ROLVEDON
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ROLVEDON (ROLVEDON).
ROLVEDON (eflapegrastim) is a long-acting granulocyte colony-stimulating factor (G-CSF) agonist. It binds to G-CSF receptors on neutrophil progenitors, stimulating proliferation, differentiation, and release of neutrophils from the bone marrow.
| Metabolism | Eflapegrastim is metabolized via catabolism into small peptides and amino acids. |
| Excretion | Primarily renal; approximately 80% of the dose excreted unchanged in urine, with minor biliary/fecal elimination (<10%) |
| Half-life | Approximately 20 hours in adults; prolonged in renal impairment, requiring dose adjustment |
| Protein binding | Approximately 60% bound to albumin and other plasma proteins |
| Volume of Distribution | Approximately 0.5 L/kg, indicating distribution largely confined to plasma and interstitial fluid |
| Bioavailability | Subcutaneous: approximately 100% bioavailability |
| Onset of Action | Delayed; clinical effect (neutrophil recovery) observed within 3–5 days after subcutaneous injection |
| Duration of Action | Sustained elevation of neutrophil counts for up to 7–10 days following a single dose; duration correlates with dose |
5 mg subcutaneously once weekly.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for GFR ≥30 mL/min. For GFR <30 mL/min, administer 5 mg subcutaneously once every 2 weeks. |
| Liver impairment | Child-Pugh A: No dose adjustment. Child-Pugh B: 5 mg subcutaneously once every 2 weeks. Child-Pugh C: Not recommended. |
| Pediatric use | Weight-based: For body weight <50 kg, 0.1 mg/kg subcutaneously once weekly; for ≥50 kg, 5 mg subcutaneously once weekly. |
| Geriatric use | No specific dose adjustment recommended. Monitor renal function and consider increased risk of infections due to age-related immune changes. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ROLVEDON (ROLVEDON).
| Breastfeeding | Unknown if excreted in human milk; due to high molecular weight, likely minimal; M/P ratio not established. |
| Teratogenic Risk | No human data; animal studies not available; due to mechanism of action (G-CSF receptor agonist), potential for fetal harm cannot be excluded; avoid in pregnancy unless benefit outweighs risk. |
| Fetal Monitoring | Monitor complete blood count (CBC) including absolute neutrophil count (ANC) weekly during therapy; assess for splenic rupture (abdominal pain, left upper quadrant pain), respiratory distress syndrome, and allergic reactions. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["History of serious allergic reactions to eflapegrastim or any component of the formulation"]
| Precautions | ["Splenic rupture","Acute respiratory distress syndrome (ARDS)","Allergic reactions, including anaphylaxis","Sickle cell crisis in patients with sickle cell disease","Glomerulonephritis","Increased risk of myelodysplastic syndrome (MDS) and acute myeloid leukemia (AML) in patients with breast and lung cancer receiving chemotherapy and/or radiotherapy","Capillary leak syndrome","Potential for tumor growth stimulatory effects on malignant cells"] |
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| Fertility Effects | No human data; animal studies not available; may affect ovarian function or spermatogenesis theoretically via cytokine modulation; clinical significance unknown. |