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
Plerixafor
Plerixafor

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

Moderate: leukocytosis, renal impairment, thrombocytopenia

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

*** Taking medicines without doctor's advice can cause long-term problems.
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