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
Structure for Macitentan (DB08932)
- 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
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Who group 1 pulmonary arterial hypertension •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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.
Target Actions Organism AEndothelin-1 receptor antagonistHumans UEndothelin B receptor antagonistHumans - 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.
Hover over products below to view reaction partners
- 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- 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 Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Macitentan which could result in a higher serum level. Abaloparatide Abaloparatide may increase the hypotensive activities of Macitentan. Abametapir The serum concentration of Macitentan can be increased when it is combined with Abametapir. Acebutolol Acebutolol may increase the hypotensive activities of Macitentan. Aceclofenac The therapeutic efficacy of Macitentan can be decreased when used in combination with Aceclofenac. - Food Interactions
- Take with or without food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Opsumit Tablet, film coated 10 mg Oral Janssen Cilag International Nv 2020-12-22 Not applicable EU 
Opsumit Tablet 10 mg Oral Janssen Pharmaceuticals 2014-01-15 Not applicable Canada 
Opsumit Tablet, film coated 10 mg/1 Oral Actelion Pharmaceuticals US, Inc. 2013-11-04 Not applicable US 
Opsumit Tablet, film coated 10 mg Oral Janssen Cilag International Nv 2020-12-22 Not applicable EU Opsumit Tablet, film coated 10 mg Oral Janssen Cilag International Nv 2020-12-22 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Opsynvi Macitentan (10 mg) + Tadalafil (40 mg) Tablet Oral Janssen Pharmaceuticals 2021-11-25 Not applicable Canada
Categories
- ATC Codes
- C02KX04 — Macitentan
- C02KX — Antihypertensives for pulmonary arterial hypertension
- C02K — OTHER ANTIHYPERTENSIVES
- C02 — ANTIHYPERTENSIVES
- C — CARDIOVASCULAR SYSTEM
- Drug Categories
- Amides
- Antihypertensive Agents
- Antihypertensives for Pulmonary Arterial Hypertension
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Drugs that are Mainly Renally Excreted
- Endothelin A Receptor Antagonists
- Endothelin B Receptor Antagonists
- Endothelin Receptor Antagonists
- Sulfones
- Sulfur Compounds
- Vasodilating Agents
- 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
- 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]
- 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]
- 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]
- 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]
- FDA Approved Drug Products: OPSUMIT (macitentan) tablets [Link]
- DPD Approved Drug Products: Opsynvi (tadalafil/macitentan) combination tablets [Link]
- External Links
- KEGG Drug
- D10135
- PubChem Compound
- 16004692
- PubChem Substance
- 175427162
- ChemSpider
- 13134960
- BindingDB
- 50395626
- 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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Other Cardiac Allograft Vasculopathy 1 4 Completed Treatment Portopulmonary Hypertension 1 4 Completed Treatment Pulmonary Arterial Hypertension (PAH) 1 4 Terminated Treatment Pulmonary Arterial Hypertension (PAH) 1 4 Unknown Status Treatment Pulmonary Arterial Hypertension (PAH) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 10 mg Tablet, coated Oral 10 mg Tablet, film coated Oral Tablet, film coated Oral 10 mg/1 Tablet, film coated Oral 10 mg Tablet, film coated Oral 10.00 mg Tablet Oral Tablet Oral 10.000 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8268847 No 2012-09-18 2029-04-18 US US8367685 No 2013-02-05 2028-10-04 US US9265762 No 2016-02-23 2027-05-29 US US7094781 No 2006-08-22 2022-10-12 US US10946015 No 2021-03-16 2026-11-25 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 134-136°C MSDS - Predicted Properties
Property Value Source Water Solubility 0.00668 mg/mL ALOGPS logP 3.05 ALOGPS logP 3.69 Chemaxon logS -4.9 ALOGPS pKa (Strongest Acidic) 7.76 Chemaxon pKa (Strongest Basic) 3.26 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 9 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 128.22 Å2 Chemaxon Rotatable Bond Count 9 Chemaxon Refractivity 126.98 m3·mol-1 Chemaxon Polarizability 50.55 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 204.09677 predictedDeepCCS 1.0 (2019) [M-H]- 204.09677 predictedDeepCCS 1.0 (2019) [M+H]+ 206.45477 predictedDeepCCS 1.0 (2019) [M+H]+ 206.45477 predictedDeepCCS 1.0 (2019) [M+Na]+ 213.27028 predictedDeepCCS 1.0 (2019) [M+Na]+ 213.27028 predictedDeepCCS 1.0 (2019)
Targets
- 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
- 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]
- 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]
- 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]
- FDA Approved Drug Products: OPSUMIT (macitentan) tablets [Link]
- 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
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- 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
- 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]
- 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]
- FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
- 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
- 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]
- 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]
- 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
- 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]
- 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]
- 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
- 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]
- 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]
- 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
Drug created at December 29, 2013 18:30 / Updated at March 03, 2023 17:28