INN monograph
Basiliximab
Interleukin-2 Receptor Blocking Antibody [EPC] · POM
Verified · Updated 01 Aug 2026 · Source: Local active-ingredient clinical extract; FDA drug label via OpenFDA/DailyMed; Professional class pharmacology (Therapeutic agent (verify pharmacological class))
Kenya market
Wholesale / list prices where loaded
Risk first
Contraindications
- CONTRAINDICATIONS Simulect ® (basiliximab) is contraindicated in patients with known hypersensitivity to basiliximab or any other component of the formulation.
- See composition of Simulect under DESCRIPTION.
- WARNINGS.
- See Boxed WARNING.
- General Simulect ® (basiliximab) should be administered under qualified medical supervision.
- Patients should be informed of the potential benefits of therapy and the risks associated with administration of immunosuppressive therapy.
- While neither the incidence of lymphoproliferative disorders nor opportunistic infections was higher in Simulect-treated patients than in placebo-treated patients, patients on immunosuppressive therapy are at increased risk for developing these complications and should be monitored accordingly.
- Hypersensitivity Severe acute (onset within 24 hours) hypersensitivity reactions, including anaphylaxis have been observed both on initial exposure to Simulect and/or following re-exposure after several months.
- These reactions may include hypotension, tachycardia, cardiac failure, dyspnea, wheezing, bronchospasm, pulmonary edema, respiratory failure, urticaria, rash, pruritus, and/or sneezing.
- Extreme caution should be exercised in all patients previously given Simulect when being administered a subsequent course of Simulect.
- A subgroup of patients may be particularly at risk of developing severe hypersensitivity reactions on re-administration.
- These are patients in whom concomitant immunosuppression was discontinued prematurely (e.g., due to abandoned transplantation or early loss of the graft) following the initial administration of Simulect.
Precautions
- Obtain allergy and medication history.
- Adjust for renal/hepatic impairment, pregnancy, lactation, extremes of age and interacting drugs.
- Use the lowest effective dose for the shortest appropriate duration.
- Monitor for expected class adverse effects.
Point of care
Dosing
Adult
DOSAGE AND ADMINISTRATION Simulect ® (basiliximab) is used as part of an immunosuppressive regimen that includes cyclosporine, USP (MODIFIED) and corticosteroids. Simulect is for central or peripheral intravenous administration only. Reconstituted Simulect should be given either as a bolus injection or diluted to a volume of 25 mL (10-mg vial) or 50 mL (20-mg vial) with 0.9% Sodium Chloride Injection, USP or 5% Dextrose Injection, USP and administered as an intravenous infusion over 20 to 30 minutes. Bolus administration may be associated with nausea, vomiting and local reactions, including pain. Simulect should only be administered once it has been determined that the patient will receive the graft and concomitant immunosuppression. Patients previously administered Simulect should only be re-exposed to a subsequent course of therapy with extreme caution due to the potential risk of hypersensitivity (see WARNINGS). Parenteral drug products should be inspected visually for particulate matter and discoloration before administration. After reconstitution, Simulect should be a clear-to-opalescent, colorless solution. If particulate matter is present or the solution is colored, do not use. Care must be taken to assure sterility of the prepared solution because the drug product does not contain any antimicrobial preservatives or bacteriostatic agents. It is recommended that after reconstitution, the solution should be used immediately. If not used immediately, it can be stored at 2ºC to 8ºC (36ºF to 46ºF) for 24 hours or at room temperature for 4 hours. Discard the reconstituted solution if not used within 24 hours. No incompatibility between Simulect and polyvinyl chloride bags or infusion sets has been observed. No data are available on the compatibility of Simulect with other intravenous substances. Other drug substances should not be added or infused simultaneously through the same intravenous line. Adults In adult patients, the recommended regimen is two doses of 20 mg each. The first 20-mg dose should be given within 2 hours prior to transplantation surgery. The recommended second 20-mg dose should be given 4 days after transplantation. The second dose should be withheld if complications, such as severe hypersensitivity reactions to Simulect or graft loss occur. Pediatric In pediatric patients weighing less than 35 kg, the recommended regimen is two doses of 10 mg each. In pediatric patients weighing 35 kg or more, the recommended regimen is two doses of 20 mg each. The first dose should be given within 2 hours prior to transplantation surgery. The recommended second dose should be given 4 days after transplantation. The second dose should be withheld if complications, such as severe hypersensitivity reactions to Simulect or graft loss occur. Reconstitution of 10 mg Simulect ® Vial To prepare the reconstituted solution, add 2.5 mL of Sterile Water for Injection, USP, using aseptic technique, to the vial containing the Simulect powder. Shake the vial gently to dissolve the powder. The reconstituted solution is isotonic and may be given either as a bolus injection or diluted to a volume of 25 mL with 0.9% Sodium Chloride Injection, USP or 5% Dextrose Injection, USP for infusion. When mixing the solution, gently invert the bag in order to avoid foaming; DO NOT SHAKE . Reconstitution of 20 mg Simulect ® Vial To prepare the reconstituted solution, add 5 mL of Sterile Water for Injection, USP, using aseptic technique, to the vial containing the Simulect powder. Shake the vial gently to dissolve the powder. The reconstituted solution is isotonic and may be given either as a bolus injection or diluted to a volume of 50 mL with 0.9% Sodium Chloride Injection, USP or 5% Dextrose Injection, USP for infusion. When mixing the solution, gently invert the bag in order to avoid foaming; DO NOT SHAKE .
Paediatric
Pediatric Use No randomized, placebo-controlled studies have been completed in pediatric patients. In a safety and pharmacokinetic study, 41 pediatric patients (1-11 years of age [n = 27], 12-16 years of age [n = 14], median age 8.1 years) were treated with Simulect via intravenous bolus injection in addition to standard immunosuppressive agents, including cyclosporine, USP (MODIFIED), corticosteroids, azathioprine, and mycophenolate mofetil. The acute rejection rate at 6 months was comparable to that in adults in the triple-therapy trials. The most frequently reported adverse events were hypertension, hypertrichosis, and rhinitis (49% each), urinary tract infections (46%), and fever (39%). Overall, the adverse event profile was consistent with general clinical experience in the pediatric renal transplantation population and with the profile in the controlled adult renal transplantation studies. The available pharmacokinetic data in children and adolescents are described in CLINICAL PHARMACOLOGY and DOSAGE AND ADMINISTRATION. It is not known whether the immune response to vaccines, infection, and other antigenic stimuli administered or encountered during Simulect therapy is impaired or whether such response will remain impaired after Simulect therapy.
Renal
Review renal impairment dosing; many agents need CrCl/eGFR adjustment.
- CrCl 0–120: Confirm renal dosing in product SmPC / primary label.
Hepatic
Review hepatic impairment dosing; monitor LFTs if agent is hepatically cleared or hepatotoxic.
Safety
Drug interactions
- Adults: 2 doses of 20mg each
- the first 20-mg dose should be given within 2 hours prior to transplantation surgery while the second 20-mg dose should be given 4 days after transplantation.
- Children less than 35 kg: two doses of 10 mg each.
- Children weighing 35kg: two doses of 20 mg each, first dose within 2 hours prior to transplantation surgery while second dose should be given 4 days after transplantation.
Safety
Adverse effects
- ADVERSE REACTIONS Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
- The adverse reaction information from clinical trials does, however, provide a basis for identifying the adverse events that appear to be related to drug use and for approximating rates.
- The incidence of adverse events for Simulect ® (basiliximab) was determined in four randomized, double-blind, placebo-controlled clinical trials for the prevention of renal allograft rejection.
- Two of the studies (Study 1 and Study 2), used a dual maintenance immunosuppressive regimen comprised of cyclosporine, USP (MODIFIED) and corticosteroids, whereas the other two studies (Study 3 and Study 4) used a triple-immunosuppressive regimen comprised of cyclosporine, USP (MODIFIED), corticosteroids, and either azathioprine or mycophenolate mofetil.
- Simulect did not appear to add to the background of adverse events seen in organ transplantation patients as a consequence of their underlying disease and the concurrent administration of immunosuppressants and other medications.
- Adverse events were reported by 96% of the patients in the placebo-treated group and 96% of the patients in the Simulect-treated group.
- In the four placebo-controlled studies, the pattern of adverse events in 590 patients treated with the recommended dose of Simulect was similar to that in 594 patients treated with placebo.
- Simulect did not increase the incidence of serious adverse events observed compared with placebo.
- The most frequently reported adverse events were gastrointestinal disorders, reported in 69% of Simulect-treated patients and 67% of placebo-treated patients.
- The incidence and types of adverse events were similar in Simulect-treated and placebo-treated patients.
- The following adverse events occurred in ≥ 10% of Simulect-treated patients: Gastrointestinal System: constipation, nausea, abdominal pain, vomiting, diarrhea, dyspepsia
- Body as a Whole-General: pain, peripheral edema, fever, viral infection
- Metabolic and Nutritional: hyperkalemia, hypokalemia, hyperglycemia, hypercholesterolemia, hypophosphatemia, hyperuricemia
- Urinary System: urinary tract infection
Use
Indications
- INDICATIONS AND USAGE Simulect ® (basiliximab) is indicated for the prophylaxis of acute organ rejection in patients receiving renal transplantation when used as part of an immunosuppressive regimen that includes cyclosporine, USP (MODIFIED), and corticosteroids.
- The efficacy of Simulect for the prophylaxis of acute rejection in recipients of other solid organ allografts has not been demonstrated.
Pharmacology
Mode of action
: Basiliximab functions as an IL-2 receptor antagonist by binding with high affinity (K a = 1 x 10 10 M -1 ) to the alpha chain of the high affinity IL-2 receptor complex and inhibiting IL-2 binding.
Full mechanism text
: Basiliximab functions as an IL-2 receptor antagonist by binding with high affinity (K a = 1 x 10 10 M -1 ) to the alpha chain of the high affinity IL-2 receptor complex and inhibiting IL-2 binding. Basiliximab is specifically targeted against IL-2Rα, which is selectively expressed on the surface of activated T-lymphocytes. This specific high affinity binding of Simulect ® (basiliximab) to IL-2Rα competitively inhibits IL-2-mediated activation of lymphocytes, a critical pathway in the cellular immune response involved in allograft rejection. While in the circulation, Simulect impairs the 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 Simulect is cleared is unknown (see PRECAUTIONS).
ADME
Pharmacokinetics & PD
| Onset | Product-specific |
|---|---|
| Duration | Product-specific |
| Route | INTRAVENOUS |
| Distribution | at steady state is 8.6 ± 4.1 L. The extent and degree of distribution to various body compartments have not been fully studied. The terminal |
| Elimination | half-life was not influenced by age (20-69 years), gender or race (see DOSAGE AND ADMINISTRATION). Pediatric : The pharmacokinetics of Simulect have been assessed in 39 pediatric patients undergoing renal transplantation. In infants and children (1-11 years of age, n = 25), the |
| Half-life | is 7.2 ± 3.2 days. Total body clearance is 41 ± 19 mL/h. No clinically relevant influence of body weight or gender on |
Full PK/PD text
CLINICAL PHARMACOLOGY General Mechanism of Action: Basiliximab functions as an IL-2 receptor antagonist by binding with high affinity (K a = 1 x 10 10 M -1 ) to the alpha chain of the high affinity IL-2 receptor complex and inhibiting IL-2 binding. Basiliximab is specifically targeted against IL-2Rα, which is selectively expressed on the surface of activated T-lymphocytes. This specific high affinity binding of Simulect ® (basiliximab) to IL-2Rα competitively inhibits IL-2-mediated activation of lymphocytes, a critical pathway in the cellular immune response involved in allograft rejection. While in the circulation, Simulect impairs the 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 Simulect is cleared is unknown (see PRECAUTIONS). Pharmacokinetics Adults : Single-dose and multiple-dose pharmacokinetic studies have been conducted in patients undergoing first kidney transplantation. Cumulative doses ranged from 15 mg up to 150 mg. Peak mean ± SD serum concentration following intravenous infusion of 20 mg over 30 minutes is 7.1 ± 5.1 mg/L. There is a dose-proportional increase in C max and area under the curve (AUC) up to the highest tested single dose of 60 mg. The volume of distribution at steady state is 8.6 ± 4.1 L. The extent and degree of distribution to various body compartments have not been fully studied. The terminal half-life is 7.2 ± 3.2 days. Total body clearance is 41 ± 19 mL/h. No clinically relevant influence of body weight or gender on distribution volume or clearance has been observed in adult patients. Elimination half-life was not influenced by age (20-69 years), gender or race (see DOSAGE AND ADMINISTRATION). Pediatric : The pharmacokinetics of Simulect have been assessed in 39 pediatric patients undergoing renal transplantation. In infants and children (1-11 years of age, n = 25), the distribution volume and clearance were reduced by about 50% compared to adult renal transplantation patients. The volume of distribution at steady state was 4.8 ± 2.1 L, half-life was 9.5 ± 4.5 days and clearance was 17 ± 6 mL/h. Disposition parameters were not influenced to a clinically relevant extent by age (1-11 years of age), body weight (9-37 kg) or body surface area (0.44-1.20 m 2 ) in this age group. In adolescents (12-16 years of age, n = 14), disposition was similar to that in adult renal transplantation patients. The volume of distribution at steady state was 7.8 ± 5.1 L, half-life was 9.1 ± 3.9 days and clearance was 31 ± 19 mL/h (see DOSAGE AND ADMINISTRATION). Pharmacodynamics Complete and consistent binding to IL-2Rα in adults is maintained as long as serum Simulect levels exceed 0.2 mcg/mL. As concentrations fall below this threshold, the IL-2Rα sites are no longer fully bound and the number of T-cells expressing unbound IL-2Rα returns to pretherapy values within 1-2 weeks. The relationship between serum concentration and receptor saturation was assessed in 13 pediatric patients and was similar to that characterized in adult renal transplantation patients. In vitro studies using human tissues indicate that Simulect binds only to lymphocytes. The duration of clinically relevant IL-2 receptor blockade after the recommended course of Simulect is not known. When basiliximab was added to a regimen of cyclosporine, USP (MODIFIED) and corticosteroids in adult patients, the duration of IL-2Rα saturation was 36 ± 14 days (mean ± SD), similar to that observed in pediatric patients (36 ± 14 days) (see DOSAGE AND ADMINISTRATION). When basiliximab was added to a triple therapy regimen consisting of cyclosporine, USP (MODIFIED), corticosteroids, and azathioprine in adults, the duration was 50 ± 20 days and when added to cyclosporine, USP (MODIFIED), corticosteroids, and mycophenolate mofetil in adults, the duration was 59 ± 17 days (see PRECAUTIONS, Drug Interactions). No significant changes to circulating lymphocyte numbers or cell phenotypes were observed by flow cytometry.
Kenya
Brands & prices
| Brand | Company | Pack | KES |
|---|---|---|---|
| Simulect | Novartis Pharma | Standard Commercial Pack | — |
Special populations
Pregnancy & lactation
Pregnancy
Use only if potential benefit justifies potential risk; prefer agents with better reproductive data when alternatives exist.
Lactation
Nursing Mothers It is not known whether Simulect is excreted in human milk. Because many drugs, including human antibodies are excreted in human milk, and because of the potential for adverse reactions, a decision should be made to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Diet
Food & alcohol
- Drug & food interactions (label) Drug Interactions No dose adjustment is necessary when Simulect is added to triple-immunosuppression regimens, including cyclosporine, corticosteroids, and either azathioprine or mycophenolate mofetil. Three clinical trials have investigated Simulect use in combination with triple-therapy regimens. Pharmacokinetics were assessed in two of these trials. Total body clearance of Simulect was reduced by an average 22% and 51% when azathioprine and mycophenolate mofetil, respectively, were added to a regimen consisting of cyclosporine, USP (MODIFIED) and corticosteroids. Nonetheless, the range of individual Simulect clearance values in the presence of azathioprine (12-57 mL/h) or mycophenolate mofetil (7-54 mL/h) did not extend outside the range observed with dual therapy (10-78 mL/h). The following medications have been administered in clinical trials with Simulect with no increase in adverse reactions: ATG/ALG, azathioprine, corticosteroids, cyclosporine, mycophenolate mofetil, and muromonab-CD3. Carcinogenesis/Mutagenesis/Impairment of Fertility No mutagenic potential of Simulect was observed in the i n vitro assays with Salmonella (Ames) and V79 Chinese hamster cells. No long-term or fertility studies in laboratory animals have been performed to evaluate the potential of Simulect to produce carcinogenicity or fertility impairment, respectively. There are no adequate and well-controlled studies in pregnant women. No maternal toxicity, embryotoxicity, or teratogenicity was observed in cynomolgus monkeys 100 days post coitum following dosing with basiliximab during the organogenesis period; blood levels in pregnant monkeys were 13-fold higher than those seen in human patients. Immunotoxicology studies have not been performed in the offspring. Because IgG molecules are known to cross the placental barrier, because the IL-2 receptor may play an important role in development of the immune system, and because animal reproduction studies are not always predictive of human response, Simulect should only be used in pregnant women when the potential benefit justifies the potential risk to the fetus. Women of childbearing potential should use effective contraception before beginning Simulect therapy, during therapy, and for 4 months after completion of Simulect therapy. Nursing Mothers It is not known whether Simulect is excreted in human milk. Because many drugs, including human antibodies are excreted in human milk, and because of the potential for adverse reactions, a decision should be made to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Pediatric Use No randomized, placebo-controlled studies have been completed in pediatric patients. In a safety and pharmacokinetic study, 41 pediatric patients (1-11 years of age [n = 27], 12-16 years of age [n = 14], median age 8.1 years) were treated with Simulect via intravenous bolus injection in addition to standard immunosuppressive agents, including c
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Sources & disclaimer
Source: Local active-ingredient clinical extract; FDA drug label via OpenFDA/DailyMed; Professional class pharmacology (Therapeutic agent (verify pharmacological class))
Last reviewed: 01 Aug 2026
Decision support only — not a substitute for clinical judgment, product SmPC, or Kenya STG/EML.