RAD001
RAD001
RAD001, also known as everolimus, is an immunosuppressant drug used primarily in the treatment of various types of cancer and in the prevention of organ transplant rejection. It is a derivative of sirolimus (rapamycin) and functions as an mTOR (mammalian target of rapamycin) inhibitor.
Mechanism of Action[edit | edit source]
Everolimus works by inhibiting the mTOR pathway, which is crucial for cell growth, proliferation, and survival. The mTOR pathway is often dysregulated in cancer, leading to uncontrolled cell division and tumor growth. By inhibiting mTOR, everolimus can slow down or stop the growth of cancer cells.
Medical Uses[edit | edit source]
Everolimus is approved for use in several medical conditions, including:
- Renal Cell Carcinoma: It is used in the treatment of advanced kidney cancer.
- Breast Cancer: Specifically, hormone receptor-positive, HER2-negative breast cancer in postmenopausal women.
- Neuroendocrine Tumors: Used for certain types of neuroendocrine tumors of pancreatic origin.
- Tuberous Sclerosis Complex: For the treatment of subependymal giant cell astrocytoma (SEGA) and renal angiomyolipoma associated with tuberous sclerosis complex.
- Organ Transplantation: Used to prevent rejection in liver and kidney transplants.
Side Effects[edit | edit source]
Common side effects of everolimus include:
- Stomatitis (mouth ulcers)
- Infections
- Fatigue
- Diarrhea
- Rash
- Edema
Serious side effects can include:
- Non-infectious pneumonitis
- Hyperglycemia
- Hyperlipidemia
- Renal failure
Pharmacokinetics[edit | edit source]
Everolimus is administered orally and has a bioavailability of approximately 30%. It is metabolized in the liver by the cytochrome P450 3A4 enzyme and is excreted primarily in the feces.
Research and Development[edit | edit source]
Everolimus continues to be the subject of research for its potential use in other types of cancer and diseases. Ongoing clinical trials are exploring its efficacy in combination with other therapies.
Also see[edit | edit source]
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Contributors: Bonnu, Prab R. Tumpati, MD
