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
Metabolism	Hepatic
Elimination half-life	12.5 hours
Identifiers
IUPAC name (2S)-2-(4,6-Dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-di(phenyl)propanoic acid
CAS Number	171714-84-4 Y
PubChem CID	177236
IUPHAR/BPS	3508
ChemSpider	154336 N
UNII	33JD57L6RW
ChEMBL	ChEMBL23261 N
CompTox Dashboard (EPA)	DTXSID1057664
ECHA InfoCard	100.126.841
Chemical and physical data
Formula	C22H22N2O6
Molar mass	410.426 g·mol−1
3D model (JSmol)	Interactive image
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

• Ambrisentan