Everolimus – mTOR Inhibitor Therapy

Everolimus is a potent selective inhibitor of the mammalian target of rapamycin (mTOR), possessing significant anti-tumor and immunosuppressive properties. The drug blocks the specific mTORC1 protein, which acts as a central regulator of cell division and metabolism.

The mechanism of action involves binding to the intracellular protein FKBP-12. The resulting complex inhibits the activity of the mTOR kinase, leading to cell cycle arrest in the G1 phase. This blocks the proliferation of tumor cells, suppresses angiogenesis (the formation of new blood vessels), and reduces glucose uptake by cancer cells. In transplantation, the drug inhibits T-lymphocyte activation, thereby preventing organ rejection.

Everolimus is administered orally once daily, ensuring a stable concentration of the active substance in the systemic circulation.

Wikipedia page
Everolimus

Indications

Everolimus is used in both oncology and transplantation settings:

  • Breast Cancer: treatment of advanced HR-positive, HER2-negative breast cancer in postmenopausal women (in combination with exemestane).
  • Neuroendocrine Tumors (NET): treatment of progressive NET of pancreatic, gastrointestinal, or lung origin.
  • Renal Cell Carcinoma (RCC): therapy for advanced RCC after failure of VEGF-targeted therapy.
  • Tuberous Sclerosis Complex (TSC): treatment of renal angiomyolipoma and subependymal giant cell astrocytoma (SEGA).
  • Transplantation: prophylaxis of organ rejection in kidney or heart transplant recipients.

Dosage and administration

Everolimus dosing depends on the medical indication and requires regular monitoring of organ function.

  • Standard Oncology Dose: typically 10 mg taken once daily.
  • Administration: should be taken at the same time each day, either consistently with or without food.
  • Restrictions: avoid grapefruit juice and St. John’s wort, as they significantly affect drug metabolism.
  • Monitoring: in transplantation, therapeutic drug monitoring (TDM) of whole blood levels is required.
  • Adjustments: the dose should be reduced in patients with moderate hepatic impairment.

The use of everolimus is contraindicated in the following cases:

  • Hypersensitivity: allergic reactions to everolimus, sirolimus, or any excipients.
  • Pregnancy and Lactation: potential fetal harm; breastfeeding is prohibited during therapy.
  • Severe Hepatic Impairment: Child-Pugh Class C.
  • Pediatric Use: age restrictions apply depending on the specific condition being treated (e.g., SEGA).

Everolimus therapy may be associated with the following adverse reactions:

  • Mucosal: stomatitis and oral ulcerations (the most common side effect).
  • Respiratory: risk of non-infectious pneumonitis (requires monitoring).
  • Metabolic: increased levels of blood cholesterol, triglycerides, and glucose.
  • Infections: increased susceptibility to bacterial, fungal, and viral infections.
  • Hematologic: anemia, lymphopenia, and thrombocytopenia.
  • General: skin rash, fatigue, and peripheral edema.

Frequently Asked Questions

Everolimus is an mTOR inhibitor that regulates cell division and the growth of blood vessels in tumors. It is used to treat advanced renal cell carcinoma, hormone receptor-positive breast cancer, and neuroendocrine tumors (NET) of pancreatic, lung, or gastrointestinal origin.
Afinitor is the original drug by Novartis. Indian generics (e.g., Evermil, Evelimus) available on Unifarm contain the same active ingredient in 5mg and 10mg dosages. They provide the same therapeutic effect but at a significantly lower cost.
The medication is taken once daily at the same time each day. Tablets must be swallowed whole with water. It is important to be consistent: either always take it with food or always on an empty stomach to maintain steady levels in the blood.
Common side effects include stomatitis (mouth sores), rash, fatigue, diarrhea, and an increased risk of infections. Everolimus can also increase blood sugar and cholesterol levels, so regular laboratory monitoring is required during treatment.
Grapefruit juice and grapefruit inhibit the enzyme that breaks down everolimus. This leads to a sharp increase in drug levels in the body, significantly increasing toxicity and the risk of serious complications.
The price depends on the dosage (5mg or 10mg) and the manufacturer. Unifarm offers Indian generics at the most competitive prices compared to the original. Current pricing can be found in the catalog or by contacting our specialist.
You can place an order on the Unifarm website. We provide fast delivery of medications throughout Ukraine. If you have questions about the availability of a specific brand, please contact us via the contact form or by phone.

List of medicines by active substance Everolimus

-17%
Evermil 10 mg Glenmark
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Glenmark

Evermil

Everolimus
10 mg 10 tablets
4395₴ 5274₴
✅ All products loaded (1)

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