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
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
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 |
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
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P61073 Gene ID: 7852.0 Gene Symbol: CXCR4 Target Organism: Homo sapiens (Human) |
44.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | MOZOBIL Approved UseMozobil (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 Date2008 |
|||
Primary | MOZOBIL Approved UseMozobil (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 Date2008 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse 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: |
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: |
Disc. AE: Premature ventricular contractions... AEs leading to discontinuation/dose reduction: Premature ventricular contractions (1 patient) Sources: |
20 ug/kg/h multiple, intravenous Dose: 20 ug/kg/h Route: intravenous Route: multiple Dose: 20 ug/kg/h Sources: |
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: |
Disc. AE: Hepatic enzyme increased, Orthostatic hypotension... AEs leading to discontinuation/dose reduction: Hepatic enzyme increased (1 patient) Sources: Orthostatic hypotension (1 patient) |
40 ug/kg/h multiple, intravenous Dose: 40 ug/kg/h Route: intravenous Route: multiple Dose: 40 ug/kg/h Sources: |
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: |
Disc. AE: Ventricular ectopics... AEs leading to discontinuation/dose reduction: Ventricular ectopics (1 patient) Sources: |
5 ug/kg/h multiple, intravenous Dose: 5 ug/kg/h Route: intravenous Route: multiple Dose: 5 ug/kg/h Sources: |
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: |
Disc. AE: Thrombocytopenia... AEs leading to discontinuation/dose reduction: Thrombocytopenia (serious, 1 patient) Sources: |
80 ug/kg/h multiple, intravenous Dose: 80 ug/kg/h Route: intravenous Route: multiple Dose: 80 ug/kg/h Sources: |
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: |
Disc. AE: Paresthesia... AEs leading to discontinuation/dose reduction: Paresthesia (1 patient) Sources: |
160 ug/kg single, oral Dose: 160 ug/kg Route: oral Route: single Dose: 160 ug/kg Sources: |
healthy, >18 years n = 3 Health Status: healthy Age Group: >18 years Sex: M+F Population Size: 3 Sources: |
|
80 ug/kg single, intravenous Dose: 80 ug/kg Route: intravenous Route: single Dose: 80 ug/kg Sources: |
healthy, >18 years n = 12 Health Status: healthy Age Group: >18 years Sex: M+F Population Size: 12 Sources: |
Other AEs: Diaphoresis... |
320 ug/kg single, subcutaneous Highest studied dose Dose: 320 ug/kg Route: subcutaneous Route: single Dose: 320 ug/kg Sources: Page: p. 83 |
healthy, adult n = 10 Health Status: healthy Age Group: adult Population Size: 10 Sources: Page: p. 83 |
Other AEs: Injection site erythema, Paresthesia... Other AEs: Injection site erythema Sources: Page: p. 83Paresthesia Chest discomfort |
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: Page: p.97 |
unhealthy, adult n = 72 Health Status: unhealthy Age Group: adult Population Size: 72 Sources: Page: p.97 |
Disc. AE: Anxiety, Arrhythmia... AEs leading to discontinuation/dose reduction: Anxiety (1 patient) Sources: Page: p.97Arrhythmia (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) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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: |
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: |
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: |
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: |
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: |
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: |
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: |
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: |
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: |
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: |
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: |
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: |
Diaphoresis | 1 patient | 80 ug/kg single, intravenous Dose: 80 ug/kg Route: intravenous Route: single Dose: 80 ug/kg Sources: |
healthy, >18 years n = 12 Health Status: healthy Age Group: >18 years Sex: M+F Population Size: 12 Sources: |
Chest discomfort | 320 ug/kg single, subcutaneous Highest studied dose Dose: 320 ug/kg Route: subcutaneous Route: single Dose: 320 ug/kg Sources: Page: p. 83 |
healthy, adult n = 10 Health Status: healthy Age Group: adult Population Size: 10 Sources: 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: Page: p. 83 |
healthy, adult n = 10 Health Status: healthy Age Group: adult Population Size: 10 Sources: 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: Page: p. 83 |
healthy, adult n = 10 Health Status: healthy Age Group: adult Population Size: 10 Sources: 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: Page: p.97 |
unhealthy, adult n = 72 Health Status: unhealthy Age Group: adult Population Size: 72 Sources: 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: Page: p.97 |
unhealthy, adult n = 72 Health Status: unhealthy Age Group: adult Population Size: 72 Sources: 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: Page: p.97 |
unhealthy, adult n = 72 Health Status: unhealthy Age Group: adult Population Size: 72 Sources: 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: Page: p.97 |
unhealthy, adult n = 72 Health Status: unhealthy Age Group: adult Population Size: 72 Sources: 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: Page: p.97 |
unhealthy, adult n = 72 Health Status: unhealthy Age Group: adult Population Size: 72 Sources: 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: Page: p.97 |
unhealthy, adult n = 72 Health Status: unhealthy Age Group: adult Population Size: 72 Sources: 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: Page: p.97 |
unhealthy, adult n = 72 Health Status: unhealthy Age Group: adult Population Size: 72 Sources: 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: Page: p.97 |
unhealthy, adult n = 72 Health Status: unhealthy Age Group: adult Population Size: 72 Sources: 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: Page: p.97 |
unhealthy, adult n = 72 Health Status: unhealthy Age Group: adult Population Size: 72 Sources: 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: Page: p.97 |
unhealthy, adult n = 72 Health Status: unhealthy Age Group: adult Population Size: 72 Sources: 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: Page: p.97 |
unhealthy, adult n = 72 Health Status: unhealthy Age Group: adult Population Size: 72 Sources: 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: Page: p.97 |
unhealthy, adult n = 72 Health Status: unhealthy Age Group: adult Population Size: 72 Sources: Page: p.97 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 60, 104 |
inconclusive | |||
Page: 58, 104 |
inconclusive | |||
Page: 9, 42, 80 |
no [IC50 >100 uM] | |||
Page: 9, 42, 80 |
no [IC50 >100 uM] | |||
Page: 9, 42, 80 |
no [IC50 >100 uM] | |||
Page: 9, 42, 80 |
no [IC50 >100 uM] | |||
Page: 55.0 |
no [IC50 >100 uM] | |||
Page: 9, 42, 80 |
no [IC50 >100 uM] | |||
Page: 55.0 |
no [IC50 >100 uM] | |||
Page: 80.0 |
no | |||
Page: 11.0 |
no | |||
Page: 59.0 |
no | |||
Page: 11.0 |
no | |||
Page: 80.0 |
no | |||
Page: 11.0 |
no | |||
Page: 80.0 |
no | |||
Page: 80.0 |
no | |||
Page: 80.0 |
no |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 58, 104 |
inconclusive | |||
Page: 15, 102 |
no |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 17, 34, 40 |
PubMed
Title | Date | PubMed |
---|---|---|
Microenvironmental considerations in the application of human mesenchymal stem cells in regenerative therapies. | 2008 Dec |
|
A phase II study of plerixafor (AMD3100) plus G-CSF for autologous hematopoietic progenitor cell mobilization in patients with Hodgkin lymphoma. | 2008 Nov |
|
A novel CXCR4 antagonist for hematopoietic stem cell mobilization. | 2008 Nov |
|
Plerixafor, a CXCR4 antagonist for the mobilization of hematopoietic stem cells. | 2008 Nov |
|
Impact of mobilization and remobilization strategies on achieving sufficient stem cell yields for autologous transplantation. | 2008 Sep |
|
Targeted antagonism of CXCR4 mobilizes progenitor cells under investigation for cardiovascular disease. | 2009 |
|
A combination of granulocyte-colony-stimulating factor (G-CSF) and plerixafor mobilizes more primitive peripheral blood progenitor cells than G-CSF alone: results of a European phase II study. | 2009 |
|
CXCR4 and mobilization of hematopoietic precursors. | 2009 |
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Plerixafor: in patients with non-Hodgkin's lymphoma or multiple myeloma. | 2009 |
|
CXCR4 chemokine receptor antagonists: perspectives in SCLC. | 2009 Apr |
|
Bis-14-membered ring diketal diamines: synthesis and evaluation of their anti-HIV and anti-tumoral activities. | 2009 Aug |
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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 |
|
Plerixafor. | 2009 Feb |
|
Treatment with plerixafor in non-Hodgkin's lymphoma and multiple myeloma patients to increase the number of peripheral blood stem cells when given a mobilizing regimen of G-CSF: implications for the heavily pretreated patient. | 2009 Feb |
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Pharmacokinetics and pharmacodynamics of plerixafor in patients with non-Hodgkin lymphoma and multiple myeloma. | 2009 Jan |
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CXCR4 antagonists: targeting the microenvironment in leukemia and other cancers. | 2009 Jan |
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Plerixafor approved for autologous hematopoietic stem-cell transplantation. | 2009 Jan 15 |
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Plerixafor hydrochloride: a novel agent for the mobilization of peripheral blood stem cells. | 2009 Jul |
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Rescue from failed growth factor and/or chemotherapy HSC mobilization with G-CSF and plerixafor (AMD3100): an institutional experience. | 2009 Jun |
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Plerixafor and G-CSF versus placebo and G-CSF to mobilize hematopoietic stem cells for autologous stem cell transplantation in patients with multiple myeloma. | 2009 Jun 4 |
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AMD3100 is a CXCR7 ligand with allosteric agonist properties. | 2009 May |
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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 |
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[Stem cell harvesting after plerixafor treatment]. | 2009 Nov 16 |
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[Mobilisation of haematopoietic stem cells with plerixafor--secondary publication]. | 2009 Nov 2 |
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Plerixafor inhibits chemotaxis toward SDF-1 and CXCR4-mediated stroma contact in a dose-dependent manner resulting in increased susceptibility of BCR-ABL+ cell to Imatinib and Nilotinib. | 2009 Oct |
|
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 |
|
Phase III prospective randomized double-blind placebo-controlled trial of plerixafor plus granulocyte colony-stimulating factor compared with placebo plus granulocyte colony-stimulating factor for autologous stem-cell mobilization and transplantation for patients with non-Hodgkin's lymphoma. | 2009 Oct 1 |
|
Advances in mobilization for the optimization of autologous stem cell transplantation. | 2009 Sep |
|
Plerixafor (AMD3100) and granulocyte colony-stimulating factor (G-CSF) mobilize different CD34+ cell populations based on global gene and microRNA expression signatures. | 2009 Sep 17 |
|
CXCR4 in clinical hematology. | 2010 |
|
Anticancer Role of PPARgamma Agonists in Hematological Malignancies Found in the Vasculature, Marrow, and Eyes. | 2010 |
|
Molecular Medicine - CHI's 17th International Tri-Conference: Mastering Medicinal Chemistry - CHI's Seventh Annual Conference. | 2010 Apr |
|
Binding of multivalent anionic porphyrins to V3 loop fragments of an HIV-1 envelope and their antiviral activity. | 2010 Apr 1 |
|
Plerixafor (Mozobil). | 2010 Apr 5 |
|
Plerixafor and pegylated filgrastim: a case of safe and effective hematopoietic stem cell mobilization. | 2010 Aug |
|
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 |
|
Synthesis and structure-activity relationships of azamacrocyclic C-X-C chemokine receptor 4 antagonists: analogues containing a single azamacrocyclic ring are potent inhibitors of T-cell tropic (X4) HIV-1 replication. | 2010 Feb 11 |
|
Plerixafor for stem cell mobilization in patients with non-Hodgkin's lymphoma and multiple myeloma. | 2010 Jan |
|
Peripheral blood stem cell mobilization tactics. | 2010 Jan |
|
A pharmacokinetic study of plerixafor in subjects with varying degrees of renal impairment. | 2010 Jan |
|
Safety and efficacy assessment of plerixafor in patients with multiple myeloma proven or predicted to be poor mobilizers, including assessment of tumor cell mobilization. | 2010 Jan |
|
Safety and preliminary efficacy of plerixafor (Mozobil) in combination with chemotherapy and G-CSF: an open-label, multicenter, exploratory trial in patients with multiple myeloma and non-Hodgkin's lymphoma undergoing stem cell mobilization. | 2010 Jan |
|
A low-molecular-weight entry inhibitor of both CCR5- and CXCR4-tropic strains of human immunodeficiency virus type 1 targets a novel site on gp41. | 2010 Jul |
|
Plerixafor given before the third leukapheresis to rescue an unsuccessful stem cell mobilization with CY and G-CSF. | 2010 Jun |
|
Expression and function of CXCL12/CXCR4 in rat urinary bladder with cyclophosphamide-induced cystitis. | 2010 Mar |
|
Plerixafor: a peripheral blood stem cell mobilizer. | 2010 May |
|
Plerixafor (Mozobil) alone to mobilize hematopoietic stem cells from multiple myeloma patients for autologous transplantation. | 2010 May |
|
Molecular imaging of CXCR4 receptor expression in human cancer xenografts with [64Cu]AMD3100 positron emission tomography. | 2010 May 15 |
Patents
Sample Use Guides
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18416455
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
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Fri Dec 15 16:15:52 GMT 2023
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admin
on
Fri Dec 15 16:15:52 GMT 2023
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Record UNII |
S915P5499N
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
167903
Created by
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FDA ORPHAN DRUG |
346111
Created by
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WHO-VATC |
QL03AX16
Created by
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EMA ASSESSMENT REPORTS |
MOZOBIL (AUTHORIZED: HEMATOPOIETIC STEM CELL TRANSPLANTATION)
Created by
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NDF-RT |
N0000178324
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WHO-ATC |
L03AX16
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EMA ASSESSMENT REPORTS |
MOZOBIL (AUTHORIZED: LYMPHOMA)
Created by
admin on Fri Dec 15 16:15:52 GMT 2023 , Edited by admin on Fri Dec 15 16:15:52 GMT 2023
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EMA ASSESSMENT REPORTS |
MOZOBIL (AUTHORIZED: MULTIPLE MYELOMA)
Created by
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EU-Orphan Drug |
EU/3/11/931
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NDF-RT |
N0000178326
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NCI_THESAURUS |
C63817
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SUB28849
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844
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65015
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DTXSID70869520
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733003
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4410
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CHEMBL18442
Created by
admin on Fri Dec 15 16:15:52 GMT 2023 , Edited by admin on Fri Dec 15 16:15:52 GMT 2023
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110078-46-1
Created by
admin on Fri Dec 15 16:15:52 GMT 2023 , Edited by admin on Fri Dec 15 16:15:52 GMT 2023
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DB06809
Created by
admin on Fri Dec 15 16:15:52 GMT 2023 , Edited by admin on Fri Dec 15 16:15:52 GMT 2023
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C1777
Created by
admin on Fri Dec 15 16:15:52 GMT 2023 , Edited by admin on Fri Dec 15 16:15:52 GMT 2023
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S915P5499N
Created by
admin on Fri Dec 15 16:15:52 GMT 2023 , Edited by admin on Fri Dec 15 16:15:52 GMT 2023
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125354
Created by
admin on Fri Dec 15 16:15:52 GMT 2023 , Edited by admin on Fri Dec 15 16:15:52 GMT 2023
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100000092971
Created by
admin on Fri Dec 15 16:15:52 GMT 2023 , Edited by admin on Fri Dec 15 16:15:52 GMT 2023
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8513
Created by
admin on Fri Dec 15 16:15:52 GMT 2023 , Edited by admin on Fri Dec 15 16:15:52 GMT 2023
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S915P5499N
Created by
admin on Fri Dec 15 16:15:52 GMT 2023 , Edited by admin on Fri Dec 15 16:15:52 GMT 2023
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PP-79
Created by
admin on Fri Dec 15 16:15:52 GMT 2023 , Edited by admin on Fri Dec 15 16:15:52 GMT 2023
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PLERIXAFOR
Created by
admin on Fri Dec 15 16:15:52 GMT 2023 , Edited by admin on Fri Dec 15 16:15:52 GMT 2023
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m8919
Created by
admin on Fri Dec 15 16:15:52 GMT 2023 , Edited by admin on Fri Dec 15 16:15:52 GMT 2023
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PRIMARY | Merck Index |
Related Record | Type | Details | ||
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EXCRETED UNCHANGED |
AMOUNT EXCRETED
URINE
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BINDER->LIGAND |
BINDING
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SALT/SOLVATE -> PARENT | |||
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TARGET -> INHIBITOR |
Related Record | Type | Details | ||
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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SC DOSE |
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Volume of Distribution | PHARMACOKINETIC |
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