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Barbiturate
Darusentan
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    Darusentan

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    Darusentan
    Darusentan.svg
    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
    • (2S)-2-(4,6-Dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-di(phenyl)propanoic acid
    CAS Number
    PubChem CID
    IUPHAR/BPS
    ChemSpider
    UNII
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard 100.126.841
    Chemical and physical data
    Formula C22H22N2O6
    Molar mass 410.426 g·mol−1
    3D model (JSmol)
    • 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
     ☒NcheckY (what is this?)  (verify)

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

    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.

    See also



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