruitingTreatmentBlood Pressures / Stroke, Ischemic1
4CompletedBasic ScienceType 2 Diabetes Mellitus1
4CompletedDiagnosticCongestive Heart Failure (CHF) / High Blood Pressure (Hypertension) / Ischaemic Heart Diseases / Strokes1
4CompletedOtherHeart Failure With Reduced Ejection Fraction (HFrEF)1
4CompletedPreventionBlood Pressures / Hypertension Complicated / Left Ventricular Hypertrophy1
4CompletedPreventionHigh Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
4CompletedPreventionNon-Hodgkin's Lymphoma (NHL)1
4CompletedSupportive CareHearth Failure With Reduced Ejection Fraction (HFrEF)1
4CompletedTreatmentAlbuminuria / High Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
4CompletedTreatmentBlood Pressures1
4CompletedTreatmentCardiovascular Disease (CVD) / Chronic Kidney Disease (CKD) / Hypertension,Essential / Strokes1
4CompletedTreatmentCardiovascular Disease (CVD) / Deficiency, Vitamin D / Osteoporosis / Secondary Hyp1
4CompletedTreatmentChronic Kidney Disease (CKD) / High Blood Pressure (Hypertension)1
4CompletedTreatmentCongestive Cardiomyopathy1
4CompletedTreatmentCongestive Heart Failure (CHF) / 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) / 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
4CompletedTreatmentEssential,Hypertension1
4CompletedTreatmentGlomerulonephritis / IgA Nephropathy1
4CompletedTreatmentHealthy Volunteers1
4CompletedTreatmentHeart Failure, Unspecified / Ventricular Dysfunction, Left1
4CompletedTreatmentHigh Blood Pressure (Hypertension)36
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Impaired Glucose Tolerance (IGT)1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Left Ventricular Hypertrophy1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Metabolic Syndromes1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Proteinuria / Type 2 Diabetes Mellitus1
4CompletedTreatmentHypertension, Dyslypidaemia1
4CompletedTreatmentHypertension,Essential3
4CompletedTreatmentMicroalbuminuria / Proteinuria1
4CompletedTreatmentMitral Valve Insufficiency / Symptomatic left ventricular ejection fraction ≤ 35% Chronic heart failure1
4CompletedTreatmentMyocardial Infarction1
4CompletedTreatmentPostoperative pain1
4CompletedTreatmentStage 2 Hypertension1
4CompletedTreatmentStage 2 Systolic Hypertension1
4Not Yet RecruitingTreatmentHypertension;Nephropathy1
4RecruitingOtherHeart Failure, Unspecified1
4RecruitingPreventionBlood Pressures / High Blood Pressure (Hypertension) / Strokes1
4RecruitingPreventionFirst Time Dual Chamber Pacemaker Implantation1
4RecruitingSupportive CareAcute Heart Failure (AHF)1
4RecruitingTreatmentDiabetes Mellitus (DM) / Heart Failure, Unspecified1
4RecruitingTreatmentHeart Failure With Preserved Ejection Fraction (HFpEF)1
4RecruitingTreatmentHeart Failure With Reduced Ejection Fraction (HFrEF)1
4RecruitingTreatmentHeart Failure, Systolic1
4RecruitingTreatmentHeart Failure, Unspecified4
4RecruitingTreatmentHigh Blood Pressure (Hypertension)1
4RecruitingTreatmentPrimary IgA Nephropathy1
4TerminatedPreventionHigh Blood Pressure (Hypertension)1
4TerminatedTreatmentDiabetic Nephropathies / Glomerulonephritis, Membranous / Glomerulopathy (Obesity-associated) / Glomerulosclerosis, Focal Segmental / Hypertensive Nephrosclerosis / IgA Nephropathy / Proteinuric Kidney Disease1
4TerminatedTreatmentDiabetic Nephropathies / High Blood Pressure (Hypertension)1
4TerminatedTreatmentNonvalvular Atrial Fibrillation1
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 (CHF) / High Blood Pressure (Hypertension) / Ischaemic Heart Diseases1
4Unknown StatusTreatmentDiabetes Mellitus (DM)1
4Unknown StatusTreatmentHypertension,Essential1
4Unknown StatusTreatmentLipotoxicity / Metabolic Syndromes1
4Unknown StatusTreatmentMajor Depressive Disorder (MDD)1
4Unknown StatusTreatmentSmall Abdominal Aortic Aneurysm1
4WithdrawnTreatmentCongestive Heart Failure (CHF) / High Blood Pressure (Hypertension)1
4WithdrawnTreatmentHeart Failure With Reduced Ejection Fraction (HFrEF)1
4WithdrawnTreatmentStroke, Acute1
Not AvailableActive Not RecruitingNot AvailableHeart Failure, Unspecified1
Not AvailableActive Not RecruitingTreatmentRenal Dysfunction / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableHealthy Normotensive Participants2
Not AvailableCompletedNot AvailableHealthy Volunteers2
Not AvailableCompletedPreventionAtherosclerosis1
Not AvailableCompletedTreatmentRenal Function Disorder1
Not AvailableNot Yet RecruitingNot AvailableHeart Failure With Reduced Ejection Fraction (HFrEF)1
Not AvailableNot Yet RecruitingNot AvailableHeart Failure, Systolic1
Not AvailableNot Yet RecruitingTreatmentHigh Blood Pressure (Hypertension)1
Not AvailableRecruitingNot AvailableLower Leg Edema / Orthostatic Hypertension1
Not AvailableRecruitingNot AvailableObesity, Morbid1
Not AvailableRecruitingOtherChronic Heart Failure (CHF) / Sleep Apnea Syndrome1
Not AvailableRecruitingTreatmentCongestive 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 Accidents1

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
CapsuleOral160 mg/1
CapsuleOral80 mg/1
TabletOral160 mg/1
TabletOral320 mg/1
TabletOral320 mg
TabletOral40 mg/1
TabletOral40 mg
TabletOral80 mg/1
CapsuleOral160 mg
TabletOral160 mg
CapsuleOral80 mg
TabletOral80 mg
TabletOral
Tablet, film coatedOral
SolutionOral4 mg/1mL
Tablet, film coatedOral160 mg/1
Tablet, film coatedOral320 mg/1
Tablet, film coatedOral40 mg/1
Tablet, film coatedOral80 mg/1
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

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)116-117 °CNot Available
logP5.8Not Available
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
Human
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]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da

Transporters

Kind
Protein
Organism
Human
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]
Kind
Protein
Organism
Human
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]

Drug created on June 13, 2005 07:24 / Updated on November 18, 2018 04:39