Ferric carboxymaltose, a polynuclear iron (III)-hydroxide carbohydrate complex, is a stable non-dextran iron formulation used to replenish and maintain the total body content of iron; the drug has pharmacologic actions similar to those of other parenteral iron preparations.1, 2, 3, 4, 7
Iron Deficiency Anemia Not Amenable to Oral Iron Therapy
Ferric carboxymaltose is used for the treatment of iron deficiency anemia in adults who are intolerant of or have had an unsatisfactory response to oral iron preparations.1, 5 Available evidence indicates that a 2-dose regimen of IV ferric carboxymaltose is at least as effective as more frequent dosing of IV iron sucrose or oral iron in increasing hemoglobin concentrations in such patients.1, 2, 5, 7
Efficacy and safety of ferric carboxymaltose have been established in an open-label, randomized, active-controlled, noninferiority study in 1011 patients with iron deficiency anemia who had an unsatisfactory response to or were intolerant of oral iron during a 14-day run-in period of oral iron treatment (ferrous sulfate 325 mg 3 times daily).1, 2 The mean patient age was 43 years (range: 18-94 years); 94% were female; and 42, 32, 24, or 2% were white, black, Hispanic, or of other races, respectively.1 Iron deficiency anemia was secondary to heavy uterine bleeding in 47% of patients and to GI disorders in 17% of patients.1 Patients who had an unsatisfactory response to oral iron (increase from baseline hemoglobin of less than 1 g/dL) received ferric carboxymaltose (administered as 2 doses of 15 mg/kg [up to 750 mg per dose] IV given on days 0 and 7) or continued oral iron for 14 days.1, 2 Patients who were intolerant of oral iron received either the 2-dose IV ferric carboxymaltose regimen or 1-14 (usually 3) doses of another IV iron preparation per standard of care (iron sucrose in approximately 90% of patients).1, 2
In the cohort of patients who had an unsatisfactory response to oral iron, the mean increase in hemoglobin (from a baseline of 10.6 g/dL) was 1.6 g/dL in those receiving IV ferric carboxymaltose and 0.8 g/dL in those receiving oral iron.1, 2, 5 In the cohort of patients who were intolerant of oral iron, the mean increase in hemoglobin (from a baseline of 9-9.1 g/dL) was 2.9 g/dL in patients receiving IV ferric carboxymaltose and 2.2 g/dL in those receiving another IV iron preparation.1, 2, 5 Increases from baseline of 218.2-264.2 ng/mL in mean ferritin and of 13-20% in mean transferrin saturation were observed at day 35 in patients receiving ferric carboxymaltose.1
Iron Deficiency Anemia in Patients with Non-Dialysis-Dependent Chronic Kidney Disease
Ferric carboxymaltose is used for the treatment of iron deficiency anemia in adults with non-dialysis-dependent chronic kidney disease.1, 5
Efficacy and safety of ferric carboxymaltose have been established in an open-label, randomized, active-controlled noninferiority study in 2561 patients with non-dialysis-dependent chronic kidney disease.1, 3, 4 The mean patient age was 67 years (range: 19-96 years); 64% were female, and 54, 26, 18, or 2% were white, black, Hispanic, or of other races, respectively.1, 3 In this study, ferric carboxymaltose treatment (total dose of up to 1.5 g given as 2 doses of 15 mg/kg [up to 750 mg per dose] IV on days 0 and 7) increased hemoglobin concentration more than iron sucrose (total dose of 1 g given as 5 doses of 200 mg IV over 14 days) while allowing administration of a higher dosage of iron in fewer infusions and over a shorter period of time.1, 3, 7 The mean increase in hemoglobin from baseline (mean 10.3 g/dL) to highest observed value between baseline and day 56 or time of intervention was 1.1 g/dL in patients receiving ferric carboxymaltose versus 0.9 g/dL in those receiving iron sucrose.1, 3, 5, 7 In addition, increases from baseline of 734.7 ng/mL in mean ferritin and of 30% in transferrin saturation were observed at day 56 in patients receiving ferric carboxymaltose.1
Ferric carboxymaltose is administered by slow IV injection or IV infusion only.1 When given by slow IV injection, the drug is administered undiluted at a rate of approximately 100 mg (2 mL)/minute.1 When given by IV infusion, up to 750 mg of iron should be diluted in no more than 250 mL of 0.9% sodium chloride injection, providing a concentration of no less than 2 mg/mL of iron; the diluted solution should be administered over at least 15 minutes.1
When added to an infusion bag containing 0.9% sodium chloride injection, ferric carboxymaltose solutions containing 2-4 mg/mL of iron are physically and chemically stable for 72 hours when stored at room temperature.1 Any unused portion of the diluted or undiluted ferric carboxymaltose solution should be discarded.1 Ferric carboxymaltose injection and diluted solutions of the drug should be inspected visually for particulate matter and discoloration prior to administration.1
Extravasation of ferric carboxymaltose should be avoided.1 Extravasation of the drug may cause brown discoloration of the extravasation site, which may be long lasting.1 The injection site should be monitored for extravasation during administration of ferric carboxymaltose.1 If extravasation occurs, ferric carboxymaltose administration at the affected site should be discontinued.1
Patients should be monitored for hypersensitivity reactions during and for at least 30 minutes after administration of ferric carboxymaltose until clinically stable.1 Ferric carboxymaltose should be administered only when appropriate agents and personnel for the treatment of serious hypersensitivity reactions are readily available.1
Dosage of ferric carboxymaltose is expressed in terms of elemental iron.1 Each mL of ferric carboxymaltose injection contains the equivalent of 50 mg of elemental iron.1
Iron Deficiency Anemia Not Amenable to Oral Iron Therapy
For the treatment of iron deficiency anemia in adults who are intolerant of or have had an unsatisfactory response to oral iron therapy, the recommended dosage of ferric carboxymaltose per treatment course in patients weighing at least 50 kg is 1.5 g, given as 2 doses of 750 mg each by slow IV injection or IV infusion at least 7 days apart.1 In patients weighing less than 50 kg, the recommended dosage of ferric carboxymaltose per treatment course is 30 mg/kg, given as 2 doses of 15 mg/kg (up to 750 mg per dose) by slow IV injection or IV infusion at least 7 days apart.1 The total cumulative dosage per treatment course should not exceed 1.5 g.1 Ferric carboxymaltose treatment may be repeated if iron deficiency anemia reoccurs.1
Iron Deficiency Anemia in Patients with Non-Dialysis-Dependent Chronic Kidney Disease
For the treatment of iron deficiency anemia in adults with non-dialysis-dependent chronic kidney disease, the recommended total dosage of ferric carboxymaltose per treatment course in patients weighing at least 50 kg is 1.5 g, given as 2 doses of 750 mg by slow IV injection or IV infusion at least 7 days apart; the total cumulative dosage of iron per treatment course should not exceed 1.5 g.1 In patients weighing less than 50 kg, the recommended total dosage of ferric carboxymaltose per treatment course is 30 mg/kg, given as 2 doses of 15 mg/kg (up to 750 mg per dose) by slow IV injection or IV infusion at least 7 days apart; the total cumulative dosage of iron per treatment course should not exceed 1.5 g.1 Ferric carboxymaltose treatment may be repeated if iron deficiency anemia reoccurs.1
No special populations dosage recommendations are available at this time.1
Known hypersensitivity to ferric carboxymaltose or any ingredient in the formulation.1
Hypersensitivity reactions, including serious or life-threatening and fatal anaphylactic-type reactions, have been reported in patients receiving ferric carboxymaltose.1, 2, 3, 5 Serious hypersensitivity reactions, which may manifest as shock, clinically important hypotension, loss of consciousness, and/or collapse, have been reported in 0.1% of patients receiving ferric carboxymaltose in clinical trials; other serious or severe reactions potentially associated with hypersensitivity (e.g., pruritus, rash, urticaria, wheezing, hypotension) have occurred in 1.5% of such patients.1
Hypertension1, 3, 5 was reported in 3.8% of patients receiving ferric carboxymaltose in clinical trials.1 Transient elevations in systolic blood pressure, sometimes accompanied by facial flushing, dizziness, or nausea, were reported in 6% of patients; these elevations usually occurred immediately after administration of the drug and resolved within 30 minutes.1 Patients should be monitored for signs and symptoms of hypertension following each dose of ferric carboxymaltose.1
Serum iron transferrin-bound iron concentrations may be falsely elevated when assessed in the 24 hours following injection of ferric carboxymaltose because the iron present in the drug may also be measured.
Category C.1 (See Users Guide.)
In lactating women with postpartum iron deficiency anemia, mean breast milk iron concentrations were higher in women receiving IV ferric carboxymaltose than in those receiving oral ferrous sulfate.1 Ferric carboxymaltose should be used with caution in nursing women.1
Safety and efficacy of ferric carboxymaltose have not been established in pediatric patients.1
In overall clinical trials of ferric carboxymaltose, 50% of patients were 65 years of age or older, while 25% were 75 years of age and older.1 Although no overall differences in efficacy or safety were observed between geriatric and younger patients, and other clinical experience has revealed no evidence of age-related differences, the possibility that some older patients may exhibit increased sensitivity to the drug cannot be ruled out.1
Adverse effects reported in at least 1% of patients receiving ferric carboxymaltose in 2 randomized clinical trials include nausea,1, 2, 3 hypertension,1, 3 flushing/hot flush,1, 3 hypophosphatemia,1, 2, 3 dizziness,1, 3 vomiting,1 injection site discoloration,1 headache,1 increased serum ALT concentration,1 dysgeusia,1, 3 and hypotension.1, 3
Formal studies examining drug interactions with ferric carboxymaltose have not been performed to date.1
Ferric carboxymaltose is a polynuclear iron (III)-hydroxide carbohydrate complex with a molecular weight of approximately 150,000.1, 4, 7 Ferric carboxymaltose is a stable, non-dextran iron formulation that permits uptake of iron by the reticuloendothelial system without the release of free iron.4 In patients with iron deficiency, erythrocyte uptake of iron at 24 days following administration of radiolabeled ferric carboxymaltose ranged from 91 to 99% of the dose.1 An erythrocyte iron uptake of 61-84% was reported 24 days following administration of radiolabeled ferric carboxymaltose in patients with renal anemia.1
Risk of hypersensitivity reactions.1 Importance of informing clinician if any signs or symptoms of hypersensitivity reactions (e.g., rash, pruritus, dizziness, lightheadedness, dyspnea, wheezing, swelling) occur.1
Importance of informing clinician of prior hypersensitivity or unusual reactions to parenteral iron preparations.1
Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary and herbal supplements (e.g., oral iron supplements), as well as any concomitant illnesses (e.g., liver disease may increase likelihood of iron overload).1
Importance of women informing clinician if they are or plan to become pregnant or plan to breast-feed.1
Importance of informing patients of other important precautionary information.1 (See Cautions.)
Additional Information
Overview® (see Users Guide). For additional information on this drug until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Parenteral | Injection, for IV use only | equivalent to 50 mg of elemental iron per mL |
AHFS® Drug Information. © Copyright, 1959-2025, Selected Revisions April 14, 2015. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.
1. American Regent, Inc. Injectafer® (ferric carboxymaltose injection) prescribing information. Shirley, NY; 2013 Jul.
2. Onken JE, Bregman DB, Harrington RA et al. A multicenter, randomized, active-controlled study to investigate the safety and efficacy of intravenous ferric carboxymaltose in patients with iron deficiency anemia. Transfusion . 2014; 54:306-15. [PubMed 23772856]
3. Onken JE, Bregman DB, Harrington RA et al. Ferric carboxymaltose in patients with iron-deficiency anemia and impaired renal function: the REPAIR-IDA trial. Nephrol Dial Transplant . 2013; 0:1-12.
4. Szczech LA, Bregman DB, Harrington RA et al. Randomized Evaluation of efficacy and safety of ferric carboxymaltose in Patients with iron deficiency Anaemia and Impaired Renal function (REPAIR-IDA): rationale and study design. Nephrol Dial Transplant . 2010; 25:2368-75. [PubMed 20466657]
5. Anon. Ferric carboxymaltose (Injectafer) for iron deficiency anemia. Med Lett . 2013; 55:99-100.
6. Geisser P, Banké-Bochita J. Pharmacokinetics, safety, and tolerability of intravenous ferric carboxymaltose: a dose-escalation study in volunteers with mild iron-deficiency anemia. Arzneimittelforschung . 2010; 60:362-72. [PubMed 20648928]
7. Cada DJ, Levien TL, Baker DE. Ferric carboxymaltose. Hosp Pharm . 2014; 49:52-69. [PubMedCentral][PubMed 24421564]
8. Geisser P, Rumyantsev V. Pharmacodynamics and safety of ferric carboxymaltose: a multiple-dose study in patients with iron-deficiency anaemia secondary to a gastrointestinal disorder. Arzneimittelforschung . 2010; 60:373-85. [PubMed 20648929]