Basiliximab (Simulect) is a recombinant chimeric murine/human IgG1 monoclonal anti-interleukin-2 receptor antibody that is indicated for the prevention of acute organ rejection in adult and pediatric renal transplant recipients in combination with other immunosuppressive agents. Induction therapy with two doses (day 0 and day 4) of intravenous basiliximab as part of double- or triple-immunotherapy regimens in adult renal transplant recipients reduces acute rejection episodes without increasing the incidence of adverse events. Compared with rabbit-derived antithymocyte globulin (RATG), basiliximab is generally associated with similar efficacy in standard-risk patients, but reduced efficacy in high-risk patients. Initial results indicate that induction with basiliximab is associated with a higher rate of biopsy-proven acute rejection than alemtuzumab induction. Basiliximab is generally associated with a tolerability profile that is similar to that reported with placebo, and better than that reported with RATG. As with other induction agents, basiliximab has not demonstrated improved graft or patient survival over the long term (periods of up to 7 years). Basiliximab induction allows for reduced dosage of corticosteroids or calcineurin inhibitors, while maintaining adequate immunosuppression, thereby reducing the potential for adverse effects associated with these coadministered agents. Thus, basiliximab provides an effective, well tolerated option for the prophylaxis of acute renal transplant rejection.