Basiliximab (Simulect) for transplant rejection: Uses, Dose, Brands, Side effects

Basiliximab (Simulect) is a chimeric monoclonal antibody that inhibits the binding of IL-2 to its receptors. It is primarily used as an immunosuppressant in patients with organ transplantation.

A It is used in the following conditions:  

  • For the prophylactic treatment of acute Renal transplant rejection in combination with cyclosporin and corticosteroids.
    • Except in patients at high immunologic risk, KDIGO recommendations advise against using interleukin 2 receptor antagonist (basiliximab/simulect) as the first-line induction medication to prevent acute kidney transplant rejection.
  • It is also used as an Off Label medicine in the following conditions:
    • for the purpose of treating acute graft-versus-host disease that is refractory
    • for the preventative management of acute heart transplant rejection
    • for the preventative management of acute liver transplant rejection
    • for the preventative management of acute lung transplant rejection

Basiliximab Dose in Adults

Note: Re-exposure is associated with severe anaphylactic reactions and should be used with extreme caution. 

Basiliximab dose in the prophylactic treatment of acute Renal transplant rejection:  

  • 20 mg intravenously two hours prior to the transplant procedure, and a second 20 mg dosage four days following the transplant.
  • Patients who develop severe allergic reactions to the first dose should not be given the second dose.

Basiliximab dose for off-label use in patients with refractory acute graft-versus-host disease (aGVHD)

  • 20 mg intravenous on days 1 and 4.
  • The dose may be repeated.

Off-label use to prevent acute Heart transplant rejection:

  • 20 mg intravenous on the day of the transplant, immediately and preferably within one hour after the transplant.
  • The second 20 mg dose is administered on the fourth day after transplantation along with other immunosuppressants.

Off-label use to prevent acute rejection of Liver transplant:  

  • 20 mg intravenous on the day of the transplant, administered during the procedure after securing hemostasis, immediately after the transplant, or within 6 hours of organ perfusion.
  • The second dose is given as 20 mg intravenous on the fourth day after transplantation along with other immunosuppressants.

Off-label use to prevent acute rejection of lung transplant:

  • 20 mg intravenous before the transplant.
  • A second dose of 20 mg should be administered 4 days after the transplant along with other immunosuppressants.

Basiliximab (Simulect) Dose in Children

Note: Re-exposure is associated with severe anaphylactic reactions and should be used with extreme caution. 

Simulect Dose in the Treatment of Heart Transplantation:

  • Patients weighing less than 35 kgs:
    • 10 mg given either before surgery or six hours after organ perfusion followed by a repeat dose after 4 days of transplantation.
  • Patients weighing more than 35 kg:
    • 20 milligrams; administered IV either before the surgery or six hours after perfusion, followed by a repeat dose four days after the transplantation.

Basiliximab Dose in the Treatment of Liver Transplantation:

  • Patients weighing less than 35 kgs:
    • 10 mg IV within six hours of organ perfusion, followed by 10 mg four days after the surgery.
    • A third dose may be given 8 to 10 days after transplantation to patients who have ascites of more than 5 liters or who lose more than 70 ml/kg of body fluid during the surgery.
  • Patients weighing more than 35 kg:
    • 20 mg IV within six hours of organ perfusion, followed by 20 mg four days after the surgery.
    • A third dose may be given 8 to 10 days after transplantation to patients who have ascites of more than 5 liters or who lose more than 70 ml/kg of body fluid during the surgery.

Basiliximab dose for kidney transplantation in children:  

  • Children and Adolescents:
    • Patients weighing more than 35 kg:
      • 20 mg administered IV  two hours before the kidney transplant, followed by a repeat 20 mg four days after the procedure.
    • Patients weighing less than 35 kgs:
      • 10 mg given IV two hours prior to the kidney transplant procedure, followed by 10 mg four days after the procedure.

Pregnancy Risk Factor: B

  • It is an IL-2 receptor-specific monoclonal chimeric IgG antibody.
  • The manufacturer suggests that effective contraception be used before and for at least 4 months following the last dose.
  • IgG antibodies cross over the placental boundary, but adverse fetal events were not observed in animal studies.

Use Basiliximab while breastfeeding

  • It is not clear if the drug can be absorbed into breast milk.
  • However, there is a risk of serious adverse events due to the fact that immunoglobulins can be found in breast milk.
  • During the treatment, it is important to stop breastfeeding.

Basiliximab Dose in Renal Disease:

No recommendations are available regarding dose adjustment in renal disease.

Basiliximab Dose in Liver Disease:

No recommendations are available regarding dose adjustment in liver disease.

Side Effects of Basiliximab Include:

  • Central Nervous System:
    • Headache
    • Insomnia
    • Pain
  • Endocrine & Metabolic:
    • Hyperuricemia,
    • Hypokalemia
    • Hypercholesterolemia
    • Hyperglycemia
    • Hyperkalemia
    • Hypophosphatemia
  • Cardiovascular:
    • Hypertension
    • Peripheral Edema
  • Dermatologic:
    • Acne Vulgaris
  • Genitourinary:
    • Urinary Tract Infection
  • Gastrointestinal:
    • Nausea and vomiting
    • Abdominal Pain
    • Constipation or Diarrhea
    • Dyspepsia
  • Hematologic & Oncologic:
    • Anemia
  • Neuromuscular & Skeletal:
    • Tremor
  • Respiratory:
    • Dyspnea
    • Upper Respiratory Infection
  • Infection:
    • Viral Infection
  • Miscellaneous:
    • Fever
    • Postoperative Wound Complication

Less Common Side Effects Of Basiliximab:

  • Cardiovascular:
    • Cardiac
    • Low BP
    • Tachycardia
    • Thrombosis
    • Arrhythmia
    • Cardiac Failure
    • Abnormal Heart Sounds
    • Angina Pectoris
    • Atrial Fibrillation
    • Chest Pain
  • Central Nervous System:
    • Blackouts
    • Fatigue
    • Hypoesthesia
    • Agitation
    • Anxiety
    • Depression
    • Malaise
    • Rigors
  • Dermatologic:
    • Hypertrichosis
    • Pruritus
    • Dermal Ulcer
    • Dermatological Disease
    • Skin Rash
  • Endocrine & Metabolic:
    • Diabetes Mellitus
    • Hypertriglyceridemia
    • Acidosis
    • Albuminuria
    • Anasarca
    • Dehydration
    • Hypervolemia
    • Hypocalcemia
    • Hypoglycemia
    • Hypomagnesemia
    • Hyponatremia
    • Increased Nonprotein Nitrogen
    • Increased
    • Serum Glucocorticoids
    • Hypercalcemia
    • Hyperlipidemia
    • Weight Gain
  • Gastrointestinal:
    • Gastroenteritis
    • Melena
    • Stomatitis
    • Gastrointestinal Hemorrhage
    • Gi Moniliasis
    • Gingival Hyperplasia
    • Enlargement Of Abdomen
    • Esophagitis
    • Flatulence
    • Hernia
  • Hematologic & Oncologic:
    • Polycythemia
    • Purpura
    • Thrombocytopenia
    • Infection
    • Hematoma
    • Hemorrhage
    • Sepsis
    • Hypoproteinemia
    • Leukopenia
    • Cytomegalovirus Disease
    • Herpes simplex and herpes Zoster Virus Infection
  • Genitourinary:
    • Urinary Frequency
    • Urinary Retention
    • Hematuria
    • Impotence
    • Oliguria
    • Ureteral Disease
    • Bladder Dysfunction
    • Dysuria
    • Genital Edema (Male)
  • Ophthalmic:
    • Cataract
    • Conjunctivitis
    • Visual Disturbance
  • Neuromuscular & Skeletal:
    • Bone Fracture
    • Leg Pain
    • Neuropathy
    • Paresthesia
    • Muscle
    • Cramps
    • Myalgia
    • Arthralgia
    • Arthropathy
    • Back Pain
    • Weakness
  • Miscellaneous:
    • Accidental Injury
    • Cyst
  • Renal:
    • Renal Insufficiency
    • Renal Tubular Necrosis
  • Respiratory:
    • Pharyngitis
    • Pneumonia
    • Pulmonary Edema
    • Bronchitis
    • Bronchospasm
    • Cough
    • Rhinitis
    • Sinusitis

Contraindications to Basiliximab (Simulect):

  • allergies to basiliximab and any of the components of the formulation

Cautions and alerts

Anaphylactoid reactions and hypersensitivity reactions

  • Severe allergic reactions can occur, especially during the first 24 hours of administering the drug. Allergic reactions can occur even months after the dose is administered.
  • Patients who have been previously exposed to basiliximab should be cautious when using it. If you notice serious adverse reactions, they should be stopped immediately.
  • Anaphylactic reactions such as epinephrine should be treated with medication.

Diabetes:

  • NODAT (New-onset Diabetes Mellitus after Transplant) and PTDM (Post-Transplant Diabetes Mellitus), are well-known entities.
  • It could be due to the transplant or drugs such as basiliximab plus prednisone and cyclosporine.

Opportunistic Infections

  • The use of immunosuppressive therapy can lead to opportunistic infections that could be potentially life-threatening.

Anti-human antibodies against murine (HAMA)

  • Although HAMA may be developed through its use, it is not yet known if HAMA has any clinical value.

Lymphoproliferative diseases:

  • Immunosuppressive treatment may cause a rise in lymphoproliferative diseases.

Monitoring Parameters:

  • Monitor for allergic reactions during the infusion and clinical features of rejection.

How to administer Basiliximab?

  • It should only be administered via the intravenous route.
  • It may be infused over 20 - 30 minutes as a bolus through a peripheral or a central venous line.
  • Bolus infusion may be associated with pain at the injection site, nausea, and vomiting.

Mechanism of action of Basiliximab:

  • Basiliximab, a monoclonal immunosuppressant monoclonal anti-immune suppressant chimeric (combined human and murine antibody), is called. 
  • It prevents the interleukin-2 receptor complex's alpha chain from functioning (IL-2).
  • On activated T lymphocytes, the Interleukin-2 receptor can be found. 
  • It is one of the key steps that results in cell-mediated rejection.

It has a median duration of action of 36 days +/- 14 days.

It has a half-life of 5-13 days for children and 4-10 days for adults. A significant amount of drugs is lost in the liver of patients undergoing liver transplants. This increases the total body clearance and decreases the duration of CD 25 (IL-2R) receptor saturation. These cases may require that the dose be adjusted.    

International Brands of Basiliximab:

  • Simulect

Basiliximab Brands in Pakistan:

Basiliximab [Inj 20 mg/vial]

Simulect

Novartis Pharma (Pak) Ltd