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Plerixafor

Pronunciation: (pler-IX-a-fore)
Class: Stem cell mobilizer

Trade Names:
Mozobil
- Injection, solution 20 mg/mL

Pharmacology

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).

Pharmacokinetics

Absorption

Following subcutaneous administration, T _max is 30 to 60 min.

Distribution

Up to 58% bound to human plasma protein. Vd is 0.3 L/kg, primarily in the extravascular fluid space.

Metabolism

Not metabolized and does not inhibit major CYP metabolizing enzymes.

Elimination

Approximately 70% excreted in urine during first 24 h. Terminal half-life in plasma ranges between 3 and 5 h.

Special Populations

Renal 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.

Contraindications

Standard considerations.

Dosage and Administration

Adults

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
Adults

Subcutaneous CrCl 50 mL/min or less: Administer 0.16 mg/kg once daily (max, 27 mg/day).

General Advice

Use the patient's actual body weight to calculate the volume of drug to be administered.

Storage/Stability

Store at 59° to 86°F. Discard any unused drug remaining after injection.

Drug Interactions

Drugs 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.

Adverse Reactions

CNS

Fatigue (27%); headache (22%); dizziness (11%); insomnia (7%); malaise (less than 5%); paresthesia.

Dermatologic

Excessive sweating (less than 5%).

GI

Diarrhea (37%); nausea (34%); vomiting (10%); flatulence (7%); abdominal distention, abdominal pain, constipation, dry mouth, dyspepsia, oral hypoesthesia, stomach discomfort (less than 5%).

Hematologic-Lymphatic

Hematoma, hemorrhage.

Local

Injection-site reactions (erythema, pruritus, rash, urticaria), induration, inflammation, irritation, pain, swelling (34%).

Musculoskeletal

Arthralgia (13%); musculoskeletal pain (less than 5%).

Precautions

Monitor

Monitor WBC counts. Monitor platelet counts in patients who receive plerixafor and then undergo apheresis.

Pregnancy

Category D .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

No difference in safety and efficacy has been observed in elderly individuals compared with younger subjects.

Renal Function

Reduce dose in patients with moderate and severe renal impairment.

Leukocytosis

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.

Thrombocytopenia

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.

Overdosage

Symptoms

GI disorders, orthostatic hypotension, syncope, vasovagal reaction.

Patient Information

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.