Everolimus is an mTOR inhibitor with anti-tumor and immunomodulatory effects, mainly used to treat specific cancers and rejection reactions after organ transplantation. The following will provide a detailed explanation of its effects and drug interactions, ensuring the safety and effectiveness of clinical medication.

1. Effect of action

(1) Antitumor effect: It blocks tumor cell proliferation and angiogenesis by inhibiting mTOR signal pathway, and is used to treat advanced renal cell carcinoma, breast cancer, etc.

(2) Immunosuppressive effect: Inhibits T cell activation and is used to prevent rejection reactions after organ transplantation.

(3) Other functions: It can also be used to treat subarachnoid giant cell astrocytomas and renal angiomyolipomas related to tuberous sclerosis.

2. Drug interactions

(1) CYP3A4 inhibitor

Co administration with potent CYP3A4 inhibitors such as ketoconazole and clarithromycin can increase the blood concentration of everolimus, requiring a 50% reduction in dosage.

(2) CYP3A4 inducer

Co administration with potent CYP3A4 inducers such as rifampicin and carbamazepine can reduce the blood concentration of everolimus, requiring a 50% increase in dosage.

(3) P-gp inhibitor

Co administration with P-gp inhibitors such as verapamil and quinidine may increase the absorption of everolimus, and adverse reactions need to be closely monitored.

(4) Other interactions

Avoid co administration with live vaccines; Co administration with angiotensin-converting enzyme inhibitors may increase the risk of angioedema; The use of warfarin requires strengthened INR monitoring.

3. Precautions

(1) During the treatment period, regular monitoring of blood routine, renal function, blood glucose, and lipid levels is required.

(2) Avoid consuming grapefruit or grapefruit juice as it may increase drug concentration.

(3) Effective contraceptive measures should be taken during the treatment period and within 8 weeks after discontinuation of medication for patients of childbearing age.