CD4-directed post-attachment HIV-1 inhibitor
HIV-1 infection in heavily treatment-experienced adults with multidrug resistant HIV-1 infection who are failing their current antiretroviral regimen (in combination with other antiretroviral agents).
Monoclonal antibody that blocks HIV-1 from infecting CD4+ T cells by binding to CD4 and interfering with post-attachment steps required for the entry of HIV-1 virus particles into host cells and preventing viral transmission. Blocks viral entry into host cells without causing immunosuppression. Active against CCR5 and CXCR4 isolates.
Reduction in viral load.
Absorption: IV administration results in complete bioavailability.
Distribution: Minimally distributed to tissues.
Metabolism and Excretion: Unknown.
Half-life: 2.7–64 hr (dose dependent).
TIME/ACTION PROFILE (plasma concentrations)
- Lactation: Breastfeeding not recommended in HIV-positive mothers.
Use Cautiously in:
- OB: May cause reversible immunosuppression in infants exposed in utero; use during pregnancy only if potential maternal benefit justifies potential fetal risk;
- Pedi: Safety and effectiveness not established in children.
Adverse Reactions/Side Effects
Endo: hyperglycemia, hyperuricemia
GI: diarrhea, hyperbilirubinemia, ↑ lipase, nausea
GU: ↑ serum creatinine
Hemat: anemia, leukopenia, neutropenia, thrombocytopenia
Misc: HYPERSENSITIVITY REACTIONS (including anaphylaxis), INFUSION REACTIONS, immune reconstitution inflammatory syndrome
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
IV (Adults): 2000 mg single dose (loading dose), then 800 mg every 2 wk.
Solution for injection: 150 mg/mL
- Monitor for change in severity of HIV symptoms and for symptoms of opportunistic infection before and during therapy.
Monitor for signs and symptoms of infusion reaction (dyspnea, angioedema, wheezing, chest pain, chest tightness, cough, hot flush, nausea, vomiting) for 1 hr after first infusion. If no reactions occur, monitor for 15 min following subsequent infusions. If signs of anaphylactic reaction occur, discontinue infusion immediately and treat symptoms.
Lab Test Considerations:
Monitor viral load and CD4 count before and routinely during therapy to determine response.
- If a maintenance dose (800 mg) is missed by ≥3 days, administer a loading dose (2,000 mg) as soon as possible. Then resume maintenance dosing (800 mg) every 14 days.
- Intermittent Infusion: Dilution: Withdraw 1.33 mL from each vial and transfer to 250 mL bag of 0.9% NaCl. Do not use other diluents. Discard unused solution.Diluted solution is stable for up to 4 hr at room temperature or 24 hr if refrigerated. Allow refrigerated solution to stand at room temperature for at least 30 min before infusion. Solution is colorless to slightly yellow and clear to slightly opalescent; do not infuse solutions that are cloudy, discolored, or contain particulate matter.
- Rate: Administer infusion in the cephalic vein of the arm. If this vein is not accessible, an appropriate vein located elsewhere can be used. Do not administer IV push or bolus. Infuse loading dose over at least 30 min. If no infusion-related reactions occur, infuse subsequent infusions over at least 15 min. Flush line with 30 mL of 0.9% NaCl after infusion.
- Explain purpose of ibalizumab and importance of every 2 wk infusions to patient; do not change dosing schedule without consulting health care professional. Advise patient to read Patient Information before starting therapy and periodically in case of changes.
Advise patient to notify health care professional immediately if signs and symptoms of hypersensitivity reactions (trouble breathing, cough, swelling in throat, hot flush, wheezing, nausea, chest pain, vomiting, chest tightness) or Immune Reconstitution Syndrome (signs and symptoms of an infection) occur.
- Caution patient to avoid crowds and persons with known infections.
- Inform patient that ibalizumab does not cure AIDS and may reduce the risk of transmission of HIV to others through sexual contact or blood contamination. Caution patient to use a condom and avoid sharing needles or donating blood to prevent spreading HIV to others.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
- Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. May cause reversible immunosuppression (CD4+ T cell and B cell lymphocytopenia) in infants exposed to ibalizumab in utero. Inform pregnant women of the pregnancy exposure registry that monitors pregnancy outcomes in women exposed to antiretrovirals during pregnancy. Register patient in the Antiretroviral Pregnancy Registry by calling 1-800-258-4263.
- Delayed progression of AIDS and decreased opportunistic infections in patients with HIV.
- Decrease in viral load and improvement in CD4 cell counts.