Everolimus

EDTA Blood, 1ml

Type of drug: Immunosuppressive
Metabolism: CYP3A4, P-gp(ABCB1)
Half life t½: 26-38h
Steady State: 1-2 weeks
TDM: highly recommended/ norm of treatment
Additional informations: Levels of >15µg/l should be avoided due to the higher likelihood of side effects. Beware of interactions with CYP3A4 and P-gp(ABCB1) inhibitors.

Everolimus, as gained from actinomycytes, blocks the antigens’ activated T-cell proliferation of the G1-phase into the S-phase of the cell cycle by means of its immune suppressive characteristics. The mechanism is based on the bonding of the active agent with the mTOR protein, which leads to the inhibition of the cytokinin mediated signal transduction: i.e. the inhibition of the activating of the S6 ribosome proteins and the formation complex of the p34cdc2-kinase with cyclin E. For this reason everolimus is primarily administered after heart- and kidney –transplantations, but also for the therapy of kidney carcinomas. Moreover, the active agent can decelerate growth in polycystic kidneys and enhance kidney function. Possible side effects are infections, anaemia and thrombocytopenia.