Which drugs does everolimus interact with?

Everolimus is an immunosuppressant used primarily to reduce the risk of organ rejection after kidney and heart transplants and to treat advanced renal cell carcinoma and certain neuroendocrine tumors. However, drug interactions may occur when everolimus is used in combination with other drugs, affecting its efficacy or increasing the risk of potential adverse reactions. The following are some drugs that may interact with everolimus:

CYP3A4Inhibitors:

StrongCYP3A4Inhibitors: Concomitant use with everolimus should be avoided because these drugs may significantly inhibit the metabolism of everolimus, leading to an increase in everolimus blood concentration and increasing the risk of adverse reactions.

ModerateCYP3A4Inhibitors: If combined use is necessary, use caution and reduce the dose of everolimus to maintain appropriate plasma concentrations.

CYP3A4Inducer:

StrongCYP3A4Inducers: The simultaneous use with everolimus should also be avoided, because these drugs may accelerate the metabolism of everolimus, resulting in a decrease in the blood concentration of everolimus and weakening the efficacy of the drug. If coadministration cannot be avoided, the dose of everolimus may need to be increased.

Antifungal drugs:

Such as itraconazole, fluconazole and clotrimazole, these drugs may inhibit the activity ofCYP3A enzyme, thereby affecting the metabolism of everolimus and increasing the plasma concentration of everolimus.

Immunosuppressants:

Such as cyclosporine, tacrolimus, etc., when these drugs are combined with everolimus, they may increase the overall effect of immunosuppression, making patients more susceptible to infection. Therefore, patients' immune function needs to be closely monitored and dosage adjustments made as needed.

Other medicines:

Some anti-epileptic drugs (such as carbamazepine, phenytoin, etc.) and anti-tuberculosis drugs may induce the activity of CYP3A enzyme and accelerate the metabolism of everolimus; while some drugs (such as lithium nalsamine and high-dose cimetidine) may inhibit the activity of CYP3A enzyme and increase the plasma concentration of everolimus. Therefore, everolimus should be carefully monitored for efficacy and adverse effects when used concomitantly with these drugs.

In addition, there are interactions between everolimus and food. Food can significantly affect the absorption of everolimus, so patients are advised to maintain a consistent dosing regimen to avoid fluctuations in drug exposure.

References:

https://www.medicalnewstoday.com/articles/drugs-afinitor-interactions