Class: Stem cell mobilizer
- Injection, solution 20 mg/mL
Inhibits the CXCR4 chemokine receptor and blocks binding to the marrow compartment of its cognate ligand, stromal cell–derived factor-1 alpha, which play a role in the trafficking and homing of human hematopoietic stem cells (HSC).
Following subcutaneous administration, T max is 30 to 60 min.
Up to 58% bound to human plasma protein. Vd is 0.3 L/kg, primarily in the extravascular fluid space.
Not metabolized and does not inhibit major CYP metabolizing enzymes.
Approximately 70% excreted in urine during first 24 h. Terminal half-life in plasma ranges between 3 and 5 h.
Special PopulationsRenal Function Impairment
Cl is reduced in patients with renal impairment.
Indications and Usage
In combination with granulocyte-colony stimulating factor (G-CSF) to mobilize HSC to the peripheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin lymphoma and multiple myeloma.
Dosage and AdministrationAdults
Subcutaneous 0.24 mg/kg once daily (max, 40 mg/day) after the patient has received G-CSF once daily for 4 days. Administer plerixafor approximately 11 h prior to initiation of apheresis for up to 4 consecutive days. The recommended dose of G-CSF is 10 mcg/kg daily in the morning for 4 days prior to the first evening dose of plerixafor and each day prior to apheresis.Renal Impairment
Subcutaneous CrCl 50 mL/min or less: Administer 0.16 mg/kg once daily (max, 27 mg/day).
- Use the patient's actual body weight to calculate the volume of drug to be administered.
Store at 59° to 86°F. Discard any unused drug remaining after injection.
Drug InteractionsDrugs that reduce renal function or compete for active tubular secretion
Plerixafor plasma concentrations may be elevated; however, this possible interaction has not been evaluated.
Laboratory Test Interactions
None well documented.
Fatigue (27%); headache (22%); dizziness (11%); insomnia (7%); malaise (less than 5%); paresthesia.
Excessive sweating (less than 5%).
Diarrhea (37%); nausea (34%); vomiting (10%); flatulence (7%); abdominal distention, abdominal pain, constipation, dry mouth, dyspepsia, oral hypoesthesia, stomach discomfort (less than 5%).
Injection-site reactions (erythema, pruritus, rash, urticaria), induration, inflammation, irritation, pain, swelling (34%).
Arthralgia (13%); musculoskeletal pain (less than 5%).
Monitor WBC counts. Monitor platelet counts in patients who receive plerixafor and then undergo apheresis.
Category D .
Safety and efficacy not established.
No difference in safety and efficacy has been observed in elderly individuals compared with younger subjects.
Reduce dose in patients with moderate and severe renal impairment.
Coadministration with G-CSF increases circulating leukocytes as well as HSC populations.
Splenic enlargement and rupture
Evaluate patients who receive plerixafor in combination with G-CSF and who report left upper abdominal pain and/or scapular or shoulder pain for splenic enlargement.
Has been reported.
Tumor cell mobilization
For the purpose of HSC mobilization, plerixafor may cause mobilization of leukemic cells and subsequent contamination of the apheresis product. When used in combination with G-CSF for HSC mobilization, tumor cells may be released from the marrow and subsequently collected in the leukapharesis product.
GI disorders, orthostatic hypotension, syncope, vasovagal reaction.
- Advise patients to contact health care provider immediately if symptoms of vasovagal reactions (eg, orthostatic hypotension, syncope) occur shortly after injection.
- Advise patients to notify health care provider if they experience itching, rash, or a reaction at the site of injection.
- Advise women with reproductive potential to use effective contraceptive methods.
- Advise patients to inform health care provider if GI disorders (eg, diarrhea, nausea, vomiting, flatulence, abdominal pain) occur or persist.
Copyright © 2009 Wolters Kluwer Health.