Introduction
Everolimus is an orally administered mTOR inhibitor, which is a type of antineoplastic drug. It is used to treat advanced renal cell carcinoma (RCC) and subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis complex (TSC). It is believed to act by inhibiting mTOR, the target of rapamycin, a protein involved in the regulation of cell cycle progression, proliferation, angiogenesis, and metabolism.
Uses
Everolimus is used to treat advanced renal cell carcinoma (RCC) and subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis complex (TSC).
| Brand Name | Everolimus |
|---|---|
| Type | |
| Weight | |
| Generic | Everolimus |
| Manufacturer | |
| Available in | English বাংলা |
Mechanism of Action
Everolimus works by inhibiting mTOR, the target of rapamycin, a protein involved in the regulation of cell cycle progression, proliferation, angiogenesis, and metabolism.
How Long Does It Take to Work?
Everolimus usually begins to work within the first few weeks of treatment, with the effects becoming more noticeable over time. Patients treated with Everolimus may experience improvement in symptoms within 8-12 weeks.
Absorption
Everolimus is rapidly and almost completely absorbed following oral administration.
Route of Elimination
Everolimus is primarily eliminated via the bile.
Dosage
Everolimus are two different dosage forms. Select the recommended dosage form based on the indication. Do not combine Everolimus to achieve the total dose. Modify the dosage for patients with hepatic impairment or for patients taking drugs that inhibit or induce P glycoprotein (P-gp) and CYP3A4.Hormone Receptor-Positive, HER2-Negative Breast Cancer: The recommended dosage of Everolimus is 10 mg orally once daily until disease progression or unacceptable toxicity.
Neuroendocrine Tumors (NET): The recommended dosage of Everolimus is 10 mg orally once daily until disease progression or unacceptable toxicity.
Renal Cell Carcinoma (RCC): The recommended dosage of Everolimus is 10 mg orally once daily until disease progression or unacceptable toxicity.
Tuberous Sclerosis Complex (TSC): Associated Renal Angiomyolipoma: The recommended dosage of Everolimus is 10 mg orally once daily until disease progression or unacceptable toxicity.
Tuberous Sclerosis Complex (TSC)-Associated Subependymal Giant Cell Astrocytoma (SEGA): The recommended starting dosage of Everolimus is 4.5 mg/m2 orally once daily until disease progression or unacceptable toxicity.
Tuberous Sclerosis Complex (TSC)-Associated Partial-Onset Seizures: The recommended starting dosage of Everolimus is 5 mg/m2 orally once daily until disease progression or unacceptable toxicity.
For the treatment of advanced RCC, the recommended dosage of Everolimus is 10 mg orally once daily.
Administration
Everolimus should be taken orally, once daily, with or without food.
Side Effects
Common side effects of Everolimus include fatigue, diarrhea, anemia, nausea, stomatitis, asthenia, constipation, decreased appetite, fever, infection, vomiting, cough, mucositis, abdominal pain, and rash.
Toxicity
Everolimus is generally well-tolerated; the most severe toxicities associated with its use are infections and gastrointestinal inflammation. Other side effects that may occur include hypercholesterolemia, hypertension, hypertriglyceridemia, hypophosphatemia, hyperglycemia, and hypokalemia.
Precaution
Patients should be monitored closely for signs and symptoms of infection while taking Everolimus and should be instructed to contact their healthcare provider for any symptoms. Patients may also be at risk of developing severe and potentially fatal complications associated with the use of Everolimus , including interstitial lung disease, hepatotoxicity, and immune-mediated events.
Interactions
Everolimus can interact with a variety of medications and other drugs, and patients should discuss any potential drug interactions with their healthcare provider. Patients should also be aware of potential food–drug interactions and should avoid eating grapefruit or drinking grapefruit juice while taking Everolimus .
Disease Interaction
Everolimus may interact with certain medical conditions, and should be taken with caution in patients with a history of diabetes mellitus, cholestasis, hepatic impairment, severe infections, or autoimmune diseases.
Drug Interactions
Everolimus may interact with certain drugs, and should not be taken with ACE inhibitors, cyclosporine, hypotension-inducing agents, or specific antifungal agents.
Food Interactions
Grapefruit and grapefruit juice should be avoided while taking Everolimus .
Pregnancy Use
Everolimus is not recommended for use in pregnant women. Animal studies have not shown any evidence of fetal harm, but the potential risks to humans are not known.
Lactation Use
Everolimus is not recommended for use in nursing mothers. It is not known whether Everolimus is excreted in breast milk, and the potential risks to an infant are not known.
Acute Overdose
The most commonly reported symptoms following an Everolimus overdose are fatigue, dizziness, and nausea. If an overdose is suspected, it is important to contact a healthcare provider immediately for appropriate medical care.
Contraindication
Everolimus is contraindicated in patients with a history of hypersensitivity to Everolimus or its excipients.
Use Direction
Take Everolimus by mouth, once daily, with or without food. Swallow the capsule whole with water. Do not break, crush, or chew the capsule. Take your Everolimus at the same time each day.
Storage Condition
Keep Everolimus at room temperature, away from light and moisture. Store the capsule in its original container and keep tightly closed.
Volume of Distribution
The volume of distribution of Everolimus is approximately 32L.
Half Life
The half-life of Everolimus is approximately 24 hours.
Clearance
The clearance of Everolimus is approximately 589 mL/min.
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