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. |
| Molecular Weight | 1232.86 |
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 | Limited human data; animal studies show no evidence of fetal harm. Use only if clearly needed. |
| 2nd trimester | Limited human data; no known risk from available information. Use if benefit outweighs risk. |
| 3rd trimester | Limited human data; no known risk. Consider use only if benefit outweighs risk. |
Clinical note
Comprehensive clinical and safety monograph for TROGARZO (TROGARZO).
| Placental transfer | Expected to cross placenta due to molecular weight; no data on extent. |
| Breastfeeding | No data on presence in human milk; potential for viral resistance in breastfed infants if HIV-1 suppressed. Advise against breastfeeding in HIV-1 infection per public health guidelines. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Serious Effects |
Patients with a history of hypersensitivity to ibalizumab-uiyk 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 |
| Food/Dietary | No known food interactions. Take with or without food. No dietary restrictions. |
| Clinical Pearls | Trogarzo (ibalizumab-uiyk) is a CD4-directed post-attachment HIV-1 inhibitor used in heavily treatment-experienced adults with multidrug-resistant HIV-1. It is administered intravenously every 2 weeks after a single loading dose. Monitor for immune reconstitution inflammatory syndrome (IRIS) and infusion-related reactions. Do not use in patients with prior hypersensitivity to ibalizumab. Always combine with an optimized background regimen (OBR). Renal impairment requires no dose adjustment; hepatic safety data limited. |
Loading safety data…
| L3 |
| 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). |
| 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. |
| Patient Advice | Trogarzo is given intravenously every 2 weeks after the first dose; do not miss appointments. · You must continue taking your other HIV medicines as prescribed. · Report any signs of allergic reaction during infusion: fever, chills, rash, itching, difficulty breathing. · Trogarzo does not cure HIV or prevent transmission; practice safe sex and avoid sharing needles. · Tell your doctor if you are pregnant, breastfeeding, or planning to become pregnant. |