Dosing & Uses
Dosage Forms & Strengths
solution for injection
- 150mg/mL (200mg/1.33mL single-dose vial)
- Must dilute further, see Administration
HIV Infection
Indicated for human immunodeficiency virus-1 (HIV-1) infection in heavily treated adults with multidrug-resistant infection failing their current antiretroviral therapy (ART) regimen; use in combination with other ART drugs
First dose (single loading dose): 2000 mg IV infused over at least 30 min; begin maintenance doses 2 weeks after loading dose; if no infusion-associated adverse reactions occur, subsequent infusions (maintenance doses) can be decreased to 15 minutes or given IV push
Maintenance doses: 800 mg IV q2Weeks infused over 15-30 min or IV push over 30 seconds
Dosage Modifications
Dose modifications of ibalizumab are not required when administered with any other ARTs or any other treatments
Safety and efficacy not established
Adverse Effects
1-10%
Diarrhea (8%)
Dizziness (8%)
Nausea (5%)
Rash (5%)
Laboratory abnormalities ≥grade 3
- Creatinine >1.8x ULN or 1.5x baseline (10%)
- Bilirubin ≥2.6x ULN (5%)
- Lipase >3x ULN (5%)
- Leukocytes <1.5 x 10^9 cells/L (5%)
- Neutrophils <0.6 x 10^9 cell/L (5%)
- Direct bilirubin >ULN (3%)
- Blood glucose >250 mg/dL (3%)
- Uric acid >3x ULN (3%)
- Hemoglobin <8.5 g/dL (3%)
- Platelets <50,000/mm³ (3%)
- Leukocytes <1.5 x 10^9 cells/L (5%)
Postmarketing Reports
- Immune system disorders: Hypersensitivity reactions including infusion-related reactions and anaphylactic reactions reported
- Skin and subcutaneous tissue disorders: Pruritus
Warnings
Contraindications
Prior hypersensitivity reaction to drug or product components
Cautions
Immune reconstitution inflammatory syndrome reported in 1 patient treated with ibalizumab in combination with other ARTs
During the initial phase of combination ARTs, patients whose immune systems respond may develop an inflammatory response to indolent or residual opportunistic infections, which may necessitate further evaluation and treatment
Hypersensitivity reactions including infusion-related reactions and anaphylactic reactions reported following infusion during post-approval use; if signs and symptoms of anaphylactic or other clinically significant hypersensitivity reaction occur, immediately discontinue administration and initiate appropriate treatment
Pregnancy
Pregnancy
There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to antiretrovirals during pregnancy; this registry does not include Trogarzo, but likely includes patients’ concomitant antiretroviral drugs
Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1–800–258–4263
Based on animal data, ibalizumab-uiyk use during pregnancy may cause reversible immunosuppression (CD4+ T cell and B cell lymphocytopenia) in infants exposed to ibalizumab-uiyk in utero; immunoglobulin G (IgG) antibodies, such as ibalizumab-uiyk, are transported across placenta in significant amounts, especially near term; therefore, ibalizumab-uiyk has potential to be transferred from mother to developing fetus
There are no available data on ibalizumab-uiyk use in pregnant women to evaluate for a drug- associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes
Immunoglobulin G (IgG) antibodies are increasingly transported across placenta as pregnancy progresses, with largest amount transferred during third trimester; administration during pregnancy may affect immune responses in the in utero-exposed infant; for infants with perinatal exposure to drug, immune phenotyping of peripheral blood, including CD4+ T cell and B cell counts, recommended; expert consultation is also recommended to provide guidance on monitoring and management (eg, need for antibiotic or immunoprophylaxis) of exposed infants based on degree of immunosuppression observed; safety of administering live or live-attenuated vaccines in exposed infants is unknown
Animal data
- In a reproductive study in monkeys, reversible decreases in CD4+ T cells and B cells and increases in CD8+ T cells were observed within first 4 weeks after birth in infants born to pregnant monkeys receiving ibalizumab-uiyk intravenously; lymphocyte counts returned to near normal levels by 3 months of age; one infant monkey died from a systemic viral infection that may be related to ibalizumab-uiyk-induced immunosuppression; no malformations or premature births were observed in this study
Lactation
Unknown if distributed into breast milk
The Centers for Disease Control and Prevention recommend that HIV-1-infected mothers in United States not breastfeed infants to avoid risking postnatal transmission of HIV-1 infection
Owing to the potential for HIV transmission (in HIV-negative infants), developing viral resistance (in HIV-positive infants), and adverse reactions in a breastfed infant, instruct mothers not to breastfeed
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
CD4-directed post-attachment HIV-1 inhibitor
Recombinant humanized monoclonal antibody; blocks HIV-1 from infecting CD4+ T cells by binding to domain 2 of CD4 and interfering with post-attachment steps required for the entry of HIV-1 virus particles into host cells and preventing the viral transmission that occurs via cell-cell fusion
Binding specificity of ibalizumab to domain 2 of CD4 allows ibalizumab to block viral entry into host cells without causing immunosuppression
Absorption
Single-dose administrations of ibalizumab
- AUC-time curve increased in a greater than dose-proportional manner
Single loading dose followed by a maintenance dose q2wk
- Steady-state concentrations were reached after the first 800-mg maintenance dose with mean concentrations >30 mcg/mL throughout the dosing interval
Distribution
Vd was approximately that of serum volume, at 4.8 L
Excretion
Clearance decreased from 9.54 to 0.36 mL/h/kg
Elimination half-life increased from 2.7 to 64 hr as the dose increased from 0.3 to 25 mg/kg
Administration
IV Compatibilities
0.9% NaCl
IV Preparation
Inspect solution; should appear colorless to slightly yellow and clear to slightly opalescent with no visible particles
Discard vial if solution is cloudy, there is pronounced discoloration, or foreign particulate matter is present
Select appropriate number of vials (200 mg/1.33 mL) required to prepare loading dose (2000 mg) or maintenance doses (800 mg)
Loading dose administered as diluted IV infusion; maintenance dose may be administered as diluted IV infusion or undiluted IV push
IV infusion (diluted)
- Remove flip-off cap from single-dose vial and wipe stopper with alcohol swab
- Insert sterile syringe needle into vial through center of stopper and withdraw 1.33 mL from each vial (small residual amount may remain in vial)
- Discard unused portion and transfer into a 250-mL IV bag of 0.9% NaCl; other IV solutions must not be used to prepare dose
- Once diluted, administer immediately
IV push (undiluted)
- Allow vials to stand at room temperature for ~5 minutes
- Remove flip-off cap from single-dose vial and wipe stopper with alcohol swab
- Insert sterile syringe needle into vial through center of stopper and withdraw 1.33 mL from each vial (small residual amount may remain in vial); discard unused portion
- Administer undiluted solution immediately
IV Administration
Administer by trained medical professional
Administer as an IV infusion or IV push in cephalic vein in right or left arm; if this vein is not accessible, an appropriate vein located elsewhere can be used
IV infusion: Administer loading dose (and optionally, maintenance doses) IV over 30 minutes; after completion, flush line with 30 mL 0.9% NaCl
IV push (maintenance doses only): Administer IV over 30-seconds; after completion, flush line with 2-5 mL 0.9% NaCl
All patients must be observed for 1 hr after completing infusion for at least the first infusion; if the patient does not experience an infusion-associated adverse reaction, the postinfusion observation time can be reduced to 15 minutes thereafter
Missed maintenance dose
- If a maintenance dose (800 mg) is missed by ≥3 days beyond the scheduled dosing day, administer a loading dose (2000 mg) as early as possible
- Resume maintenance dosing (800 mg) every 14 days thereafter
Storage
Unopened vials
- Refrigerate at 2-8°C (36-46°F)
- Do not freeze
- Protect from light
Diluted solution
- If not administered immediately, store at room temperature (20-25°C [68-77°F]) for up to 4 hr OR
- Refrigerate at 2-8°C (36-46°F) for up to 24 hr
- If refrigerated, allow the diluted solution to stand at room temperature (20-25°C [68-77°F]) for at least 30 minutes but no more than 4 hr before administration
Images
BRAND | FORM. | UNIT PRICE | PILL IMAGE |
---|---|---|---|
Trogarzo intravenous - | 200 mg/1.33 mL (150 mg/mL) vial | ![]() | |
Trogarzo intravenous - | 200 mg/1.33 mL (150 mg/mL) vial | ![]() |
Copyright © 2010 First DataBank, Inc.
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