plerixafor ๐Ÿถ Veterinary Use | 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-1ฮฑ 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 ยตM/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
Venoocclusive liver disease 65.03 32.61 15 855 4246 50600008
Febrile neutropenia 41.80 32.61 24 846 97643 50506611
Thrombocytopenia 35.88 32.61 24 846 127649 50476605

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
Brain teratoma 59.51 30.50 7 733 14 29573773
Febrile neutropenia 37.32 30.50 27 713 112213 29461574

FDA Adverse Event Reporting System (Geriatric)

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 108.18 33.60 60 1302 187597 64309773
Mucosal inflammation 81.42 33.60 35 1327 62549 64434821
Venoocclusive liver disease 62.32 33.60 18 1344 9997 64487373
Thrombocytopenia 57.22 33.60 43 1319 223758 64273612
Ascites 44.40 33.60 23 1339 61978 64435392
Blood stem cell harvest failure 41.85 33.60 6 1356 92 64497278
Herpes simplex 40.17 33.60 13 1349 10523 64486847
Escherichia infection 39.28 33.60 14 1348 15154 64482216

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L03AX16 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSTIMULANTS
IMMUNOSTIMULANTS
Other immunostimulants
MeSH PA D019380 Anti-HIV Agents
MeSH PA D000890 Anti-Infective Agents
MeSH PA D044966 Anti-Retroviral Agents
MeSH PA D000998 Antiviral Agents
FDA PE N0000178324 Increased Hematopoietic Stem Cell Mobilization
FDA EPC N0000178326 Hematopoietic Stem Cell Mobilizer
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:50847 Immunologic adjuvant
CHEBI has role CHEBI:64946 anti-AIDS agent
CHEBI has role CHEBI:145438 CXCR4 antagonists

Drug Use | Suggest Off label Use Form| |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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

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-HODGKINS 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-HODGKINS 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
C-C chemokine receptor type 2 GPCR IC50 10.40 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-X-C chemokine receptor type 4 GPCR IC50 6.97 CHEMBL

External reference:

IDSource
D08971 KEGG_DRUG
4028232 VUID
N0000177944 NUI
4028232 VANDF
C1955474 UMLSCUI
CHEBI:125354 CHEBI
CHEMBL18442 ChEMBL_ID
CHEMBL2311028 ChEMBL_ID
DB06809 DRUGBANK_ID
C088327 MESH_SUPPLEMENTAL_RECORD_UI
844 IUPHAR_LIGAND_ID
8513 INN_ID
S915P5499N UNII
65015 PUBCHEM_CID
733003 RXNORM
159539 MMSL
26078 MMSL
d07372 MMSL
012924 NDDF
442206008 SNOMEDCT_US
442264009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Mozobil HUMAN PRESCRIPTION DRUG LABEL 1 0024-5862 INJECTION, SOLUTION 24 mg SUBCUTANEOUS NDA 26 sections