||Actions and Uses |
Basiliximab (Simulect®) (glycoprotein; mol. wt = 144 kd) is a chimeric (murine 40% /human 60%) monoclonal antibody (IgG1k) produced by recombinant DNA technology. It works by binding to the IL-2 receptor. It gained FDA approval in May 1998 and it is marketed by Novartis Pharmaceuticals Corporation (East Hanover, NJ).
- Basiliximab binds with high affinity and pecificity to the IL-2 receptor a-chain (IL-2Ra or CD25 antigen) on the surface of activated T-lymphocytes. It functions as an IL-2 receptor antagonist inhibiting IL-2-mediated stimulation of lymphocytes, a critical event in the process of allograft rejection.
- It is indicated for the prophylaxis of acute organ rejection in patients receiving renal transplants. It is used as part of an immunosuppressive regimen that may include cyclosporine (or tacrolimus?), and corticosteroids.
- During the 1st year post-transplant, the addition of basiliximab to the standard immunosuppressive regimen resulted in a ~30% reduction in the incidence of acute allograft rejection.
- Basiliximab's volume of distribution is about 9 L in adults and 5 L in children.
- The Total body clearance is 41 ± 19 mL/hr and terminal elimination half-life is 7 days.
- Clearance is not affected by body weight or gender. Also, among adult patients, elimination half-life is not influenced by gender, race, or age (20-69 years) .
- Compared to adults, children (2 - 15 yrs) have a lower clearance and a longer half-life (11.5 days).
||Contraindications and Warnings|
- Cases of significant hypersensitivity reactions have been reported.
- Contraindicated in patients who experienced a serious hypersensitivity reaction in the past.
Lyophilisate (powder) for injection. Each vial contains 20 mg of basiliximab to be reconstitued in 5 mL of sterile water for injection to yield a clear, sterile colorless preservative-free phosphate-buffered solution. This must be further diluted in 50 mL NS before iv administration (see below).
||Dose and Administration|
- Adults: The recommended regimen consists of two 20-mg doses given iv. The 1st dose should be given within 2 hrs prior to the transplant surgery. The second dose should be given 4 days after the transplant.
- Pediatric (2 - 15 years of age) protocol is similar to that for adults except that the recommended dose is 12 mg / m2 BSA, up to a maximum of 20 mg.
- Each dose should be diluted in 50 mL of normal saline (or D5W) and infused inravenously over 20 minutes via a peripheral or a central line.
- The solution should not be shaken and should be used within a few hrs of reconstitution (it is stable for 4 hrs at room temperature and for 24 hrs when refrigerated) .
- Pre-medication is recommended. See administration protocol
- Although there is no need for a test dose, medications for the treatment of severe hypersensitivity reactions (e.g., epinephrine) should be available for immediate use.
||Main Side Effects |
- Data are still very limited.
- Addition of basiliximab did not increase the incidence of side effects, that are usually observed with the standard immunosuppressive regimen.
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- Ponticelli C, Tarantino A. Promising new agents in the prevention of transplant rejection. Drugs R D. 1999; 1(1):55-60.
- Berard JL, Velez RL, Freeman RB, Tsunoda SM.
A review of interleukin-2 receptor antagonists in solid organ transplantation. Pharmacotherapy. 1999;19(10):1127-37.
- Onrust SV, Wiseman LR. Basiliximab. Drugs. 1999;57(2):207-13
- Kirkman RL. New usage paradigms in antibody therapy: induction or true prophylaxis? Transplant Proc. 1999;31(1-2):1234-5.