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Plerixafor

Blocks CXCR4, a chemokine receptor, which acts as a co-receptor for certain strains of HIV.

Blocks binding CXRCR4 cognate ligand SDF-alpha.

A small molecule inhibitor of CXC chemokine receptor for axis.

Peripheral blood stem cell mobilization, which is important as a source of hematopoietic stem cells for transplantation, is generally performed using granulocyte colony-stimulating factor (G-CSF), but is ineffective in around 15 to 20% of patients.

Plerixafor is a drug that directly blocks the CXCR4 receptor. 

Plerixafor is a very efficient inducer of hematopoietic stem cell mobilization.

Indicated in combination with granulocyte colony-stimulating factor to mobilize hematopoietic stem cells to the peripheral blood flow collection and subsequent autologous hematopoietic stem cell transplantation.

Parenterally administered small molecule competitive antagonist of CXCR4 with a half-life of approximately five hours.

It increases circulating levels of mature and immature leukocytes and is approved in combination with G-CSF for hematopoetic stem cell mobilization for transplantation in patients with hematologic malignancies.

Combination of G-CSF with plerixafor increases the percentage of persons that respond to the therapy and produce enough stem cells for transplantation.

Results in a modest reduction of bone marrow failure engraftment rates when combined with G CSF in patients with myeloma and lymphoma.

The drug is approved for patients with lymphoma and multiple myeloma.

Administered 11 hours prior to initiation of apheresis.

A single dose of 240 mcg/kg mobilizes most stem cells.

Mobilizes a similar number of CD34+ cells as G-CSF.

When added to G-CSF stem cell augmentation occurs.

Recommended dose 0.24 mg per kilogram, not to exceed 40 mg per day, and repeat doses up to 4 consecutive days.

Doses are modified by one third for moderate to severe renal impairment.

May mobilize leukemic cells and is not indicated for patients with leukemia.

It may increase circulating leukocytes, and may release tumor cells from the bone marrow.

May be associated with thrombocytopenia.

Most frequent adverse reactions include diarrhea, nausea, fatigue, headache, arthralgias, dizziness, vomiting, and injection site reactions.

The pre-emptive administration of stem cell mobilization agent plerixafor enhanced collection efficiency and resulted in more than $10,000 in cost savings compared with standard administration, according to the results of a recent study published in Leukemia Research.

The benefits of using plerixafor as a stem cell mobilization regimen may be further enhanced by a pre-emptive schedule where plerixafor administration is initiated on the evening prior to the first day of stem cell collection.

Preemptive plerixafor resulted in significant improvements in stem cell collection compared with standard plerixafor.

The median CD34+ cell count in peripheral blood for preemtive plerixafor was 21 compared with 8 for standard plerixafor.

Median total CD34+ cell count collected on the first day was 6.75 X 106 for preemptive plerixafor compared with 1.96 X 106 in patients receiving standard plerixafor.

Pre-emptive plerixafor administration in myeloma patients undergoing ASCT may improve clinical and economic outcomes.

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