RELEUKO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for RELEUKO (RELEUKO).
Recombinant human granulocyte colony-stimulating factor (G-CSF) that stimulates proliferation, differentiation, and activation of neutrophil progenitor cells.
| Metabolism | Primarily metabolized by proteolytic degradation; renal clearance contributes to elimination. |
| Excretion | Primarily renal (approximately 70% as intact drug). Minor biliary/fecal elimination (<5%). |
| Half-life | Terminal half-life approximately 5.3 hours (range 4.5–6.2 hours) in adults with normal renal function. |
| Protein binding | Approximately 70–85% bound to albumin. |
| Volume of Distribution | Vd approximately 0.5–0.8 L/kg, suggesting distribution largely within extracellular fluid. |
| Bioavailability | Subcutaneous: approximately 60–70%. |
| Onset of Action | Subcutaneous: 1–2 hours; peak effect at 6–8 hours. |
| Duration of Action | Approximately 24 hours; clinical effect wanes as drug is cleared, requiring daily dosing. |
5 mcg/kg subcutaneously once daily for up to 10 days or until neutrophil count >10,000/mcL after nadir.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for renal impairment; however, safety and efficacy not established in severe renal dysfunction. |
| Liver impairment | No specific dose adjustments recommended; use with caution in severe hepatic impairment due to limited data. |
| Pediatric use | 5 mcg/kg subcutaneously once daily; safety and efficacy not established in neonates. |
| Geriatric use | No dose adjustment necessary; monitor for adverse events and clinical response. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RELEUKO (RELEUKO).
| Breastfeeding | No data available on excretion into human milk. Manufacturer recommends caution due to potential for serious adverse reactions in nursing infants. M/P ratio unknown. Consider developmental and health benefits of breastfeeding along with mother's clinical need for the drug. |
| Teratogenic Risk | FDA Pregnancy Category C. Animal studies have shown fetal toxicity at doses 2.5 times the human dose. There are no adequate and well-controlled studies in pregnant women. Risk cannot be ruled out. Use only if potential benefit justifies potential risk to the fetus. Limited data suggest no increased risk of major malformations with therapeutic use in first trimester. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to filgrastim or any component of the formulation","Concurrent administration with myelosuppressive chemotherapy until 24 hours after chemotherapy"]
| Precautions | ["Potential for splenic rupture (reported in patients with sickle cell disease and normal volunteers)","Acute respiratory distress syndrome (ARDS) due to neutrophil infiltration at sites of inflammation","Allergic reactions including anaphylaxis","Sickle cell crisis in patients with sickle cell disease","Glomerulonephritis","Leukocytosis (monitor white blood cell counts)","Potential for tumor growth stimulation in myelodysplastic syndromes or myeloid malignancies"] |
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| Fetal Monitoring | Monitor complete blood count (CBC) with differential and platelet count regularly during therapy. Assess for signs of infection, bleeding, or anemia. Fetal monitoring not routinely required but consider if maternal condition warrants. |
| Fertility Effects | No human studies on fertility. Animal studies have not indicated impaired fertility at therapeutic doses. Potential for ovarian suppression due to cytokine effects, but clinical significance unknown. |