Aprocitentan
Aprocitentan is a small molecule pharmaceutical. It is currently being investigated in clinical studies. It is known to target endothelin-1 receptor and endothelin receptor type B.
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Commercial
Therapeutic Areas
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Trade Name
FDA
EMA
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Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
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Labels
FDA
EMA
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Indications
FDA
EMA
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Agency Specific
FDA
EMA
No data
Patent Expiration
No data
ATC Codes
No data
HCPCS
No data
Clinical
Clinical Trials
12 clinical trials
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Indications Phases 4
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Hypertension | D006973 | EFO_0000537 | I10 | — | — | 2 | — | — | 2 |
| Chronic renal insufficiency | D051436 | N18 | — | — | 1 | — | — | 1 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Essential hypertension | D000075222 | I10 | — | 1 | — | — | — | 1 |
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Healthy volunteers/patients | — | 9 | — | — | — | — | 9 | ||
| Hepatic insufficiency | D048550 | 1 | — | — | — | — | 1 | ||
| Renal insufficiency | D051437 | HP_0000083 | N19 | 1 | — | — | — | — | 1 |
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | APROCITENTAN |
| INN | aprocitentan |
| Description | ACT-132577 is a member of the class of sulfamides in which one of the amino groups of sulfonamide is substituted by a 5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl group. An active metabolite of macitentan (obtained by oxidative depropylation), an orphan drug used for the treatment of pulmonary arterial hypertension. It has a role as an antihypertensive agent, an endothelin receptor antagonist, a drug metabolite and a xenobiotic metabolite. It is an aromatic ether, an organobromine compound, a member of pyrimidines and a member of sulfamides. It is functionally related to an ethylene glycol. |
| Classification | Small molecule |
| Drug class | endothelin receptor antagonists |
| Image (chem structure or protein) | |
| Structure (InChI/SMILES or Protein Sequence) | NS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 |
Identifiers
| PDB | — |
| CAS-ID | 1103522-45-7 |
| RxCUI | — |
| ChEMBL ID | CHEMBL2165326 |
| ChEBI ID | 76609 |
| PubChem CID | — |
| DrugBank | — |
| UNII ID | MZI81HV01P (ChemIDplus, GSRS) |
Target
Agency Approved
No data
Alternate
EDNRA
EDNRA
EDNRB
EDNRB
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)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 39 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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1 adverse events reported
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