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

Stem definition	Drug id	CAS RN
chemokine CXCR4 antagonists	4410	110078-46-1

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
16.80	mg	P

ADMET properties:

Property	Value	Reference
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:

Date	Agency	Company	Orphan
July 30, 2009	EMA	Sanofi B.V.
Dec. 15, 2008	FDA	GENZYME

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Venoocclusive liver disease	71.37	34.57	16	889	4819	63483298
Febrile neutropenia	47.11	34.57	26	879	118423	63369694
Thrombocytopenia	38.73	34.57	25	880	151132	63336985

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Brain teratoma	59.87	32.70	7	824	14	34956086
Febrile neutropenia	35.90	32.70	28	803	136821	34819279

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Febrile neutropenia	111.18	35.34	63	1432	230936	79511957
Mucosal inflammation	105.75	35.34	43	1452	75537	79667356
Venoocclusive liver disease	65.99	35.34	19	1476	11752	79731141
Thrombocytopenia	59.64	35.34	45	1450	265214	79477679
Blood stem cell harvest failure	49.26	35.34	7	1488	114	79742779
Escherichia infection	46.15	35.34	16	1479	18001	79724892
Ascites	45.50	35.34	24	1471	75538	79667355
Herpes simplex	39.82	35.34	13	1482	12174	79730719

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
Solid malignant tumours	indication	81920005
Multiple myeloma	indication	109989006	DOID:9538
Malignant lymphoma	indication	118600007	DOID:0060058
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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
C-X-C chemokine receptor type 4	GPCR	P61073	CXCR4_HUMAN	PARTIAL AGONIST	Ki	6.05	CHEMBL	CHEMBL
C-C chemokine receptor type 2	GPCR	P41597	CCR2_HUMAN		IC50	10.40	CHEMBL
Stromal cell-derived factor 1	Cytokine	P48061	SDF1_HUMAN				WOMBAT-PK
C-C chemokine receptor type 4	GPCR	P51679	CCR4_HUMAN	ANTAGONIST	IC50	6.19	IUPHAR
Atypical chemokine receptor 3	GPCR	P25106	ACKR3_HUMAN	AGONIST	EC50	6.85	IUPHAR
C-X-C chemokine receptor type 4	GPCR		CXCR4_RAT		IC50	6.97	CHEMBL

External reference:

ID	Source
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
360503	MMSL
d07372	MMSL
012924	NDDF
442206008	SNOMEDCT_US
442264009	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Mozobil	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5862	INJECTION, SOLUTION	24 mg	SUBCUTANEOUS	NDA	26 sections
Mozobil	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5862	INJECTION, SOLUTION	24 mg	SUBCUTANEOUS	NDA	26 sections
Mozobil	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5862	INJECTION, SOLUTION	24 mg	SUBCUTANEOUS	NDA	26 sections
Plerixafor	HUMAN PRESCRIPTION DRUG LABEL	1	0480-4320	INJECTION, SOLUTION	24 mg	SUBCUTANEOUS	ANDA	26 sections
Plerixafor	Human Prescription Drug Label	1	55150-356	SOLUTION	24 mg	SUBCUTANEOUS	ANDA	25 sections
Plerixafor	HUMAN PRESCRIPTION DRUG LABEL	1	65219-284	INJECTION, SOLUTION	24 mg	SUBCUTANEOUS	NDA AUTHORIZED GENERIC	26 sections
plerixafor	HUMAN PRESCRIPTION DRUG LABEL	1	70121-1694	INJECTION, SOLUTION	24 mg	SUBCUTANEOUS	ANDA	25 sections
PLERIXAFOR	HUMAN PRESCRIPTION DRUG LABEL	1	70710-1208	INJECTION	24 mg	SUBCUTANEOUS	ANDA	22 sections
PLERIXAFOR	HUMAN PRESCRIPTION DRUG LABEL	1	70771-1776	INJECTION	24 mg	SUBCUTANEOUS	ANDA	1 sections
Plerixafor	HUMAN PRESCRIPTION DRUG LABEL	1	71288-155	SOLUTION	24 mg	SUBCUTANEOUS	ANDA	26 sections
Plerixafor	Human Prescription Drug Label	1	72205-249	INJECTION, SOLUTION	24 mg	SUBCUTANEOUS	ANDA	25 sections