Azilsartan medoxomil

Identification

Summary

Azilsartan medoxomil is an angiotensin II receptor blocker used to treat hypertension alone or in combination with other antihypertensive agents, such as chlorthalidone.

Brand Names
Edarbi, Edarbyclor
Generic Name
Azilsartan medoxomil
DrugBank Accession Number
DB08822
Background

Azilsartan medoxomil is a prodrug that is broken down to azilsartan, which belongs in the angiotensin-receptor blocking (ARB) drug class. It is a selective AT1 subtype angiotensin II receptor antagonist. Azilsartan medoxomil is a relatively recently-developed antihypertensive drug that was first approved by the FDA in February 2011.1 Many guidelines recommend the use of ARBs as first-line therapy when initiating antihypertensive therapy and indicate that the clinical efficacy of ARBs is comparable to angiotensin-converting enzyme (ACE) inhibitors that are also used as first-line treatment for hypertension.3

Azilsartan medoxomil is marketed under the brand name Edarbi. It is used to treat hypertension as monotherapy or in combination with other antihypertensive drugs. It is also available in a combination product with chlorthalidone. As hypertension is a major risk factor for cardiovascular disease,1 early management of hypertension has several implications on patients' survival rate and quality of life in the future. Lowering blood pressure is associated with a reduced risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.6 Azilsartan medoxomil is thus speculated to lower mortality rates and the onset of cardiovascular disease. Although there is no clinical significance yet determined, azilsartan medoxomil may have potential off-label uses in patients with a history of myocardial infarction or heart failure.3

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 568.5336
Monoisotopic: 568.159413764
Chemical Formula
C30H24N4O8
Synonyms
  • Azilsartan
  • Azilsartan kamedoxomil
  • Azilsartan médoxomil
  • Azilsartan medoxomil
  • Azilsartán medoxomilo
  • Azilsartanum medoxomilum
External IDs
  • TAK 491
  • TAK-491
  • TAK-536

Pharmacology

Indication

Azilsartan medoxomil is indicated for the treatment of hypertension to lower blood pressure in patients over 18 years of age. It may be used either alone or in combination with other antihypertensive agents. Some antihypertensive drugs have lesser effects on blood pressure in black patients.6

Azilsartan medoxomil is available as a fixed-dose combination product with chlorthalidone, which is indicated for the treatment of hypertension in patients whose hose blood pressure is not adequately controlled on monotherapy. It may be used as initial therapy if a patient is likely to need multiple drugs to achieve blood pressure goals.7

Azilsartan medoxomil belongs to the angiotensin-receptor blocking (ARB) class of drugs, which are used to decrease the progression of moderate-to-severe albuminuria and prevent the recurrence of atrial fibrillation as off-label uses in patients with diabetes mellitus and hypertension.3

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Pharmacodynamic effects of azilsartan medoxomil are mediated by its active metabolite, azilsartan. Azilsartan inhibits the pressor effects of an angiotensin II infusion in a dose-related manner.1 At a single 32 mg dose, azilsartan inhibited the maximal pressor effect by approximately 90% at peak plasma concentrations and by 60% at 24 hours after administration. In healthy subjects receiving single and repeated doses of azilsartan medoxomil, plasma angiotensin I and II concentrations and plasma renin activity increased, while plasma aldosterone concentrations decreased.6 Like other ARBs, azilsartan causes dose-dependent decrease in peripheral resistance and decreases smooth muscle vascular tone.4 As azilsartan blocks the angiotensin II receptor, the negative regulatory feedback of angiotensin II on renin secretion is inhibited; however, the resulting increased plasma renin activity and angiotensin II circulating levels do not overcome the blood pressure-lowering effect of azilsartan. Blood pressure-lowering effects of antihypertensive agents can be reduced in patients of African descent.6 However, there are no recommended dosage adjustment of azilsartan on the basis of a patient’s sex, race, or degree of renal or hepatic impairment.5

Azilsartan medoxomil has negligible effects on serum potassium or sodium levels. Azilsartan does not affect the biosynthesis of angiotensin II nor bradykinin levels. It also does not bind to any ion channels that are involved in cardiovascular regulation.6

Mechanism of action

The renin-angiotensin-aldosterone system regulates blood pressure. Angiotensin II is a peptide hormone that is a principal pressor agent in the renin-angiotensin-aldosterone system.1 It is a potent, direct vasoconstrictor that binds to the angiotensin II type 1 receptor (AT1 receptor) to stimulate the synthesis and release of aldosterone and promote cardiac stimulation. Angiotensin II promotes renal tubular reabsorption of sodium, resulting in water retention.1,6 It also inhibits further secretion of renin. AT1 receptors are highly expressed in vascular smooth muscle and the adrenal gland.3

Azilsartan medoxomil is a prodrug that is hydrolyzed to its active metabolite, azilsartan, in the gastrointestinal tract following oral administration. Azilsartan selectively binds to AT1 receptors as an antagonist, blocking vasoconstrictor and aldosterone-secreting effects of angiotensin II. Azilsartan has more than a 10,000-fold greater affinity for the AT1 receptor than for the AT2 receptor, which is predominantly involved in cardiovascular homeostasis.6 Azilsartan appears to dissociate from AT1 receptors much more slowly than other ARBs,2 which explains its longer duration of action when compared to other ARBs.4

TargetActionsOrganism
AType-1 angiotensin II receptor
antagonist
Humans
Absorption

During absorption, azilsartan medoxomil is hydrolyzed to azilsartan. The parent drug is not detectable in plasma after oral administration. The absolute bioavailability of azilsartan is estimated to be 60%. Tmax ranges from 1.5 to three hours. Steady-state levels of azilsartan are achieved within five days, and no accumulation in plasma occurs with repeated once-daily dosing.6

Volume of distribution

The volume of distribution of azilsartan is approximately 16 L. In rats, a minimal amount of radiolabelled drug crossed the blood-brain barrier. Azilsartan crossed the placental barrier in pregnant rats and was distributed to the fetus.6

Protein binding

Azilsartan is >99% bound to human plasma proteins, mainly serum albumin. Protein binding is constant at azilsartan plasma concentrations well above the range achieved with recommended doses.6

Metabolism

After azilsartan medoxomil is hydrolyzed into its active metabolite, azilsartan is metabolized to two primary metabolites, which are pharmacologically inactive. The major metabolite in plasma is metabolite M-II, which is formed via O-dealkylation mediated by CYP2C9. The minor metabolite is metabolite M-I, which is formed via decarboxylation mediated by CYP2C8 and CYP2B6. MII has approximately 50% systemic exposure of azilsartan, and MI has less than 1% systemic exposure of azilsartan.5,6

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Route of elimination

Following oral administration of 14C-labeled azilsartan medoxomil, approximately 55% of radioactivity was recovered in feces and approximately 42% in urine. Of the recovered dose in urine, about 15% was excreted as azilsartan.6

Half-life

The elimination half-life of azilsartan is approximately 11 hours.6

Clearance

Renal clearance of azilsartan is approximately 2.3 mL/min.6

Adverse Effects
Adverseeffects
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Toxicity

No maximum toxic doses have been established yet for azilsartan.3 There is limited human data available related to azilsartan medoxomil overdosage. In clinical trials, healthy subjects tolerated once-daily doses up to 320 mg of azilsartan medoxomil well. In the event of drug overdose, supportive measures should be initiated as azilsartan is not dialyzable.6

Azilsartan is a teratogenic agent with a risk of congenital abnormalities. Azilsartan and other ARB drugs are considered fetotoxic during the second and third trimesters.3,6

Pathways
Not Available
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
AcebutololAcebutolol may increase the hypotensive activities of Azilsartan medoxomil.
AceclofenacThe risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Azilsartan medoxomil is combined with Aceclofenac.
AcemetacinThe risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Azilsartan medoxomil is combined with Acemetacin.
Acetylsalicylic acidThe risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Azilsartan medoxomil is combined with Acetylsalicylic acid.
AlclofenacThe risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Azilsartan medoxomil is combined with Alclofenac.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Azilsartan medoxomil.
AlfentanilAlfentanil may decrease the antihypertensive activities of Azilsartan medoxomil.
AlfuzosinAlfuzosin may increase the hypotensive activities of Azilsartan medoxomil.
AliskirenAliskiren may increase the hypotensive and hyperkalemic activities of Azilsartan medoxomil.
AlmotriptanAlmotriptan may decrease the antihypertensive activities of Azilsartan medoxomil.
Interactions
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Food Interactions
  • Take with or without food. Food does not affect the bioavailability.

Products

Products2
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
EdarbiTablet80 mgOralTakeda Pharma A/S2020-12-16Not applicableEU flag
EdarbiTablet20 mgOralTakeda Pharma A/S2020-12-16Not applicableEU flag
EdarbiTablet40 mgOralTakeda Pharma A/S2020-12-16Not applicableEU flag
EdarbiTablet20 mgOralTakeda Pharma A/S2020-12-16Not applicableEU flag
EdarbiTablet40 mg/1OralArbor Pharmaceuticals2013-02-01Not applicableUS flag
EdarbiTablet80 mgOralTakeda Pharma A/S2020-12-16Not applicableEU flag
EdarbiTablet80 mgOralBausch Health, Canada Inc.2012-11-08Not applicableCanada flag
EdarbiTablet20 mgOralTakeda Pharma A/S2020-12-16Not applicableEU flag
EdarbiTablet40 mgOralTakeda Pharma A/S2020-12-16Not applicableEU flag
EdarbiTablet80 mgOralTakeda Pharma A/S2020-12-16Not applicableEU flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
EDARBI CLD®Azilsartan medoxomil (40 mg) + Chlorthalidone (25 mg)Tablet, coatedOralBAXALTA COLOMBIA S.A.S.2014-04-10Not applicableColombia flag
EDARBI CLD® 40MG/12.5MGAzilsartan medoxomil (40 mg) + Chlorthalidone (12.5 mg)Tablet, coatedOralBAXALTA COLOMBIA S.A.S.2014-04-22Not applicableColombia flag
EdarbyclorAzilsartan medoxomil (40 mg/1) + Chlorthalidone (12.5 mg/1)TabletOralArbor Pharmaceuticals2013-02-01Not applicableUS flag
EdarbyclorAzilsartan medoxomil (40 mg/1) + Chlorthalidone (25 mg/1)TabletOralTakeda2011-12-232018-05-01US flag
EdarbyclorAzilsartan medoxomil (80 mg) + Chlorthalidone (12.5 mg)TabletOralBausch Health, Canada Inc.2013-03-21Not applicableCanada flag
EdarbyclorAzilsartan medoxomil (80 mg/1) + Chlorthalidone (12.5 mg/1)TabletOralTakeda Pharmaceuticals America, Inc.2011-12-232011-12-14US flag
EdarbyclorAzilsartan medoxomil (40 mg) + Chlorthalidone (25 mg)TabletOralBausch Health, Canada Inc.2013-03-21Not applicableCanada flag
EdarbyclorAzilsartan medoxomil (40 mg/1) + Chlorthalidone (12.5 mg/1)TabletOralTakeda2011-12-232018-05-01US flag
EdarbyclorAzilsartan medoxomil (40 mg/1) + Chlorthalidone (25 mg/1)TabletOralArbor Pharmaceuticals2013-02-01Not applicableUS flag
EdarbyclorAzilsartan medoxomil (20 mg/1) + Chlorthalidone (12.5 mg/1)TabletOralTakeda Pharmaceuticals America, Inc.2011-12-232011-12-14US flag

Categories

ATC Codes
C09CA09 — Azilsartan medoxomilC09DA09 — Azilsartan medoxomil and diuretics
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as biphenyls and derivatives. These are organic compounds containing to benzene rings linked together by a C-C bond.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Biphenyls and derivatives
Direct Parent
Biphenyls and derivatives
Alternative Parents
Phenyloxadiazoles / Benzimidazoles / Alkyl aryl ethers / N-substituted imidazoles / Carbonic acid diesters / Vinylogous amides / Heteroaromatic compounds / Carboxylic acid esters / Oxacyclic compounds / Monocarboxylic acids and derivatives
show 5 more
Substituents
1,2,4-oxadiazole / Alkyl aryl ether / Aromatic heteropolycyclic compound / Azacycle / Azole / Benzimidazole / Biphenyl / Carbonic acid diester / Carboxylic acid derivative / Carboxylic acid ester
show 17 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
aromatic ether, carboxylic ester, dioxolane, cyclic carbonate ester, benzimidazoles, 1,2,4-oxadiazole (CHEBI:68845)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
LL0G25K7I2
CAS number
863031-21-4
InChI Key
QJFSABGVXDWMIW-UHFFFAOYSA-N
InChI
InChI=1S/C30H24N4O8/c1-3-38-28-31-23-10-6-9-22(27(35)39-16-24-17(2)40-30(37)41-24)25(23)34(28)15-18-11-13-19(14-12-18)20-7-4-5-8-21(20)26-32-29(36)42-33-26/h4-14H,3,15-16H2,1-2H3,(H,32,33,36)
IUPAC Name
(5-methyl-2-oxo-2H-1,3-dioxol-4-yl)methyl 2-ethoxy-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl]methyl}-1H-1,3-benzodiazole-7-carboxylate
SMILES
CCOC1=NC2=C(N1CC1=CC=C(C=C1)C1=CC=CC=C1C1=NOC(=O)N1)C(=CC=C2)C(=O)OCC1=C(C)OC(=O)O1

References

Synthesis Reference

Kohara Y, Kubo K, Imamiya E, Wada T, Inada Y, Naka T: Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisosteres. J Med Chem. 1996 Dec 20;39(26):5228-35.

General References
  1. Jones JD, Jackson SH, Agboton C, Martin TS: Azilsartan Medoxomil (Edarbi): The Eighth Angiotensin II Receptor Blocker. P T. 2011 Oct;36(10):634-40. [Article]
  2. Kurtz TW, Kajiya T: Differential pharmacology and benefit/risk of azilsartan compared to other sartans. Vasc Health Risk Manag. 2012;8:133-43. doi: 10.2147/VHRM.S22595. Epub 2012 Feb 28. [Article]
  3. Hardin MD, Jacobs TF: Azilsartan . [Article]
  4. Pradhan A, Tiwari A, Sethi R: Azilsartan: Current Evidence and Perspectives in Management of Hypertension. Int J Hypertens. 2019 Nov 3;2019:1824621. doi: 10.1155/2019/1824621. eCollection 2019. [Article]
  5. De Caterina AR, Harper AR, Cuculi F: Critical evaluation of the efficacy and tolerability of azilsartan. Vasc Health Risk Manag. 2012;8:299-305. doi: 10.2147/VHRM.S22589. Epub 2012 May 14. [Article]
  6. FDA Approved Drug Products: Edarbi (azilsartan medoxomil) oral tablets [Link]
  7. FDA Approved Drug Products: EDARBYCLOR (azilsartan medoxomil and chlorthalidone) tablets, for oral use [Link]
KEGG Drug
D08865
PubChem Compound
11238823
PubChem Substance
175427104
ChemSpider
9413866
RxNav
1294597
ChEBI
68845
ChEMBL
CHEMBL2028661
ZINC
ZINC000014210642
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Azilsartan
FDA label
Download (381 KB)
MSDS
Download (34.9 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentEssential Hypertension Complicated by Type 2 Diabetes Mellitus1
4CompletedTreatmentHigh Blood Pressure (Hypertension)1
4CompletedTreatmentHypertension, Essential Hypertension / Type 2 Diabetes Mellitus1
4WithdrawnTreatmentEssential Hypertension With Stable Angina and Dyslipidemia1
3CompletedTreatmentHigh Blood Pressure (Hypertension)13
3CompletedTreatmentHypertension, Essential Hypertension6
3CompletedTreatmentPediatric Hypertension2
3CompletedTreatmentSafety1
3RecruitingTreatmentHigh Blood Pressure (Hypertension)1
3TerminatedTreatmentDiabetes / High Blood Pressure (Hypertension)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
TabletOral20 MG
TabletOral40 mg/1
TabletOral80 mg/1
TabletOral40 mg
TabletOral80 mg
Tablet, coatedOral
TabletOral
Tablet, film coated
TabletOral
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US9169238No2015-10-272030-02-25US flag
US7572920No2009-08-112025-01-07US flag
US9066936No2015-06-302028-03-26US flag
US7157584No2007-01-022025-05-22US flag
US9387249No2016-07-122031-07-01US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility<1 mg/mLhttps://www.selleck.cn/msds/MSDS_S3057.pdf
Predicted Properties
PropertyValueSource
Water Solubility0.00703 mg/mLALOGPS
logP4.94ALOGPS
logP6.03ChemAxon
logS-4.9ALOGPS
pKa (Strongest Acidic)5.91ChemAxon
pKa (Strongest Basic)1.48ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area139.57 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity149.52 m3·mol-1ChemAxon
Polarizability57.45 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.915
Caco-2 permeable-0.5843
P-glycoprotein substrateSubstrate0.5619
P-glycoprotein inhibitor INon-inhibitor0.5061
P-glycoprotein inhibitor IINon-inhibitor0.7217
Renal organic cation transporterNon-inhibitor0.8851
CYP450 2C9 substrateNon-substrate0.834
CYP450 2D6 substrateNon-substrate0.8338
CYP450 3A4 substrateSubstrate0.5128
CYP450 1A2 substrateNon-inhibitor0.7445
CYP450 2C9 inhibitorInhibitor0.5531
CYP450 2D6 inhibitorNon-inhibitor0.8779
CYP450 2C19 inhibitorInhibitor0.5915
CYP450 3A4 inhibitorInhibitor0.8507
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.594
Ames testNon AMES toxic0.5227
CarcinogenicityNon-carcinogens0.7059
BiodegradationNot ready biodegradable0.9962
Rat acute toxicity2.5320 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8853
hERG inhibition (predictor II)Non-inhibitor0.6952
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 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

Targets

Drugtargets2
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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. [Article]
  2. Miura S, Matsuo Y, Nakayama A, Tomita S, Suematsu Y, Saku K: Ability of the new AT1 receptor blocker azilsartan to block angiotensin II-induced AT1 receptor activation after wash-out. J Renin Angiotensin Aldosterone Syst. 2014 Mar;15(1):7-12. doi: 10.1177/1470320313482170. Epub 2013 Apr 5. [Article]
  3. Jones JD, Jackson SH, Agboton C, Martin TS: Azilsartan Medoxomil (Edarbi): The Eighth Angiotensin II Receptor Blocker. P T. 2011 Oct;36(10):634-40. [Article]
  4. Hardin MD, Jacobs TF: Azilsartan . [Article]
  5. FDA Approved Drug Products: Edarbi (azilsartan medoxomil) oral tablets [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
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. Jones JD, Jackson SH, Agboton C, Martin TS: Azilsartan Medoxomil (Edarbi): The Eighth Angiotensin II Receptor Blocker. P T. 2011 Oct;36(10):634-40. [Article]
  2. FDA Approved Drug Products: Edarbi (azilsartan medoxomil) oral tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
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
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. De Caterina AR, Harper AR, Cuculi F: Critical evaluation of the efficacy and tolerability of azilsartan. Vasc Health Risk Manag. 2012;8:299-305. doi: 10.2147/VHRM.S22589. Epub 2012 May 14. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
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
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. De Caterina AR, Harper AR, Cuculi F: Critical evaluation of the efficacy and tolerability of azilsartan. Vasc Health Risk Manag. 2012;8:299-305. doi: 10.2147/VHRM.S22589. Epub 2012 May 14. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
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
References
  1. FDA Approved Drug Products: Edarbi (azilsartan medoxomil) oral tablets [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. De Caterina AR, Harper AR, Cuculi F: Critical evaluation of the efficacy and tolerability of azilsartan. Vasc Health Risk Manag. 2012;8:299-305. doi: 10.2147/VHRM.S22589. Epub 2012 May 14. [Article]

Drug created on December 21, 2012 17:01 / Updated on September 19, 2021 19:53