Darusentan

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 ;
PubChem CID	177236;
IUPHAR/BPS	3508;
ChemSpider	154336 ;
UNII	33JD57L6RW;
ChEMBL	ChEMBL23261 ;
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 ; Key:FEJVSJIALLTFRP-LJQANCHMSA-N ;
	(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]

References

^ 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.
^ Gilead Sciences^{[permanent dead link‍]}
^ "Darusentan - Gilead Sciences". Adis Insight. Springer Nature Switzerland AG.
^ 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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[pmid20660536-1] 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^{[permanent dead link‍]}

[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

[1]

[2]

[3]

[4]

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)

Darusentan

See also

References