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Plerixafor

Medically reviewed by Drugs.com. Last updated on Jul 27, 2019.

Pronunciation

(pler IX a fore)

Index Terms

  • AMD3100
  • LM3100

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Subcutaneous [preservative free]:

Mozobil: 24 mg/1.2 mL (1.2 mL)

Brand Names: U.S.

  • Mozobil

Pharmacologic Category

  • Hematopoietic Agent
  • Hematopoietic Stem Cell Mobilizer

Pharmacology

Plerixafor reversibly inhibits binding of stromal cell-derived factor-1-alpha (SDF-1α), expressed on bone marrow stromal cells, to the CXC chemokine receptor 4 (CXCR4), resulting in mobilization of hematopoietic stem and progenitor cells from bone marrow into peripheral blood. Plerixafor used in combination with filgrastim results in synergistic increase in CD34+ cell mobilization. Mobilized CD34+ cells are capable of engrafting with extended repopulating capacity.

Absorption

SubQ: Rapid; exposure using the mg/kg dosing increases with increasing body weight; the fixed dosing (20 mg) results in higher exposure than the mg/kg dose, but the median time to reach the target cell count is the same for both dosing regimens

Distribution

0.3 L/kg; primarily to extravascular fluid space

Metabolism

Not metabolized

Excretion

Urine (~70%; as parent drug)

Onset of Action

Peak CD34+ mobilization (healthy volunteers): Plerixafor monotherapy: 6 to 9 hours after administration; Plerixafor + filgrastim: 10 to14 hours

Time to Peak

Plasma: SubQ: 30 to 60 minutes

Duration of Action

Sustained elevation in CD34+ cells (healthy volunteers): 4 to 18 hours after administration

Half-Life Elimination

Terminal: 3 to 5 hours

Protein Binding

≤58%

Special Populations: Renal Function Impairment

Clearance is reduced in patients with renal impairment. When compared to patients with normal renal function, the mean AUC was increased 7% in patients with mild renal impairment (CrCl 51 to 80 mL/minute), 32% for moderate renal impairment (CrCl 31 to 50 mL/minute), and 39% with severe renal impairment (CrCl <31 mL/minute).

Use: Labeled Indications

Peripheral stem cell mobilization: Mobilization of hematopoietic stem cells (HSCs) for collection and subsequent autologous transplantation (in combination with filgrastim) in patients with non-Hodgkin lymphoma (NHL) and multiple myeloma (MM)

Contraindications

History of hypersensitivity to plerixafor or any component of the formulation (anaphylactic shock has occurred).

Dosing: Adult

Note: Dosing is based on actual body weight. Begin plerixafor after patient has received filgrastim for 4 days (refer to Filgrastim monograph for filgrastim dose); plerixafor, filgrastim, and apheresis should be continued daily until sufficient cell collection up to a maximum of 4 days.

Hematopoietic stem cell mobilization (in non-Hodgkin lymphoma and multiple myeloma): SubQ: Administer ~11 hours prior to apheresis

Patients ≤83 kg: 20 mg fixed dose or 0.24 mg/kg once daily for up to 4 consecutive days

Patients >83 kg: 0.24 mg/kg once daily for up to 4 consecutive days; maximum dose: 40 mg daily

Dosing: Geriatric

Refer to adult dosing.

Dosing: Obesity

The manufacturer recommends calculating the dose based on actual weight for patients weighing up to 175% of ideal body weight (maximum dose: 40 mg daily). Dosing in patients >175% of ideal body weight has not been studied.

Administration

SubQ: Administer subcutaneously, ~11 hours prior to initiation of apheresis. In some clinical trials, plerixafor administration began in the evening prior to apheresis; filgrastim was begun on day 1, plerixafor initiated in the evening on day 4 and apheresis in the morning on day 5; with filgrastim, plerixafor, and apheresis then continued daily until sufficient cell collection for autologous transplant (DiPersio 2009a; DiPersio 2009b).

Storage

Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Drug Interactions

There are no known significant interactions.

Adverse Reactions

Adverse reactions reported with filgrastim combination therapy.

>10%:

Central nervous system: Fatigue (27%), headache (22%), dizziness (11%)

Gastrointestinal: Diarrhea (37%), nausea (34%)

Local: Injection site reaction (34%, including edema, erythema, hematoma, hemorrhage, induration, inflammation, irritation, pain, paresthesia, pruritus, skin rash, urticaria)

Neuromuscular & skeletal: Arthralgia (13%)

1% to 10%:

Central nervous system: Insomnia (7%), malaise (<5%)

Dermatologic: Erythema (<5%), hyperhidrosis (<5%)

Gastrointestinal: Vomiting (10%), flatulence (7%), abdominal distension (<5%), abdominal distress (<5%), abdominal pain (<5%), constipation (<5%), dyspepsia (<5%), oral hypoesthesia (<5%), xerostomia (<5%)

Hematologic & oncologic: Hyperleukocytosis (7%)

Neuromuscular & skeletal: Musculoskeletal pain (<5%)

<1%, postmarketing, and/or case reports: Abnormal dreams, anaphylaxis, diaphoresis, dyspnea, hypersensitivity reaction, hypoxia, leukocytosis, nightmares, orthostatic hypotension, periorbital swelling, syncope, thrombocytopenia

Warnings/Precautions

Concerns related to adverse effects:

• Anaphylactic shock/hypersensitivity: Serious hypersensitivity reactions, including anaphylactic-type reactions (may be life-threatening with serious hypotension and shock) have been reported. Observe patients for hypersensitivity symptoms during, for 30 minutes after administration, and until clinically stable. Medication, personnel, and equipment for hypersensitivity management should be immediately available. Mild-to-moderate allergic reactions may also occur, usually within 30 minutes of administration.

• Hematologic effects: Increases circulating leukocytes when used in conjunction with filgrastim; monitor WBC counts. Thrombocytopenia has been observed; monitor platelet counts.

• Splenic enlargement/rupture: Cases of splenomegaly and/or splenic rupture have been reported with plerixafor when used in conjunction with filgrastim; instruct patients to report left upper quadrant pain or scapular/shoulder tip pain; promptly evaluate in any patient who report these symptoms.

Disease-related concerns:

• Leukemia: Not intended for mobilization in patients with leukemia; may contaminate apheresis product by mobilizing leukemic cells.

• Renal impairment: Primary route of elimination is renal; dosage reduction is recommended in patients with moderate-to-severe renal impairment (CrCl ≤50 mL/minute).

Concurrent drug therapy issues:

• Nephrotoxic drugs: Medications that may reduce renal function or compete for active tubular secretion may increase serum concentrations of plerixafor.

Special populations:

• Obese patients: Use has not been studied in patients weighing >175% of ideal body weight.

Other warnings/precautions:

• Tumor cell mobilization: When used in combination with filgrastim, tumor cells released from marrow could be collected in leukapheresis product; potential effect of tumor cell reinfusion is unknown.

Monitoring Parameters

CBC with differential and platelets; monitor for signs/symptoms of hypersensitivity (during, for 30 minutes after administration, and until clinically stable) and for signs/symptoms of splenomegaly

Evaluate pregnancy status prior to use in females of reproductive potential.

Pregnancy Considerations

Based on data from animal reproduction studies, in utero exposure to plerixafor may cause fetal harm. Pregnancy should be avoided during therapy.

Evaluate pregnancy status prior to use in females of reproductive potential. Females of reproductive potential should use adequate contraception during treatment and for 1 week after the final plerixafor dose.

Patient Education

What is this drug used for?

• It is used to raise the number of stem cells.

Frequently reported side effects of this drug

• Loss of strength and energy

• Headache

• Insomnia

• Injection site irritation

• Nausea

• Vomiting

• Abdominal pain

• Diarrhea

• Flatulence

• Joint pain

Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:

• Enlarged or ruptured spleen like left upper abdominal pain or left shoulder pain

• Severe dizziness

• Passing out

• Bruising

• Bleeding

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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