Basiliximab

Allopathic
Indications
  • Prevention of acute organ rejection in patients receiving renal (kidney) transplantation.
  • Used as part of an immunosuppressive regimen including corticosteroids and other immunosuppressants.
  • Off-label: Occasionally used in heart and liver transplantation to prevent rejection.
Dosage & Administration
  • Route: Intravenous infusion.
  • Adult dose for renal transplant: 20 mg IV within 2 hours prior to transplantation, followed by a second 20 mg dose 4 days after transplantation.
  • Pediatrics: Safety and efficacy not well established; use with caution.
  • Elderly: No specific dose adjustment recommended; monitor closely.
  • Renal or hepatic impairment: No dose adjustment necessary.
  • Administration: Infuse over 20–30 minutes; do not administer as a bolus.
Mechanism of Action (MOA)

Basiliximab is a chimeric monoclonal antibody that binds specifically to the alpha subunit (CD25) of the interleukin-2 receptor on activated T lymphocytes. By blocking IL-2 binding, it inhibits T-cell proliferation and activation, reducing the immune response that causes acute organ rejection.

Pharmacokinetics
  • Absorption: Administered intravenously, ensuring complete bioavailability.
  • Distribution: Primarily stays within the vascular space; volume of distribution approximately 0.15 L/kg.
  • Metabolism: Catabolized by proteolytic enzymes into small peptides and amino acids.
  • Elimination: Half-life about 7 days after repeated dosing; clearance decreases with repeated doses due to receptor saturation.
  • Onset: Rapid receptor binding following infusion.
  • Duration: Effects persist approximately 4 to 6 weeks post-administration.
Pregnancy Category & Lactation
  • Pregnancy: Category C. Animal studies show potential fetal risks; no adequate human studies. Use only if benefits justify risks.
  • Lactation: Unknown if excreted in breast milk; caution advised.
Therapeutic Class
  • Immunosuppressant
  • Monoclonal antibody
  • IL-2 receptor antagonist
Contraindications
  • Known hypersensitivity to basiliximab or its components.
  • History of severe allergic reactions to monoclonal antibodies.
Warnings & Precautions
  • Increased susceptibility to infections and malignancies due to immunosuppression.
  • Monitor for hypersensitivity reactions during and after infusion.
  • Use caution in patients with active infections or pre-existing malignancies.
  • Not indicated for treatment of acute rejection.
Side Effects
  • Common: Peripheral edema, hypertension, nausea, vomiting, diarrhea, tremor, fever.
  • Serious/Rare: Anaphylaxis, increased infection risk, post-transplant lymphoproliferative disorder (PTLD), cardiovascular events.
Drug Interactions
  • No known direct drug interactions.
  • Concomitant immunosuppressants may increase risk of infections; monitor accordingly.
  • Not metabolized by CYP450 enzymes; no CYP450-related interactions.
Recent Updates or Guidelines
  • Basiliximab remains a recommended induction agent for renal transplantation in patients at low to moderate immunologic risk.
  • Enhanced monitoring protocols for infections and malignancies have been emphasized in recent guidelines.
  • No significant changes in dosing or approved indications by regulatory authorities.
Storage Conditions
  • Store refrigerated at 2°C to 8°C (36°F to 46°F).
  • Protect from light and do not freeze.
  • Keep in original carton until use.
  • Single-use vial; discard unused portion.