Basiliximab is an immunosuppressant used to prevent rejection in renal allograft recipients. Like daclizumab, basiliximab is a recombinant, chimeric (murine/human) monoclonal antibody (IgG1) against CD25, the interleukin-2 receptor alpha-chain. When used prophylactically in combination with cyclosporine and corticosteroids, basiliximab reduces biopsy-confirmed rejection episodes in patients undergoing renal transplantation. The reduction in acute rejection achieved with basiliximab is similar to that observed with daclizumab. In contrast to less specific immunosuppressants such as cyclosporine, the adverse event profile of basiliximab is comparable to that of placebo. Other potential benefits of basiliximab therapy include lack of myelosuppression and no increased risk of lymphoma or other malignancies. The FDA granted final approval of basiliximab for prevention of renal allograft rejection in May 1998. Basiliximab has also been studied in the prevention of liver transplant rejection.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
-Anaphylactic reactions following the administration of basiliximab have been reported. Medications for the treatment of severe hypersensitivity reactions should be available for immediate use during administration of the drug.
-Withhold the second dose of a treatment course if a severe hypersensitivity reaction or graft loss occurs.
-Patients previously treated with basiliximab should receive any subsequent courses with extreme caution.
Route-Specific Administration
Injectable Administration
-Basiliximab is administered by intravenous bolus or infusion via central or peripheral venous access.
-Visually inspect parenteral products for particulate matter and discoloration prior to administration whenever solution and container permit.
Intravenous Administration
Reconstitution:
-Reconstitute 10 mg vials with 2.5 mL and 20 mg vials with 5 mL of Sterile Water for Injection for a final concentration of 4 mg/mL. Shake vial gently to dissolve the powder.
-After reconstitution, the solution should be clear to opalescent. If particulate matter is present or the solution is colored, do not use.
-The solution should be used immediately after preparation. If not used immediately, it can be stored at 2-8 degrees C for 24 hours or at room temperature for 4 hours.
Intravenous injection:
-Further dilution is not necessary. Administer as a bolus injection. Discard any unused drug; the solution does not contain preservatives.
-Bolus administration may be associated with nausea, vomiting, and local reactions including pain.
Dilution:
-Dilute 10 mg in 25 mL or 20 mg in 50 mL of 0.9% Sodium Chloride or 5% Dextrose injection. Discard any unused drug; the solution does not contain preservatives.
-When mixing the solution, gently invert the bag. In order to avoid foaming; do not shake.
Intravenous infusion:
-Infuse IV over 20-30 minutes. Do not mix basiliximab with other medicines or administer other medications through the same intravenous line.
In a pooled analysis of clinical trials, accidental trauma and increased drug levels were reported in 3-10% of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection.
In a pooled analysis of clinical trials, vascular disorder occurred in 3-10% of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection.
In pooled results from 4 randomized, double-blind, placebo-controlled trials, gastrointestinal (GI) adverse events including abdominal pain, constipation, diarrhea, dyspepsia, nausea, and vomiting were reported in 10% or greater of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection; the incidence and type of adverse effects were similar in basiliximab-treated patients (n = 590) and patients who received placebo (n = 594). Additionally, enlarged abdomen, esophagitis, flatulence, GI disorder, gastro-enteritis, GI bleeding, gingival hyperplasia, melena, candidiasis (moniliasis), and ulcerative stomatitis were reported in 3-10% of basiliximab-treated patients in a pooled analysis of clinical trials.
In pooled results from 4 randomized, double-blind, placebo-controlled trials, dermatologic adverse events including surgical wound complications and acne vulgaris were reported in 10% or greater of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection; the incidence and type of adverse effects were similar in basiliximab-treated patients (n = 590) and patients who received placebo (n = 594). Additionally, cyst, hypertrichosis, pruritus, rash (unspecified), skin disorder, and skin ulcer were reported in 3-10% of basiliximab-treated patients in a pooled analysis of clinical trials. An injection site reaction consisting of pain is associated with bolus administration of basiliximab.
In pooled results from 4 randomized, double-blind, placebo-controlled trials, insomnia was reported in 10% or greater of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection; the incidence of insomnia was similar in basiliximab-treated patients (n = 590) and patients who received placebo (n = 594). Additionally, agitation, anxiety, and depression were reported in 3-10% of basiliximab-treated patients in a pooled analysis of clinical trials.
In pooled results from 4 randomized, double-blind, placebo-controlled trials, anemia was reported in 10% or greater of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection; the incidence of anemia was similar in basiliximab-treated patients (n = 590) and patients who received placebo (n = 594). Additionally, hematoma, bleeding, leukopenia, polycythemia, purpura, thrombocytopenia, and thrombosis were reported in 3-10% of basiliximab-treated patients in a pooled analysis of clinical trials. Leukopenia occurred more often when basiliximab was used in combination with triple-agent immunosuppression therapy (with azathioprine and mycophenolate mofetil) compared with dual-agent immunosuppression therapy.
Anti-idiotype antibody formation occurred in 4 of 339 renal transplantation patients (1.2%) who received basiliximab. No adverse clinical effects occurred due to antibody formation; accelerated basiliximab clearance or a decreased receptor saturation period was not observed. In one study, human anti-murine antibody (HAMA) formation occurred following basiliximab therapy in 2 of 138 renal transplant patients (1.4%) who had not received prior treatment with muromonab-CD3 and in 4 of 34 patients (11.8%) who subsequently received muromonab-CD3.
The risk of developing an opportunistic infection is increased with the use of immunosuppressive therapy; monitor patients who receive basiliximab for signs and symptoms of infection. The incidence of infection, serious infection, and the types of infectious organisms were similar in basiliximab- and placebo-treated patients who received dual- and triple-agent immunosuppression therapy. In pooled results from 4 randomized, double-blind, placebo-controlled trials, viral, urinary tract, and upper respiratory tract infections were reported in 10% or greater of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection. Cytomegalovirus (CMV) infections (15% vs 17%) occurred at a similar rate in basiliximab-treated patients (n = 590) and patients who received placebo (n = 594) in this analysis; however, CMV infection occurred more often than placebo when basiliximab was used in combination with triple-agent maintenance immunosuppression therapy (11% vs 5%). Additionally, herpes simplex infection, herpes zoster infection, infection, pneumonia, and sepsis were reported in 3-10% of basiliximab-treated patients in a pooled analysis of clinical trials.
The risk of developing a malignancy is increased with the use of immunosuppressive therapy; monitor patients who receive basiliximab for malignancy. In pooled results from randomized, double-blind, placebo-controlled trials, malignancy occurred at a similar rate (1.5% vs 2%) in patients who received basiliximab (n = 590) or placebo (n = 594) as part of a maintenance immunosuppressive regimen for the prevention of kidney allograft rejection. After 5-years of follow-up, malignancy was reported in 7.1% and 7.2% of patients who received basiliximab and placebo, respectively. Post-transplant lymphoproliferative disorder (PTLD) was reported in less than 1% of basiliximab-treated patients and at a similar incidence as patients who received placebo.
In pooled results from 4 randomized, double-blind, placebo-controlled trials, metabolic adverse events including hyperkalemia, hypokalemia, hyperglycemia, hypercholesterolemia, hypophosphatemia, and hyperuricemia were reported in 10% or greater of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection; the incidence and type of adverse effects were similar in basiliximab-treated patients (n = 590) and patients who received placebo (n = 594). Additionally, metabolic acidosis, dehydration, diabetes mellitus, fluid retention/overload, hypercalcemia, hyperlipidemia, hypertriglyceridemia, hypocalcemia, hypoglycemia, hypomagnesemia, hypoproteinemia, increased glucocorticoid levels, and weight gain were reported in 3-10% of basiliximab-treated patients in a pooled analysis of clinical trials. Hypertriglyceridemia occurred more often when basiliximab was used in combination with triple-agent immunosuppression therapy (with azathioprine and mycophenolate mofetil) compared with dual-agent immunosuppression therapy.
In pooled results from 4 randomized, double-blind, placebo-controlled trials, hypertension was reported in 10% or greater of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection; the incidence of hypertension was similar in basiliximab-treated patients (n = 590) and patients who received placebo (n = 594). Additionally, abnormal heart sounds, aggravated hypertension, angina pectoris, arrhythmia, atrial fibrillation, heart failure, chest pain (unspecified), hypotension, and sinus tachycardia were reported in 3-10% of basiliximab-treated patients in a pooled analysis of clinical trials.
In pooled results from 4 randomized, double-blind, placebo-controlled trials, dyspnea was reported in 10% or greater of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection; the incidence of dyspnea was similar in basiliximab-treated patients (n = 590) and patients who received placebo (n = 594). Additionally, bronchitis, bronchospasm, abnormal chest sounds, cough, pharyngitis, pulmonary disorder, pulmonary edema, rhinitis, and sinusitis were reported in 3-10% of basiliximab-treated patients in a pooled analysis of clinical trials.
In pooled results from 4 randomized, double-blind, placebo-controlled trials, nervous system adverse events including headache and tremor were reported in 10% or greater of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection; the incidence and type of adverse effects were similar in basiliximab-treated patients (n = 590) and patients who received placebo (n = 594). Additionally, dizziness, peripheral neuropathy, paresthesias, and hypoesthesia were reported in 3-10% of basiliximab-treated patients in a pooled analysis of clinical trials.
In pooled results from 4 randomized, double-blind, placebo-controlled trials, fever was reported in 10% or greater of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection; the incidence of fever was similar in basiliximab-treated patients (n = 590) and patients who received placebo (n = 594). Additionally, chills were reported in 3-10% of basiliximab-treated patients in a pooled analysis of clinical trials.
Edema has been reported with basiliximab therapy. In pooled results from 4 randomized, double-blind, placebo-controlled trials, peripheral edema was reported in 10% or greater of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection; the incidence of peripheral edema was similar in basiliximab-treated patients (n = 590) and patients who received placebo (n = 594). Additionally, face edema, dependent edema, generalized edema, leg edema, and genital edema were reported in 3-10% of basiliximab-treated patients in a pooled analysis of clinical trials.
In pooled results from 4 randomized, double-blind, placebo-controlled trials, pain was reported in 10% or greater of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection; the incidence of pain was similar in basiliximab-treated patients (n = 590) and patients who received placebo (n = 594). Additionally, arthralgia, arthropathy, back pain, bone fractures, muscle cramps, hernia, myalgia, and leg pain were reported in 3-10% of basiliximab-treated patients in a pooled analysis of clinical trials.
In a pooled analysis of clinical trials, asthenia, fatigue, and malaise were reported in 3-10% of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection.
In a pooled analysis of clinical trials, impotence (erectile dysfunction) was reported in 3-10% of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection.
In a pooled analysis of clinical trials, urinary adverse events including albuminuria (proteinuria), bladder disorder, dysuria, increased urinary frequency, hematuria, increased non-protein nitrogen levels, oliguria, abnormal renal function, renal tubular necrosis, surgery, ureteral disorder, and urinary retention were reported in 3-10% of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection.
In a pooled analysis of clinical trials, ophthalmologic adverse events including cataracts, conjunctivitis, and visual impairment were reported in 3-10% of patients who received basiliximab as part of an immunosuppressive regimen for the prevention of kidney allograft rejection.
Acute hypersensitivity reactions, including anaphylactoid reactions, occurring within 24 hours of basiliximab administration have been reported both with initial exposure and/or following re-exposure after several months. Symptoms included hypotension, tachycardia, cardiac arrest, dyspnea, wheezing, bronchospasm, pulmonary edema, respiratory arrest, urticaria, rash, pruritus, and sneezing. Permanently discontinue basiliximab in patients who develop a severe hypersensitivity reaction.
Basiliximab is contraindicated in patients with known hypersensitivity to basiliximab or to any other component of the formulation.
Human anti-murine antibody (HAMA) has been reported in patients who have received basiliximab with or without previous exposure to muromonab CD3. The available clinical data on the use of muromonab-CD3 in patients previously treated with basiliximab suggest that subsequent use of muromonab-CD3 or other murine anti-lymphocytic antibody preparations is not precluded.
Basiliximab therapy requires an experienced clinician in immunosuppressive therapy and management of organ transplantation patients. The health care provider responsible for basiliximab administration should have complete information requisite for the follow-up of the patient. Basiliximab administration also requires a specialized care setting, facilities that are equipped and staffed with adequate laboratory and supportive medical resources. While neither the incidence of lymphoproliferative disorders nor opportunistic infections was higher in basiliximab-treated patients than in placebo-treated patients, patients on immunosuppression therapy are at increased risk for developing these complications and should be monitored accordingly.
It is not known whether the immune response to vaccination administered during basiliximab therapy is impaired or whether such response will remain impaired after basiliximab therapy.
Use basiliximab during pregnancy only when the potential benefit justifies the potential risk to the fetus. The IL-2 receptor may play an important role in the development of the immune system, and IgG molecules are known to cross the placental barrier. There are no adequate and well-controlled studies of basiliximab in pregnant women. In a study involving cynomolgus monkeys, basiliximab administration during organogenesis was not associated with maternal toxicity, embryotoxicity, or teratogenicity. Blood concentrations in pregnant monkeys were 13-fold higher than those seen in human patients.
It is not known whether basiliximab is excreted in human milk. Because many drugs, including human antibodies are excreted in human milk, and because of the potential for adverse reactions, discontinue breast-feeding or discontinue basiliximab, taking into account the importance of the drug to the mother.
Basiliximab may be associated with reproductive risk. The IL-2 receptor may play an important role in the development of the immune system, and IgG molecules are known to cross the placental barrier. Discuss contraception requirements with females of reproductive potential. Advise females of childbearing potential to use effective contraception before initiating therapy, during treatment, and for 4 months after completion of basiliximab therapy.
For acute kidney transplant rejection prophylaxis when used as part of an immunosuppressive regimen that includes cyclosporine and corticosteroids:
NOTE: Basiliximab should only be administered once it has been determined that the patient will receive the graft and concomitant immunosuppression.
NOTE: Do not give the second basiliximab dose on day 4 after transplantation if graft loss or a severe hypersensitivity reaction occurs after the initial dose.
NOTE: Patients previously administered basiliximab should only be re-exposed to a subsequent course of therapy with extreme caution. The potential risks of another treatment course, specifically those associated with immunosuppression and/or the occurrence of anaphylaxis/anaphylactoid reactions, are not known.
Intravenous dosage:
Adults, Adolescents, and Children >= 35 kg: 20 mg IV within 2 hours prior to transplantation surgery, followed by 20 mg IV 4 days after transplantation. Guidelines recommend induction therapy with an interleukin-2 receptor antagonist such as basiliximab as part of the initial immunosuppressive regimen for patients at low or moderate immunologic risk.
Children and Adolescents < 35 kg: 10 mg IV within 2 hours prior to transplantation surgery, followed by 10 mg IV 4 days after transplantation. Guidelines recommend induction therapy with an interleukin-2 receptor antagonist such as basiliximab as part of the initial immunosuppressive regimen for patients at low or moderate immunologic risk.
For acute liver transplant rejection prophylaxis* when used as part of an immunosuppressive regimen that includes cyclosporine and corticosteroids:
Intravenous dosage:
Adults: 20 mg IV on the day of transplant (day 0) and a second 20 mg dose on day 4 post-transplant. In clinical trials, the first basiliximab dose was primarily administered at the time of liver reperfusion; however, in 3 studies it was given once hemostasis had been achieved or immediately post-transplant, within 6 hours of reperfusion, or 8 hours of reperfusion. In these studies, basiliximab was given in combination with a calcineurin inhibitor (tacrolimus or cyclosporine) with or without a steroid (methylprednisolone or hydrocortisone); mycophenolate mofetil was also given in one study.
For the treatment of acute graft-versus-host disease (GVHD)*:
Intravenous dosage:
Adults: 20 mg IV once daily on days 1 and 4. May repeat course in cases of recurrence. Guidelines suggest basiliximab as a second-line treatment option for steroid-refractory acute GVHD.
Maximum Dosage Limits:
-Adults
20 mg IV as a single dose.
-Elderly
20 mg IV as a single dose.
-Adolescents
>= 35 kg: 20 mg IV as a single dose.
< 35 kg: 10 mg IV as a single dose.
-Children
>= 35 kg: 20 mg IV as a single dose.
< 35 kg: 10 mg IV as a single dose.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
Abatacept: (Moderate) Concomitant use of immunosuppressives may potentially increase the risk of serious infection in abatacept treated patients. Advise patients taking abatacept to seek immediate medical advice if they develop signs and symptoms suggestive of infection.
Albuterol; Budesonide: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Alpha interferons: (Moderate) Additive myelosuppressive effects may be seen when alpha interferons are given concurrently with other myelosuppressive agents, such as antineoplastic agents or immunosuppressives.
Azathioprine: (Minor) Because azathioprine is an immunosuppressant with myelosuppressive actions, additive affects may be seen with other immunosuppressives.
Azelastine; Fluticasone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Bacillus Calmette-Guerin Vaccine, BCG: (Contraindicated) Do not administer live vaccines to basiliximab recipients; no data are available regarding the risk of secondary transmission of infection by live vaccines in patients receiving basiliximab. At least 2 weeks before initiation of basiliximab therapy, consider completion of all age appropriate vaccinations per current immunization guidelines. Basiliximab recipients may receive inactivated vaccines, but the immune response to vaccines or toxoids may be decreased.
Beclomethasone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Betamethasone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Budesonide: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Budesonide; Formoterol: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Budesonide; Glycopyrrolate; Formoterol: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Canakinumab: (Major) Avoid the concomitant use of canakinumab with other interleukin inhibitors, such as basilixumab; coadministration has not been studied and may result in additive immunosuppression and increased risk of infection.
Certolizumab pegol: (Moderate) The safety and efficacy of certolizumab in patients with immunosuppression have not been evaluated. Patients receiving immunosuppressives along with certolizumab may be at a greater risk of developing an infection. Many of the serious infections occurred in patients on immunosuppressive therapy who received certolizumab.
Chikungunya Vaccine, Live: (Contraindicated) Do not administer live vaccines to basiliximab recipients; no data are available regarding the risk of secondary transmission of infection by live vaccines in patients receiving basiliximab. At least 2 weeks before initiation of basiliximab therapy, consider completion of all age appropriate vaccinations per current immunization guidelines. Basiliximab recipients may receive inactivated vaccines, but the immune response to vaccines or toxoids may be decreased.
Ciclesonide: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Cladribine: (Minor) Concurrent use of purine analogs with other agents which cause bone marrow or immune suppression such as other antineoplastic agents may result in additive effects. A dosage reduction of the purine analog may be indicated when used in combination with other myelosuppressive chemotherapy.
Corticosteroids: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Cortisone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Cyclosporine: (Minor) Because basiliximab is an immunosuppressant, additive effects may be seen with other immunosuppressives.
Deflazacort: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Dexamethasone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Dichlorphenamide: (Moderate) Use dichlorphenamide and basiliximab together with caution as both drugs can cause metabolic acidosis. Concurrent use may increase the severity of metabolic acidosis. Measure sodium bicarbonate concentrations at baseline and periodically during dichlorphenamide treatment. If metabolic acidosis occurs or persists, consider reducing the dose or discontinuing dichlorphenamide therapy.
Elbasvir; Grazoprevir: (Moderate) Administering elbasvir; grazoprevir with basiliximab may cause the plasma concentrations of elbasvir and grazoprevir to increase; thereby increasing the potential for adverse effects (i.e., elevated ALT concentrations and hepatotoxicity). Basiliximab is a mild CYP3A inhibitor. Both elbasvir and grazoprevir are metabolized by CYP3A. If these drugs are used together, closely monitor for signs of hepatotoxicity.
Fludarabine: (Minor) Concurrent use of purine analogs with other agents which cause bone marrow or immune suppression such as other antineoplastic agents may result in additive effects. A dosage reduction of the purine analog may be indicated when used in combination with other myelosuppressive chemotherapy.
Fludrocortisone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Flunisolide: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Fluticasone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Fluticasone; Salmeterol: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Fluticasone; Umeclidinium; Vilanterol: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Fluticasone; Vilanterol: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Formoterol; Mometasone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Golimumab: (Moderate) The safety and efficacy of golimumab in patients with immunosuppression have not been evaluated. Patients receiving immunosuppressives along with golimumab may be at a greater risk of developing an infection.
Hydrocortisone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Interferon Alfa-2b: (Moderate) Additive myelosuppressive effects may be seen when alpha interferons are given concurrently with other myelosuppressive agents, such as antineoplastic agents or immunosuppressives.
Interferon Alfa-n3: (Moderate) Additive myelosuppressive effects may be seen when alpha interferons are given concurrently with other myelosuppressive agents, such as antineoplastic agents or immunosuppressives.
Intranasal Influenza Vaccine: (Contraindicated) Do not administer live vaccines to basiliximab recipients; no data are available regarding the risk of secondary transmission of infection by live vaccines in patients receiving basiliximab. At least 2 weeks before initiation of basiliximab therapy, consider completion of all age appropriate vaccinations per current immunization guidelines. Basiliximab recipients may receive inactivated vaccines, but the immune response to vaccines or toxoids may be decreased.
Live Vaccines: (Contraindicated) Do not administer live vaccines to basiliximab recipients; no data are available regarding the risk of secondary transmission of infection by live vaccines in patients receiving basiliximab. At least 2 weeks before initiation of basiliximab therapy, consider completion of all age appropriate vaccinations per current immunization guidelines. Basiliximab recipients may receive inactivated vaccines, but the immune response to vaccines or toxoids may be decreased.
Measles Virus; Mumps Virus; Rubella Virus; Varicella Virus Vaccine, Live: (Contraindicated) Do not administer live vaccines to basiliximab recipients; no data are available regarding the risk of secondary transmission of infection by live vaccines in patients receiving basiliximab. At least 2 weeks before initiation of basiliximab therapy, consider completion of all age appropriate vaccinations per current immunization guidelines. Basiliximab recipients may receive inactivated vaccines, but the immune response to vaccines or toxoids may be decreased.
Measles/Mumps/Rubella Vaccines, MMR: (Contraindicated) Do not administer live vaccines to basiliximab recipients; no data are available regarding the risk of secondary transmission of infection by live vaccines in patients receiving basiliximab. At least 2 weeks before initiation of basiliximab therapy, consider completion of all age appropriate vaccinations per current immunization guidelines. Basiliximab recipients may receive inactivated vaccines, but the immune response to vaccines or toxoids may be decreased.
Mercaptopurine, 6-MP: (Minor) Concurrent use of purine analogs with other agents which cause bone marrow or immune suppression such as other antineoplastic agents may result in additive effects. A dosage reduction of the purine analog may be indicated when used in combination with other myelosuppressive chemotherapy.
Methotrexate: (Minor) Because basiliximab is an immunosuppressant, additive effects may be seen with other immunosuppressives such as methotrexate.
Methylprednisolone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Mometasone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Mycophenolate: (Minor) Because mycophenolate mofetil is an immunosuppressant, additive effects may be seen with other immunosuppressives. While therapy is designed to take advantage of this effect, patients may be predisposed to over-immunosuppression resulting in an increased risk for the development of severe infections, malignancies including lymphoma and leukemia, myelodysplastic syndromes, and lymphoproliferative disorders. The risk is related to the intensity and duration of immunosuppression rather than the specific agents.
Natalizumab: (Major) The concomitant use of natalizumab and immunosuppressives, such as basiliximab, may further increase the risk of serious infections over the risk observed with use of natalizumab alone. The safety and efficacy of natalizumab in combination with basiliximab has not been evaluated. Patients receiving chronic immunosuppressant therapy should not ordinarily be treated with natalizumab.
Olopatadine; Mometasone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Peginterferon Alfa-2a: (Moderate) Additive myelosuppressive effects may be seen when alpha interferons are given concurrently with other myelosuppressive agents, such as antineoplastic agents or immunosuppressives.
Peginterferon Alfa-2b: (Moderate) Additive myelosuppressive effects may be seen when alpha interferons are given concurrently with other myelosuppressive agents, such as antineoplastic agents or immunosuppressives.
Penicillamine: (Major) Agents such as immunosuppressives have adverse reactions similar to those of penicillamine. Concomitant use of penicillamine with these agents is contraindicated because of the increased risk of developing severe hematologic and renal toxicity.
Pentostatin: (Minor) Concurrent use of purine analogs with other agents which cause bone marrow or immune suppression such as other antineoplastic agents may result in additive effects. A dosage reduction of the purine analog may be indicated when used in combination with other myelosuppressive chemotherapy.
Prednisolone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Prednisone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Purine analogs: (Minor) Concurrent use of purine analogs with other agents which cause bone marrow or immune suppression such as other antineoplastic agents may result in additive effects. A dosage reduction of the purine analog may be indicated when used in combination with other myelosuppressive chemotherapy.
Rilonacept: (Moderate) Patients receiving immunosuppressives along with rilonacept may be at a greater risk of developing an infection.
Ropeginterferon alfa-2b: (Moderate) Additive myelosuppressive effects may be seen when alpha interferons are given concurrently with other myelosuppressive agents, such as antineoplastic agents or immunosuppressives.
Rotavirus Vaccine: (Contraindicated) Do not administer live vaccines to basiliximab recipients; no data are available regarding the risk of secondary transmission of infection by live vaccines in patients receiving basiliximab. At least 2 weeks before initiation of basiliximab therapy, consider completion of all age appropriate vaccinations per current immunization guidelines. Basiliximab recipients may receive inactivated vaccines, but the immune response to vaccines or toxoids may be decreased.
Saquinavir: (Moderate) Both saquinavir boosted with ritonavir and basiliximab are inhibitors of CYP3A4; an isoenzyme responsible for the metabolism of saquinavir. The use of saquinavir/ritonavir with basiliximab may result in large increases in saquinavir plasma concentrations, which could cause adverse events such as life threatening cardiac arrhythmias (e.g., torsades de pointes [TdP]).
Smallpox and Monkeypox Vaccine, Live, Nonreplicating: (Contraindicated) Do not administer live vaccines to basiliximab recipients; no data are available regarding the risk of secondary transmission of infection by live vaccines in patients receiving basiliximab. At least 2 weeks before initiation of basiliximab therapy, consider completion of all age appropriate vaccinations per current immunization guidelines. Basiliximab recipients may receive inactivated vaccines, but the immune response to vaccines or toxoids may be decreased.
Smallpox Vaccine, Vaccinia Vaccine: (Contraindicated) Do not administer live vaccines to basiliximab recipients; no data are available regarding the risk of secondary transmission of infection by live vaccines in patients receiving basiliximab. At least 2 weeks before initiation of basiliximab therapy, consider completion of all age appropriate vaccinations per current immunization guidelines. Basiliximab recipients may receive inactivated vaccines, but the immune response to vaccines or toxoids may be decreased.
Sofosbuvir; Velpatasvir: (Moderate) Use caution when administering velpatasvir with basiliximab. Taking these drugs together may increase velpatasvir plasma concentrations, potentially resulting in adverse events. Velpatasvir is a substrate of CYP3A4. Basiliximab may cause a down-regulation of 3A4 activity by increasing IL-2 binding to IL-2 receptors on hepatic and intestinal cells.
Sofosbuvir; Velpatasvir; Voxilaprevir: (Moderate) Use caution when administering velpatasvir with basiliximab. Taking these drugs together may increase velpatasvir plasma concentrations, potentially resulting in adverse events. Velpatasvir is a substrate of CYP3A4. Basiliximab may cause a down-regulation of 3A4 activity by increasing IL-2 binding to IL-2 receptors on hepatic and intestinal cells.
Tacrolimus: (Major) Basiliximab acts as an IL-2 receptor antagonist. Binding of basiliximab to the IL-2 receptors on activated T cells may allow circulating IL-2 to bind to IL-2 receptors on hepatic and intestinal cells, which may cause a down-regulation of CYP3A4 enzyme activity. Reduced CYP3A4 activity may increase concentrations of CYP3A4 substrates such as tacrolimus. In a retrospective evaluation, the tacrolimus dose needed to achieve a trough concentration of 15 to 20 ng/ml was lower among basiliximab recipients as compared with antithymocyte globulin recipients. Over the 60 days after transplantation, tacrolimus dose requirements were 0.16 mg/kg/day for basiliximab recipients and 0.24 mg/kg/day for antithymocyte globulin recipients. All patients initially received oral tacrolimus 0.075 to 0.15 mg/kg with the dose titrated to achieve the desired trough concentration. On day 3 after transplantation, tacrolimus trough concentrations were higher than 20 ng/ml in 6 of 12 adults who also got basiliximab 20 mg on the day of transplantation and 4 days later; three patients with an elevated trough concentration had acute tubular necrosis and underwent hemodialysis. In contrast, 2 of 8 patients who got antithymocyte globulin daily for the first 7 days had a tacrolimus trough concentration higher than 20 ng/ml - no significant adverse effects were noted. The half-life of basiliximab is 7.2 days, so the tacrolimus dose may need upward adjustment as the effects of basiliximab on IL-2 dissipate. For example, one month after transplantation, 6 of the 12 basiliximab recipients had tacrolimus trough concentrations below the targeted range of 15 to 20 ng/ml.
Thioguanine, 6-TG: (Minor) Concurrent use of purine analogs with other agents which cause bone marrow or immune suppression such as other antineoplastic agents may result in additive effects. A dosage reduction of the purine analog may be indicated when used in combination with other myelosuppressive chemotherapy.
Tocilizumab: (Major) Avoid using tocilizumab with immunosuppressive biological agents such as basilixumab because of the possibility of increased immunosuppression and increased risk of infection. The concurrent use of tocilizumab with other biological agents has not been studied. Most patients taking tocilizumab who developed serious infections were taking concomitant immunosuppressives.
Triamcinolone: (Minor) Because systemically administered corticosteroids have immunosuppressive effects when given in high doses and/or for extended periods, additive effects may be seen with other immunosuppressives.
Typhoid Vaccine: (Contraindicated) Do not administer live vaccines to basiliximab recipients; no data are available regarding the risk of secondary transmission of infection by live vaccines in patients receiving basiliximab. At least 2 weeks before initiation of basiliximab therapy, consider completion of all age appropriate vaccinations per current immunization guidelines. Basiliximab recipients may receive inactivated vaccines, but the immune response to vaccines or toxoids may be decreased.
Varicella-Zoster Virus Vaccine, Live: (Contraindicated) Do not administer live vaccines to basiliximab recipients; no data are available regarding the risk of secondary transmission of infection by live vaccines in patients receiving basiliximab. At least 2 weeks before initiation of basiliximab therapy, consider completion of all age appropriate vaccinations per current immunization guidelines. Basiliximab recipients may receive inactivated vaccines, but the immune response to vaccines or toxoids may be decreased.
Yellow Fever Vaccine, Live: (Contraindicated) Do not administer live vaccines to basiliximab recipients; no data are available regarding the risk of secondary transmission of infection by live vaccines in patients receiving basiliximab. At least 2 weeks before initiation of basiliximab therapy, consider completion of all age appropriate vaccinations per current immunization guidelines. Basiliximab recipients may receive inactivated vaccines, but the immune response to vaccines or toxoids may be decreased.
Basiliximab binds to and blocks the interleukin-2 receptor alpha-chain receptor (IL-2Ralpha), also known as CD25 antigen or Tac subunit. The IL-2Ralpha is only expressed on the surface of activated T-cells and is important in the clonal expansion of activated T-cells. The specific, high-affinity binding of basiliximab to IL-2Ralpha competitively inhibits IL-2 mediated activation of T-lymphocytes, a critical pathway in the cellular immune response involved in allograft rejection. In vitro studies using human tissues indicate that basiliximab binds only to lymphocytes. Because basiliximab has a long half-life, the IL-2Ralpha blocking effects persist for 4-6 weeks after two infusions. The effect of basiliximab differs from cyclosporine in that cyclosporine inhibits interleukin-2 release while basiliximab acts as an IL-2 receptor antagonist. Basiliximab does not appear to significantly change circulating lymphocyte numbers or cell phenotypes. While in the systemic circulation, basiliximab impairs the normal response of the immune system to antigenic challenges. Whether the ability to respond to repeated or ongoing challenges with those antigens returns to normal after basiliximab is cleared is unknown.
Basiliximab is administered intravenously. The extent and degree of distribution to various body compartments have not been fully evaluated. The elimination half-life of basiliximab is roughly 7.2 days.
Complete binding of basiliximab to the interleukin-2 receptor alpha-chain (IL-2Ralpha) in adults is maintained as long as serum concentrations exceed 0.2 mcg/mL. Below 0.2 mcg/mL, the IL-2Ralpha sites are no longer fully bound, and the number of T-cells expressing unbound IL-2Ralpha returns to pretreatment values within 1-2 weeks. At the recommended dosage regimen, the mean duration of basiliximab saturation of IL-2Ralpha was 36 days in both adults and children. The duration of clinically-significant IL-2 receptor blockade, however, is unknown.
-Route-Specific Pharmacokinetics
Intravenous Route
The mean peak basiliximab serum concentration following 20 mg IV over 30 minutes is 7.1 mcg/ml. Dose-proportional increases in Cmax and AUC occur up to the highest tested single dose of 60 mg.
-Special Populations
Pediatrics
In children 1-11 years of age, the volume of distribution and clearance of basiliximab are reduced by about 50% as compared with values from adult renal transplantation patients; these disposition parameters were not influenced to a clinically relevant extent by age, body weight (9-37 kg), or body surface area (0.44-1.2 m2). The mean elimination half-life of basiliximab was 9.5 days.
Gender Differences
In adults, gender has not been shown to significantly affect distribution volume or clearance.
Obesity
In adults, body weight has not been shown to significantly affect distribution volume or clearance.