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Sitaxentan
Thelin (sitaxentan) is a small molecule pharmaceutical. Sitaxentan was first approved as Thelin on 2006-08-10. It has been approved in Europe to treat pulmonary hypertension. The pharmaceutical is active against endothelin-1 receptor.
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
respiratory tract diseasesD012140
cardiovascular diseasesD002318
Trade Name
FDA
EMA
No data
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
No data
Labels
FDA
EMA
No data
Indications
FDA
EMA
No data
Agency Specific
FDA
EMA
No data
Patent Expiration
No data
ATC Codes
C: Cardiovascular system drugs
— C02: Antihypertensives
— C02K: Other antihypertensives in atc
— C02KX: Antihypertensives for pulmonary arterial hypertension
— C02KX03: Sitaxentan
HCPCS
No data
Clinical
Clinical Trials
21 clinical trials
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Indications Phases 4
No data
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Pulmonary arterial hypertensionD0000810294—4—311
Pulmonary hypertensionD006976EFO_0001361I27.20—17—18
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Chronic renal insufficiencyD051436N18—2———2
Airway remodelingD056151—1———1
ProteinuriaD011507HP_0000093R80—1———1
Blood pressureD001794EFO_0004325—1———1
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
VasodilationD0146641————1
VasoconstrictionD0146611————1
Healthy volunteers/patients—1————1
Indications Without Phase
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Heart diseasesD006331EFO_0003777I51.9————11
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameSITAXENTAN
INNsitaxentan
Description
Sitaxentan is a member of benzodioxoles.
Classification
Small molecule
Drug classendothelin receptor antagonists
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2
Identifiers
PDB—
CAS-ID184036-34-8
RxCUI—
ChEMBL IDCHEMBL282724
ChEBI ID—
PubChem CID216235
DrugBankDB06268
UNII IDJ9QH779MEM (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
No data
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 964 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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122 adverse events reported
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