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Novartis AG

Drug Names(s): everolimus (transplant), RAD001, Certican

Description: BioMedTracker has separate drug profiles for everolimus. Please also see Afinitor for oncology indications.

Certican (everolimus), a proliferation signal inhibitor, prevents allograft rejection in rodent and nonhuman primate models of allotransplantation. It exerts its immunosuppressive effect byinhibiting the proliferation, and thus clonal expansion, of antigen-activated T cells which isdriven by T cell-specific interleukins, e.g. interleukin-2 and interleukin-15. Everolimusinhibits an intracellular signalling pathway which is triggered upon binding of these T cellgrowth factors to their respective receptors, and which normally leads to cell proliferation.The blockage of this signal by everolimus leads to an arrest of the cells at the G1 stage of thecell cycle.

At the molecular level, everolimus forms a complex with the cytoplasmic protein FKBP-12.In the presence of everolimus the growth factor-stimulated phosphorylation of the p70 S6kinase is inhibited. Since p70 S6 kinase phosphorylation is under the control of FRAP (alsocalled m-TOR), this finding suggests that the everolimus-FKBP-12 complex binds to and thusinterferes with the function of FRAP. FRAP is a key regulatory protein which governs cellmetabolism, growth and proliferation; disabling FRAP function thus explains the cell cyclearrest caused by everolimus.

Everolimus, thus, has a different mode of action than ciclosporin. In preclinical models ofallotransplantation, the combination of everolimus and ciclosporin was more effective than either compound alone.

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