BREKIYA (AUTOINJECTOR)
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BREKIYA (AUTOINJECTOR) (BREKIYA (AUTOINJECTOR)).
Interleukin-17A (IL-17A) antagonist; selectively binds to IL-17A and inhibits its interaction with the IL-17 receptor, thereby reducing inflammatory responses.
| Metabolism | Likely catabolized into small peptides and amino acids via general protein degradation pathways; not metabolized by CYP450 enzymes. |
| Excretion | Primarily via reticuloendothelial system catabolism; Bimekizumab is a monoclonal antibody degraded into small peptides and amino acids. Renal and fecal excretion of intact drug is minimal (<1%). |
| Half-life | Terminal elimination half-life is approximately 23-26 days. This supports every 4-week subcutaneous dosing. |
| Protein binding | Bimekizumab binds to both IL-17A and IL-17F; specific plasma protein binding data not reported. Estimated low nonspecific binding typical of monoclonal antibodies. |
| Volume of Distribution | Volume of distribution is approximately 6.4 L (about 0.09 L/kg). Consistent with limited extravascular distribution of IgG antibodies. |
| Bioavailability | Subcutaneous: Absolute bioavailability is approximately 80% after SC injection using the autoinjector. |
| Onset of Action | Subcutaneous: Clinical improvement may be observed as early as 2 weeks after the first dose. |
| Duration of Action | Subcutaneous: Sustained effect over the dosing interval of 4 weeks. Continuous therapy maintains suppression of IL-17A and IL-17F-mediated inflammation. |
Adult: 200 mg subcutaneously once weekly. Administer via autoinjector. No loading dose required.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment recommended for mild to moderate renal impairment (eGFR ≥30 mL/min/1.73 m²). Not studied in severe renal impairment (eGFR <30 mL/min/1.73 m²) or end-stage renal disease. |
| Liver impairment | No dose adjustment recommended for mild hepatic impairment (Child-Pugh Class A). Not studied in moderate (Child-Pugh Class B) or severe (Child-Pugh Class C) hepatic impairment. |
| Pediatric use | Not approved for pediatric use; safety and efficacy not established in patients <18 years of age. |
| Geriatric use | No specific dose adjustment recommended for elderly patients (≥65 years). Limited data suggest no overall differences in safety or efficacy, but greater sensitivity of some older individuals cannot be ruled out. Monitor renal function as part of baseline assessment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BREKIYA (AUTOINJECTOR) (BREKIYA (AUTOINJECTOR)).
| Breastfeeding | Unknown if brodalumab is excreted in human milk, nor if absorbed systemically in the neonate. M/P ratio not available. Because of potential for adverse reactions in breastfed infants from IgG antibodies, advise against breastfeeding during treatment and for at least 5 half-lives after last dose. |
| Teratogenic Risk | Pregnancy Category C. In animal reproduction studies, administration of brodalumab during organogenesis resulted in increased fetal malformations and embryolethality at doses 10-30 times the human exposure. No adequate human studies exist. First trimester: potential teratogenic risk based on animal data; avoid use. Second and third trimesters: may cross placenta; risk of fetal immune modulation. Use only if potential benefit justifies risk. |
■ FDA Black Box Warning
Increased risk of serious infections leading to hospitalization or death, including tuberculosis, invasive fungal infections, and other opportunistic infections.
| Serious Effects |
["Known hypersensitivity to brodalumab or any component of the formulation","Active Crohn's disease (relative)"]
| Precautions | ["Serious infections","Hypersensitivity reactions including anaphylaxis","Inflammatory bowel disease exacerbation","Vaccination avoidance with live vaccines","Hepatic impairment monitoring"] |
| Food/Dietary | No clinically significant food interactions. May be taken with or without food. |
| Clinical Pearls |
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| Fetal Monitoring | Monitor for signs of infection in mother and fetus/neonate due to immunosuppression. Ultrasound for fetal growth and anatomy if exposed during pregnancy. Monitor neonate for immune-related adverse effects. Pre-pregnancy counseling recommended. No specific fetal monitoring required. |
| Fertility Effects | No human data on fertility effects. Animal studies showed no impairment of male or female fertility at subtoxic doses. However, consider potential impact of chronic inflammatory disease on fertility; brodalumab may improve fertility by controlling disease activity. |
| Brekiya (bimekizumab) is a humanized monoclonal IgG1 antibody that inhibits both IL-17A and IL-17F. It is administered subcutaneously via autoinjector. Shake the autoinjector gently for 10 seconds before use. Do not inject into areas of active psoriasis or where skin is tender, bruised, or scarred. Rotate injection sites. Avoid live vaccines during treatment. Monitor for hypersensitivity reactions, including angioedema and urticaria. Assess for latent tuberculosis prior to initiation. |
| Patient Advice | Store Brekiya in the refrigerator at 2°C to 8°C (36°F to 46°F). Do not freeze. · Keep the autoinjector in the original carton to protect from light. · Remove the autoinjector from the refrigerator 30 minutes before injection to reach room temperature; do not warm in any other way. · Do not shake the autoinjector until instructed; gently shake for 10 seconds immediately before use. · Inject subcutaneously into the thigh, abdomen (avoid 2 inches around navel), or upper arm at a 45-90 degree angle. · Do not reuse or share the autoinjector; dispose of used devices in a puncture-resistant container. · Contact your healthcare provider if you experience signs of infection, allergic reaction, or injection site pain that persists. · Avoid live vaccinations during treatment with Brekiya. · Inform all healthcare providers of Brekiya use before any surgery or vaccination. |