Darusentan

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Darusentan
Darusentan.png
Systematic (IUPAC) name
(2S)-2-(4,6-Dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-di(phenyl)propanoic acid
Clinical data
Routes of
administration
Oral
Pharmacokinetic data
Metabolism Hepatic
Biological half-life 12.5 hours
Identifiers
CAS Number 171714-84-4 YesY
ATC code none
PubChem CID: 177236
IUPHAR/BPS 3508
ChemSpider 154336 N
UNII 33JD57L6RW N
ChEMBL CHEMBL23261 N
Chemical data
Formula C22H22N2O6
Molecular mass 410.42 g/mol
  • 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
 NYesY (what is this?)  (verify)

Darusentan (LU-135252; HMR-4005) is an endothelin receptor antagonist. Gilead Colorado, a subsidiary of Gilead Sciences,[1] 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.[2]

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.

References



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