RAD001: Difference between revisions

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A drug used with exemestane to treat some postmenopausal women with advanced breast cancer that is hormone receptor positive and HER2 negative. It is also used to treat advanced renal cell carcinoma (a type of kidney cancer) and certain types of pancreatic, lung, and gastrointestinal neuroendocrine tumors. It is used under the brand name Afinitor to treat these cancers and to treat renal angiomyolipoma (a type of benign kidney tumor) and subependymal giant cell astrocytoma (SEGA, a type of benign brain tumor) in patients who have tuberous sclerosis. RAD001 is also used under the brand name Afinitor Disperz to treat SEGA and certain types of seizures in patients who have tuberous sclerosis. It is also used under the brand name Zortress to keep the body from rejecting a kidney or liver transplant. RAD001 is also being studied in the treatment of other conditions and types of cancer. It blocks a protein involved in cell division, which may help keep abnormal cells, including cancer cells, from growing. It may also prevent the growth of new blood vessels that tumors need to grow. RAD001 also lowers the body’s immune response. It is a type of kinase inhibitor, a type of angiogenesis inhibitor, and a type of immunosuppressant. Also called everolimus.
RAD001
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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==
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==
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==
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==
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==
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==
* [[mTOR inhibitors]]
* [[Sirolimus]]
* [[Renal cell carcinoma]]
* [[Breast cancer]]
* [[Neuroendocrine tumor]]
 
{{Drugbox
| Verifiedfields = changed
| verifiedrevid = 477002123
| IUPAC_name = 40-O-(2-hydroxyethyl)-rapamycin
| image = Everolimus.svg
| width = 250
| tradename = Afinitor, Zortress
| Drugs.com =
| MedlinePlus = a608035
| pregnancy_AU = D
| pregnancy_US = C
| legal_AU = S4
| legal_CA = Rx-only
| legal_UK = POM
| legal_US = Rx-only
| routes_of_administration = Oral
| bioavailability = 30%
| protein_bound = 74%
| metabolism = Liver (CYP3A4)
| elimination_half-life = 30 hours
| excretion = Feces (80%), urine (5%)
| CAS_number = 159351-69-6
| ATC_prefix = L01
| ATC_suffix = XE10
| PubChem = 6442177
| DrugBank = DB01590
| ChemSpiderID = 4946845
| UNII = 9HW64Q8G6G
| KEGG = D03210
| ChEBI = 68478
| ChEMBL = 1201187
| synonyms = RAD001
}}
 
[[Category:Immunosuppressants]]
[[Category:Antineoplastic drugs]]
[[Category:Organ transplant rejection medications]]
[[Category:Pharmacology]]

Latest revision as of 22:29, 15 December 2024

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]

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]

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]

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]

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]

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]


RAD001
File:Everolimus.svg
INN
Drug class
Routes of administration Oral
Pregnancy category
Bioavailability 30%
Metabolism Liver (CYP3A4)
Elimination half-life 30 hours
Excretion Feces (80%), urine (5%)
Legal status
CAS Number 159351-69-6
PubChem 6442177
DrugBank DB01590
ChemSpider 4946845
KEGG D03210
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