FERUMOXYTOL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FERUMOXYTOL (FERUMOXYTOL).
Ferumoxytol is an ultrasmall superparamagnetic iron oxide nanoparticle that provides a source of iron for erythropoiesis. It is phagocytosed by macrophages of the reticuloendothelial system, and iron is released intracellularly to bind to transferrin and ferritin, replenishing iron stores.
| Metabolism | Ferumoxytol is phagocytosed by macrophages and degraded in lysosomes; iron is released and incorporated into hemoglobin, ferritin, and hemosiderin. The iron oxide core is metabolized via normal iron metabolic pathways. Complex elimination half-life is approximately 14-15 hours. |
| Excretion | Ferumoxytol is eliminated primarily through the reticuloendothelial system, with the iron moiety incorporated into hemoglobin or stored as ferritin/hemosiderin. Minimal renal or biliary excretion of intact drug; <1% excreted unchanged in urine. |
| Half-life | Terminal elimination half-life is approximately 14-21 hours in healthy adults; prolonged in patients with iron deficiency anemia (up to 30 hours) due to increased iron utilization. |
| Protein binding | Ferumoxytol is a supramagnetic iron oxide nanoparticle; binding to plasma proteins (albumin, transferrin) is minimal; the iron core is incorporated into endogenous iron pools. |
| Volume of Distribution | Vd approximately 0.5-1.0 L/kg, indicating distribution primarily into plasma and reticuloendothelial tissues (liver, spleen, bone marrow). |
| Bioavailability | Bioavailability is 100% following intravenous administration; no oral formulation exists. |
| Onset of Action | Intravenous: Onset of hemoglobin increase is within 1-2 weeks; peak effect typically occurs at 4-6 weeks. |
| Duration of Action | Duration of effect persists for weeks to months, depending on iron stores; a single dose may maintain hemoglobin for 4-8 weeks. |
510 mg intravenously once, followed by 510 mg intravenously 3 to 8 days later for a total cumulative dose of 1020 mg. Administer as a slow IV injection at 1 mL/min (30 mg/min) undiluted or diluted in 50-200 mL normal saline.
| Dosage form | SOLUTION |
| Renal impairment | Contraindicated in eGFR <15 mL/min/1.73m2 or on dialysis. For eGFR 15-30 mL/min/1.73m2, reduce dose to 510 mg as a single dose with further dosing based on iron status and renal function. No dose adjustment for eGFR >30 mL/min/1.73m2. |
| Liver impairment | No specific dose adjustment recommended for Child-Pugh A or B; use with caution in severe hepatic impairment (Child-Pugh C) due to limited data. Monitor for signs of iron overload. |
| Pediatric use | Not approved for use in pediatric patients (safety and efficacy not established). Clinical trials have not included pediatric populations. |
| Geriatric use | No specific dose adjustment recommended; monitor renal function (eGFR) due to age-related decline and potential increased risk of iron overload or hypersensitivity reactions. Use same dosing as adults if eGFR >30 mL/min/1.73m2. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FERUMOXYTOL (FERUMOXYTOL).
| Breastfeeding | Not known whether ferumoxytol is excreted in human milk. No M/P ratio available. Caution advised; consider developmental and health benefits of breastfeeding along with mother's clinical need. Iron is normally present in breast milk; supplementation may increase milk iron concentration. |
| Teratogenic Risk | Ferumoxytol is a parenteral iron preparation. No adequate and well-controlled studies in pregnant women. Animal reproduction studies have not been conducted. Risk cannot be ruled out. In first trimester, theoretical risk of iron toxicity if ferritin saturates; generally avoided. Second and third trimester: use only if clearly needed and benefit outweighs unknown fetal risks. Iron crosses placenta; potential for fetal iron overload with excessive doses. |
■ FDA Black Box Warning
WARNING: SERIOUS HYPERSENSITIVITY REACTIONS, INCLUDING FATAL ANAPHYLAXIS: FERUMOXYTOL MAY CAUSE SERIOUS HYPERSENSITIVITY REACTIONS, INCLUDING ANAPHYLAXIS AND HYPOTENSION. OBSERVE PATIENTS FOR AT LEAST 30 MINUTES FOLLOWING INJECTION. ONLY ADMINISTER WHEN RESUSCITATION EQUIPMENT AND TRAINED PERSONNEL ARE AVAILABLE.
| Serious Effects |
["Hypersensitivity to ferumoxytol or any of its components","History of serious hypersensitivity reaction to any intravenous iron product","Evidence of iron overload (e.g., hemochromatosis, hemosiderosis)","Anemia not caused by iron deficiency","Pregnancy (Category C; limited data)"]
| Precautions | ["Hypersensitivity reactions including anaphylaxis","Hypotension","Iron overload in patients with hemochromatosis or other iron overload states","Risk of allergic reactions in patients with multiple drug allergies","Do not administer if evidence of iron overload or Hgb < 10 g/dL","Monitor serum ferritin and transferrin saturation to avoid overload"] |
Loading safety data…
| Fetal Monitoring | Monitor maternal blood pressure and heart rate during infusion due to risk of hypotension and anaphylactoid reactions. Monitor hemoglobin, hematocrit, ferritin, and iron studies periodically. Assess for signs of iron overload (e.g., elevated ferritin, transferrin saturation). Fetal monitoring not routinely required unless maternal reaction occurs. |
| Fertility Effects | No data on effects on fertility. Iron deficiency may impair fertility; correction may improve reproductive outcomes. No known adverse effects on gametes or early embryo development. |