FERAHEME
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FERAHEME (FERAHEME).
Ferumoxytol is a superparamagnetic iron oxide nanoparticle coated with a semisynthetic carbohydrate shell. It serves as a source of iron for hemoglobin synthesis and replenishes iron stores. The iron core is processed intracellularly to release iron, which is then incorporated into hemoglobin or stored as ferritin. The carbohydrate shell is metabolized and eliminated.
| Metabolism | Ferumoxytol is taken up by macrophages of the reticuloendothelial system (liver, spleen, bone marrow). The iron is released and incorporated into hemoglobin or stored as ferritin. The carbohydrate shell is metabolized via endogenous pathways. |
| Excretion | Renal: minimal (<1% as intact drug); primarily degraded endogenously with iron incorporated into hemoglobin; fecal/biliary elimination of unabsorbed iron is negligible. |
| Half-life | Terminal half-life of ferumoxytol (iron core) is approximately 14-21 hours; for the intact nanoparticle (carbohydrate shell), half-life is about 15 hours. Clinically, iron is continuously released and incorporated, extending effects beyond half-life. |
| Protein binding | Ferumoxytol binds minimally to plasma proteins; iron released from ferumoxytol binds to transferrin (saturation-dependent). |
| Volume of Distribution | Vd approximately 200-300 mL/kg (~0.2-0.3 L/kg), reflecting distribution primarily in blood volume and iron stores (reticuloendothelial system). |
| Bioavailability | Intravenous: 100%. |
| Onset of Action | Intravenous: Reticulocyte count begins to rise within 7-10 days; hemoglobin increase typically seen within 2-4 weeks. |
| Duration of Action | Duration of hemoglobin correction persists for weeks; single dose can supply iron for up to 4-6 weeks depending on iron deficiency severity. |
510 mg intravenously once, followed by a second 510 mg dose 3 to 8 days later, not exceeding 1020 mg per course.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for any degree of renal impairment, including end-stage renal disease on dialysis. |
| Liver impairment | No specific Child-Pugh based adjustments; contraindicated in patients with evidence of iron overload. |
| Pediatric use | Safety and efficacy not established in pediatric patients under 18 years of age. |
| Geriatric use | No specific dose adjustment required; use caution due to potential comorbidities and polypharmacy. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FERAHEME (FERAHEME).
| Breastfeeding | It is not known whether ferumoxytol is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when FERAHEME is administered to a nursing woman. There is no available data on the milk-to-plasma (M/P) ratio. |
| Teratogenic Risk | FERAHEME (ferumoxytol) is classified as FDA Pregnancy Category C. Animal reproduction studies have not been conducted. It is not known whether ferumoxytol can cause fetal harm when administered to a pregnant woman. Use during pregnancy only if clearly needed and potential benefit justifies potential risk to the fetus. There are no adequate and well-controlled studies in pregnant women. Risk cannot be ruled out. |
■ FDA Black Box Warning
WARNING: SERIOUS HYPERSENSITIVITY REACTIONS, INCLUDING ANAPHYLAXIS, AND HYPOTENSION. FERAHEME may cause serious hypersensitivity reactions, including anaphylaxis, and hypotension. Observe patients for at least 30 minutes after each injection. Only administer when personnel and therapies are immediately available for treatment of anaphylaxis and other hypersensitivity reactions.
| Serious Effects |
["History of hypersensitivity to ferumoxytol or any of its components","History of drug reaction with eosinophilia and systemic symptoms (DRESS) due to ferumoxytol","Evidence of iron overload (e.g., hemochromatosis, thalassemia)"]
| Precautions | ["Hypersensitivity reactions including anaphylaxis","Hypotension","Iron overload in patients with chronic iron overload conditions","Risk of serious hypersensitivity reactions requiring emergency treatment","Administration only when personnel and therapies for anaphylaxis are immediately available"] |
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| Fetal Monitoring | Monitor for signs and symptoms of hypersensitivity reactions, including anaphylaxis, during and after administration. Monitor blood pressure and heart rate. Assess for extravasation at injection site. No specific fetal monitoring is recommended, but standard obstetric monitoring applies if used in pregnancy. |
| Fertility Effects | No studies have been conducted to assess the effect of ferumoxytol on fertility. Animal reproduction studies have not been performed. It is not known whether ferumoxytol can affect reproductive capacity. |