TROGARZO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TROGARZO (TROGARZO).
Ibalizumab is a humanized monoclonal antibody that binds to the CD4 receptor on T cells, blocking HIV-1 entry into host cells without interfering with CD4's normal immune function.
| Metabolism | Ibalizumab is a monoclonal antibody; metabolism is not via CYP450 enzymes. Clearance likely via proteolytic catabolism. |
| Excretion | Renal: negligible. Biliary/fecal: primarily eliminated as unchanged drug via biliary secretion into feces. No significant renal elimination. |
| Half-life | Terminal half-life approximately 27 days. This long half-life supports monthly intravenous dosing intervals in HIV-1 treatment. |
| Protein binding | Approximately 99.9% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Vd ≈ 0.09 L/kg (approximately 6.5 L for a 70 kg adult), indicating minimal distribution beyond plasma volume, consistent with a large monoclonal antibody. |
| Bioavailability | Intravenous: 100% (only route of administration). Not administered orally or via other routes. |
| Onset of Action | Intravenous: clinical antiviral effect observed within 1–2 weeks after first dose, with maximal viral load reduction achieved by 2–4 weeks. |
| Duration of Action | Duration of antiviral effect extends beyond the dosing interval (every 4 weeks) due to long half-life; viral suppression maintained throughout the monthly dosing period. |
Trogarzo (ibalizumab-uiyk) is administered intravenously. The recommended dose is a single loading dose of 2000 mg, followed by a maintenance dose of 800 mg every 2 weeks. Each dose is infused over 15-30 minutes after dilution in 0.9% Sodium Chloride Injection.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment is required for patients with renal impairment, including those on hemodialysis. Trogarzo has not been studied in patients with end-stage renal disease, but based on its metabolism, no adjustment is expected. |
| Liver impairment | No dose adjustment is required for patients with mild to moderate hepatic impairment (Child-Pugh class A or B). Trogarzo has not been studied in patients with severe hepatic impairment (Child-Pugh class C). |
| Pediatric use | The safety and efficacy of Trogarzo in pediatric patients less than 18 years of age have not been established. No dosing recommendations are available. |
| Geriatric use | No specific dose adjustment is recommended for elderly patients. Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Dose selection should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TROGARZO (TROGARZO).
| Breastfeeding | It is not known whether ibalizumab is present in human breast milk, affects the breastfed infant, or affects milk production. Due to the potential for HIV-1 transmission (in HIV-negative infants) and possible adverse effects, breastfeeding is not recommended for HIV-infected women. The M/P ratio is not known. |
| Teratogenic Risk | Trogarzo (ibalizumab-uiyk) is a CD4-directed post-attachment HIV-1 inhibitor. No adequate and well-controlled studies in pregnant women. In animal reproduction studies, no evidence of fetal harm was observed at doses up to 10 times the human dose. However, because animal studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed. The risk of neural tube defects is highest in the first trimester; HIV infection itself poses risks to the fetus. Placental transfer of ibalizumab is expected to be low due to its large molecular weight (approximately 150 kDa). |
■ FDA Black Box Warning
None
| Serious Effects |
["History of hypersensitivity to ibalizumab or any component of the formulation"]
| Precautions | ["Immune reconstitution syndrome","Hypersensitivity reactions including anaphylaxis","Increased risk of infections","Interference with CD4 and HIV viral load monitoring"] |
Loading safety data…
| Fetal Monitoring | Monitor maternal CD4 count, HIV viral load, and clinical status throughout pregnancy. Assess for infusion-related reactions (e.g., rash, pyrexia, chills). Perform standard obstetric monitoring. Fetal ultrasound may be considered if maternal condition warrants. |
| Fertility Effects | No data on the effect of ibalizumab on fertility in humans. Animal studies have not shown impairment of male or female fertility at doses up to 10 times the human dose. |