Darusentan

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
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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
 ☒NcheckY (what is this?)  (verify)

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.

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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