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Basiliximab

Pronunciation

(ba si LIK si mab)

Dosage Forms

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.

  • Simulect

Pharmacologic Category

  • Immunosuppressant Agent
  • Monoclonal Antibody

Pharmacology

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

Distribution

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

Excretion

Clearance:

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)

Half-Life Elimination

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

Use: Labeled Indications

Renal transplant (prophylaxis of acute rejection): Prophylaxis of acute organ rejection in renal transplantation in combination with cyclosporine (modified) and corticosteroids

Guideline recommendations: While basiliximab is FDA-approved for prophylaxis of acute organ rejection in renal transplantation in combination with cyclosporine (modified) and corticosteroids, cyclosporine is no longer recommended as the first line agent of choice. The Kidney Disease: Improving Global Outcomes (KDIGO) clinical practice guidelines for care of kidney transplant recipients recommend induction as part of the initial immunosuppressive regimen for all kidney transplants to reduce the risk of acute rejection. KDIGO recommends an interleukin 2 receptor antagonist (eg,basiliximab) as the first line induction agent for acute rejection prophylaxis except in those patients at high immunologic risk. (KDIGO [Kasiske 2009]).

Off Label Uses

Acute graft-versus-host disease, refractory (treatment)

Data from a small nonrandomized phase II study in patients with steroid refractory acute graft-versus-host-disease (aGVHD) following allogeneic stem cell transplant suggest that basiliximab may be beneficial in the treatment of refractory aGVHD [Schmidt-Hieber 2005]. Additional data may be necessary to further define the role of basiliximab in this condition.

Heart transplant (prophylaxis of acute rejection)

Data from a randomized, placebo-controlled, double blind, multicenter study in de novo heart transplant recipients supports the use of basiliximab (in combination with other immunosuppressants [ie, cyclosporine, mycophenolate, and prednisone]) in the prevention cardiac transplant rejection [Mehra 2005]. Additional trials may be necessary to further define the role of basiliximab in this condition.

Liver transplant (prophylaxis of acute rejection)

Data from a multicenter, randomized, open-label phase IIIb trial in liver transplant patients supports the use of basiliximab (in combination with tacrolimus) for the prevention of acute rejection [Trunecka 2015]. Additional data from a multicenter, randomized, placebo-controlled, double blind study in liver transplant recipients supports the use of basiliximab (in combination with other immunosuppressants [ie, cyclosporine and corticosteroids]) in the prevention of liver transplant rejection [Neuhaus 2002]. A meta analysis evaluating rejection prevention in liver transplant recipients suggests that interleukin 2 receptor antagonist therapy (eg, basiliximab) may be beneficial in reducing episodes of acute rejection, but does not appear to improve overall survival in these patients [Zhang 2016]. Additional trials may be necessary to further define the role of basiliximab in this condition.

Lung transplant (prophylaxis of acute rejection)

A retrospective analysis of data obtained from the United Network for Organ Sharing (UNOS) registry supports the use of basiliximab as induction therapy in patients receiving double lung transplants [Furuya 2016]. Data from other retrospective reviews suggest that basiliximab may be beneficial in prevention of lung transplant rejection [Clinckart 2009], [Swarup 2011]. Additional data may be necessary to further define the role of basiliximab in prevention of lung transplant rejection.

Contraindications

Known hypersensitivity to basiliximab or any component of the formulation

Dosing: Adult

Note: Patients previously administered basiliximab should only be re-exposed to a subsequent course of therapy with extreme caution.

Renal transplant (prophylaxis of acute rejection): IV: 20 mg within 2 hours prior to transplant surgery, followed by a second 20 mg dose 4 days after transplantation (in combination with other immunosuppressants). The second dose should be withheld if complications occur (including severe hypersensitivity reactions or graft loss). Timing of basiliximab dosing may vary based on clinical and institutional factors; refer to institutional protocol for specific information.

Acute graft-versus-host disease (aGVHD), refractory (treatment) (off-label use): 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.

Heart transplant (prophylaxis of acute rejection) (off-label use): IV: 20 mg on the day of transplant, followed by a second 20 mg dose on day 4 post-transplantation (in combination with other immunosuppressants) (Mehra 2005). The first dose is usually administered immediately prior to transplant or within the first hours postoperatively.

Liver transplant (prophylaxis of acute rejection) (off-label use): IV: 20 mg on the day of transplant (day 0), followed by a second 20 mg dose on day 4 post-transplantation (in combination with other immunosuppressants) (Neuhaus 2002; Trunecka 2015). In clinical trials, the first dose was administered during the procedure once hemostasis was achieved or immediately post-transplant, or within 6 hours of organ reperfusion.

Lung transplant (prophylaxis of acute rejection) (off-label use): IV: 20 mg prior to transplantation, followed by a second 20 mg dose 4 days after transplantation (in combination with other immunosuppressants) (Clinckart 2009; Swarup 2011). Additional trials may be necessary to further define the role of basiliximab in this condition.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Note: Patients previously administered basiliximab should only be re-exposed to a subsequent course of therapy with extreme caution.

Renal transplant (prophylaxis of acute rejection): IV:

Children <35 kg: 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). Timing of basiliximab dosing may vary based on clinical and institutional factors; refer to institutional protocol for specific information.

Children and Adolescents ≥35 kg: Refer to adult dosing

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling.

Reconstitution

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.

Administration

For intravenous administration only. Infuse as a bolus or IV infusion over 20 to 30 minutes (bolus dosing is associated with nausea, vomiting, and local pain at the injection site); may be administered through either a peripheral or central line. 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).

Storage

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.

Drug Interactions

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

Nivolumab: Immunosuppressants may diminish the therapeutic effect of Nivolumab. Consider therapy modification

Ocrelizumab: May enhance the immunosuppressive effect of Immunosuppressants. Monitor therapy

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

Tertomotide: Immunosuppressants may diminish the therapeutic effect of Tertomotide. Monitor therapy

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. Consider therapy modification

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

Adverse Reactions

Frequency not defined. 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.

>10%:

Cardiovascular: Hypertension, peripheral edema

Central nervous system: Headache, insomnia, pain

Dermatologic: Acne vulgaris

Endocrine & metabolic: Hypercholesterolemia, hyperglycemia, hyperkalemia, hyperuricemia, hypokalemia, hypophosphatemia

Gastrointestinal: Abdominal pain, constipation, diarrhea, dyspepsia, nausea, vomiting

Genitourinary: Urinary tract infection

Hematologic & oncologic: Anemia

Infection: Viral infection

Neuromuscular & skeletal: Tremor

Respiratory: Dyspnea, upper respiratory infection

Miscellaneous: Fever, postoperative wound complication

3% to 10%:

Cardiovascular: Abnormal heart sounds, angina pectoris, atrial fibrillation, cardiac arrhythmia, cardiac failure, chest pain, hypotension, tachycardia, thrombosis

Central nervous system: Agitation, anxiety, depression, dizziness, fatigue, hypoesthesia, malaise, rigors

Dermatologic: Dermal ulcer, dermatological disease, hypertrichosis, pruritus, skin rash

Endocrine & metabolic: Acidosis, albuminuria, anasarca, dehydration, diabetes mellitus, hypercalcemia, hyperlipidemia, hypertriglyceridemia, hypervolemia, hypocalcemia, hypoglycemia, hypomagnesemia, hyponatremia, increased nonprotein nitrogen, increased serum glucocorticoids, weight gain

Gastrointestinal: Enlargement of abdomen, esophagitis, flatulence, gastroenteritis, gastrointestinal hemorrhage, GI moniliasis, gingival hyperplasia, hernia, melena, stomatitis (including ulcerative)

Genitourinary: Bladder dysfunction, dysuria, genital edema (male), hematuria, impotence, oliguria, ureteral disease, urinary frequency, urinary retention

Hematologic & oncologic: Hematoma, hemorrhage, hypoproteinemia, leukopenia, polycythemia, purpura, thrombocytopenia

Infection: Cytomegalovirus disease, herpes virus infection (simplex and zoster), infection, sepsis

Neuromuscular & skeletal: Arthralgia, arthropathy, back pain, bone fracture, leg pain, muscle cramps, myalgia, neuropathy, paresthesia, weakness

Ophthalmic: Cataract, conjunctivitis, visual disturbance

Renal: Renal insufficiency, renal tubular necrosis

Respiratory: Bronchitis, bronchospasm, cough, pharyngitis, pneumonia, pulmonary edema, rhinitis, sinusitis

Miscellaneous: Accidental injury, cyst

<1% (Limited to important or life-threatening): Anaphylaxis, capillary leak syndrome, cytokine release syndrome, diabetes (new onset), hypersensitivity reaction (includes bronchospasm, cardiac failure, dyspnea, hypotension, pruritus, pulmonary edema, respiratory failure, skin rash, sneezing, tachycardia, urticaria), impaired glucose tolerance, increase in fasting plasma glucose, lymphoproliferative disorder

ALERT: U.S. Boxed Warning

Experienced physician:

Only physicians experienced in immunosuppression therapy and management of organ transplantation patients should prescribe basiliximab. The physician responsible for basiliximab administration should have complete information requisite for the follow-up of the patient. Patients receiving the drug should be managed in facilities equipped with adequate laboratory and supportive medical resources.

Warnings/Precautions

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.

Other warnings/precautions:

• 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.

Monitoring Parameters

Signs and symptoms of acute rejection; hypersensitivity, infection

Pregnancy Risk Factor

B

Pregnancy Considerations

Adverse effects were not observed in animal reproduction studies. Basiliximab is a monoclonal IgG antibody which targets IL-2 receptors. IgG is known to cross the placenta; 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) is a registry which follows pregnancies which occur in maternal transplant recipients or those fathered by male transplant recipients. The NTPR encourages reporting of pregnancies following solid organ transplant by contacting them at 877-955-6877 or NTPR@giftoflifeinstitute.org.

Patient Education

• 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 electrolyte problems (mood changes, confusion, muscle pain or weakness, abnormal heartbeat, seizures, lack of appetite, or severe nausea or vomiting), signs of high blood sugar (confusion, fatigue, increased thirst, increased hunger, polyuria, flushing, fast breathing, or breath that smells like fruit), signs of a urinary tract infection (hematuria, burning or painful urination, polyuria, fever, lower abdominal pain, or pelvic pain), severe dizziness, passing out, angina, tachycardia, shortness of breath, excessive weight gain, swelling of arms or legs, sneezing, severe headache, tremors, severe loss of strength and energy, vision changes, or wound site pain, edema, or drainage (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 health care 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.

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