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Plerixafor

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

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 (HSC) 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 (10 mcg/kg once daily) for 4 days; 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

US labeling:

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

Canadian labeling: 0.24 mg/kg once daily for up to 4 consecutive days; maximum dose: 40 mg daily

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

Note: Creatinine clearance estimate based on Cockcroft-Gault formula:

US labeling:

CrCl >50 mL/minute: No dosage adjustment necessary.

CrCl ≤50 mL/minute:

Patients ≤83 kg: 13 mg fixed dose or 0.16 mg/kg once daily

Patients >83 kg and <160 kg: 0.16 mg/kg once daily; maximum dose: 27 mg daily

Hemodialysis: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

Canadian labeling:

CrCl >50 mL/minute: No dosage adjustment necessary

CrCl 20 to 50 mL/minute: 0.16 mg/kg once daily; maximum dose: 27 mg daily

CrCl <20 mL/minute and hemodialysis: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling.

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

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).

Hazardous agent; use appropriate precautions for handling and disposal (NIOSH 2014 [group 3]).

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%)

5% to 10%:

Central nervous system: Insomnia (7%)

Gastrointestinal: Vomiting (10%), flatulence (7%)

Hematologic & oncologic: Hyperleukocytosis (7%)

<5% (Limited to important or life-threatening): Hypersensitivity reaction, hypoxia, leukocytosis, 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 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.

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:

• Filgrastim: Splenomegaly and splenic rupture have been reported (rarely) with filgrastim use; instruct patients to report left upper quadrant pain or scapular/shoulder tip pain; promptly evaluate in any patient who report these symptoms.

• 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.

Special handling:

• Hazardous agent: Use appropriate precautions for handling and disposal (NIOSH 2014 [group 3]).

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

Pregnancy Risk Factor

D

Pregnancy Considerations

Adverse effects have been observed in animal reproduction studies. May cause fetal harm if administered to pregnant women. Women of childbearing potential should use effective contraceptive measures to avoid becoming pregnant during treatment.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience loss of strength and energy, headache, injection site irritation or edema, nausea, vomiting, diarrhea, flatulence, or joint pain. Have patient report immediately to prescriber signs of enlarged or ruptured spleen (left upper abdominal pain or left shoulder pain), eye or eyelid edema; severe dizziness; passing out; shortness of breath; bruising; bleeding; or black, tarry, or bloody stools (HCAHPS).

• 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.

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