BRIUMVI
Clinical safety rating
cautionComprehensive clinical and safety monograph for BRIUMVI (BRIUMVI).
Comprehensive clinical and safety monograph for BRIUMVI (BRIUMVI).
Relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults
BRIUMVI (ublituximab) is a recombinant, chimeric, humanized monoclonal antibody that binds to CD20, a transmembrane antigen expressed on pre-B and mature B lymphocytes. Binding to CD20 results in antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC), leading to B-cell depletion.
| Metabolism | Ublituximab is a monoclonal antibody catabolized into small peptides and amino acids via general protein degradation pathways; no specific metabolic enzymes are involved. |
| Excretion | BRIUMVI (ublituximab) is a monoclonal antibody. Elimination occurs via intracellular catabolism and is not excreted renally or fecally in significant amounts. No specific excretion data available. |
| Half-life | Terminal elimination half-life is approximately 19-20 days (range 11-30 days) in patients with relapsing multiple sclerosis. The long half-life supports every-6-month dosing. |
| Protein binding | Not extensively bound to plasma proteins (expected low binding for monoclonal antibodies); specific % not reported. |
| Volume of Distribution | Approximately 3.5 L (not weight-based; ~0.05 L/kg for a 70 kg patient). Small Vd consistent with limited extravascular distribution of monoclonal antibodies. |
| Bioavailability | 100% (intravenous administration only; not administered via other routes). |
| Onset of Action | IV infusion: Clinical effect on MRI lesions (reduction in new Gd-enhancing lesions) observed within 12 weeks. Time to maximum B-cell depletion: 2-4 weeks post-dose. |
| Duration of Action | B-cell depletion lasts approximately 4-6 months post-dose, with gradual recovery over 6-12 months. Dosing every 6 months maintains suppression. |
| Molecular Weight | 150000 |
BRIUMVI (ublituximab) 150 mg administered as an intravenous infusion over 4 hours once weekly for 3 weeks, then 150 mg once every 6 months thereafter.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment is recommended for patients with mild to moderate renal impairment. Not studied in severe renal impairment (GFR <30 mL/min) or end-stage renal disease. |
| Liver impairment | No dose adjustment recommended for mild hepatic impairment (Child-Pugh A). Not studied in moderate (Child-Pugh B) or severe (Child-Pugh C) hepatic impairment. |
| Pediatric use | Safety and effectiveness in pediatric patients (age <18 years) have not been established. No recommended dosing. |
| Geriatric use | No specific dose adjustment is recommended. Clinical studies did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger patients. |
| 1st trimester | Limited data; based on mechanism (CD20-directed cytolytic antibody), potential for fetal B-cell depletion. Use only if benefit outweighs risk. |
| 2nd trimester | May cause fetal B-cell depletion and transient lymphocytopenia; consider risks. |
| 3rd trimester | May cause neonatal B-cell depletion and hematologic abnormalities; avoid near term unless necessary. |
Clinical note
Comprehensive clinical and safety monograph for BRIUMVI (BRIUMVI).
| Placental transfer | Substantial transfer, especially in second and third trimesters (monoclonal IgG1 antibody) |
| Breastfeeding | Unknown if excreted in human milk; due to large molecular weight (approx. 150 kDa), passage into milk is likely limited but not confirmed. Consider risks of infant exposure, including potential for B-cell depletion. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | BRIUMVI (ublituximab) is a monoclonal antibody, and IgG antibodies are known to cross the placenta increasingly after the first trimester, with highest transfer in the third trimester. Based on its mechanism of action (CD20-mediated B-cell depletion), there is a potential risk of transient peripheral B-cell depletion in the fetus. Animal studies have not been conducted with ublituximab; however, other anti-CD20 antibodies have shown no teratogenicity but can cause neonatal B-cell depletion. The drug should be avoided during pregnancy unless the benefit justifies the potential risk. |
| Fetal Monitoring | Monitor for infusion reactions during administration. In pregnant women, consider monitoring fetal B-cell counts via cord blood at delivery if exposure occurred in the third trimester. Assess neonatal immunizations as live vaccines are contraindicated after in utero exposure. |
| Fertility Effects | No formal fertility studies have been conducted with ublituximab. Based on its pharmacological action (B-cell depletion), it may impact fertility by affecting immune regulation, but no specific data are available. Menstrual irregularities or effects on ovarian reserve have not been reported. |
■ FDA Black Box Warning
None
| Serious Effects |
Active hepatitis B infectionSevere active infections
| Precautions | Infusion reactions (may require premedication and monitoring), Increased risk of infections (including serious and life-threatening infections), Progressive multifocal leukoencephalopathy (PML) in patients treated with anti-CD20 therapies, Hepatitis B reactivation (perform HBV screening before initiation), Immunoglobulin levels reduction requiring monitoring, Increased risk of malignancies (breast cancer observed in clinical trials) |
| Food/Dietary | No known food interactions. Grapefruit and other CYP450 modulators are not expected to affect ublituximab as it is a monoclonal antibody cleared via catabolism. |
| Clinical Pearls | Premedicate with corticosteroids, antihistamines, and acetaminophen to reduce infusion reactions. Monitor for hypersensitivity reactions, especially during first infusion. Screen for hepatitis B and tuberculosis before initiation. Avoid live vaccines during treatment. Consider JCV antibody status due to risk of progressive multifocal leukoencephalopathy (PML) with anti-CD20 therapies. |
| Patient Advice | You must take premedications before each infusion to lower the risk of allergic reactions. · Report any symptoms like fever, chills, rash, or difficulty breathing during or after infusion. · Inform your doctor if you have a history of hepatitis B, tuberculosis, or any infections. · Do not receive live vaccines while on this medication and for a period after stopping. · This drug may increase your risk of infections; contact your doctor if you develop signs of infection. · You will need regular blood tests to monitor for side effects. |
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