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    Plerixafor

    ACTIVE PHARMA INGREDIENTS

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    2D Structure
    Also known as: 110078-46-1, Mozobil, 1,4-bis((1,4,8,11-tetraazacyclotetradecan-1-yl)methyl)benzene, Amd3100, Amd 3100, Bicyclam jm-2987
    Molecular Formula
    C28H54N8
    Molecular Weight
    502.8  g/mol
    InChI Key
    YIQPUIGJQJDJOS-UHFFFAOYSA-N
    FDA UNII
    S915P5499N
    Plerixafor is a bicyclam with hematopoietic stem cell-mobilizing activity. Plerixafor blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4, resulting in hematopoietic stem cell (HSC) release from bone marrow and HSC movement into the peripheral circulation.
    Plerixafor is a Hematopoietic Stem Cell Mobilizer. The physiologic effect of plerixafor is by means of Increased Hematopoietic Stem Cell Mobilization.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    1-[[4-(1,4,8,11-tetrazacyclotetradec-1-ylmethyl)phenyl]methyl]-1,4,8,11-tetrazacyclotetradecane
    2.1.2 InChI
    InChI=1S/C28H54N8/c1-9-29-15-17-31-13-3-21-35(23-19-33-11-1)25-27-5-7-28(8-6-27)26-36-22-4-14-32-18-16-30-10-2-12-34-20-24-36/h5-8,29-34H,1-4,9-26H2
    2.1.3 InChI Key
    YIQPUIGJQJDJOS-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3
    2.2 Other Identifiers
    2.2.1 UNII
    S915P5499N
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. 1,1'-(1,4-phenylenebis(methylene))bis(1,4,8,11-tetraazacyclotetradecane)octahydrochloride Dihydrate

    2. 1,1'-(1,4-phenylenebis-(methylene))-bis-1,4,8,11-tetraazacyclotetradecane

    3. 1,1'-(1,4-phenylenebis-(methylene))-bis-1,4,8,11-tetraazacyclotetradecane Octahydrochloride Dihydrate

    4. Amd 3100

    5. Amd 3329

    6. Amd-3100

    7. Amd-3329

    8. Amd3100

    9. Jm 3100

    10. Jm3100

    11. Mezobil

    12. Mozobil

    13. Plerixafor Hydrochloride

    14. Plerixafor Octahydrobromide

    15. Plerixafor Octahydrochloride

    16. Rpa Bicyclam

    2.3.2 Depositor-Supplied Synonyms

    1. 110078-46-1

    2. Mozobil

    3. 1,4-bis((1,4,8,11-tetraazacyclotetradecan-1-yl)methyl)benzene

    4. Amd3100

    5. Amd 3100

    6. Bicyclam Jm-2987

    7. Plerixafor Hydrochloride

    8. Sdz Sid 791

    9. Plerixafor (amd3100)

    10. Amd-3100

    11. Jm3100

    12. Jm 3100

    13. 1-[[4-(1,4,8,11-tetrazacyclotetradec-1-ylmethyl)phenyl]methyl]-1,4,8,11-tetrazacyclotetradecane

    14. Jkl 169

    15. Jm-3100

    16. Chembl18442

    17. 1,1'-[1,4-phenylenebis(methylene)]bis-1,4,8,11-tetraazacyclotetradecane

    18. S915p5499n

    19. 1,1'-[1,4-phenylenebis(methylene)]bis[1,4,8,11-tetraazacyclotetradecane]

    20. 1-{[4-(1,4,8,11-tetraazacyclotetradecan-1-ylmethyl)phenyl]methyl}-1,4,8,11-tetraazacyclotetradecane

    21. 1,4,8,11-tetraazacyclotetradecane, 1,1'-(1,4-phenylenebis(methylene))bis-

    22. Mozobil (tn)

    23. Plerixafor [usan]

    24. Plerixaforum

    25. Plerixafor [usan:inn:ban]

    26. Sid791

    27. 1,1'-[1,4-phenylenebis(methylene)]bis(1,4,8,11-tetraazacyclotetradecane)

    28. Unii-s915p5499n

    29. 1,1'-(1,4-phenylenebis(methylene))bis-1,4,8,11-tetraazacyclotetradecane

    30. Gna & Amd-3100

    31. Hha & Amd-3100

    32. Jm 2987

    33. Plerixafor [mi]

    34. Plerixafor [inn]

    35. Plerixafor [jan]

    36. Plerixafor [vandf]

    37. Plerixafor [mart.]

    38. Plerixafor-d4 (deuterated)

    39. Plerixafor [who-dd]

    40. Schembl19038

    41. Gtpl844

    42. Plerixafor (jan/usan/inn)

    43. Plerixafor [ema Epar]

    44. Plerixafor [orange Book]

    45. Dtxsid70869520

    46. Amd-3100 (cxcr4)

    47. Chebi:125354

    48. Bcpp000104

    49. Bcp02337

    50. Ex-a1762

    51. Bdbm50035696

    52. Mfcd05662218

    53. Nsc754363

    54. Nsc761388

    55. S8030

    56. Zinc22443609

    57. 1,1'-{1,4-phenylenebis(methylene)}-bis{1,4,8,11-tetraaza-cyclotetradecane}

    58. Akos005266706

    59. Ccg-269710

    60. Cs-0451

    61. Db06809

    62. Nsc-754363

    63. Nsc-761388

    64. Ncgc00165722-01

    65. Ncgc00165722-02

    66. Ncgc00165722-03

    67. 1,1'-[1,4-phenylenebis(methylene)]bis[1,4,8,11-tetraazacyclotetradecane] & Galanthus Nivalis Agglutinin (gna)

    68. Ac-26837

    69. As-42504

    70. Hy-10046

    71. Ft-0660392

    72. Ft-0673966

    73. P2678

    74. A25446

    75. D08971

    76. Ab01566900_01

    77. 078p461

    78. A809618

    79. L000104

    80. Q905835

    81. Sr-01000941593

    82. J-503718

    83. Sr-01000941593-1

    84. 11''''-xylyl Bis-1,4,8,11-tetraazacyclotetradecane

    85. Brd-k33240821-367-01-8

    86. Z2196779619

    87. 1,1''''-{1,4-phenylenebis(methylene)}-bis{1,4,8,11-tetraaza-cyclotetradecane}

    88. 1,1'-(benzene-1,4-diyldimethanediyl)bis(1,4,8,11-tetraazacyclotetradecane)

    89. 1,1'[1,4-phenylene-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane

    90. 1,1'-[1,4-phenylenebis(methylene)]bis[1,4,8,11-tetraazacyclotetradecane] & Hippeastrum Hybrid Agglutinin( Hha)

    91. 1,4,8,11-tetraazacyclotetradecanyl[4-(1,4,8,11-tetraazacyclotetradecanylmethyl)phenyl]methane

    92. 1,4,8,11-tetraazacyclotetradecanyl[4-(1,4,8,11-tetraazacyclotetradecanylmethyl)phenyl]methane(8hbr.2h2o)

    93. 1,4-bis((1,4,8,11-tetraazacyclotetradecan-1-yl)methyl)benzene Octahydrochloride;plerixafor Octahydrochloride

    94. 1-({4-[(1,4,8,11-tetraazacyclotetradecan-1-yl)methyl]phenyl}methyl)-1,4,8,11-tetraazacyclotetradecane

    95. 11-{4-[4,8, 11-1,4,8,11tetraaza-cyclotetradec-1-ylmethyl]-benzyl}-1,4,8,11tetraaza-cyclotetradecane-1,4,8-tricarboxylic Acid Tri-tert-butyl Ester

    2.4 Create Date
    2005-08-01
    3 Chemical and Physical Properties
    Molecular Weight 502.8 g/mol
    Molecular Formula C28H54N8
    XLogP30
    Hydrogen Bond Donor Count6
    Hydrogen Bond Acceptor Count8
    Rotatable Bond Count4
    Exact Mass502.44714376 g/mol
    Monoisotopic Mass502.44714376 g/mol
    Topological Polar Surface Area78.7 Ų
    Heavy Atom Count36
    Formal Charge0
    Complexity456
    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 Information
    1 of 2  
    Drug NameMozobil
    PubMed HealthPlerixafor (Injection)
    Drug ClassesHematopoietic
    Drug LabelMozobil (plerixafor injection) is a sterile, preservative-free, clear, colorless to pale yellow, isotonic solution for subcutaneous injection. Each mL of the sterile solution contains 20 mg of plerixafor. Each single-use vial is filled to deliver 1...
    Active IngredientPlerixafor
    Dosage FormSolution
    RouteSubcutaneous
    Strength24mg/1.2ml (20mg/ml)
    Market StatusPrescription
    CompanyGenzyme

    2 of 2  
    Drug NameMozobil
    PubMed HealthPlerixafor (Injection)
    Drug ClassesHematopoietic
    Drug LabelMozobil (plerixafor injection) is a sterile, preservative-free, clear, colorless to pale yellow, isotonic solution for subcutaneous injection. Each mL of the sterile solution contains 20 mg of plerixafor. Each single-use vial is filled to deliver 1...
    Active IngredientPlerixafor
    Dosage FormSolution
    RouteSubcutaneous
    Strength24mg/1.2ml (20mg/ml)
    Market StatusPrescription
    CompanyGenzyme

    4.2 Drug Indication

    Used in combination with granulocyte-colony stimulating factor (G-CSF, filgrastim) to mobilize hematopoietic stem cells to the peripheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkins lymphoma (NHL) and multiple myeloma (MM).

    FDA Label

    Mozobil is indicated in combination with granulocyte-colony-stimulating factor to enhance mobilisation of haematopoietic stem cells to the peripheral blood for collection and subsequent autologous transplantation in patients with lymphoma and multiple myeloma whose cells mobilise poorly.

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Plerixafor is a bicyclam derivative that antagonizes CXCR4 by binding to three acidic residues in the ligand-binding pocket: Asp171, Asp262, and Glu288. Blood levels of CD34+ cells peaked at 9 hours after administration of 0.24 mg/kg plerixafor in healthy subjects. In patients that have non-Hodgkins lymphoma or multiple myeloma, blood levels of CD34+ peaked at 6 hours. In combination with a G-CSF, circulating CD34+ cells in the peripheral blood peaked at 9-14 hours.

    5.2 MeSH Pharmacological Classification

    Anti-HIV Agents

    Agents used to treat AIDS and/or stop the spread of the HIV infection. These do not include drugs used to treat symptoms or opportunistic infections associated with AIDS. (See all compounds classified as Anti-HIV Agents.)

    5.3 FDA Pharmacological Classification
    5.3.1 Active Moiety
    PLERIXAFOR
    5.3.2 FDA UNII
    S915P5499N
    5.3.3 Pharmacological Classes
    Increased Hematopoietic Stem Cell Mobilization [PE]; Hematopoietic Stem Cell Mobilizer [EPC]
    5.4 ATC Code

    L03AX16

    L03AX16

    S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355

    L - Antineoplastic and immunomodulating agents

    L03 - Immunostimulants

    L03A - Immunostimulants

    L03AX - Other immunostimulants

    L03AX16 - Plerixafor

    5.5 Absorption, Distribution and Excretion

    Absorption

    Pharmacokinetic profile follows a two-compartment model with first-order absorption. A median peak plasma concentration of 0.24 mg/kg of plerixafor occurred 30-60 minutes after subcutaneous dose.

    Route of Elimination

    0.24 mg/kg, healthy subjects: ~70% of the parent drug is excreted in urine in the first 24 hours.

    Volume of Distribution

    0.3 L/kg

    Clearance

    Total plasma clearance: 4.38 L/h; Renal clearance: 3.15 L/h

    5.6 Metabolism/Metabolites

    Metabolism does not involved CYP isoenzymes

    5.7 Biological Half-Life

    Terminal elimination half-life, NHL patients: 4.4 hours; Terminal elimination half-life, MM patients: 5.6 hours; Terminal elimination half-life, Hodgkin's lymphoma patients: 3.5 hours; Distribution half-life: 0.3 hours

    5.8 Mechanism of Action

    Plerixafor inhibits the CXCR4 chemokine receptors on CD34+ cells and reversibly blocks binding of the ligand, stromal cell-derived factor-1-alpha (SDF-1). By blocking the interaction between SDF-1 and CXCR4 with plerixafor, mobilization of progenitor cells is triggered. Filgrastim, a granulocyte-colony stimulating factor, is added to enhance CD34+ cell mobilization, thus increasing the yield of stem cells- an important determinant of graft adequacy.