MOZOBIL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for MOZOBIL (MOZOBIL).

How it works

Plerixafor is a selective antagonist of the chemokine receptor CXCR4. It blocks the binding of stromal cell-derived factor-1α (SDF-1α) to CXCR4, disrupting the retention of hematopoietic stem cells in the bone marrow and promoting their mobilization into peripheral blood.

What the body does with it

Metabolism	Plerixafor undergoes minimal metabolism primarily via the liver, with involvement of cytochrome P450 enzymes (CYP2D6 and CYP3A4). It is mainly excreted unchanged in urine.
Excretion	Primarily biliary and fecal excretion (approximately 75% of dose); renal excretion accounts for ~25% as unchanged drug and metabolites.
Half-life	Terminal elimination half-life is 5–6 hours in healthy adults; may be prolonged in patients with renal impairment (up to 11 hours in severe renal dysfunction).
Protein binding	Approximately 70–85% bound to plasma proteins, primarily albumin.
Volume of Distribution	Volume of distribution is approximately 0.3–0.5 L/kg, suggesting distribution into total body water and some tissue binding.
Bioavailability	Subcutaneous injection: absolute bioavailability is approximately 85–90%.
Onset of Action	Subcutaneous administration: peak mobilization of CD34+ cells occurs at 6–9 hours after a single dose; onset of clinically meaningful stem cell mobilization is typically observed after 4–5 days of daily dosing.
Duration of Action	After a single subcutaneous dose, elevated circulating CD34+ cell counts persist for approximately 24–48 hours; peak effect at 6–9 hours. For stem cell collection, apheresis is typically performed 2–6 hours after the last dose to capture the mobilization peak.

Classification & Brands

Dosing & administration

0.24 mg/kg subcutaneously once daily for up to 5 consecutive days.

Dosage form	SOLUTION
Renal impairment	If creatinine clearance (CrCl) ≤ 50 mL/min, dose should be reduced to 0.16 mg/kg subcutaneously once daily.
Liver impairment	No dose adjustment required for hepatic impairment.
Pediatric use	Safety and efficacy in pediatric patients have not been established. Not recommended.
Geriatric use	No specific dose adjustment solely based on age, but renal function should be monitored as elderly may have reduced creatinine clearance.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for MOZOBIL (MOZOBIL).

Breastfeeding	Not recommended. It is unknown if Mozobil is excreted in human milk. Given the potential for serious adverse reactions in nursing infants, breastfeeding should be discontinued during treatment. No M/P ratio available.
Teratogenic Risk	Pregnancy category D. Based on animal studies and its mechanism of action (CXCR4 antagonist), there is potential for fetal harm. Human data are limited, but the drug should be avoided during pregnancy unless clearly needed. First trimester: possible teratogenicity based on animal evidence. Second and third trimesters: potential for fetal hematopoietic disruption.

Warnings & precautions

■ FDA Black Box Warning

None (No FDA black box warning assigned).

Side Effect Profile

Serious Effects

Absolute Contraindications

["History of hypersensitivity to plerixafor or any component of the formulation.","Patients with known hypersensitivity or allergic reactions to mannitol-containing products."]

Clinical Precautions

Precautions

["Risk of tumor cell mobilization in patients with hematologic malignancies (e.g., leukemia); caution when administering for stem cell mobilization in such patients.","Potential for splenic rupture (rare, but reported).","Hypersensitivity reactions including anaphylaxis.","Potential for leukocytosis and thrombocytopenia; monitor blood counts."]

Clinical Tips & Counseling

Drug interactions

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MOZOBIL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for MOZOBIL (MOZOBIL).

How it works

What the body does with it

Metabolism	Plerixafor undergoes minimal metabolism primarily via the liver, with involvement of cytochrome P450 enzymes (CYP2D6 and CYP3A4). It is mainly excreted unchanged in urine.
Excretion	Primarily biliary and fecal excretion (approximately 75% of dose); renal excretion accounts for ~25% as unchanged drug and metabolites.
Half-life	Terminal elimination half-life is 5–6 hours in healthy adults; may be prolonged in patients with renal impairment (up to 11 hours in severe renal dysfunction).
Protein binding	Approximately 70–85% bound to plasma proteins, primarily albumin.
Volume of Distribution	Volume of distribution is approximately 0.3–0.5 L/kg, suggesting distribution into total body water and some tissue binding.
Bioavailability	Subcutaneous injection: absolute bioavailability is approximately 85–90%.
Onset of Action	Subcutaneous administration: peak mobilization of CD34+ cells occurs at 6–9 hours after a single dose; onset of clinically meaningful stem cell mobilization is typically observed after 4–5 days of daily dosing.
Duration of Action	After a single subcutaneous dose, elevated circulating CD34+ cell counts persist for approximately 24–48 hours; peak effect at 6–9 hours. For stem cell collection, apheresis is typically performed 2–6 hours after the last dose to capture the mobilization peak.

Classification & Brands

Dosing & administration

0.24 mg/kg subcutaneously once daily for up to 5 consecutive days.

Dosage form	SOLUTION
Renal impairment	If creatinine clearance (CrCl) ≤ 50 mL/min, dose should be reduced to 0.16 mg/kg subcutaneously once daily.
Liver impairment	No dose adjustment required for hepatic impairment.
Pediatric use	Safety and efficacy in pediatric patients have not been established. Not recommended.
Geriatric use	No specific dose adjustment solely based on age, but renal function should be monitored as elderly may have reduced creatinine clearance.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for MOZOBIL (MOZOBIL).

Breastfeeding	Not recommended. It is unknown if Mozobil is excreted in human milk. Given the potential for serious adverse reactions in nursing infants, breastfeeding should be discontinued during treatment. No M/P ratio available.
Teratogenic Risk	Pregnancy category D. Based on animal studies and its mechanism of action (CXCR4 antagonist), there is potential for fetal harm. Human data are limited, but the drug should be avoided during pregnancy unless clearly needed. First trimester: possible teratogenicity based on animal evidence. Second and third trimesters: potential for fetal hematopoietic disruption.

Warnings & precautions

■ FDA Black Box Warning

None (No FDA black box warning assigned).

Side Effect Profile

Serious Effects

Absolute Contraindications

["History of hypersensitivity to plerixafor or any component of the formulation.","Patients with known hypersensitivity or allergic reactions to mannitol-containing products."]