Plerixafor is a hematopoietic stem cell mobilizer. It is used to stimulate the release of stem cells from the bone marrow into the blood in patients with non-Hodgkin lymphoma and multiple myeloma. These stem cells are then collected and used in autologous stem cell transplantation to replace blood-forming cells that were destroyed by chemotherapy. Plerixafor has orphan drug status in the United States and European Union; it was approved by the U.S. Food and Drug Administration on December 15, 2008. |
Brands | Mozobil
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Synonyms | AMD3100
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indication
Used in combination with granulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the peripheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin’s lymphoma (NHL) and multiple myeloma (MM).
pharmacology
Plerixafor increases circulating CD34+ cells in the peripheral blood, with a peak effect about 6-9 hours.
mechanism of action
Plerixafor inhibits the CXCR4 chemokine receptor and blocks binding to the marrow compartment of its cognate ligand, SDF-1alpha, which play a role in the trafficking and homing of human hematopoietic stem cells.
absorption
Plerixafor is rapidly absorbed after subcutaneous injection (Tmax = 30-60 min).
half life
Terminal half-life ranges from 3 to 5 hours.
route of elimination
Approximately 70% of the parent drug is excreted in urine during first 24 h.