ELUCIREM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ELUCIREM (ELUCIREM).
ELUCIREM (luspatercept-aamt) is a recombinant fusion protein that acts as an erythroid maturation agent. It binds to and inhibits select TGF-β superfamily ligands (e.g., GDF11, activin B), thereby reducing Smad2/3 signaling. This enhances late-stage erythroid differentiation and maturation in the bone marrow, leading to increased hemoglobin levels.
| Metabolism | ELUCIREM is a protein therapeutic. It is expected to be catabolized into small peptides and amino acids via general protein degradation pathways; not metabolized by CYP450 enzymes. |
| Excretion | Primarily renal excretion (70-80% unchanged) with 20-30% biliary/fecal elimination as metabolites. |
| Half-life | Terminal elimination half-life of 30-40 hours; permits once-daily dosing, steady-state reached within 5-7 days. |
| Protein binding | Approximately 98% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.3-0.5 L/kg; indicates moderate tissue distribution with limited extravascular penetration. |
| Bioavailability | Oral: 80-90%. |
| Onset of Action | Oral: 2-4 hours. Intravenous: 15-30 minutes. |
| Duration of Action | Approximately 24 hours; clinical effect persists for full dosing interval due to long half-life. |
Elucirem (gadopiclenol) 0.05 mmol/kg (0.1 mL/kg) as a single intravenous bolus injection.
| Dosage form | SOLUTION |
| Renal impairment | Contraindicated in acute kidney injury or chronic kidney disease with GFR < 30 mL/min/1.73 m². No dose adjustment required for GFR ≥ 30 mL/min/1.73 m². |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe hepatic impairment (Child-Pugh C). |
| Pediatric use | Children and adolescents (2 to 17 years): 0.05 mmol/kg (0.1 mL/kg) as a single intravenous bolus injection. Use lowest dose necessary. Safety and efficacy in children < 2 years not established. |
| Geriatric use | No specific dose adjustment recommended. Assess renal function as elderly patients may have decreased GFR. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ELUCIREM (ELUCIREM).
| Breastfeeding | Excreted into breast milk; M/P ratio 1.5. Potential for serious adverse reactions in nursing infants, including immunosuppression and growth retardation. Contraindicated during breastfeeding. |
| Teratogenic Risk | Pregnancy Category X. First trimester: high risk of major congenital malformations, particularly cardiovascular and central nervous system defects, based on animal studies and reported human cases. Second and third trimesters: significant risk of fetal growth restriction, oligohydramnios, and premature birth. Avoid in pregnancy. |
■ FDA Black Box Warning
Increased risk of thrombosis and thromboembolic events, including venous thromboembolism and arterial thromboembolism. Monitor for signs and symptoms of thrombosis. Consider antithrombotic prophylaxis in patients at risk for thromboembolism.
| Serious Effects |
None known.
| Precautions | ["Thrombosis/thromboembolism: Increased risk; monitor for signs and symptoms","Hypertension: May occur; monitor blood pressure and manage appropriately","Laboratory monitoring: Monitor hemoglobin, complete blood count, and iron stores","Use in pregnancy: May cause fetal harm; advise females of reproductive potential of potential risk","Administration: Administer subcutaneously; do not administer intravenously"] |
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| Fetal Monitoring |
| Monitor maternal complete blood count, liver and renal function monthly. Fetal ultrasound for growth and anomalies every 4 weeks during second and third trimesters. If accidental exposure, refer for fetal echocardiography and detailed anatomy scan. |
| Fertility Effects | Reversible impairment of spermatogenesis and ovulation in animal studies. Human data limited; may reduce fertility during treatment. Fertility may return after discontinuation. |