Drug Information

Drug General Information
Drug ID
D0R7YY
Former ID
DIB015427
Drug Name
Darusentan
Synonyms
Endothelin antagonist, BASF; HMR-4005; LU-127043; LU-135252
Drug Type
Small molecular drug
Indication Hypotension [ICD9: 458, 796.3; ICD10:I95] Phase 3 [521903], [540446]
Company
Gilead Sciences; Knoll GmbH
Formula
C22H22N2O6
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
InChIKey
FEJVSJIALLTFRP-LJQANCHMSA-N
PubChem Compound ID
177236
PubChem Substance ID
7979815, 10258564, 12015030, 14904202, 14928792, 33500713, 49881054, 53788749, 57395363, 76344031, 103191671, 104003423, 104426232, 118855309, 126681579, 127834770, 135154690, 137249396, 139988415, 152133971, 163884607, 170466416, 175426886, 178100494, 179150062, 187071946, 198954978, 198979503, 198991928, 223661592, 227075098
Target and Pathway
Target(s) Endothelin-1 receptor Target Info Antagonist [528154]
KEGG Pathway Calcium signaling pathway
cGMP-PKG signaling pathway
cAMP signaling pathway
Neuroactive ligand-receptor interaction
Vascular smooth muscle contraction
Renin secretion
Pathways in cancer
NetPath Pathway IL4 Signaling Pathway
PANTHER Pathway Endothelin signaling pathway
Pathway Interaction Database Endothelins
EGFR-dependent Endothelin signaling events
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
WikiPathways Prostaglandin Synthesis and Regulation
GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Peptide GPCRs
Endothelin Pathways
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
Ref 521903ClinicalTrials.gov (NCT00389779) DORADO-AC - Optimized Doses of Darusentan as Compared to an Active Control in Resistant Hypertension. U.S. National Institutes of Health.
Ref 540446(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3508).
Ref 528154Endothelin ETA receptor blockade with darusentan increases sodium and potassium excretion in aging rats. J Cardiovasc Pharmacol. 2006 Mar;47(3):456-62.

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