Identification

Summary

Macitentan is an endothelin receptor antagonist used to manage pulmonary arterial hypertension to delay disease progression.

Brand Names
Opsumit
Generic Name
Macitentan
DrugBank Accession Number
DB08932
Background

Macitentan is a dual endothelin receptor antagonist used in the treatment of pulmonary arterial hypertension.5 It was first approved by the FDA in 2013. Macitentan differs from its predecessor bosentan due to its lower risk of hepatotoxicity.

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 588.273
Monoisotopic: 585.963349142
Chemical Formula
C19H20Br2N6O4S
Synonyms
  • Macitentán
  • Macitentan
  • Macitentanum
External IDs
  • ACT 064992
  • ACT-064992
  • ACT064992

Pharmacology

Indication

Macitentan is indicated for the treatment of WHO group 1 pulmonary arterial hypertension (PAH) both alone and in combination with tadalafil.5,6

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Macitentan acts primarily by reducing vasoconstriction and cell proliferation due to endothelin overexpression.5,6

Mechanism of action

Macitentan is an antagonist which binds to the endothelin A and B receptors (EA and EB) and blocks signaling from endothelin-1 and -2.5,6,3 Pulmonary arterial hypertension has many different mechanisms which contribute to the development of endothelial dysfunction including elevated cytosolic calcium, genetic factors, epigenetic changes, and mitochondrial dysfunction.2 The focus of macitentan's mechanism relates to the role of overexpressed endothelin from the vascular endothelium. Endothelins are released in both a constitutive fashion from secretory vesicles and in response to stimuli via Weibel-Palade storage granules.1 Endothelins bind to the EA and EB receptors, with endothelins -1 and -2 having more affinity than endothelin-3.3 Binding to the Gq coupled EA receptor triggers Ca2+ release from the sarcoplasmic reticulum of smooth muscle cells via the phospholipase C (PLC) pathway. Downstream protein kinase C activation may also contribute to increased Ca2+ sensitivity of the contractile apparatus. EA receptor activation is also known to contribute to pulmonary artery smooth muscle cell proliferation. The binding of endothelins to the EB receptors acts in opposition to EA signaling by activating the same PLC cascade in endothelial cells to activate endothelial nitric oxide synthase. The subsequent release of nitric oxide produces vasodilation through the cyclic guanosine monophosphate cascade.1 Despite the greater presence of EB receptors on endothelial cells, they are still present on smooth muscle cells and may contribute to cell proliferation through the same mechanisms as EA receptors.3 Macitentan is thought to provide its therapeutic effect primarily via blocking signaling through EA which produces both decreased vasoconstriction via reduced smooth muscle cell contractility and attenuation of the hyperproliferation of smooth muscle cells found in PAH. Blockade of EB is less likely to contribute to a therapeutic effect as this signaling is responsible for the counter-regulatory vasodilatory signal.

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

Macitentan has a median Tmax of 8h although some studies have found up to 30h at higher doses.6,4 Although the bioavailability has not been experimentally determined, pharmacokinetic modeling has estimated it at 74%.4 Food has not been found to have a significant effect on absorption.

Volume of distribution

Macitentan has an apparent volume of distribution of 40-50L.6,4

Protein binding

Macitentan is >99% bound to plasma proteins, primarily to albumin and to a lesser extent α1-acid glycoprotein.6,4

Metabolism

Macitentan undergoes oxidative depropylation of the sulfonamide moiety via CYP3A4, 2C8, 2C9, and 2C19 to form the active metabolite M6.4 The ethylene glycol moiety undergoes oxidative cleavage via CYP2C9 to the alcohol metabolite M4. M4 is oxidized to its corresponding acid, M5, then hydrolyzed to the metabolite termed m/z 324. Oxidative depropylation of a distal carbon atom via CYP2C8, 2C9, and 2C19 forms M7. Hydrolysis of both macitentan and M5 produces M3. Finally M5 may be further metabolized via hydrolysis and hydroxylation to M2 or via glucuronidation to a glucuronide metabolite, M1.

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Route of elimination

Eliminated 50% through urine and 24% through feces.6,4 Of the 50% excreted through the urine, none of the recovered dose was in the form of the parent drug nor the active metabolite.

Half-life

The half-life of elimination of macitentan is 16 hours.6,4 The half-life of elimination of the active metabolite is 40-66h

Clearance

Clearance data was not found.

Adverse Effects
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Toxicity

At high doses, macitentan may produce headache, nausea, and vomiting.6 In case of overdose standard supportive measures are recommended. Hemodialysis is not expected to contribute significantly to macitentan clearance due to its high degree of plasma protein binding.

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
AbacavirAbacavir may decrease the excretion rate of Macitentan which could result in a higher serum level.
AbametapirThe serum concentration of Macitentan can be increased when it is combined with Abametapir.
AcebutololAcebutolol may increase the hypotensive activities of Macitentan.
AceclofenacThe therapeutic efficacy of Macitentan can be decreased when used in combination with Aceclofenac.
AcemetacinThe therapeutic efficacy of Macitentan can be decreased when used in combination with Acemetacin.
AcetaminophenAcetaminophen may decrease the excretion rate of Macitentan which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Macitentan which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acidAcetylsalicylic acid may decrease the antihypertensive activities of Macitentan.
AclidiniumAclidinium may decrease the excretion rate of Macitentan which could result in a higher serum level.
AcrivastineMacitentan may decrease the excretion rate of Acrivastine which could result in a higher serum level.
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Food Interactions
  • Take with or without food.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
OpsumitTablet, film coated10 mgOralJanssen Cilag International Nv2020-12-22Not applicableEU flag
OpsumitTablet, film coated10 mg/1OralActelion Pharmaceuticals US, Inc.2013-11-04Not applicableUS flag
OpsumitTablet, film coated10 mgOralJanssen Cilag International Nv2020-12-22Not applicableEU flag
OpsumitTablet, film coated10 mgOralJanssen Cilag International Nv2020-12-22Not applicableEU flag
OpsumitTablet10 mgOralJanssen Pharmaceuticals2014-01-15Not applicableCanada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
OpsynviMacitentan (10 mg) + Tadalafil (40 mg)TabletOralJanssen Pharmaceuticals2021-11-25Not applicableCanada flag

Categories

ATC Codes
C02KX04 — Macitentan
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as halopyrimidines. These are aromatic compounds containing a halogen atom linked to a pyrimidine ring. 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
Halopyrimidines
Alternative Parents
Bromobenzenes / Alkyl aryl ethers / Sulfuric acid diamides / Imidolactams / Aryl bromides / Heteroaromatic compounds / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Organobromides
show 2 more
Substituents
Alkyl aryl ether / Aromatic heteromonocyclic compound / Aryl bromide / Aryl halide / Azacycle / Benzenoid / Bromobenzene / Ether / Halobenzene / Halopyrimidine
show 14 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
organobromine compound, aromatic ether, pyrimidines, ring assembly, sulfamides (CHEBI:76607)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
Z9K9Y9WMVL
CAS number
441798-33-0
InChI Key
JGCMEBMXRHSZKX-UHFFFAOYSA-N
InChI
InChI=1S/C19H20Br2N6O4S/c1-2-7-26-32(28,29)27-17-16(13-3-5-14(20)6-4-13)18(25-12-24-17)30-8-9-31-19-22-10-15(21)11-23-19/h3-6,10-12,26H,2,7-9H2,1H3,(H,24,25,27)
IUPAC Name
{[5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl]sulfamoyl}(propyl)amine
SMILES
CCCNS(=O)(=O)NC1=C(C(OCCOC2=NC=C(Br)C=N2)=NC=N1)C1=CC=C(Br)C=C1

References

Synthesis Reference

Bolli MH, Boss C, Binkert C, Buchmann S, Bur D, Hess P, Iglarz M, Meyer S, Rein J, Rey M, Treiber A, Clozel M, Fischli W, Weller T: The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-p ropylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist. J Med Chem. 2012 Sep 13;55(17):7849-61. doi: 10.1021/jm3009103. Epub 2012 Aug 16. Pubmed

General References
  1. Davenport AP, Hyndman KA, Dhaun N, Southan C, Kohan DE, Pollock JS, Pollock DM, Webb DJ, Maguire JJ: Endothelin. Pharmacol Rev. 2016 Apr;68(2):357-418. doi: 10.1124/pr.115.011833. [Article]
  2. Thenappan T, Ormiston ML, Ryan JJ, Archer SL: Pulmonary arterial hypertension: pathogenesis and clinical management. BMJ. 2018 Mar 14;360:j5492. doi: 10.1136/bmj.j5492. [Article]
  3. Bedan M, Grimm D, Wehland M, Simonsen U, Infanger M, Kruger M: A Focus on Macitentan in the Treatment of Pulmonary Arterial Hypertension. Basic Clin Pharmacol Toxicol. 2018 Aug;123(2):103-113. doi: 10.1111/bcpt.13033. Epub 2018 Jun 5. [Article]
  4. Sidharta PN, Treiber A, Dingemanse J: Clinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentan. Clin Pharmacokinet. 2015 May;54(5):457-71. doi: 10.1007/s40262-015-0255-5. [Article]
  5. FDA Approved Drug Products: OPSUMIT (macitentan) tablets [Link]
  6. DPD Approved Drug Products: Opsynvi (tadalafil/macitentan) combination tablets [Link]
KEGG Drug
D10135
PubChem Compound
16004692
PubChem Substance
175427162
ChemSpider
13134960
BindingDB
50395626
RxNav
1442132
ChEBI
76607
ChEMBL
CHEMBL2103873
ZINC
ZINC000043202140
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Macitentan
FDA label
Download (836 KB)
MSDS
Download (105 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentPortopulmonary Hypertension1
4CompletedTreatmentPulmonary Arterial Hypertension (PAH)1
4RecruitingOtherCardiac Allograft Vasculopathy1
4TerminatedTreatmentPulmonary Arterial Hypertension (PAH)1
4Unknown StatusTreatmentPulmonary Arterial Hypertension (PAH)1
4WithdrawnTreatmentLung Transplant Rejection1
3CompletedTreatmentCongenital Heart Disease (CHD)1
3CompletedTreatmentCongenital Heart Disease With Fontan Circulation1
3CompletedTreatmentPulmonary Arterial Hypertension (PAH)6
3CompletedTreatmentSystemic; Sclerosis, Progressive / Ulcers1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
TabletOral10 mg
Tablet, coatedOral10 mg
Tablet, film coatedOral
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral10 mg
Tablet, film coatedOral10.00 mg
TabletOral
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8268847No2012-09-182029-04-18US flag
US8367685No2013-02-052028-10-04US flag
US9265762No2016-02-232027-05-29US flag
US7094781No2006-08-222022-10-12US flag
US10946015No2021-03-162026-11-25US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)134-136°CMSDS
Predicted Properties
PropertyValueSource
Water Solubility0.00668 mg/mLALOGPS
logP3.05ALOGPS
logP3.69ChemAxon
logS-4.9ALOGPS
pKa (Strongest Acidic)7.76ChemAxon
pKa (Strongest Basic)3.26ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count9ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area128.22 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity126.98 m3·mol-1ChemAxon
Polarizability50.55 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

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

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Details
1. 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. Bolli MH, Boss C, Binkert C, Buchmann S, Bur D, Hess P, Iglarz M, Meyer S, Rein J, Rey M, Treiber A, Clozel M, Fischli W, Weller T: The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-p ropylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist. J Med Chem. 2012 Sep 13;55(17):7849-61. doi: 10.1021/jm3009103. Epub 2012 Aug 16. [Article]
  2. Bedan M, Grimm D, Wehland M, Simonsen U, Infanger M, Kruger M: A Focus on Macitentan in the Treatment of Pulmonary Arterial Hypertension. Basic Clin Pharmacol Toxicol. 2018 Aug;123(2):103-113. doi: 10.1111/bcpt.13033. Epub 2018 Jun 5. [Article]
  3. Thenappan T, Ormiston ML, Ryan JJ, Archer SL: Pulmonary arterial hypertension: pathogenesis and clinical management. BMJ. 2018 Mar 14;360:j5492. doi: 10.1136/bmj.j5492. [Article]
  4. FDA Approved Drug Products: OPSUMIT (macitentan) tablets [Link]
Details
2. Endothelin B receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. Bolli MH, Boss C, Binkert C, Buchmann S, Bur D, Hess P, Iglarz M, Meyer S, Rein J, Rey M, Treiber A, Clozel M, Fischli W, Weller T: The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-p ropylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist. J Med Chem. 2012 Sep 13;55(17):7849-61. doi: 10.1021/jm3009103. Epub 2012 Aug 16. [Article]
  2. Bedan M, Grimm D, Wehland M, Simonsen U, Infanger M, Kruger M: A Focus on Macitentan in the Treatment of Pulmonary Arterial Hypertension. Basic Clin Pharmacol Toxicol. 2018 Aug;123(2):103-113. doi: 10.1111/bcpt.13033. Epub 2018 Jun 5. [Article]
  3. Thenappan T, Ormiston ML, Ryan JJ, Archer SL: Pulmonary arterial hypertension: pathogenesis and clinical management. BMJ. 2018 Mar 14;360:j5492. doi: 10.1136/bmj.j5492. [Article]
  4. FDA Approved Drug Products: OPSUMIT (macitentan) tablets [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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. Bedan M, Grimm D, Wehland M, Simonsen U, Infanger M, Kruger M: A Focus on Macitentan in the Treatment of Pulmonary Arterial Hypertension. Basic Clin Pharmacol Toxicol. 2018 Aug;123(2):103-113. doi: 10.1111/bcpt.13033. Epub 2018 Jun 5. [Article]
  2. Sidharta PN, Treiber A, Dingemanse J: Clinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentan. Clin Pharmacokinet. 2015 May;54(5):457-71. doi: 10.1007/s40262-015-0255-5. [Article]
  3. FDA Approved Drug Products: OPSUMIT (macitentan) tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Bedan M, Grimm D, Wehland M, Simonsen U, Infanger M, Kruger M: A Focus on Macitentan in the Treatment of Pulmonary Arterial Hypertension. Basic Clin Pharmacol Toxicol. 2018 Aug;123(2):103-113. doi: 10.1111/bcpt.13033. Epub 2018 Jun 5. [Article]
  2. Sidharta PN, Treiber A, Dingemanse J: Clinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentan. Clin Pharmacokinet. 2015 May;54(5):457-71. doi: 10.1007/s40262-015-0255-5. [Article]
  3. FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
  4. FDA Approved Drug Products: OPSUMIT (macitentan) 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
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Bedan M, Grimm D, Wehland M, Simonsen U, Infanger M, Kruger M: A Focus on Macitentan in the Treatment of Pulmonary Arterial Hypertension. Basic Clin Pharmacol Toxicol. 2018 Aug;123(2):103-113. doi: 10.1111/bcpt.13033. Epub 2018 Jun 5. [Article]
  2. Sidharta PN, Treiber A, Dingemanse J: Clinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentan. Clin Pharmacokinet. 2015 May;54(5):457-71. doi: 10.1007/s40262-015-0255-5. [Article]
  3. FDA Approved Drug Products: OPSUMIT (macitentan) 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. Bedan M, Grimm D, Wehland M, Simonsen U, Infanger M, Kruger M: A Focus on Macitentan in the Treatment of Pulmonary Arterial Hypertension. Basic Clin Pharmacol Toxicol. 2018 Aug;123(2):103-113. doi: 10.1111/bcpt.13033. Epub 2018 Jun 5. [Article]
  2. Sidharta PN, Treiber A, Dingemanse J: Clinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentan. Clin Pharmacokinet. 2015 May;54(5):457-71. doi: 10.1007/s40262-015-0255-5. [Article]
  3. FDA Approved Drug Products: OPSUMIT (macitentan) tablets [Link]

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. Sidharta PN, Treiber A, Dingemanse J: Clinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentan. Clin Pharmacokinet. 2015 May;54(5):457-71. doi: 10.1007/s40262-015-0255-5. [Article]
  2. Bedan M, Grimm D, Wehland M, Simonsen U, Infanger M, Kruger M: A Focus on Macitentan in the Treatment of Pulmonary Arterial Hypertension. Basic Clin Pharmacol Toxicol. 2018 Aug;123(2):103-113. doi: 10.1111/bcpt.13033. Epub 2018 Jun 5. [Article]
  3. FDA Approved Drug Products: OPSUMIT (macitentan) tablets [Link]
Kind
Protein group
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...

Components:
References
  1. Sidharta PN, Treiber A, Dingemanse J: Clinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentan. Clin Pharmacokinet. 2015 May;54(5):457-71. doi: 10.1007/s40262-015-0255-5. [Article]
  2. FDA Approved Drug Products: OPSUMIT (macitentan) tablets [Link]

Drug created at December 29, 2013 18:30 / Updated at June 24, 2022 08:21