Plerixafor
Plerixafor Uses, Dosage, Side Effects, Food Interaction and all others data.
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 for the purpose of stimulating the immune system. 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.
Plerixafor is a bicyclam derivative that antagonizes CXCR4 by binding to three acidic residues in the ligand-binding pocket: Asp171, Asp262, and Glu288. Blood levels of CD34+ cells peaked at 9 hours after administration of 0.24 mg/kg plerixafor in healthy subjects. In patients that have non-Hodgkin’s lymphoma or multiple myeloma, blood levels of CD34+ peaked at 6 hours. In combination with a G-CSF, circulating CD34+ cells in the peripheral blood peaked at 9-14 hours.
| Trade Name | Plerixafor |
| Availability | Prescription only |
| Generic | Plerixafor |
| Plerixafor Other Names | Plerixafor |
| Related Drugs | methotrexate, rituximab, Rituxan, Revlimid, cyclophosphamide, vincristine, Imbruvica, Velcade, Darzalex, Pomalyst |
| Weight | 20mg/ml, |
| Type | Subcutaneous Solution, Subcutaneous |
| Formula | C28H54N8 |
| Weight | Average: 502.782 Monoisotopic: 502.447143768 |
| Protein binding | 58% |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Plerixafor is a selective chemokine receptor (CXCR4) antagonist used with filgrastim to mobilize hematopoietic stem cells to the peripheral blood for collection and autologous transplantation in patients with non-Hodgkin’s lymphoma (NHL) and multiple myeloma (MM).
Used in combination with granulocyte-colony stimulating factor (G-CSF, filgrastim) 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).
Plerixafor is also used to associated treatment for these conditions: Mobilization of hematopoietic stem cells
How Plerixafor works
Plerixafor inhibits the CXCR4 chemokine receptors on CD34+ cells and reversibly blocks binding of the ligand, stromal cell-derived factor-1-alpha (SDF-1α). By blocking the interaction between SDF-1α and CXCR4 with plerixafor, mobilization of progenitor cells is triggered. Filgrastim, a granulocyte-colony stimulating factor, is added to enhance CD34+ cell mobilization, thus increasing the yield of stem cells- an important determinant of graft adequacy.
Toxicity
LD50, mouse, SC: 16.3 mg/kg; LD50, rat, SC: >50 mg/kg; LD50, mouse and rat, IV injection: 5.2 mg/kg
Food Interaction
No interactions found.Plerixafor Disease Interaction
Volume of Distribution
0.3 L/kg
Elimination Route
Pharmacokinetic profile follows a two-compartment model with first-order absorption. A median peak plasma concentration of 0.24 mg/kg of plerixafor occurred 30-60 minutes after subcutaneous dose.
Half Life
Terminal elimination half-life, NHL patients: 4.4 hours; Terminal elimination half-life, MM patients: 5.6 hours; Terminal elimination half-life, Hodgkin's lymphoma patients: 3.5 hours; Distribution half-life: 0.3 hours
Clearance
Total plasma clearance: 4.38 L/h; Renal clearance: 3.15 L/h
Elimination Route
0.24 mg/kg, healthy subjects: ~70% of the parent drug is excreted in urine in the first 24 hours.
Innovators Monograph
You find simplified version here Plerixafor
