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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

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

Use: Unlabeled

Treatment of refractory acute graft-versus-host disease (GVHD); prevention of liver or cardiac 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.

Acute renal transplant rejection prophylaxis: 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): 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): 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): 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.

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.

Acute renal transplant rejection prophylaxis: IV: Note: Use in pediatric patients is not approved in the Canadian labeling (limited pharmacokinetic data available).

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)

Children ≥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 20-30 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).

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

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

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, wound complication

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

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 fasting glucose, impaired glucose tolerance, 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. 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.

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 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.

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