(ba si LIK si mab)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution Reconstituted, Intravenous [preservative free]:
Simulect: 10 mg (1 ea); 20 mg (1 ea)
Brand Names: U.S.
- Immunosuppressant Agent
- Monoclonal Antibody
Chimeric (murine/human) immunosuppressant monoclonal antibody which blocks the alpha-chain of the interleukin-2 (IL-2) receptor complex; this receptor is expressed on activated T lymphocytes and is a critical pathway for activating cell-mediated allograft rejection
Mean: Vd: Children 1 to 11 years: 4.8 ± 2.1 L; Adolescents 12 to 16 years: 7.8 ± 5.1 L; Adults: 8.6 ± 4.1 L
Children 1 to 11 years: 17 ± 6 mL/hour; in pediatric liver transplant patients, significant basiliximab loss through ascites fluid can increase total body clearance and reduce IL-2R (CD25) saturation duration; dosage adjustments may be necessary (Cintorino 2006; Kovarik 2002; Spada 2006)
Adolescents 12 to 16 years: 31 ±19 mL/hour
Adults: 41 ± 19 mL/hour
Duration of Action
Mean: 36 ± 14 days (determined by IL-2R alpha saturation in patients also on cyclosporine and corticosteroids)
Children 1 to 11 years: 9.5 ± 4.5 days; Adolescents 12 to 16 years: 9.1 ± 3.9 days; Adults: Mean: 7.2 ± 3.2 days
Special Populations: Children
Distribution volume and clearance are reduced about 50% compared with adult renal transplant patients.
Use: Labeled Indications
Renal transplant rejection: Prophylaxis of acute organ rejection in renal transplantation in combination with cyclosporine (modified) and corticosteroids
Treatment of refractory acute graft-versus-host disease (GVHD); prevention of liver or cardiac transplant rejection
Known hypersensitivity to basiliximab or any component of the formulation
Note: Patients previously administered basiliximab should only be re-exposed to a subsequent course of therapy with extreme caution.
Acute renal transplant rejection prophylaxis: Note: Use in pediatric patients is not approved in the Canadian labeling (limited pharmacokinetic data available).
Children <35 kg: IV: 10 mg within 2 hours prior to transplant surgery, followed by a second 10 mg dose 4 days after transplantation; the second dose should be withheld if complications occur (including severe hypersensitivity reactions or graft loss)
Children ≥35 kg and Adults: IV: 20 mg within 2 hours prior to transplant surgery, followed by a second 20 mg dose 4 days after transplantation; the second dose should be withheld if complications occur (including severe hypersensitivity reactions or graft loss)
Acute cardiac transplant rejection prophylaxis (off-label use): Adults: IV: 20 mg on the day of transplant, followed by a second dose 4 days after transplantation (Mehra, 2005); usually given within the first hour postoperatively
Acute liver transplant rejection prophylaxis (off-label use): Adults: IV: 20 mg within 6 hours of organ reperfusion, followed by a second 20 mg dose 4 days after transplantation (Neuhaus, 2002)
Treatment of refractory acute GVHD (off-label use): Adults: IV: 20 mg on days 1 and 4; may repeat for recurrent acute GVHD (Schmidt-Hieber, 2005). Additional data may be necessary to further define the role of basiliximab in this condition.
Dosage adjustment in renal impairment: There are no dosage adjustments provided in the manufacturer’s labeling.
Dosage adjustment in hepatic impairment: There are no dosage adjustments provided in the manufacturer’s labeling.
Reconstitute with preservative-free sterile water for injection (reconstitute 10 mg vial with 2.5 mL, 20 mg vial with 5 mL). Shake gently to dissolve. May further dilute reconstituted solution with 25 mL (10 mg) or 50 mL (20 mg) 0.9% sodium chloride or dextrose 5% in water. When mixing the solution, gently invert the bag to avoid foaming. Do not shake solutions diluted for infusion.
For intravenous administration only. Infuse as a bolus or IV infusion over 20-30 minutes. (Bolus dosing is associated with nausea, vomiting, and local pain at the injection site.) Administer only after assurance that patient will receive renal graft and immunosuppression. For the treatment of acute GVHD (off-label use), the dose was diluted in 250 mL NS and administered over 30 minutes (Schmidt-Hieber, 2005).
Store intact vials refrigerated at 2°C to 8°C (36°F to 46°F). Should be used immediately after reconstitution; however, if not used immediately, reconstituted solution may be stored at 2°C to 8°C for up to 24 hours or at room temperature for up to 4 hours. Discard the reconstituted solution if not used within 24 hours.
BCG (Intravesical): Immunosuppressants may diminish the therapeutic effect of BCG (Intravesical). Avoid combination
Belimumab: Monoclonal Antibodies may enhance the adverse/toxic effect of Belimumab. Avoid combination
Coccidioides immitis Skin Test: Immunosuppressants may diminish the diagnostic effect of Coccidioides immitis Skin Test. Monitor therapy
Denosumab: May enhance the adverse/toxic effect of Immunosuppressants. Specifically, the risk for serious infections may be increased. Monitor therapy
Echinacea: May diminish the therapeutic effect of Immunosuppressants. Consider therapy modification
Fingolimod: Immunosuppressants may enhance the immunosuppressive effect of Fingolimod. Management: Avoid the concomitant use of fingolimod and other immunosuppressants when possible. If combined, monitor patients closely for additive immunosuppressant effects (eg, infections). Consider therapy modification
Leflunomide: Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly. Consider therapy modification
Natalizumab: Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Avoid combination
Pimecrolimus: May enhance the adverse/toxic effect of Immunosuppressants. Avoid combination
Roflumilast: May enhance the immunosuppressive effect of Immunosuppressants. Consider therapy modification
Sipuleucel-T: Immunosuppressants may diminish the therapeutic effect of Sipuleucel-T. Monitor therapy
Tacrolimus (Topical): May enhance the adverse/toxic effect of Immunosuppressants. Avoid combination
Tofacitinib: Immunosuppressants may enhance the immunosuppressive effect of Tofacitinib. Management: Concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted, and this warning seems particularly focused on more potent immunosuppressants. Avoid combination
Trastuzumab: May enhance the neutropenic effect of Immunosuppressants. Monitor therapy
Vaccines (Inactivated): Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Management: Vaccine efficacy may be reduced. Complete all age-appropriate vaccinations at least 2 weeks prior to starting an immunosuppressant. If vaccinated during immunosuppressant therapy, revaccinate at least 3 months after immunosuppressant discontinuation. Consider therapy modification
Vaccines (Live): Immunosuppressants may enhance the adverse/toxic effect of Vaccines (Live). Immunosuppressants may diminish the therapeutic effect of Vaccines (Live). Management: Avoid use of live organism vaccines with immunosuppressants; live-attenuated vaccines should not be given for at least 3 months after immunosuppressants. Avoid combination
Administration of basiliximab did not appear to increase the incidence or severity of adverse effects in clinical trials. Adverse events were reported in 96% of both the placebo and basiliximab groups.
Cardiovascular: Hypertension, peripheral edema
Central nervous system: Fever, headache, insomnia, pain
Dermatologic: Acne, wound complications
Endocrine & metabolic: Hypercholesterolemia, hyperglycemia, hyper-/hypokalemia, hyperuricemia, hypophosphatemia
Gastrointestinal: Abdominal pain, constipation, diarrhea, dyspepsia, nausea, vomiting
Genitourinary: Urinary tract infection
Neuromuscular & skeletal: Tremor
Respiratory: Dyspnea, infection (upper respiratory)
Miscellaneous: Viral infection
3% to 10%:
Cardiovascular: Abnormal heart sounds, angina, arrhythmia, atrial fibrillation, chest pain, generalized edema, heart failure, hypotension, tachycardia
Central nervous system: Agitation, anxiety, depression, dizziness, fatigue, hypoesthesia, malaise
Dermatologic: Cyst, hypertrichosis, pruritus, rash, skin disorder, skin ulceration
Endocrine & metabolic: Acidosis, dehydration, diabetes mellitus, fluid overload, glucocorticoids increased, hyper-/hypocalcemia, hyperlipemia, hypertriglyceridemia, hypoglycemia, hypomagnesemia, hyponatremia, hypoproteinemia
Gastrointestinal: Abdomen enlarged, esophagitis, flatulence, gastroenteritis, GI hemorrhage, gingival hyperplasia, melena, moniliasis, stomatitis (including ulcerative), weight gain
Genitourinary: Bladder disorder, dysuria, genital edema (male), impotence, ureteral disorder, urinary frequency, urinary retention
Hematologic: Hematoma, hemorrhage, leukopenia, polycythemia, purpura, thrombocytopenia, thrombosis
Neuromuscular & skeletal: Arthralgia, arthropathy, back pain, cramps, fracture, hernia, leg pain, myalgia, neuropathy, paresthesia, rigors, weakness
Ocular: Abnormal vision, cataract, conjunctivitis
Renal: Albuminuria, hematuria, nonprotein nitrogen increased, oliguria, renal function abnormal, renal tubular necrosis
Respiratory: Bronchitis, bronchospasm, cough, pharyngitis, pneumonia, pulmonary edema, rhinitis, sinusitis
Miscellaneous: Accidental trauma, cytomegalovirus (CMV) infection, herpes infection (simplex and zoster), infection, sepsis
Postmarketing and/or case reports: Anaphylaxis, capillary leak syndrome, cytokine release syndrome, diabetes (new onset), fasting glucose impaired, glucose intolerance, hypersensitivity reaction (including heart failure, hypotension, tachycardia, bronchospasm, dyspnea, pulmonary edema, respiratory failure, sneezing, pruritus, rash, urticaria), lymphoproliferative disease
Concerns related to adverse effects:
• Anaphylactoid/hypersensitivity reactions: Severe hypersensitivity reactions, occurring within 24 hours, have been reported. Reactions, including anaphylaxis, have occurred both with the initial exposure and/or following re-exposure after several months; use caution during re-exposure to a subsequent course of therapy in a patient who has previously received basiliximab. Patients in whom concomitant immunosuppression was prematurely discontinued due to abandoned transplantation or early graft loss are at increased risk for developing a severe hypersensitivity reaction upon re-exposure. Discontinue permanently if a severe reaction occurs. Medications for the treatment of hypersensitivity reactions should be available for immediate use.
• Diabetes: In renal transplant patients receiving basiliximab plus prednisone, cyclosporine, and mycophenolate, new-onset diabetes, glucose intolerance, and impaired fasting glucose were observed at rates significantly higher than observed in patients receiving prednisone, cyclosporine, and mycophenolate without basiliximab (Aasebo, 2010).
• Human antimurine antibodies (HAMA): Treatment may result in the development of HAMA; however, limited evidence suggesting the use of muromonab-CD3 or other murine products is not precluded.
• Lymphoproliferative disorders: The incidence of lymphoproliferative disorders may be increased by immunosuppressive therapy.
• Opportunistic infections: The incidence of opportunistic infections may be increased by immunosuppressive therapy.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
• Appropriate use: To be used as a component of an immunosuppressive regimen which includes cyclosporine and corticosteroids.
• Experienced physician: [U.S. Boxed Warning]: Should be administered under the supervision of a physician experienced in immunosuppression therapy and organ transplant management.
Signs and symptoms of acute rejection; hypersensitivity, infection
Pregnancy Risk Factor
Adverse effects were not observed in animal reproduction studies. IL-2 receptors play an important role in the development of the immune system. Women of childbearing potential should use effective contraceptive measures before beginning treatment, during, and for 4 months after completion of basiliximab treatment. The National Transplantation Pregnancy Registry (NTPR, Temple University) is a registry for pregnant women taking immunosuppressants following any solid organ transplant. The NTPR encourages reporting of all immunosuppressant exposures during pregnancy in transplant recipients at 877-955-6877.
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience insomnia, acne, constipation, diarrhea, nausea, vomiting, abdominal pain, or heartburn. Have patient report immediately to prescriber signs of infection, signs of high blood sugar (confusion, feeling sleepy, more thirst, hunger, passing urine more often, flushing, fast breathing, or breath that smells like fruit), signs of low potassium (muscle pain or weakness, muscle cramps, or an abnormal heartbeat), severe dizziness, passing out, angina, tachycardia, shortness of breath, excessive weight gain, swelling of arm or leg, sneezing, severe headache, tremors, loss of strength and energy, burning or numbness feeling, urinary retention, bruising, bleeding, or vision changes (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.
More about basiliximab
- Other brands: Simulect