Darusentan

Darusentan (LU-135252; HMR-4005) is an endothelin receptor antagonist.[1] Gilead Colorado, a subsidiary of Gilead Sciences,[2] under license from Abbott Laboratories, is developing darusentan for the potential treatment of uncontrolled hypertension.

Darusentan
Clinical data
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • Investigational
Pharmacokinetic data
MetabolismHepatic
Elimination half-life12.5 hours
Identifiers
IUPAC name
  • (2S)-2-(4,6-Dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-di(phenyl)propanoic acid
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.126.841
Chemical and physical data
FormulaC22H22N2O6
Molar mass410.426 g·mol−1
3D model (JSmol)
SMILES
  • COC1=CC(=NC(=N1)O[C@H](C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)OC
InChI
  • 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
 NY (what is this?)  (verify)

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 efficacy phase 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

References
  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
  3. "Darusentan - Gilead Sciences". Adis Insight. Springer Nature Switzerland AG.
  4. Clinical trial number NCT00389675 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)" at ClinicalTrials.gov


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