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 no less than 15 minutes
Maintenance doses: 800 mg IV q2Weeks infused over at least 15-30 min
Also see Administration
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 components of the product
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
No data are available to determine risk during pregnancy
Monoclonal antibodies are transported across the placenta as pregnancy progresses; therefore, ibalizumab has the potential to be transmitted from the mother to the developing fetus
Healthcare providers are encouraged to enroll patients in the Antiretroviral Pregnancy Registry at www.apregistry.com or call 800-258-4263 (Canada and US)
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)
Remove the flip-off cap from the single-dose vial and wipe with an alcohol swab
Insert sterile syringe needle into the vial through the center of the stopper and withdraw 1.33 mL from each vial (a small residual amount may remain in the 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, solution should be administered immediately (also see Storage)
IV Administration
Do not administer as IV push or bolus
Diluted solution should be administered by a trained medical professional
Administer as an IV infusion in the cephalic vein in right or left arm; if this vein is not accessible, an appropriate vein located elsewhere can be used
Duration of the first infusion (loading dose) should be no less than 30 minutes; if no infusion-associated adverse reactions occur, the duration of the subsequent infusions (maintenance doses) can be decreased to no less than 15 minutes
After the infusion is complete, flush IV line with 30 mL of 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
Patient Handout
Formulary
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- Compare formulary status to other drugs in the same class.
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