U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C28H54N8
Molecular Weight 502.782
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PLERIXAFOR

SMILES

C(N1CCCNCCNCCCNCC1)C2=CC=C(CN3CCCNCCNCCCNCC3)C=C2

InChI

InChIKey=YIQPUIGJQJDJOS-UHFFFAOYSA-N
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

HIDE SMILES / InChI
Molecular Formula C28H54N8
Molecular Weight 502.782
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Plerixafor is a bicyclam molecule, which has been identified as a specific antagonist of CXCR4. It had originally been developed as an inhibitor of T-tropic human immunodeficiency virus, but later demonstrated to be an effective mobilizer of hematopoietic stem cells. Plerixafor was approved by FDA for autologous transplantation (in combination with granulocyte-colony stimulating factor) in patients with non-Hodgkin's lymphoma and multiple myeloma under the name Mozobil.

CNS Activity

Originator

Approval Year

2008
172
Targets

Targets

Primary TargetPharmacologyConditionPotency
C-X-C chemokine receptor type 4
5
Target ID: P61073
Gene ID: 7852.0
Gene Symbol: CXCR4
Target Organism: Homo sapiens (Human)
Antagonist
2737
 44.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8307
MOZOBIL

Approved Use

Mozobil (plerixafor) injection is indicated in combination with granulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells (HSCs) to the peripheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma (NHL) and multiple myeloma (MM).

Launch Date

1.22929925E12
Primary
Approved
8307
MOZOBIL

Approved Use

Mozobil (plerixafor) injection is indicated in combination with granulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells (HSCs) to the peripheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma (NHL) and multiple myeloma (MM).

Launch Date

1.22929925E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1029 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/19135941
240 μg/kg bw single, subcutaneous
dose: 240 μg/kg bw
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
PLERIXAFOR plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
5260 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/19135941
240 μg/kg bw single, subcutaneous
dose: 240 μg/kg bw
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
PLERIXAFOR plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
5.6 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/19135941
240 μg/kg bw single, subcutaneous
dose: 240 μg/kg bw
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
PLERIXAFOR plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
160 ug/kg/h multiple, intravenous
Highest studied dose
Dose: 160 ug/kg/h
Route: intravenous
Route: multiple
Dose: 160 ug/kg/h
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
unhealthy, 40.2 years
n = 3
Health Status: unhealthy
Condition: HIV-1 Infection
Age Group: 40.2 years
Sex: M+F
Population Size: 3
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
Disc. AE: Premature ventricular contractions...
AEs leading to
discontinuation/dose reduction:
Premature ventricular contractions (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
20 ug/kg/h multiple, intravenous
Dose: 20 ug/kg/h
Route: intravenous
Route: multiple
Dose: 20 ug/kg/h
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
unhealthy, 40.2 years
n = 8
Health Status: unhealthy
Condition: HIV-1 Infection
Age Group: 40.2 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
Disc. AE: Hepatic enzyme increased, Orthostatic hypotension...
AEs leading to
discontinuation/dose reduction:
Hepatic enzyme increased (1 patient)
Orthostatic hypotension (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
40 ug/kg/h multiple, intravenous
Dose: 40 ug/kg/h
Route: intravenous
Route: multiple
Dose: 40 ug/kg/h
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
unhealthy, 40.2 years
n = 8
Health Status: unhealthy
Condition: HIV-1 Infection
Age Group: 40.2 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
Disc. AE: Ventricular ectopics...
AEs leading to
discontinuation/dose reduction:
Ventricular ectopics (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
5 ug/kg/h multiple, intravenous
Dose: 5 ug/kg/h
Route: intravenous
Route: multiple
Dose: 5 ug/kg/h
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
unhealthy, 40.2 years
n = 7
Health Status: unhealthy
Condition: HIV-1 Infection
Age Group: 40.2 years
Sex: M+F
Population Size: 7
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
Disc. AE: Thrombocytopenia...
AEs leading to
discontinuation/dose reduction:
Thrombocytopenia (serious, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
80 ug/kg/h multiple, intravenous
Dose: 80 ug/kg/h
Route: intravenous
Route: multiple
Dose: 80 ug/kg/h
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
unhealthy, 40.2 years
n = 5
Health Status: unhealthy
Condition: HIV-1 Infection
Age Group: 40.2 years
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
Disc. AE: Paresthesia...
AEs leading to
discontinuation/dose reduction:
Paresthesia (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
160 ug/kg single, oral
Dose: 160 ug/kg
Route: oral
Route: single
Dose: 160 ug/kg
Sources:
https://pubmed.ncbi.nlm.nih.gov/10817726
healthy, >18 years
n = 3
Health Status: healthy
Age Group: >18 years
Sex: M+F
Population Size: 3
Sources:
https://pubmed.ncbi.nlm.nih.gov/10817726
Sources:
https://pubmed.ncbi.nlm.nih.gov/10817726
80 ug/kg single, intravenous
Dose: 80 ug/kg
Route: intravenous
Route: single
Dose: 80 ug/kg
Sources:
https://pubmed.ncbi.nlm.nih.gov/10817726
healthy, >18 years
n = 12
Health Status: healthy
Age Group: >18 years
Sex: M+F
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/10817726
Other AEs: Diaphoresis...
Other AEs:
Diaphoresis (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/10817726
320 ug/kg single, subcutaneous
Highest studied dose
Dose: 320 ug/kg
Route: subcutaneous
Route: single
Dose: 320 ug/kg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p. 83
healthy, adult
n = 10
Health Status: healthy
Age Group: adult
Population Size: 10
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p. 83
Other AEs: Injection site erythema, Paresthesia...
Other AEs:
Injection site erythema
Paresthesia
Chest discomfort
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p. 83
0.24 mg/kg 1 times / day multiple, subcutaneous
Recommended
Dose: 0.24 mg/kg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 0.24 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
unhealthy, adult
n = 72
Health Status: unhealthy
Age Group: adult
Population Size: 72
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
Disc. AE: Anxiety, Arrhythmia...
AEs leading to
discontinuation/dose reduction:
Anxiety (1 patient)
Arrhythmia (1 patient)
Erythema (1 patient)
Decreased appetite (1 patient)
Eructation (1 patient)
Liver function test abnormal (1 patient)
Nausea (2 patients)
Vomiting (2 patients)
Postural hypotension (1 patient)
Sinus tachycardia (1 patient)
Staphylococcal bacteremia (1 patient)
Insomnia (1 patient)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
AEs

AEs

AESignificanceDosePopulation
Premature ventricular contractions 1 patient
Disc. AE
160 ug/kg/h multiple, intravenous
Highest studied dose
Dose: 160 ug/kg/h
Route: intravenous
Route: multiple
Dose: 160 ug/kg/h
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
unhealthy, 40.2 years
n = 3
Health Status: unhealthy
Condition: HIV-1 Infection
Age Group: 40.2 years
Sex: M+F
Population Size: 3
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
Hepatic enzyme increased 1 patient
Disc. AE
20 ug/kg/h multiple, intravenous
Dose: 20 ug/kg/h
Route: intravenous
Route: multiple
Dose: 20 ug/kg/h
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
unhealthy, 40.2 years
n = 8
Health Status: unhealthy
Condition: HIV-1 Infection
Age Group: 40.2 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
Orthostatic hypotension 1 patient
Disc. AE
20 ug/kg/h multiple, intravenous
Dose: 20 ug/kg/h
Route: intravenous
Route: multiple
Dose: 20 ug/kg/h
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
unhealthy, 40.2 years
n = 8
Health Status: unhealthy
Condition: HIV-1 Infection
Age Group: 40.2 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
Ventricular ectopics 1 patient
Disc. AE
40 ug/kg/h multiple, intravenous
Dose: 40 ug/kg/h
Route: intravenous
Route: multiple
Dose: 40 ug/kg/h
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
unhealthy, 40.2 years
n = 8
Health Status: unhealthy
Condition: HIV-1 Infection
Age Group: 40.2 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
Thrombocytopenia serious, 1 patient
Disc. AE
5 ug/kg/h multiple, intravenous
Dose: 5 ug/kg/h
Route: intravenous
Route: multiple
Dose: 5 ug/kg/h
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
unhealthy, 40.2 years
n = 7
Health Status: unhealthy
Condition: HIV-1 Infection
Age Group: 40.2 years
Sex: M+F
Population Size: 7
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
Paresthesia 1 patient
Disc. AE
80 ug/kg/h multiple, intravenous
Dose: 80 ug/kg/h
Route: intravenous
Route: multiple
Dose: 80 ug/kg/h
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
unhealthy, 40.2 years
n = 5
Health Status: unhealthy
Condition: HIV-1 Infection
Age Group: 40.2 years
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/15385732
Diaphoresis 1 patient
80 ug/kg single, intravenous
Dose: 80 ug/kg
Route: intravenous
Route: single
Dose: 80 ug/kg
Sources:
https://pubmed.ncbi.nlm.nih.gov/10817726
healthy, >18 years
n = 12
Health Status: healthy
Age Group: >18 years
Sex: M+F
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/10817726
Chest discomfort
320 ug/kg single, subcutaneous
Highest studied dose
Dose: 320 ug/kg
Route: subcutaneous
Route: single
Dose: 320 ug/kg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p. 83
healthy, adult
n = 10
Health Status: healthy
Age Group: adult
Population Size: 10
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p. 83
Injection site erythema
320 ug/kg single, subcutaneous
Highest studied dose
Dose: 320 ug/kg
Route: subcutaneous
Route: single
Dose: 320 ug/kg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p. 83
healthy, adult
n = 10
Health Status: healthy
Age Group: adult
Population Size: 10
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p. 83
Paresthesia
320 ug/kg single, subcutaneous
Highest studied dose
Dose: 320 ug/kg
Route: subcutaneous
Route: single
Dose: 320 ug/kg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p. 83
healthy, adult
n = 10
Health Status: healthy
Age Group: adult
Population Size: 10
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p. 83
Anxiety 1 patient
Disc. AE
0.24 mg/kg 1 times / day multiple, subcutaneous
Recommended
Dose: 0.24 mg/kg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 0.24 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
unhealthy, adult
n = 72
Health Status: unhealthy
Age Group: adult
Population Size: 72
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
Arrhythmia 1 patient
Disc. AE
0.24 mg/kg 1 times / day multiple, subcutaneous
Recommended
Dose: 0.24 mg/kg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 0.24 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
unhealthy, adult
n = 72
Health Status: unhealthy
Age Group: adult
Population Size: 72
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
Decreased appetite 1 patient
Disc. AE
0.24 mg/kg 1 times / day multiple, subcutaneous
Recommended
Dose: 0.24 mg/kg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 0.24 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
unhealthy, adult
n = 72
Health Status: unhealthy
Age Group: adult
Population Size: 72
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
Eructation 1 patient
Disc. AE
0.24 mg/kg 1 times / day multiple, subcutaneous
Recommended
Dose: 0.24 mg/kg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 0.24 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
unhealthy, adult
n = 72
Health Status: unhealthy
Age Group: adult
Population Size: 72
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
Erythema 1 patient
Disc. AE
0.24 mg/kg 1 times / day multiple, subcutaneous
Recommended
Dose: 0.24 mg/kg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 0.24 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
unhealthy, adult
n = 72
Health Status: unhealthy
Age Group: adult
Population Size: 72
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
Insomnia 1 patient
Disc. AE
0.24 mg/kg 1 times / day multiple, subcutaneous
Recommended
Dose: 0.24 mg/kg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 0.24 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
unhealthy, adult
n = 72
Health Status: unhealthy
Age Group: adult
Population Size: 72
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
Liver function test abnormal 1 patient
Disc. AE
0.24 mg/kg 1 times / day multiple, subcutaneous
Recommended
Dose: 0.24 mg/kg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 0.24 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
unhealthy, adult
n = 72
Health Status: unhealthy
Age Group: adult
Population Size: 72
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
Postural hypotension 1 patient
Disc. AE
0.24 mg/kg 1 times / day multiple, subcutaneous
Recommended
Dose: 0.24 mg/kg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 0.24 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
unhealthy, adult
n = 72
Health Status: unhealthy
Age Group: adult
Population Size: 72
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
Sinus tachycardia 1 patient
Disc. AE
0.24 mg/kg 1 times / day multiple, subcutaneous
Recommended
Dose: 0.24 mg/kg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 0.24 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
unhealthy, adult
n = 72
Health Status: unhealthy
Age Group: adult
Population Size: 72
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
Staphylococcal bacteremia 1 patient
Disc. AE
0.24 mg/kg 1 times / day multiple, subcutaneous
Recommended
Dose: 0.24 mg/kg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 0.24 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
unhealthy, adult
n = 72
Health Status: unhealthy
Age Group: adult
Population Size: 72
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
Nausea 2 patients
Disc. AE
0.24 mg/kg 1 times / day multiple, subcutaneous
Recommended
Dose: 0.24 mg/kg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 0.24 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
unhealthy, adult
n = 72
Health Status: unhealthy
Age Group: adult
Population Size: 72
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
Vomiting 2 patients
Disc. AE
0.24 mg/kg 1 times / day multiple, subcutaneous
Recommended
Dose: 0.24 mg/kg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 0.24 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
unhealthy, adult
n = 72
Health Status: unhealthy
Age Group: adult
Population Size: 72
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022311s000_MedR.pdf
Page: p.97
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1695

inducer
372
inhibitor
1789

inducer
97
inhibitor
1570

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1463

CYP2A6
670

CYP2B6
770

CYP2C8
869

CYP2C19
1410

CYP3A4/5
261

P-gp
1401

CYP2E1
846

CYP4A9/11
34
CYP
252

P-gp
1491
CYP1A2
671

CYP2B6
521

CYP3A4/5
112

P-gp
252

CYP2C19
283
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
P-gp
1588
 inconclusive
P-gp
1588
 inconclusive
CYP1A2
1620
 no [IC50 >100 uM]
CYP2C19
1484
 no [IC50 >100 uM]
CYP2C9
1747
 no [IC50 >100 uM]
CYP2D6
1826
 no [IC50 >100 uM]
CYP2E1
929
 no [IC50 >100 uM]
CYP3A4/5
314
 no [IC50 >100 uM]
CYP4A9/11
34
 no [IC50 >100 uM]
CYP1A2
1620
 no
CYP2A6
702
 no
CYP2B6
946
 no
CYP2B6
946
 no
CYP2C19
1484
 no
CYP2C8
923
 no
CYP2C9
1747
 no
CYP2D6
1826
 no
CYP3A4/5
314
 no
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
P-gp
1491
 inconclusive
CYP
252
 no
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1603
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:125354
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:125354
ChemicalBook
CB11011749
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB11011749
MolPort
MolPort-009-019-417
https://www.molport.com/shop/molecule-link/MolPort-009-019-417
Selleck Chemicals
plerixafor
http://www.selleckchem.com/products/plerixafor.html
ZINC
ZINC000022443609
http://zinc15.docking.org/substances/ZINC000022443609
eMolecules
6842643
https://www.emolecules.com/cgi-bin/more?vid=6842643
PubMed

PubMed

TitleDatePubMed
Resistance of the human immunodeficiency virus to the inhibitory action of negatively charged albumins on virus binding to CD4.
1999 Nov 20
Viral entry through CXCR4 is a pathogenic factor and therapeutic target in human immunodeficiency virus type 1 disease.
2000 Jan
A point mutation that confers constitutive activity to CXCR4 reveals that T140 is an inverse agonist and that AMD3100 and ALX40-4C are weak partial agonists.
2002 Jul 5
The CCR5 and CXCR4 coreceptors are both used by human immunodeficiency virus type 1 primary isolates from subtype C.
2003 Apr
A duodenally absorbable CXC chemokine receptor 4 antagonist, KRH-1636, exhibits a potent and selective anti-HIV-1 activity.
2003 Apr 1
Characterization of the molecular pharmacology of AMD3100: a specific antagonist of the G-protein coupled chemokine receptor, CXCR4.
2006 Aug 28
Carbohydrate-binding agents efficiently prevent dendritic cell-specific intercellular adhesion molecule-3-grabbing nonintegrin (DC-SIGN)-directed HIV-1 transmission to T lymphocytes.
2007 Jan
Microenvironmental considerations in the application of human mesenchymal stem cells in regenerative therapies.
2008 Dec
Plerixafor: in patients with non-Hodgkin's lymphoma or multiple myeloma.
2009
CXCR4 chemokine receptor antagonists: perspectives in SCLC.
2009 Apr
Tumor biology and cancer therapy - an evolving relationship.
2009 Aug 13
BIO5192, a small molecule inhibitor of VLA-4, mobilizes hematopoietic stem and progenitor cells.
2009 Aug 13
Successful stem cell remobilization using plerixafor (mozobil) plus granulocyte colony-stimulating factor in patients with non-hodgkin lymphoma: results from the plerixafor NHL phase 3 study rescue protocol.
2009 Dec
AMD3100 is a CXCR7 ligand with allosteric agonist properties.
2009 May
Mantle cell lymphoma cells express high levels of CXCR4, CXCR5, and VLA-4 (CD49d): importance for interactions with the stromal microenvironment and specific targeting.
2009 May 7
International myeloma working group (IMWG) consensus statement and guidelines regarding the current status of stem cell collection and high-dose therapy for multiple myeloma and the role of plerixafor (AMD 3100).
2009 Oct
Anticancer Role of PPARgamma Agonists in Hematological Malignancies Found in the Vasculature, Marrow, and Eyes.
2010
Binding of multivalent anionic porphyrins to V3 loop fragments of an HIV-1 envelope and their antiviral activity.
2010 Apr 1
Mobilization of peripheral blood stem cells for autologous transplant in non-Hodgkin's lymphoma and multiple myeloma patients by plerixafor and G-CSF and detection of tumor cell mobilization by PCR in multiple myeloma patients.
2010 Feb
Plerixafor for stem cell mobilization in patients with non-Hodgkin's lymphoma and multiple myeloma.
2010 Jan
Plerixafor given before the third leukapheresis to rescue an unsuccessful stem cell mobilization with CY and G-CSF.
2010 Jun
Patents

Patents

20040122064
4
20060100240
3
JP2002529502A
3

Sample Use Guides

In Vivo Use Guide
Begin treatment with plerixafor (Mozobil) after the patient has received G-CSF once daily for four days. The recommended dose of plerixafor by subcutaneous injection is based on body weight: 20 mg fixed dose or 0.24 mg/kg of body weight for patients weighing ≤83 kg; 0.24 mg/kg of body weight for patients weighing >83 kg. Administer by subcutaneous injection approximately 11 hours prior to initiation of apheresis.
Route of Administration: Other
In Vitro Use Guide
Human colorectal cancer cell line SW480 was treated with plerixafor at different final concentrations (10, 100, 1000 ng/ml) for 2h. Then, CXCL12 was added daily at 20 ng/mL. MTT assays were performed after 24, 48 and 72 h of plerixafor treatment. Cell viability was significantly suppressed by the drug in a dose-dependent manner. The drug (100 and 1000 ng/mL) significantly inhibited the invasion ability of SW480 cells.
Substance Class Chemical
Created
by admin
on Fri Dec 16 19:42:50 UTC 2022
Edited
by admin
on Fri Dec 16 19:42:50 UTC 2022
Record UNII
S915P5499N
Record Status Validated (UNII)
Record Version
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Name Type Language
PLERIXAFOR
DASH   EMA EPAR   INN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
PLERIXAFOR [ORANGE BOOK]
Common Name English
PLERIXAFOR [JAN]
Common Name English
PLERIXAFOR [EMA EPAR]
Common Name English
Plerixafor [WHO-DD]
Common Name English
PLERIXAFOR [USAN]
Common Name English
PLERIXAFOR [MART.]
Common Name English
plerixafor [INN]
Common Name English
PLERIXAFOR [VANDF]
Common Name English
PLERIXAFOR [MI]
Common Name English
1,1'-(1,4-PHENYLENEBIS(METHYLENE))BIS-1,4,8,11-TETRAAZACYCLOTETRADECANE
Systematic Name English
1,4,8,11-TETRAAZACYCLOTETRADECANE, 1,1'-(1,4-PHENYLENEBIS(METHYLENE))BIS-
Systematic Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 167903
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
FDA ORPHAN DRUG 346111
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
WHO-VATC QL03AX16
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
EMA ASSESSMENT REPORTS MOZOBIL (AUTHORIZED: HEMATOPOIETIC STEM CELL TRANSPLANTATION)
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
NDF-RT N0000178324
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
WHO-ATC L03AX16
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
EMA ASSESSMENT REPORTS MOZOBIL (AUTHORIZED: LYMPHOMA)
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
EMA ASSESSMENT REPORTS MOZOBIL (AUTHORIZED: MULTIPLE MYELOMA)
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
EU-Orphan Drug EU/3/11/931
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
NDF-RT N0000178326
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
NCI_THESAURUS C63817
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
Code System Code Type Description
EVMPD
SUB28849
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
IUPHAR
844
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
PUBCHEM
65015
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
EPA CompTox
DTXSID70869520
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
RXCUI
733003
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY RxNorm
DRUG CENTRAL
4410
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
ChEMBL
CHEMBL18442
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
CAS
110078-46-1
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
DRUG BANK
DB06809
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
NCI_THESAURUS
C1777
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
DAILYMED
S915P5499N
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
CHEBI
125354
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
INN
8513
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
FDA UNII
S915P5499N
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
USAN
PP-79
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
WIKIPEDIA
PLERIXAFOR
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY
MERCK INDEX
M8919
Created by admin on Fri Dec 16 19:42:50 UTC 2022 , Edited by admin on Fri Dec 16 19:42:50 UTC 2022
PRIMARY Merck Index
Related Record Type Details
Structure of PLERIXAFOR
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Structure of PLERIXAFOR OCTAHYDROCHLORIDE
SALT/SOLVATE -> PARENT
C-X-C CHEMOKINE RECEPTOR TYPE 4
TARGET -> INHIBITOR
Related Record Type Details
Structure of 1,8-BIS((4-(1,4,8,11-TETRAAZACYCLOTETRADEC-1-YLMETHYL)PHENYL)METHYL)-1,4,8,11-TETRAAZACYCLOTETRADECANE
IMPURITY -> PARENT
Structure of 1-((4-METHYLPHENYL)METHYL)-1,4,8,11-TETRAAZACYCLOTETRADECANE
IMPURITY -> PARENT
Structure of N-(4-HYDROXYMETHYLBENZYL) CYCLAM
IMPURITY -> PARENT
Related Record Type Details
Structure of PLERIXAFOR
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC SC DOSE

Volume of Distribution PHARMACOKINETIC
NIH
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