PLERIXAFOR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PLERIXAFOR (PLERIXAFOR).
Plerixafor is a bicyclam molecule that reversibly inhibits the binding of stromal cell-derived factor-1α (SDF-1α) to its cognate receptor CXCR4 on hematopoietic stem cells, thereby blocking the retention signal and mobilizing stem cells from the bone marrow into the peripheral blood.
| Metabolism | Plerixafor is not extensively metabolized. It is primarily excreted unchanged in the urine, with minimal hepatic metabolism. Less than 10% of the dose is metabolized, and the metabolites are not characterized. CYP450 enzymes are not involved. |
| Excretion | Renal: 70% unchanged; fecal: 20% (as metabolites); biliary: <10%. |
| Half-life | Terminal half-life: 3-5 hours in healthy adults; prolonged in renal impairment (up to 15 hours in severe cases). |
| Protein binding | 55-75% bound primarily to albumin. |
| Volume of Distribution | 0.3-0.5 L/kg, indicating distribution primarily in extracellular fluid. |
| Bioavailability | Subcutaneous: approximately 100% (rapid and complete absorption). |
| Onset of Action | Subcutaneous: 1-2 hours (peak mobilization of CD34+ cells). Intravenous (if used): immediate but typically SC. |
| Duration of Action | Mobilization effect persists for approximately 24 hours post-dose; repeated daily doses required for optimal stem cell collection. |
0.24 mg/kg subcutaneously once daily for up to 4 consecutive days.
| Dosage form | SOLUTION |
| Renal impairment | For GFR < 50 mL/min, reduce dose to 0.16 mg/kg subcutaneously once daily. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe impairment (Child-Pugh C). |
| Pediatric use | Weight-based dosing: 0.24 mg/kg subcutaneously once daily for patients weighing ≤ 40 kg; 0.24 mg/kg (max 20 mg) subcutaneously once daily for patients weighing > 40 kg. Approved for use in children ≥ 1 year with multiple myeloma. |
| Geriatric use | No specific dose adjustment based on age alone; monitor renal function as elderly patients may have reduced GFR; follow renal adjustment guidelines. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PLERIXAFOR (PLERIXAFOR).
| Breastfeeding | No data on presence in human milk; risk to infant cannot be excluded. M/P ratio not known. Consider developmental benefits of breastfeeding alongside mother's clinical need for plerixafor and potential adverse effects on infant. |
| Teratogenic Risk | Animal studies show fetal harm; no adequate human data. Avoid in pregnancy unless benefit outweighs risk. First trimester: potential teratogenic effects based on animal reproductive studies. Second/third trimesters: unknown fetal risk; may cause fetal harm based on animal data. |
■ FDA Black Box Warning
There is no FDA-issued black box warning for plerixafor.
| Serious Effects |
["History of hypersensitivity to plerixafor or any of its excipients."]
| Precautions | ["Anaphylactic shock and hypersensitivity reactions: Serious allergic reactions, including anaphylaxis, have occurred. Observe patients for at least 30 minutes after the end of each dose.","Leukocytosis: White blood cell counts may increase significantly. Monitor CBC during therapy.","Thrombocytopenia: Decreased platelet counts have been observed, especially in patients with baseline thrombocytopenia.","Circulating tumor cell mobilization: In patients with multiple myeloma, the possibility of mobilizing tumor cells should be considered.","Splenic rupture: Rare cases of splenic enlargement and rupture have been reported.","Embryo-fetal toxicity: Can cause fetal harm when administered to pregnant women. Advise females of reproductive potential to use effective contraception."] |
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| Fetal Monitoring |
| Monitor maternal blood counts (neutrophil and CD34+ cell counts) during mobilization and apheresis; fetal monitoring per standard obstetrical care; assess for signs of infection, splenic rupture, or allergic reactions in mother. |
| Fertility Effects | No human fertility data; animal studies show no impairment of male or female fertility at clinically relevant doses. Potential for transient disruption of hematopoiesis. |