Skip to Content

Ibalizumab

Medically reviewed by Drugs.com. Last updated on Jun 19, 2020.

Pronunciation

(eye ba LIZ ue mab)

Index Terms

  • Ibalizumab-uiyk

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Intravenous [preservative free]:

Trogarzo: ibalizumab-uiyk 150 mg/mL (1.33 mL) [contains polysorbate 80]

Brand Names: U.S.

  • Trogarzo

Pharmacologic Category

  • Anti-CD4 Monoclonal Antibody
  • Antiretroviral, Monoclonal Antibody
  • Antiretroviral, Post-Attachment Inhibitor
  • Monoclonal Antibody

Pharmacology

Ibalizumab, a recombinant humanized monoclonal antibody, is a post-attachment inhibitor. It blocks HIV-1 from infecting CD4+ T cells by binding to domain 2 of CD4+ cell receptors leading to a conformational change that blocks the interaction of gp120 and HIV co-receptors; it is active against CCR5 and CXCR4 isolates. The selective binding to domain 2 of the CD4+ cells allows ibalizumab to block HIV entry without causing immunosuppression or depleting CD4+ cell counts (Iacob 2017).

Distribution

Vd: 4.8 L

Half-Life Elimination

3.1 to 3.3 days (Jacobson 2009)

Use: Labeled Indications

HIV-1 infection, treatment: Treatment of HIV-1 infection in combination with other antiretrovirals in heavily treatment-experienced adults with multidrug resistant HIV-1 infection failing their current antiretroviral regimen.

Contraindications

Hypersensitivity to ibalizumab or any component of the formulation.

Dosing: Adult

HIV-1 infection, treatment: IV: Initial: 2 g as a single dose, followed by a maintenance dose of 800 mg every 14 days thereafter.

Missed dose: If a maintenance dose (800 mg) is missed by ≥3 days beyond the originally scheduled dosing day, a loading dose (2 g) should be given as soon as possible. Resume maintenance dosing every 14 days thereafter.

Dosing: Geriatric

Refer to adult dosing.

Reconstitution

IV: Withdraw 1.33 mL from each vial needed for a dose (10 vials for loading dose or 4 vials for maintenance dose) and transfer total volume withdrawn into a 250 mL bag of NS. Do not mix or dilute with other medications.

Administration

IV: For IV administration only. Do not administer IV push or bolus. Administer in the cephalic vein, or if not accessible, an appropriate vein elsewhere may be used.

Administer initial infusion (loading dose) over ≥30 minutes. Observe patient for 1 hour after completion of initial infusion. If no infusion-associated adverse reactions are observed, subsequent infusions (maintenance doses) may be administered over ≥15 minutes and post-infusion observation time may be reduced to 15 minutes. Flush with 30 mL NS after completion of each infusion.

Storage

Store intact vials under refrigeration at 2ºC to 8ºC (36ºF to 46ºF). Do not freeze; protect from light. Diluted solution may be stored at 20°C to 25°C (68°F to 77°F) for ≤4 hours or under refrigeration at 2°C to 8°C (36°F to 46°F) for ≤24 hours. If refrigerated, allow to stand at room temperature for ≥30 minutes but ≤4 hours prior to administration.

Drug Interactions

There are no known significant interactions.

Adverse Reactions

Reactions reported with combination therapy.

1% to 10%:

Dermatologic: Skin rash (5%)

Endocrine & metabolic: Increased serum glucose (>250 mg/dL: 3%), increased uric acid (>12 mg/dL: 3%)

Gastrointestinal: Diarrhea (8%), increased serum lipase (>3 x ULN: 5%), nausea (5%)

Hematologic & oncologic: Decreased hemoglobin (<8.5 g/dL: 3%), decreased neutrophils (<0.6 x 109 cells/L: 5%), decreased platelet count (<50,000/mm3: 3%), leukopenia (<1.5 x 109 cells/L: 5%)

Hepatic: Increased direct serum bilirubin (> ULN: 3%), increased serum bilirubin (≥2.6 x ULN: 5%)

Nervous system: Dizziness (8%)

Renal: Increased serum creatinine (>1.8 x ULN or 1.5 x baseline: 10%)

<1%: Immunologic: Antibody development, immune reconstitution syndrome

Postmarketing:

Dermatologic: Pruritus

Hypersensitivity: Anaphylaxis, hypersensitivity reaction

Miscellaneous: Infusion related reaction

Warnings/Precautions

Concerns related to adverse effects:

• Hypersensitivity and infusion-related reactions: Hypersensitivity and infusion-related reactions, including anaphylaxis, have occurred; symptoms may include dyspnea, angioedema, wheezing, chest pain, chest tightness, cough, hot flush, nausea, and vomiting. Observe patients for 1 hour after completion of infusion for at least the first infusion; if no infusion-related reactions are observed after the first infusion, may reduce postinfusion observation time to 15 minutes for subsequent infusions. Discontinue immediately for severe hypersensitivity/anaphylaxis and initiate appropriate treatment.

• Immune reconstitution inflammatory syndrome: Patients may develop immune reconstitution inflammatory syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment; further evaluation and treatment may be required.

Disease-related concerns:

• Appropriate use: Use is not recommended in antiretroviral therapy-naïve patients.

Dosage form specific issues:

• Polysorbate 80: Contains polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer's labeling.

Monitoring Parameters

CD4 count, HIV RNA plasma levels, infusion-related reactions

Reproductive Considerations

The Health and Human Services (HHS) perinatal HIV guidelines note data are insufficient to recommend ibalizumab for females living with HIV who are not yet pregnant but are trying to conceive.

For males and females living with HIV and planning a pregnancy, maximum viral suppression below the limits of detection with antiretroviral therapy (ART), modification of therapy (if needed), optimization of the woman's health, and a discussion of the potential risks and benefits of ART therapy during pregnancy are recommended prior to conception (HHS [perinatal] 2019)

Pregnancy Considerations

Monoclonal antibodies are known to cross the placenta and fetal exposure to ibalizumab may be expected.

The Health and Human Services (HHS) perinatal HIV guidelines note data are insufficient to recommend ibalizumab for pregnant females living with HIV who are antiretroviral naive, who have had antiretroviral therapy (ART) therapy in the past but are restarting, who require a new ART regimen (due to poor tolerance or poor virologic response of current regimen), or who become pregnant while taking ibalizumab. Available pharmacokinetic data are insufficient to make dosing recommendations.

In general, ART is recommended for all pregnant females living with HIV to keep the viral load below the limit of detection and reduce the risk of perinatal transmission. Therapy should be individualized following a discussion of the potential risks and benefits of treatment during pregnancy. Monitoring of pregnant females is more frequent than in nonpregnant adults. ART should be continued postpartum for all females living with HIV and can be modified after delivery.

Health care providers are encouraged to enroll pregnant females exposed to ibalizumab as early in pregnancy as possible in the Antiretroviral Pregnancy Registry (1-800-258-4263 or http://www.APRegistry.com). Health care providers caring for pregnant females living with HIV and their infants may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2019).

Patient Education

What is this drug used for?

• It is used to treat HIV infection.

• This drug is used with other drugs. Talk with your doctor.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Diarrhea

• Dizziness

• Upset stomach

• Rash

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Chest pain

• Cough

• Hot flashes

• Very upset stomach or throwing up

• Infection

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Related questions