Darusentan

Darusentan

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
ATC code	none
PubChem	CID 177236
IUPHAR/BPS	3508
ChemSpider	154336
UNII	33JD57L6RW
ChEMBL	CHEMBL23261
Chemical data
Formula	C22H22N2O6
Molar mass	410.42 g/mol
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 Key:FEJVSJIALLTFRP-LJQANCHMSA-N
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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

1. Gilead Sciences
2. Thomson Pharma