Everolimus/Afinitor Drug Interaction Study

The drug interaction problem of Everolimus has received great attention in clinical practice, which is closely related to its clear metabolic pathway. Everolimus is mainly metabolized by the hepatic CYP3A4 enzyme system and is also a substrate of the P-glycoprotein transport system. Therefore, any drug that affects the above pathways may change its in vivo exposure level. This characteristic determines that everolimus needs to be used more cautiously when used in combination.

Research generally believes that potentCYP3A4 inhibitors may significantly increase the blood concentration of everolimus, thereby increasing the probability of oral mucositis, infection risk or metabolic abnormalities; while CYP3A4 inducers may reduce its therapeutic effect. This type of interaction is not the "toxicity enhancement" of the drug itself, but is caused by changes in pharmacokinetics in the body. Therefore, it is usually manageable through dose adjustment and medication evaluation.

In the treatment of breast cancer, everolimus is often used in combination with endocrine drugs. Existing overseas data show that there is no significant metabolic antagonism between it and aromatase inhibitors, which is also an important reason why it can be widely used after endocrine resistance. At the same time, in the management of bone metastases, when everolimus is used together with common bone protection treatments, special adjustments are generally not required, but it is still recommended to regularly monitor liver function and metabolic indicators.

With the accumulation of real-world research, clinical understanding of everolimus interactions has gradually shifted from“avoiding combined use” to “scientific management.” Through comprehensive evaluation of patients' concomitant medications, basic liver function and metabolic status, the safety of everolimus in complex treatment regimens (renal cell carcinoma, breast cancer, pancreatic neuroendocrine tumors, etc.) has been increasingly verified. This also further consolidates its stable application status in multi-line treatment.

Reference materials:https://www.drugs.com/everolimus.html