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    Roxadustat

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    2D Structure
    Also known as: Fg-4592, 808118-40-3, Fg4592, Roxadustat (fg-4592), Asp1517, N-[(4-hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl]glycine
    Molecular Formula
    C19H16N2O5
    Molecular Weight
    352.3  g/mol
    InChI Key
    YOZBGTLTNGAVFU-UHFFFAOYSA-N
    FDA UNII
    X3O30D9YMX
    Roxadustat is an orally bioavailable, hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI), with potential anti-anemic activity. Upon administration, roxadustat binds to and inhibits HIF-PHI, an enzyme responsible for the degradation of transcription factors in the HIF family under normal oxygen conditions. This prevents HIF breakdown and promotes HIF activity. Increased HIF activity leads to an increase in endogenous erythropoietin production, thereby enhancing erythropoiesis. It also reduces the expression of the peptide hormone hepcidin, improves iron availability, and boosts hemoglobin (Hb) levels. HIF regulates the expression of genes in response to reduced oxygen levels, including genes required for erythropoiesis and iron metabolism.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    2-[(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)amino]acetic acid
    2.1.2 InChI
    InChI=1S/C19H16N2O5/c1-11-15-9-13(26-12-5-3-2-4-6-12)7-8-14(15)18(24)17(21-11)19(25)20-10-16(22)23/h2-9,24H,10H2,1H3,(H,20,25)(H,22,23)
    2.1.3 InChI Key
    YOZBGTLTNGAVFU-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    CC1=C2C=C(C=CC2=C(C(=N1)C(=O)NCC(=O)O)O)OC3=CC=CC=C3
    2.2 Other Identifiers
    2.2.1 UNII
    X3O30D9YMX
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. Fg-4592

    2. Fg4592

    2.3.2 Depositor-Supplied Synonyms

    1. Fg-4592

    2. 808118-40-3

    3. Fg4592

    4. Roxadustat (fg-4592)

    5. Asp1517

    6. N-[(4-hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl]glycine

    7. Asp 1517

    8. 2-[(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)amino]acetic Acid

    9. Glycine, N-[(4-hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl]-

    10. Asp-1517

    11. X3o30d9ymx

    12. Fg-4592 (asp1517)

    13. Chembl2338329

    14. Fg 4592

    15. (4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)glycine

    16. (((4-hydroxy-1-methyl-7-phenoxyisoquinolin-3-yl)carbonyl)amino)acetic Acid

    17. Evrenzo

    18. 2-(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamido)acetic Acid

    19. N-((4-hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl)glycine

    20. N-[(4-hydroxy-1-methyl-7-phenoxyisoquinolin-3-yl)carbonyl]glycine

    21. 2-[(1-methyl-4-oxidanyl-7-phenoxy-isoquinolin-3-yl)carbonylamino]ethanoic Acid

    22. Roxadustat [usan:inn]

    23. Unii-x3o30d9ymx

    24. Roxadustatum

    25. N-((4-hydroxy-1-methyl-7-phenoxyisoquinolin-3-yl)carbonyl)glycine

    26. Glycine, N-((4-hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl)-

    27. 8ho

    28. Evrenzo (tn)

    29. Fg-4592[roxadustat]

    30. Roxadustat [inn]

    31. Roxadustat [jan]

    32. Roxadustat [usan]

    33. Roxadustat(fg-4592)

    34. Roxadustat [who-dd]

    35. Mls006010023

    36. Roxadustat (jan/usan/inn)

    37. Schembl523705

    38. Gtpl8454

    39. Dtxsid60230644

    40. Ex-a390

    41. Chebi:132774

    42. Bcpp000230

    43. Hms3654m03

    44. Amy16514

    45. Bcp02523

    46. Bdbm50431015

    47. Fg-4592,asp1517

    48. Mfcd20040519

    49. S1007

    50. Zinc71257465

    51. Akos026674331

    52. Bcp9000684

    53. Ccg-268052

    54. Cs-1094

    55. Db04847

    56. Sb16615

    57. Ncgc00346527-01

    58. Ncgc00346527-07

    59. Ac-31003

    60. As-17052

    61. Hy-13426

    62. Smr004701207

    63. Db-075703

    64. Sw219900-1

    65. D10593

    66. J-522733

    67. Q27088611

    68. 2-[[4-hydroxy-1-methyl-7-(phenoxy)isoquinoline-3-carbonyl]amino]acetic Acid

    2.4 Create Date
    2006-10-26
    3 Chemical and Physical Properties
    Molecular Weight 352.3 g/mol
    Molecular Formula C19H16N2O5
    XLogP33.4
    Hydrogen Bond Donor Count3
    Hydrogen Bond Acceptor Count6
    Rotatable Bond Count5
    Exact Mass352.10592162 g/mol
    Monoisotopic Mass352.10592162 g/mol
    Topological Polar Surface Area109 Ų
    Heavy Atom Count26
    Formal Charge0
    Complexity508
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Indication

    In clinical development for the treatment of anemia of chronic inflammatory disease.

    Evrenzo is indicated for treatment of adult patients with symptomatic anaemia associated with chronic kidney disease (CKD).

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    FG-4592 represents one of several next generation PHI that has been optimized for multiple pharmacokinetic and pharmacodynamic parameters related to erythropoiesis, including selective inhibition of HIF prolyl and asparaginyl hydroxylases, potency, iron utilization, and ADME. FG-4592 represents one of several next generation HIF-PH inhibitors designed to selectively induce the expression of genes that mediate erythropoiesis for the treatment of anemia.

    5.2 ATC Code

    B03XA05

    B - Blood and blood forming organs

    B03 - Antianemic preparations

    B03X - Other antianemic preparations

    B03XA - Other antianemic preparations

    B03XA05 - Roxadustat

    5.3 Absorption, Distribution and Excretion

    Absorption

    Orally active

    5.4 Mechanism of Action

    FG-4592 is an orally active second generation HIF-PH inhibitor. Preclinical studies show that FG-4592 increases production of endogenous erythropoietin (EPO), increases iron mobilization and utilization, and overcomes the suppressive effects of inflammation on red blood cell production.