Opsumit(macitentan)
Opsumit (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
Trade Name
FDA
EMA
Opsumit (generic drugs available since 2023-04-18)
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 |
|---|---|---|---|---|
| OPSUMIT | Actelion | N-204410 RX | 2013-10-18 | 1 products, RLD, RS |
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| opsumit | New Drug Application | 2021-01-14 |
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| pulmonary hypertension | EFO_0001361 | D006976 | I27.20 |
Agency Specific
FDA
EMA
No data
HCPCS
No data
Clinical
Clinical Trials
56 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Pulmonary arterial hypertension | D000081029 | — | 1 | 14 | 3 | 2 | 20 | ||
| Pulmonary hypertension | D006976 | EFO_0001361 | I27.20 | — | 5 | 3 | 1 | — | 7 |
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Chronic disease | D002908 | — | 1 | 1 | — | — | 1 | ||
| Interstitial lung diseases | D017563 | EFO_0004244 | J84.89 | — | 1 | 1 | — | — | 1 |
| Congenital heart defects | D006330 | HP_0001627 | Q24.9 | — | — | 1 | — | — | 1 |
| Systemic scleroderma | D012595 | EFO_0000717 | M34 | — | — | 1 | — | — | 1 |
| Ulcer | D014456 | MPATH_579 | — | — | 1 | — | — | 1 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Heart failure | D006333 | EFO_0003144 | I50 | — | 2 | — | — | — | 2 |
| Idiopathic pulmonary fibrosis | D054990 | J84.112 | — | 2 | — | — | — | 2 | |
| Sickle cell anemia | D000755 | EFO_0000697 | D57 | — | 1 | — | — | — | 1 |
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Healthy volunteers/patients | — | 12 | — | — | — | — | 12 | ||
| Glioblastoma | D005909 | EFO_0000515 | 1 | — | — | — | — | 1 |
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | MACITENTAN |
| INN | macitentan |
| 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 class | endothelin receptor antagonists |
| Image (chem structure or protein) | |
| Structure (InChI/SMILES or Protein Sequence) | CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 |
Identifiers
| PDB | — |
| CAS-ID | 441798-33-0 |
| RxCUI | 1442132 |
| ChEMBL ID | CHEMBL2103873 |
| ChEBI ID | 76607 |
| PubChem CID | 16004692 |
| DrugBank | DB08932 |
| UNII ID | Z9K9Y9WMVL (ChemIDplus, GSRS) |
Target
Agency Approved
EDNRA
EDNRA
Organism
Homo sapiens
Gene name
EDNRA
Gene synonyms
ETA, ETRA
NCBI Gene ID
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
Mouse ortholog
Ednra (13617)
endothelin-1 receptor (Q91VV2)
Alternate
EDNRB
EDNRB
Variants
Clinical Variant
No data
Financial
Opsumit - Johnson & Johnson
$
€
£
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Tabular view
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 1,778 documents
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Safety
Black-box Warning
Black-box warning for: Opsumit
Adverse Events
Top Adverse Reactions
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13,786 adverse events reported
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