plerixafor Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
4410 110078-46-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • plerixafor hydrochloride
  • plerixafor HCl
  • AMD3100
  • AMD 3100
  • plerixafor
  • mozobil
Plerixafor is an inhibitor of the CXCR4 chemokine receptor and blocks binding of its cognate ligand, stromal cell-derived factor-1alpha (SDF-1alpha). SDF-1alpha and CXCR4 are recognized to play a role in the trafficking and homing of human hematopoietic stem cells (HSCs) to the marrow compartment. Once in the marrow, stem cell CXCR4 can act to help anchor these cells to the marrow matrix, either directly via SDF-1α or through the induction of other adhesion molecules. Treatment with plerixafor resulted in leukocytosis and elevations in circulating hematopoietic progenitor cells in mice, dogs and humans. CD34+ cells mobilized by plerixafor were capable of engraftment with long-term repopulating capacity up to one year in canine transplantation models.
  • Molecular weight: 502.80
  • Formula: C28H54N8
  • CLOGP: -0.25
  • LIPINSKI: 2
  • HAC: 8
  • HDO: 6
  • TPSA: 78.66
  • ALOGS: -4.03
  • ROTB: 4

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
16.80 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 10 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 70 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.77 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Dec. 15, 2008 FDA GENZYME

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Febrile neutropenia 52.20 33.59 13 130 10869 2347073
Thrombocytopenia 36.12 33.59 11 132 19120 2338822

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Pleural effusion 46.33 43.44 13 121 11097 1735550

Pharmacologic Action:

SourceCodeDescription
ATC L03AX16 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSTIMULANTS
IMMUNOSTIMULANTS
Other immunostimulants
CHEBI has role CHEBI:50847 immunological adjuvant
CHEBI has role CHEBI:35610 antineoplastic agent
FDA EPC N0000178326 Hematopoietic Stem Cell Mobilizer
FDA PE N0000178324 Increased Hematopoietic Stem Cell Mobilization

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Multiple myeloma indication 109989006 DOID:9538
Peripheral Mobilization of Hematopoietic Stem Cells indication
Nontraumatic splenic rupture contraindication 43325004
Leukemia, disease contraindication 93143009 DOID:1240
Leukocytosis contraindication 111583006
Impaired renal function disorder contraindication 197663003
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Breastfeeding (mother) contraindication 413712001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.45 Basic
pKa2 10.85 Basic
pKa3 8.05 Basic
pKa4 7.33 Basic
pKa5 7.16 Basic
pKa6 6.94 Basic
pKa7 3.22 Basic
pKa8 2.61 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
24MG/1.2ML (20MG/ML) MOZOBIL GENZYME N022311 Dec. 15, 2008 RX SOLUTION SUBCUTANEOUS 6987102 July 22, 2023 USE IN COMBINATION WITH GRANULOCYTE-COLONY STIMULATING FACTOR (G-CSF) TO MOBILIZE HEMATOPOIETIC STEM CELLS TO PERIPHERAL BLOOD FOR COLLECTION & SUBSEQUENT AUTOLOGOUS TRANSPLANTATION IN PATIENTS WITH NON-HODGKIN'S LYMPHOMA & MULTIPLE MYELOMA
24MG/1.2ML (20MG/ML) MOZOBIL GENZYME N022311 Dec. 15, 2008 RX SOLUTION SUBCUTANEOUS 7897590 July 22, 2023 USE IN COMBINATION WITH GRANULOCYTE-COLONY STIMULATING FACTOR (G-CSF) TO MOBILIZE HEMATOPOIETIC STEM CELLS TO PERIPHERAL BLOOD FOR COLLECTION & SUBSEQUENT AUTOLOGOUS TRANSPLANTATION IN PATIENTS WITH NON-HODGKIN'S LYMPHOMA & MULTIPLE MYELOMA

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
C-X-C chemokine receptor type 4 GPCR PARTIAL AGONIST Ki 6.05 CHEMBL CHEMBL
Stromal cell-derived factor 1 Cytokine WOMBAT-PK
C-C chemokine receptor type 4 GPCR ANTAGONIST IC50 6.19 IUPHAR
Atypical chemokine receptor 3 GPCR AGONIST EC50 6.85 IUPHAR
C-C chemokine receptor type 2 GPCR IC50 10.40 CHEMBL
C-X-C chemokine receptor type 4 GPCR IC50 6.97 CHEMBL

External reference:

IDSource
D08971 KEGG_DRUG
4028232 VUID
N0000177944 NUI
C1955474 UMLSCUI
442206008 SNOMEDCT_US
733003 RXNORM
26078 MMSL
d07372 MMSL
4028232 VANDF
442264009 SNOMEDCT_US
012924 NDDF
CHEMBL18442 ChEMBL_ID
S915P5499N UNII
8513 INN_ID
DB06809 DRUGBANK_ID
CHEBI:125354 CHEBI
65015 PUBCHEM_CID
844 IUPHAR_LIGAND_ID
C088327 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Mozobil HUMAN PRESCRIPTION DRUG LABEL 1 0024-5862 SOLUTION 24 mg SUBCUTANEOUS NDA 16 sections