More from Xevirol
Other strengths and forms by Beacon Pharmaceuticals PLC
Indications & Uses
Pharmacology
Everolimus inhibits mammalian target of rapamycin (mTOR), a serine-threonine kinase acting downstream of the PI3K/AKT pathway. The mTOR pathway is dysregulated in several human cancers and in tuberous sclerosis complex (TSC). Everolimus binds to an intracellular protein, FKBP-12, forming a complex that inhibits mTOR complex 1 (mTORC1) and thereby suppresses mTOR kinase activity. Everolimus reduced the activity of S6 ribosomal protein kinase (S6K1) and eukaryotic initiation factor 4E-binding protein (4E-BP1), both downstream effectors of mTOR involved in protein synthesis. S6K1 is a substrate of mTORC1 and phosphorylates the activation domain 1 of the estrogen receptor, resulting in ligand-independent activation of the receptor. In addition, everolimus inhibited the expression of hypoxia-inducible factor (e.g., HIF-1) and reduced the expression of vascular endothelial growth factor (VEGF). Inhibition of mTOR by everolimus has been shown, in in vitro and/or in vivo studies, to reduce cell proliferation, angiogenesis, and glucose uptake.
Constitutive activation of the PI3K/Akt/mTOR pathway can contribute to endocrine resistance in breast cancer. In vitro studies show that estrogen-dependent and HER2-positive breast cancer cells are sensitive to the inhibitory effects of everolimus, and that combining everolimus with Akt, HER2, or aromatase inhibitors enhances its anti-tumor activity in a synergistic manner.
Dosage Reference
Reference Information Only
Dosages shown are general references from official sources. Always consult your doctor or pharmacist for personalized dosing.
Adults:
Everolimus comes in two different dosage forms, so pick the one that matches the indication. Don't combine Everolimus products to make up the total dose. The dose needs to be adjusted for patients with hepatic impairment, and for those 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 by mouth once daily, continued until disease progression or unacceptable toxicity.
Neuroendocrine Tumors (NET): the recommended dosage is 10 mg by mouth once daily, until disease progression or unacceptable toxicity.
Renal Cell Carcinoma (RCC): again 10 mg by mouth once daily, until disease progression or unacceptable toxicity.
Renal angiomyolipoma associated with Tuberous Sclerosis Complex (TSC): the recommended dosage is 10 mg by mouth once daily, until disease progression or unacceptable toxicity.
Subependymal Giant Cell Astrocytoma (SEGA) associated with TSC: the recommended starting dosage is 4.5 mg/m2 by mouth once daily, until disease progression or unacceptable toxicity.
Partial-onset seizures associated with TSC: the recommended starting dosage is 5 mg/m2 by mouth once daily, until disease progression or unacceptable toxicity.
Side Effects
Most common side effects (occurring in 30% or more of patients) differ by the condition being treated. For breast cancer, neuroendocrine tumours (NET), and renal cell carcinoma (RCC), these include mouth sores, infections, rash, tiredness, diarrhoea, fluid retention (swelling), abdominal pain, nausea, fever, weakness, cough, headache, and reduced appetite. For TSC-associated renal angiomyolipoma, the most common side effect is mouth sores. For TSC-associated SEGA (a type of brain tumour), the most common side effects are mouth sores and respiratory tract infection. For TSC-associated partial-onset seizures, the most common side effect is mouth sores.
Cautions & Contraindications
Warnings & Precautions
Non-infectious pneumonitis: Keep an eye out for clinical symptoms or changes on imaging. Depending on how severe it is, the medicine may need to be held or stopped for good. Infections: Watch for signs and symptoms of infection. Depending on how severe it is, the medicine may need to be held or stopped for good. Severe hypersensitivity reactions: If a clinically significant hypersensitivity reaction happens, stop the medicine for good. Angioedema: People taking angiotensin-converting-enzyme (ACE) inhibitors at the same time may be at higher risk of angioedema. If angioedema occurs, stop the medicine for good. Stomatitis: Start dexamethasone alcohol-free mouthwash when treatment begins. Renal failure: Check kidney function before treatment starts and then from time to time afterwards. Risk of impaired wound healing: Hold the medicine for at least 1 week before elective surgery. Don't give it for at least 2 weeks after major surgery, and not until the wound has healed well. It isn't known whether it is safe to restart treatment once wound healing complications have settled. Geriatric patients: Older patients need to be monitored for side effects, and the dose may need adjusting. Metabolic disorders: Check serum glucose and lipids before treatment and then from time to time. Depending on how severe the problem is, the medicine may need to be held or stopped for good. Myelosuppression: Check blood counts before treatment and then from time to time. Depending on how severe it is, the medicine may need to be held or stopped for good. Risk of infection or reduced immune response with vaccination: Avoid live vaccines, and avoid close contact with people who have had live vaccines. Complete the recommended childhood vaccinations before starting treatment. Radiation sensitization and radiation recall: Severe radiation reactions may occur. Embryo-fetal toxicity: The medicine can harm an unborn baby. Patients who could become pregnant should be told about this risk and advised to use effective contraception.
Contraindications
Do not use everolimus if you have had a clinically significant allergic reaction to everolimus or to any other rapamycin derivative.
Pregnancy & Breastfeeding
Everolimus may harm a developing baby, based on findings from animal studies and how the drug works. A few case reports describe its use during human pregnancy, but there are too few to say how it affects the risk of birth defects or miscarriage. It is not known whether everolimus or its breakdown products pass into breast milk, or what effect it might have on a nursing infant or on milk supply.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Storage
Store Everolimus below 30°C, and keep it away from light and moisture. Keep it out of the reach of children.
Drug Interactions
Common questions about Xevirol 10 mg
What is Xevirol 10 mg Tablet?
Xevirol 10 mg Tablet is a medicine that contains Everolimus. It is made by Beacon Pharmaceuticals PLC. It belongs to the Immunosuppressant group of medicines.
What is Xevirol used for?
Xevirol is used for: Epilepsy, Cancer.
What are the side effects of Xevirol?
Most common side effects (occurring in 30% or more of patients) differ by the condition being treated. For breast cancer, neuroendocrine tumours (NET), and renal cell carcinoma (RCC), these include mouth sores, infections, rash, tiredness, diarrhoea, fluid retention (swelling), abdominal pain, nausea, fever, weakness, cough, headache, and reduced appetite.
Can I take Xevirol during pregnancy or while breastfeeding?
Everolimus may harm a developing baby, based on findings from animal studies and how the drug works. A few case reports describe its use during human pregnancy, but there are too few to say how it affects the risk of birth defects or miscarriage. Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
How should I store Xevirol?
Store Everolimus below 30°C, and keep it away from light and moisture. Keep it out of the reach of children.
Can I take other medicines with Xevirol?
Some medicines can interact with Everolimus, for example: Palbociclib, Verapamil Hydrochloride. Tell your doctor or pharmacist about every medicine you take.
Do I need a prescription for Xevirol?
Xevirol is a prescription (Rx) medicine. Take it as your doctor advises.