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Drug ReportsMacitentan
Opsumit(macitentan)
Macitentan, Opsumit, Opsynvi (macitentan) is a small molecule pharmaceutical. Macitentan was first approved as Opsumit on 2013-10-18. It is used to treat pulmonary hypertension in the USA. It has been approved in Europe to treat pulmonary hypertension. The pharmaceutical is active against endothelin-1 receptor. In addition, it is known to target endothelin receptor type B.
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Commercial
Clinical
Drug
Target
Variants
Financial
Trends
Safety
Events Timeline
5D
1M
3M
6M
YTD
1Y
2Y
5Y
Max
Events
FDA approval date
EMA approval date
Patent expiration date
Study first post date
Last update post date
Start date
Primary completion date
Completion date
Results first post date
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
respiratory tract diseasesD012140
cardiovascular diseasesD002318
Trade Name
FDA
EMA
Macitentan, Opsumit (discontinued: Macitentan)
Combinations
Opsynvi
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Macitentan
Tradename
Company
Number
Date
Products
OPSUMITActelionN-204410 RX2013-10-18
1 products, RLD, RS
Macitentan
+
Tadalafil
Tradename
Company
Number
Date
Products
OPSYNVIActelionN-218490 RX2024-03-22
2 products, RLD, RS
Labels
FDA
EMA
Brand Name
Status
Last Update
opsumitNew Drug Application2025-04-11
opsynviNew Drug Application2025-04-11
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
pulmonary hypertensionEFO_0001361D006976I27.20
vasculogenic impotenceEFO_1001234D018783—
Agency Specific
FDA
EMA
No data
Patent Expiration
Patent
Expires
Flag
FDA Information
Macitentan, Opsumit, Actelion
82688472029-04-18U-1446
83676852028-10-04DPU-1445
92657622027-05-29DPU-1820
109460152026-09-11DPU-1445
70947812025-12-05DS, DP
ATC Codes
C: Cardiovascular system drugs
— C02: Antihypertensives
— C02K: Other antihypertensives in atc
— C02KX: Antihypertensives for pulmonary arterial hypertension
— C02KX04: Macitentan
— C02KX54: Macitentan and tadalafil
HCPCS
No data
Clinical
Clinical Trials
76 clinical trials
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
HypertensionD006973EFO_0000537I1015114122
Pulmonary arterial hypertensionD000081029——1—143321
Familial primary pulmonary hypertensionD065627—I27.0——93—12
Pulmonary hypertensionD006976EFO_0001361I27.201541—11
Ventricular remodelingD020257—————1—1
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Congenital heart defectsD006330—Q24.9——2——2
Heart diseasesD006331EFO_0003777I51.9——2——2
Eisenmenger complexD004541—I27.83——2——2
Systemic sclerodermaD012595EFO_0000717M34——2——2
UlcerD014456MPATH_579———2——2
Diffuse sclerodermaD045743EFO_0000404———2——2
SclerosisD012598————2——2
Skin ulcerD012883—L98.4——1——1
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Heart failureD006333EFO_0003144I50—2———2
Vascular diseasesD014652EFO_0004264I77—2———2
FibrosisD005355———2———2
Idiopathic pulmonary fibrosisD054990—J84.112—2———2
Pulmonary fibrosisD011658—J84.10—2———2
Sickle cell anemiaD000755EFO_0000697D57—1———1
Left ventricular dysfunctionD018487———1———1
Ventricular dysfunctionD018754———1———1
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Healthy volunteers/patients———10————10
GlioblastomaD005909EFO_0000515—2————2
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameMacitentan
INNmacitentan
Description
Macitentan is a member of the class of sulfamides in which the two amino groups of sulfonamide are substituted by 5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl and propyl groups. An orphan drug used for the treatment of pulmonary arterial hypertension. It has a role as an endothelin receptor antagonist, an antihypertensive agent and an orphan drug. It is an organobromine compound, a member of pyrimidines, an aromatic ether, a ring assembly and a member of sulfamides. It is functionally related to an ethylene glycol and an ACT-132577.
Classification
Small molecule
Drug classendothelin receptor antagonists
Image (chem structure or protein)Loading
Structure (InChI/SMILES or Protein Sequence)
CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1
Identifiers
PDB—
CAS-ID441798-33-0
RxCUI—
ChEMBL IDCHEMBL2103873
ChEBI ID76607
PubChem CID16004692
DrugBankDB08932
UNII IDZ9K9Y9WMVL (ChemIDplus, GSRS)
Target
Agency Approved
EDNRA
EDNRA
Organism
Homo sapiens
Gene name
EDNRA
Gene synonyms
ETA, ETRA
NCBI Gene ID
1909
Protein name
endothelin-1 receptor
Protein synonyms
endothelin receptor subtype A, Endothelin receptor type A, endothelin-1-specific receptor, ET-A, ETA-R, G protein-coupled receptor, hET-AR
Uniprot ID
P25101
Mouse ortholog
Ednra (13617)
endothelin-1 receptor (Q91VV2)
Alternate
EDNRB
EDNRB
Organism
Homo sapiens
Gene name
EDNRB
Gene synonyms
ETRB
NCBI Gene ID
1910
Protein name
endothelin receptor type B
Protein synonyms
Endothelin receptor non-selective type, endothelin receptor subtype B1, Hirschsprung disease 2
Uniprot ID
Q9UQK3
Mouse ortholog
Ednrb (13618)
endothelin receptor type B (Q542M3)
Variants
No data
Financial
Revenue by drug
$
€
£
â‚£
Opsumit – Johnson & Johnson
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Tabular view
Estimated US medical usage
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 2,603 documents
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Safety
Black-box Warning
Black-box warning for: Opsumit, Opsynvi
Adverse Events
Top Adverse Reactions
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45,876 adverse events reported
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