Bosentan

Identification

Summary

Bosentan is a dual endothelin receptor antagonist used to treat pulmonary arterial hypertension.

Brand Names
Stayveer, Tracleer
Generic Name
Bosentan
DrugBank Accession Number
DB00559
Background

Bosentan is a dual endothelin receptor antagonist marketed under the trade name Tracleer by Actelion Pharmaceuticals. Bosentan is used to treat pulmonary hypertension by blocking the action of endothelin molecules that would otherwise promote narrowing of the blood vessels and lead to high blood pressure.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 551.614
Monoisotopic: 551.183854375
Chemical Formula
C27H29N5O6S
Synonyms
  • 4-(1,1-Dimethylethyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-(2,2'-bipyrimidin)-4-yl) benzenesulfornamide
  • bosentán
  • Bosentan
  • bosentan anhydrous
  • bosentanum
  • p-tert-Butyl-N-(6-(2-hydroxyethoxy)-5-(o-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl)benzenesulfonamide

Pharmacology

Indication

Used in the treatment of pulmonary arterial hypertension (PAH), to improve exercise ability and to decrease the rate of clinical worsening (in patients with WHO Class III or IV symptoms).

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination for prophylaxis ofEye inflammationCombination Product in combination with: Dexamethasone (DB01234)••••••••••••••••••••••
Used in combination to treatEye inflammationCombination Product in combination with: Dexamethasone (DB01234)••••••••••••••••••••••
Management ofNyha functional class ii-iv pulmonary arterial hypertension••••••••••••
Used in combination to treatOcular bacterial infectionsCombination Product in combination with: Dexamethasone (DB01234)••••••••••••••••••••••
Used in combination for prophylaxis ofOcular bacterial infectionsCombination Product in combination with: Dexamethasone (DB01234)••••••••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Bosentan belongs to a class of drugs known as endothelin receptor antagonists (ERAs). Patients with PAH have elevated levels of endothelin, a potent blood vessel constrictor, in their plasma and lung tissue. Bosentan blocks the binding of endothelin to its receptors, thereby negating endothelin's deleterious effects.

Mechanism of action

Endothelin-1 (ET-1) is a neurohormone, the effects of which are mediated by binding to ETA and ETB receptors in the endothelium and vascular smooth muscle. It displays a slightly higher affinity towards ETA receptors than ETB receptors. ET-1 concentrations are elevated in plasma and lung tissue of patients with pulmonary arterial hypertension, suggesting a pathogenic role for ET-1 in this disease. Bosentan is a specific and competitive antagonist at endothelin receptor types ETA and ETB.

TargetActionsOrganism
AEndothelin B receptor
antagonist
Humans
AEndothelin-1 receptor
antagonist
Humans
Absorption

Absolute bioavailability is approximately 50% and food does not affect absorption.

Volume of distribution
  • 18 L
Protein binding

Greater than 98% to plasma proteins, mainly albumin.

Metabolism

Bosentan is metabolized in the liver by the cytochrome P450 enzymes CYP2C9 and CYP3A4 (and possibly CYP2C19), producing three metabolites, one of which, Ro 48-5033, is pharmacologically active and may contribute 10 to 20% to the total activity of the parent compound.

Hover over products below to view reaction partners

Route of elimination

Bosentan is eliminated by biliary excretion following metabolism in the liver.

Half-life

Terminal elimination half-life is about 5 hours in healthy adult subjects.

Clearance
  • 4 L/h [patients with pulmonary arterial hypertension]
Adverse Effects
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Toxicity

Bosentan has been given as a single dose of up to 2400 mg in normal volunteers, or up to 2000 mg/day for 2 months in patients, without any major clinical consequences. The most common side effect was headache of mild to moderate intensity. In the cyclosporine A interaction study, in which doses of 500 and 1000 mg b.i.d. of bosentan were given concomitantly with cyclosporine A, trough plasma concentrations of bosentan increased 30-fold, resulting in severe headache, nausea, and vomiting, but no serious adverse events. Mild decreases in blood pressure and increases in heart rate were observed. There is no specific experience of overdosage with bosentan beyond the doses described above. Massive overdosage may result in pronounced hypotension requiring active cardiovascular support.

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
AbaloparatideAbaloparatide may increase the hypotensive activities of Bosentan.
AbametapirThe serum concentration of Bosentan can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Bosentan can be increased when combined with Abatacept.
AbemaciclibThe metabolism of Abemaciclib can be increased when combined with Bosentan.
AbrocitinibThe metabolism of Abrocitinib can be increased when combined with Bosentan.
Food Interactions
  • Take with or without food. The absorption is unaffected by food.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Bosentan monohydrateQ326023R30157212-55-0SXTRWVVIEPWAKM-UHFFFAOYSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Act BosentanTablet62.5 mgOralActavis Pharma Company2012-06-052018-04-25Canada flag
Act BosentanTablet125 mgOralActavis Pharma Company2012-06-052018-04-25Canada flag
Alembic-bosentanTablet62.5 mgOralAlembic Pharmaceuticals LimitedNot applicableNot applicableCanada flag
Alembic-bosentanTablet125 mgOralAlembic Pharmaceuticals LimitedNot applicableNot applicableCanada flag
BosentanTablet125 mgOralPanda Pharmaceuticals Inc.Not applicableNot applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Accel-bosentanTablet125 mgOralAccel Pharma IncNot applicableNot applicableCanada flag
Apo-bosentanTablet125.0 mgOralApotex Corporation2017-07-14Not applicableCanada flag
Apo-bosentanTablet62.5 mgOralApotex Corporation2017-07-14Not applicableCanada flag
Auro-bosentanTablet62.5 mgOralAuro Pharma IncNot applicableNot applicableCanada flag
Auro-bosentanTablet125 mgOralAuro Pharma IncNot applicableNot applicableCanada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
OCUBRAX® SUSPENSION OFTALMICABosentan (3 mg) + Dexamethasone (1 mg)SuspensionConjunctival; OphthalmicOPHARM LTDA.2008-07-23Not applicableColombia flag

Categories

ATC Codes
G01AE10 — Combinations of sulfonamidesC02KX01 — Bosentan
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as bipyrimidines and oligopyrimidines. These are organic compounds containing two or more pyrimidine rings directly linked to each other. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazines
Sub Class
Pyrimidines and pyrimidine derivatives
Direct Parent
Bipyrimidines and oligopyrimidines
Alternative Parents
Diarylethers / Benzenesulfonamides / Phenylpropanes / Benzenesulfonyl compounds / Phenoxy compounds / Anisoles / Methoxybenzenes / Alkyl aryl ethers / Organosulfonamides / Imidolactams
show 8 more
Substituents
Alcohol / Alkyl aryl ether / Aminosulfonyl compound / Anisole / Aromatic heteromonocyclic compound / Azacycle / Benzenesulfonamide / Benzenesulfonyl group / Benzenoid / Bipyrimidine
show 22 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
sulfonamide, pyrimidines, primary alcohol (CHEBI:51450)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
XUL93R30K2
CAS number
147536-97-8
InChI Key
GJPICJJJRGTNOD-UHFFFAOYSA-N
InChI
InChI=1S/C27H29N5O6S/c1-27(2,3)18-10-12-19(13-11-18)39(34,35)32-23-22(38-21-9-6-5-8-20(21)36-4)26(37-17-16-33)31-25(30-23)24-28-14-7-15-29-24/h5-15,33H,16-17H2,1-4H3,(H,30,31,32)
IUPAC Name
4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-[2,2'-bipyrimidin]-4-yl]benzene-1-sulfonamide
SMILES
COC1=CC=CC=C1OC1=C(NS(=O)(=O)C2=CC=C(C=C2)C(C)(C)C)N=C(N=C1OCCO)C1=NC=CC=N1

References

Synthesis Reference

Maurizio TADDEI, Diletta Naldini, Pietro Allegrini, Gabriele Razzetti, Simone Mantegazza, "Process for the Preparation of Bosentan." U.S. Patent US20090156811, issued June 18, 2009.

US20090156811
General References
  1. FDA Approved Drugs: Tracleer® oral tablets [Link]
Human Metabolome Database
HMDB0014699
KEGG Drug
D01227
PubChem Compound
104865
PubChem Substance
46507154
ChemSpider
94651
BindingDB
50061101
RxNav
75207
ChEBI
51450
ChEMBL
CHEMBL957
ZINC
ZINC000001538857
Therapeutic Targets Database
DNC000341
PharmGKB
PA10034
PDBe Ligand
K86
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Bosentan
PDB Entries
5xpr
FDA label
Download (424 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceType 2 Diabetes Mellitus1
4CompletedSupportive CareType 2 Diabetes Mellitus1
4CompletedTreatmentDigital Ulcers / Systemic Sclerosis (SSc)1
4CompletedTreatmentEisenmenger's Syndrome1
4CompletedTreatmentPulmonary Arterial Hypertension (PAH)4

Pharmacoeconomics

Manufacturers
  • Actelion ltd
Packagers
  • Actelion Pharmaceuticals Inc.
  • Action Pharmaceuticals Ltd.
  • Haupt Pharma
  • Patheon Inc.
Dosage Forms
FormRouteStrength
TabletOral125.0 mg
TabletOral125 mg/1
TabletOral62.5 mg/1
Tablet, coatedOral125 mg/1
Tablet, coatedOral62.5 mg/1
Tablet, film coatedOral125 mg/1
Tablet, film coatedOral62.5 mg/1
Tablet, film coatedOral
TabletOral125.000 mg
TabletOral64.542 mg
TabletOral64.541 mg
TabletOral64.540 mg
SuspensionConjunctival; Ophthalmic
Tablet, coatedOral6250000 mg
Tablet, film coatedOral125.00 mg
Tablet, film coatedOral62.50 mg
Tablet, coatedOral129.08 mg
Tablet, coatedOral64.54 mg
TabletOral12500000 mg
Tablet, coatedOral12500000 mg
TabletOral125 mg
TabletOral62.5 mg
TabletOral62.500 mg
Tablet, coatedOral125 mg
Tablet, coatedOral62.5 mg
Tablet, for suspensionOral32 MG
Tablet, for suspensionOral32 mg/1
TabletOral33.045 mg
Tablet, film coatedOral125 mg
Tablet, film coatedOral62.5 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA2071193No1998-08-252012-06-12Canada flag
US5292740No1994-03-082015-11-20US flag
US7959945No2011-06-142027-12-28US flag
US8309126No2012-11-132026-05-15US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityPoorly soluble in water (1.0 mg/100 ml) and in aqueous solutions at low pH (0.1 mg/100 ml at pH 1.1 and 4.0; 0.2 mg/100 ml at pH 5.0). Solubility increases at higher pH values (43 mg/100 ml at pH 7.5).Not Available
logP3.7Not Available
Caco2 permeability-5.98ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.00904 mg/mLALOGPS
logP4.18ALOGPS
logP4.94Chemaxon
logS-4.8ALOGPS
pKa (Strongest Acidic)5.8Chemaxon
pKa (Strongest Basic)0.57Chemaxon
Physiological Charge-1Chemaxon
Hydrogen Acceptor Count9Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area145.65 Å2Chemaxon
Rotatable Bond Count10Chemaxon
Refractivity166.66 m3·mol-1Chemaxon
Polarizability57.89 Å3Chemaxon
Number of Rings4Chemaxon
Bioavailability1Chemaxon
Rule of FiveNoChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9253
Blood Brain Barrier-0.7419
Caco-2 permeable-0.8956
P-glycoprotein substrateNon-substrate0.5738
P-glycoprotein inhibitor INon-inhibitor0.6175
P-glycoprotein inhibitor IINon-inhibitor0.5092
Renal organic cation transporterNon-inhibitor0.9149
CYP450 2C9 substrateNon-substrate0.5926
CYP450 2D6 substrateNon-substrate0.9117
CYP450 3A4 substrateSubstrate0.5132
CYP450 1A2 substrateNon-inhibitor0.7203
CYP450 2C9 inhibitorInhibitor0.518
CYP450 2D6 inhibitorNon-inhibitor0.8755
CYP450 2C19 inhibitorNon-inhibitor0.5219
CYP450 3A4 inhibitorInhibitor0.8407
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.772
Ames testNon AMES toxic0.6147
CarcinogenicityNon-carcinogens0.6515
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.2676 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9679
hERG inhibition (predictor II)Non-inhibitor0.572
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-MSsplash10-0k9f-1404490000-6d317563fca85570bb94
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0udj-0810090000-b97444dff91ec725276d
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-1690040000-c561d9dbb5ed88285519
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0udi-0000190000-5bbd0f0f0e3fa41be023
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0udi-0100090000-b5fdc12bbe935b52d57c
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0zfr-0000390000-581f27063dce9c9d6a07
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0zfv-1303980000-418defea87908b5af3b0
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0a4i-5500890000-02d14b563a1ee937de05
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0udi-0202910000-d3f49d396eb21b23260a
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-242.1955365
predicted
DarkChem Lite v0.1.0
[M-H]-254.4531365
predicted
DarkChem Lite v0.1.0
[M-H]-211.8961
predicted
DeepCCS 1.0 (2019)
[M+H]+242.1594365
predicted
DarkChem Lite v0.1.0
[M+H]+254.9170365
predicted
DarkChem Lite v0.1.0
[M+H]+214.29167
predicted
DeepCCS 1.0 (2019)
[M+Na]+243.2314365
predicted
DarkChem Lite v0.1.0
[M+Na]+220.20421
predicted
DeepCCS 1.0 (2019)

Targets

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Details
1. Endothelin B receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Peptide hormone binding
Specific Function
Non-specific receptor for endothelin 1, 2, and 3. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
Gene Name
EDNRB
Uniprot ID
P24530
Uniprot Name
Endothelin B receptor
Molecular Weight
49643.255 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. Gardiner SM, Kemp PA, March JE, Bennett T: Effects of bosentan (Ro 47-0203), an ETA-, ETB-receptor antagonist, on regional haemodynamic responses to endothelins in conscious rats. Br J Pharmacol. 1994 Jul;112(3):823-30. [Article]
  3. Gupta SK, Saxena A, Singh U, Arya DS: Bosentan, the mixed ETA-ETB endothelin receptor antagonist, attenuated oxidative stress after experimental myocardial ischemia and reperfusion. Mol Cell Biochem. 2005 Jul;275(1-2):67-74. [Article]
  4. Marano G, Palazzesi S, Bernucci P, Grigioni M, Formigari R, Ballerini L: ET(A)/ET(B) receptor antagonist bosentan inhibits neointimal development in collared carotid arteries of rabbits. Life Sci. 1998;63(18):PL259-66. [Article]
  5. Richard V, Kaeffer N, Hogie M, Tron C, Blanc T, Thuillez C: Role of endogenous endothelin in myocardial and coronary endothelial injury after ischaemia and reperfusion in rats: studies with bosentan, a mixed ETA-ETB antagonist. Br J Pharmacol. 1994 Nov;113(3):869-76. [Article]
  6. Said SA, Ammar el SM, Suddek GM: Effect of bosentan (ETA/ETB receptor antagonist) on metabolic changes during stress and diabetes. Pharmacol Res. 2005 Feb;51(2):107-15. [Article]
Details
2. Endothelin-1 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is:...
Gene Name
EDNRA
Uniprot ID
P25101
Uniprot Name
Endothelin-1 receptor
Molecular Weight
48721.76 Da
References
  1. Albertini M, Lafortuna CL, Ciminaghi B, Mazzola S, Clement MG: Endothelin involvement in respiratory centre activity. Prostaglandins Leukot Essent Fatty Acids. 2001 Sep;65(3):157-63. [Article]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  3. Kiowski W, Sutsch G, Oechslin E, Bertel O: Hemodynamic effects of bosentan in patients with chronic heart failure. Heart Fail Rev. 2001 Dec;6(4):325-34. [Article]
  4. Kramp R, Fourmanoir P, Caron N: Endothelin resets renal blood flow autoregulatory efficiency during acute blockade of NO in the rat. Am J Physiol Renal Physiol. 2001 Dec;281(6):F1132-40. [Article]
  5. Martin C, Held HD, Uhlig S: Differential effects of the mixed ET(A)/ET(B)-receptor antagonist bosentan on endothelin-induced bronchoconstriction, vasoconstriction and prostacyclin release. Naunyn Schmiedebergs Arch Pharmacol. 2000 Aug;362(2):128-36. [Article]
  6. Sihvola RK, Pulkkinen VP, Koskinen PK, Lemstrom KB: Crosstalk of endothelin-1 and platelet-derived growth factor in cardiac allograft arteriosclerosis. J Am Coll Cardiol. 2002 Feb 20;39(4):710-7. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Vitamin d3 25-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 performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Dingemanse J, Schaarschmidt D, van Giersbergen PL: Investigation of the mutual pharmacokinetic interactions between bosentan, a dual endothelin receptor antagonist, and simvastatin. Clin Pharmacokinet. 2003;42(3):293-301. [Article]
  2. Dingemanse J, van Giersbergen PL: Clinical pharmacology of bosentan, a dual endothelin receptor antagonist. Clin Pharmacokinet. 2004;43(15):1089-115. [Article]
  3. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
  4. FDA table of interactions [Link]
  5. FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
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. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
  2. Matsunaga N, Kaneko N, Staub AY, Nakanishi T, Nunoya K, Imawaka H, Tamai I: Analysis of the Metabolic Pathway of Bosentan and of the Cytotoxicity of Bosentan Metabolites Based on a Quantitative Modeling of Metabolism and Transport in Sandwich-Cultured Human Hepatocytes. Drug Metab Dispos. 2016 Jan;44(1):16-27. doi: 10.1124/dmd.115.067074. Epub 2015 Oct 26. [Article]
  3. Cheng JW: Bosentan. Heart Dis. 2003 Mar-Apr;5(2):161-9. [Article]
  4. van Giersbergen PL, Halabi A, Dingemanse J: Single- and multiple-dose pharmacokinetics of bosentan and its interaction with ketoconazole. Br J Clin Pharmacol. 2002 Jun;53(6):589-95. [Article]
  5. Elshaboury SM, Anderson JR: Ambrisentan for the treatment of pulmonary arterial hypertension: improving outcomes. Patient Prefer Adherence. 2013 May 8;7:401-9. doi: 10.2147/PPA.S30949. Print 2013. [Article]
  6. Bosentan FDA label [File]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
References
  1. Fattinger K, Funk C, Pantze M, Weber C, Reichen J, Stieger B, Meier PJ: The endothelin antagonist bosentan inhibits the canalicular bile salt export pump: a potential mechanism for hepatic adverse reactions. Clin Pharmacol Ther. 2001 Apr;69(4):223-31. [Article]

Drug created at June 13, 2005 13:24 / Updated at March 18, 2024 16:48