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Darusentan

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Darusentan
Clinical data
Routes of
administration
Oral
ATC code
  • none
Legal status
Legal status
  • Investigational
Pharmacokinetic data
MetabolismHepatic
Eliminationhalf-life12.5 hours
Identifiers
  • (2S)-2-(4,6-Dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-di(phenyl)propanoic acid
CAS Number
PubChemCID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.126.841Edit this at Wikidata
Chemical and physical data
FormulaC22H22N2O6
Molar mass410.426 g·mol−1
3D model (JSmol)
  • COC1=CC(=NC(=N1)O[C@H](C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)OC
  • InChI=1S/C22H22N2O6/c1-27-17-14-18(28-2)24-21(23-17)30-19(20(25)26)22(29-3,15-10-6-4-7-11-15)16-12-8-5-9-13-16/h4-14,19H,1-3H3,(H,25,26)/t19-/m1/s1 ☒N
  • Key:FEJVSJIALLTFRP-LJQANCHMSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Darusentan (LU-135252; HMR-4005) is anendothelin receptor antagonist.[1] Gilead Colorado, a subsidiary ofGilead Sciences,[2] under license fromAbbott Laboratories, is developing darusentan for the potential treatment of uncontrolledhypertension.

In June 2003,Myogen licensed the compound from Abbott for its application in the cancer field.[3]

In May 2007, a randomized, double-blind, active control, parallel assignment, safety and efficacyphase III trial was initiated in subjects who had completed the maintenance period of the DAR-312 study, but was terminated because the study did not reach its primary endpoints.[4]

See also

[edit]

References

[edit]
  1. ^Enseleit F, Lüscher TF, Ruschitzka F (August 2010)."Darusentan, a selective endothelin A receptor antagonist, for the oral treatment of resistant hypertension"(PDF).Therapeutic Advances in Cardiovascular Disease.4 (4):231–40.doi:10.1177/1753944710373785.PMID 20660536.S2CID 22533124.
  2. ^Gilead Sciences[permanent dead link]
  3. ^"Darusentan - Gilead Sciences".Adis Insight. Springer Nature Switzerland AG.
  4. ^Clinical trial numberNCT00389675 for "DORADO-AC-EX - A Long-Term Safety Extension Study to the Phase 3 DORADOC-AC Study (Protocol DAR-312) of Darusentan in Resistant Hypertension (Darusentan)" atClinicalTrials.gov


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