Plerixafor (plerixafor)

CXCR4 Chemokine Receptor Antagonists Subcutaneous Vial (Ml)

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Plerixafor, a CXCR4 chemokine-receptor antagonist, is a hematopoietic stem cell mobilizer.

Plerixafor, a CXCR4 chemokine-receptor antagonist, prevents the binding of stromal cell-derived factor-1alpha (SDF-1alpha) to the CXCR4 chemokine receptor. CXCR4 and SDF-1alpha together play a role in the trafficking of hematopoietic stem cells, specifically to promote their homing to and retention within the bone marrow. By disrupting the interaction between SDF-1alpha and its receptor, plerixafor interferes with the retention of hematopoietic stem cells in the bone marrow matrix.

Subsequently, increased numbers of CD34+ hematopoietic progenitor cells are mobilized or released from the bone marrow, resulting in peripheral leukocytosis. Mobilized CD34+ cells are then collected by apheresis and used as a stem-cell infusion to promote engraftment following high-dose chemotherapy associated with autologous stem-cell transplantation.

In a study in healthy individuals, plerixafor did not prolong QT-interval or corrected QT-interval, Bazett's formula (QTc), at single doses up to 0.4 mg/kg (producing peak concentrations approximately 1.8-fold higher than those produced by the usual dose of 0.24 mg/kg).

USES: Plerixafor is used by patients with certain types of cancer (non-Hodgkin's lymphoma-NHL, multiple myeloma-MM) to prepare them for stem cell transplant. Stem cells, which are found mainly in the bone marrow, turn into red blood cells, white blood cells, and platelets. Plerixafor is used to help stem cells move from the bone marrow to the bloodstream so that the cells can be collected and stored.

The stem cells are then infused back into the patient after chemotherapy or radiation.

Generic name: plerixafor
Pronunciation: (pler-IX-a-for)
Drug class: CXCR4 Chemokine Receptor Antagonists
Therapeutic class: Hematological Agents

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

The following indications are listed for Plerixafor:

  • Peripheral Mobilization Of Hematopoietic Stem Cells

Dosing

The recommended adult dosage of plerixafor is 0.24 mg/kg (based on actual body weight) daily for up to 4 consecutive days. Plerixafor is given concomitantly with filgrastim as part of the hematopoietic stem cell mobilization regimen. Treatment with plerixafor should only begin after the patient has received the initial 4 doses of filgrastim. Plerixafor should be administered in the evening, approximately 11 hours prior to a scheduled apheresis session; the filgrastim dose should be administered in the morning prior to apheresis.

Dosage may be increased according to changes in weight, but the maximum dosage should not exceed 40 mg once daily.

Drug interactions

In vitro studies indicate that plerixafor is not a substrate, inhibitor, or inducer of cytochrome P-450 (CYP) isoenzymes. Therefore, interactions with plerixafor and other drugs involving CYP isoenzymes are unlikely.

At in vitro concentrations similar to those achieved clinically, plerixafor did not act as a substrate or inhibitor of P-glycoprotein.

Because plerixafor is excreted principally by the kidneys, concurrent administration of drugs that reduce renal function or compete for active tubular secretion may potentially increase concentrations of plerixafor or the coadministered drug. The effects of coadministration of plerixafor with drugs that are excreted by the kidneys or known to affect renal function have not been established.

Contraindications

The manufacturer states there are no contraindications to the use of plerixafor.

Adverse reactions

The most common adverse events (occurring in at least 5% of patients in controlled clinical trials) reported with the combination of plerixafor and filgrastim included diarrhea, nausea, injection site reactions, fatigue, headache, arthralgia, dizziness, vomiting, flatulence, and insomnia.

Precautions

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ICD codes

CodeTypeDescription
Peripheral mobilization of hematopoietic stem cells
6A550ZVICD10PCSPheresis of hematopoietic stem cells, single
6A551ZVICD10PCSPheresis of hematopoietic stem cells, multiple
Z52.011ICD10CMAutologous donor, stem cells

ICD code information from First Databank (FDB).

Formulary status

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Last reviewed · Source: First Databank (FDB) drug data