AFINITOR 5mg Tablets

What is AFINITOR 5mg

AFINITOR 5mg is a prescription medication whose active ingredient is Everolimus. It belongs to a class of drugs known as mTOR (mammalian target of rapamycin) inhibitors. AFINITOR is primarily used in oncology and transplant medicine, but in oncology, it is indicated for the treatment of certain types of cancers such as advanced kidney cancer (renal cell carcinoma), hormone receptor-positive breast cancer, neuroendocrine tumors of pancreatic origin, and some types of brain tumors (subependymal giant cell astrocytoma) associated with tuberous sclerosis complex.

Everolimus works by inhibiting a key protein (mTOR) that regulates cell growth, proliferation, and survival, effectively slowing down or stopping the growth of cancer cells. Additionally, it can reduce the immune system’s activity, which is why it is sometimes used in organ transplant patients to prevent rejection, though this use is separate from the cancer treatment indication.

• Class: mTOR inhibitor
• Form: Oral tablets
• Strength: 5 mg per tablet
• Packaging: 30 tablets (3 blisters of 10 tablets each)
• Uses: Treatment of various advanced cancers and some non-cancer indications related to immune modulation

Because it targets the molecular pathways critical for tumor growth, AFINITOR has become an important therapeutic option in personalized cancer care, often used when other treatments have failed or in combination with other therapies.

How to use AFINITOR 5mg

Proper use of AFINITOR 5mg tablets is crucial for maximizing treatment benefits while minimizing risks. Always follow your healthcare provider’s instructions carefully.

• Dosage: The dose depends on the type of cancer or condition being treated. Typically, it is taken once daily at the same time each day to maintain consistent blood levels.
• Administration: Swallow the tablet whole with water. Do not crush, chew, or break the tablet.
• With or without food: It can be taken with or without food, but try to be consistent with how you take it daily.
• Missed dose: If you miss a dose, take it as soon as you remember unless it is almost time for your next dose. Do not double up doses.
• Monitoring: Regular blood tests and clinical check-ups are needed to monitor blood counts, kidney and liver function, and drug levels.
• Drug adjustments: Dosage may be adjusted based on side effects or blood test results. Never adjust your dose without consulting your doctor.
• Interactions: Avoid grapefruit or grapefruit juice as it can affect drug metabolism and increase side effects.

Always inform your healthcare provider about all other medications, supplements, or herbal products you are taking before starting AFINITOR.

Mode of Action AFINITOR 5mg

AFINITOR’s active substance, Everolimus, exerts its effects by targeting the mTOR (mammalian target of rapamycin) pathway, a central regulator of cell growth, proliferation, metabolism, and survival.

• Inhibition of mTOR complex 1 (mTORC1): Everolimus binds to the intracellular protein FKBP-12 to form a complex that inhibits mTORC1.
• Cell cycle arrest: By blocking mTORC1, the drug halts progression of the cell cycle from the G1 to S phase, preventing cancer cells from proliferating.
• Reduced protein synthesis: mTOR regulates protein production necessary for cell growth. Its inhibition reduces synthesis of proteins involved in cell division.
• Anti-angiogenic effect: mTOR inhibition also decreases production of vascular endothelial growth factor (VEGF), limiting tumor blood vessel formation needed for tumor growth.
• Immunosuppressive action: In transplant patients, Everolimus suppresses immune responses by inhibiting T-cell activation and proliferation.

Through these mechanisms, AFINITOR can slow or stop the growth of tumors and reduce tumor burden, making it effective against several cancers resistant to conventional chemotherapy.

AFINITOR 5mg Interactions AFINITOR 5mg

AFINITOR (Everolimus) can interact with many drugs, affecting its effectiveness or increasing the risk of adverse effects. Key drug interactions include:

• CYP3A4 inhibitors: Drugs like ketoconazole, itraconazole, clarithromycin, and ritonavir can increase Everolimus blood levels, raising toxicity risk.
• CYP3A4 inducers: Rifampin, carbamazepine, phenytoin, and St. John’s Wort can reduce Everolimus levels, lowering efficacy.
• Immunosuppressants: Concurrent use with other immunosuppressants may increase infection risk.
• Live vaccines: Should be avoided as Everolimus suppresses immune function, increasing risk of vaccine-related infections.
• Anticoagulants: Everolimus may interact with drugs like warfarin; close monitoring of coagulation parameters is required.
• Grapefruit and grapefruit juice: These can increase Everolimus levels and side effects by inhibiting CYP3A4 enzymes in the gut.

Always disclose your full medication list to your healthcare provider and pharmacist to avoid harmful interactions.

Dosage of AFINITOR 5mg

The dosage of AFINITOR varies based on the indication, patient condition, and tolerability. Below are typical dosing guidelines:

• Renal cell carcinoma (advanced): Usually 10 mg once daily, but sometimes adjusted based on tolerability.
• Neuroendocrine tumors of pancreatic origin: 10 mg once daily.
• Hormone receptor-positive breast cancer (in combination therapy): 10 mg once daily.
• Subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis: Dosing is based on body surface area, often starting at 4.5 mg/m2 once daily.

Note: The 5 mg tablet strength may be used for dose adjustments, interruptions, or in patients requiring lower doses due to side effects or drug interactions.

Dose modifications may be necessary if severe adverse effects occur, and regular clinical monitoring is mandatory to adjust doses safely.

Possible side effects of AFINITOR 5mg

Like all medications, AFINITOR may cause side effects, ranging from mild to serious. Common and notable side effects include:

• Mouth ulcers/stomatitis: Common and sometimes painful sores in the mouth.
• Infections: Increased susceptibility to bacterial, viral, or fungal infections due to immunosuppression.
• Fatigue and weakness: General tiredness is often reported.
• Diarrhea and nausea: Gastrointestinal symptoms are frequent.
• Rash and skin reactions: Various dermatologic issues including rash, dry skin, or acne.
• Metabolic disturbances: Elevated blood sugar (hyperglycemia), cholesterol, and triglycerides.
• Interstitial lung disease: Rare but serious lung inflammation that requires immediate medical attention.
• Kidney function impairment: Possible changes in renal function; regular monitoring advised.
• Edema and swelling: Particularly in extremities.

Any severe or unusual symptoms should be reported promptly to a healthcare provider. Most side effects can be managed with dose adjustments or supportive care.

AFINITOR 5mg Contraindications AFINITOR 5mg

AFINITOR is contraindicated in certain conditions where its use would be unsafe or ineffective:

• Hypersensitivity: Known allergy to Everolimus or any component of the tablet formulation.
• Severe infections: Active serious infections contraindicate use due to immune suppression.
• Impaired liver function: Severe hepatic impairment requires caution or avoidance as metabolism may be altered.
• Pregnancy and breastfeeding: Not recommended due to potential harm to fetus or infant.
• Concomitant use with strong CYP3A4 inhibitors or inducers: May contraindicate due to risk of toxicity or loss of efficacy.

Always consult a healthcare provider for personalized assessment before starting AFINITOR.

Storage of AFINITOR 5mg

Proper storage of AFINITOR ensures its potency and safety. Follow these guidelines:

• Store tablets at room temperature, ideally between 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light by keeping tablets in their original blister packs until use.
• Keep the medication out of reach of children and pets.
• Avoid storing in bathrooms or other damp environments.
• Do not use tablets past the expiration date printed on the package.
• Dispose of unused or expired medication according to local regulations or pharmacy guidelines.

Maintaining proper storage conditions preserves drug effectiveness and reduces the risk of contamination.