AFINITOR 10mg Tablets

What is AFINITOR 10mg

AFINITOR is the brand name for oral **Everolimus**, a targeted cancer therapy belonging to the **mTOR (mammalian target of rapamycin) inhibitor** class. Each tablet contains 10 mg of the active ingredient, provided in a pack of 30 tablets (3 blisters of 10 tablets each). Over time, the active ingredient may be available in generic forms.

• Oncology uses: Advanced renal cell carcinoma, hormone receptor‑positive, HER2‑negative breast cancer (postmenopausal), unresectable or metastatic neuroendocrine tumors, renal angiomyolipoma, and SEGA in tuberous sclerosis complex :contentReference[oaicite:1]{index=1}.
• Immunosuppressive use: In transplant medicine under names such as Zortress or Certican to prevent organ rejection :contentReference[oaicite:2]{index=2}.
• Essential medicine: Recognised by WHO as vital for basic healthcare :contentReference[oaicite:3]{index=3}.

By inhibiting mTOR signaling, AFINITOR blocks tumor cell growth and angiogenesis. Its role in immunosuppression and potential in drug-eluting stents also underscores its widely diverse clinical applications.

How to use AFINITOR 10mg

Administration should follow the prescribing oncologist’s instructions. General guidelines:

• Schedule: One tablet (10 mg) orally once daily, at the same time each day — continue until disease progression or intolerable toxicity :contentReference[oaicite:4]{index=4}.
• Method: Swallow whole with a full glass of water; do not chew or split :contentReference[oaicite:5]{index=5}.
• Food: Can be taken with or without food, but maintain consistency :contentReference[oaicite:6]{index=6}.
• Missed dose: If <6 hours late, take immediately; if >6 hours, skip and resume next day. Do not double up :contentReference[oaicite:7]{index=7}.
• Monitoring: Regular check-ups—CBC, liver and kidney function, lipid panel, and glucose—are recommended, especially early in treatment :contentReference[oaicite:8]{index=8}.
• Avoid grapefruit: Grapefruit and juice should be avoided as they can raise Everolimus levels :contentReference[oaicite:9]{index=9}.

Strict consistency in dosing and vigilant follow-up helps maximize efficacy and minimize toxicity.

Mode of Action AFINITOR 10mg

Everolimus exerts its primary action by inhibiting the protein kinase **mTORC1**, a central regulator of cell growth, proliferation, metabolism, and angiogenesis.

• FKBP12 binding: Everolimus binds to FKBP12 protein, and this complex specifically inhibits mTORC1, blocking progression from G1 to S phase in the cell cycle :contentReference[oaicite:10]{index=10}.
• Antiproliferative effects: Tumor cells stop multiplying; efficacy observed in cancers and in reducing angiogenesis :contentReference[oaicite:11]{index=11}.
• Antiangiogenesis: Suppresses VEGF expression and vessel formation, limiting tumor nutrient supply :contentReference[oaicite:12]{index=12}.
• Selective targeting: Preferentially inhibits mTORC1 over mTORC2, reducing side effects like glucose intolerance :contentReference[oaicite:13]{index=13}.
• Immunomodulatory action: Dampens immune function, beneficial in transplant but requiring infection vigilance :contentReference[oaicite:14]{index=14}.

This multifunctional mechanism—both antiproliferative and antiangiogenic—enables AFINITOR to be effective in diverse oncologic and immunologic settings.

AFINITOR 10mg Interactions AFINITOR 10mg

Everolimus is primarily metabolized by **CYP3A4** and is also a substrate of **P‑glycoprotein (P‑gp)**. Numerous clinically significant drug interactions can alter blood levels of AFINITOR:

• ↑ Drug levels (CYP3A4/P‑gp inhibitors): Ketoconazole, itraconazole, clarithromycin, ritonavir, grapefruit juice—can potentiate toxicity :contentReference[oaicite:15]{index=15}.
• ↓ Drug levels (CYP3A4/P‑gp inducers): Rifampin, phenytoin, carbamazepine, St. John’s Wort—may reduce therapeutic effect :contentReference[oaicite:16]{index=16}.
• ACE Inhibitors: Combined use may increase angioedema risk :contentReference[oaicite:17]{index=17}.
• Corticosteroids & immunosuppressants: Combined use requires monitoring for infections and drug levels :contentReference[oaicite:18]{index=18}.
• Vaccines: Avoid live vaccines to reduce infection risk :contentReference[oaicite:19]{index=19}.
• Nephrotoxic drugs: NSAIDs and certain antibiotics may add to renal risk :contentReference[oaicite:20]{index=20}.

Before starting AFINITOR, share a full list of medications, including herbal supplements and over‑the‑counter drugs, to help anticipate and manage interactions effectively.

Dosage of AFINITOR 10mg

Dosing depends on condition and patient characteristics. Typical regimens include:

• Adult cancer indications (RCC, NET, breast cancer, angiomyolipoma): 10 mg orally once daily until therapy stops :contentReference[oaicite:21]{index=21}.
• TSC‑associated SEGA in pediatrics: 2.5 to 7.5 mg once daily, based on body surface area and trough levels :contentReference[oaicite:22]{index=22}.
• TSC‑associated seizures: AFINITOR DISPERZ (suspension form), 5 mg/m² once daily :contentReference[oaicite:23]{index=23}.
• Hepatic impairment or drug interactions: Dose reduction to 5 mg (or even 2.5 mg) may be necessary :contentReference[oaicite:24]{index=24}.
• Adjustments: Based on lab results, side effects like pneumonitis or myelosuppression, and drug interactions :contentReference[oaicite:25]{index=25}.
• Monitoring: Therapeutic drug monitoring (trough levels 5–15 ng/mL) is recommended, especially in pediatrics or with interacting drugs :contentReference[oaicite:26]{index=26}.

Any dose changes—reductions or interruptions—should be physician-supervised based on side effects or lab results.

Possible side effects of AFINITOR 10mg

AFINITOR has both common and potentially serious adverse effects. Monitoring and timely management are critical.

• Mouth ulcers/stomatitis (44–78% incidence) :contentReference[oaicite:27]{index=27}.
• Fatigue, weakness, loss of appetite :contentReference[oaicite:28]{index=28}.
• Rash, dry or itchy skin (up to 59%) :contentReference[oaicite:29]{index=29}.
• Gastrointestinal upset: diarrhea, constipation, nausea/vomiting :contentReference[oaicite:30]{index=30}.
• Infections (including serious types in ~10%) :contentReference[oaicite:31]{index=31}.
• Edema (hands, feet, face), abnormal taste, mouth/throat pain :contentReference[oaicite:32]{index=32}.
• Metabolic changes: hyperglycemia and hyperlipidemia (up to 75–86%) :contentReference[oaicite:33]{index=33}.

• Non‑infectious pneumonitis (19% incidence; Grade 3/4 in some) :contentReference[oaicite:34]{index=34}.
• Myelosuppression: anemia, neutropenia, thrombocytopenia (up to Grade 3/4) :contentReference[oaicite:35]{index=35}.
• Renal impairment, including acute failure :contentReference[oaicite:36]{index=36}.
• Angioedema—especially with ACE inhibitors :contentReference[oaicite:37]{index=37}.
• Severe infection risk, including opportunistic infections :contentReference[oaicite:38]{index=38}.

Patients should promptly report breathing difficulties, persistent infections, mouth pain, unexpected bleeding, or metabolic abnormalities. Dose modifications or discontinuation may be required depending on severity.

AFINITOR 10mg Contraindications AFINITOR 10mg

AFINITOR is contraindicated in certain circumstances to avoid life-threatening consequences:

• Hypersensitivity: Allergy to everolimus, other rapalogs (e.g., sirolimus), or formulation excipients :contentReference[oaicite:39]{index=39}.
• Severe hepatic impairment: Caution or avoid unless under specialist supervision :contentReference[oaicite:40]{index=40}.
• Pregnancy/breastfeeding: Can cause fetal harm; effective contraception is essential during therapy and for weeks after discontinuation :contentReference[oaicite:41]{index=41}.
• Untreated infections: Active serious infections must be controlled before starting :contentReference[oaicite:42]{index=42}.
• Live vaccine contraindication: Avoid during and shortly after treatment due to immunosuppression :contentReference[oaicite:43]{index=43}.
• Pediatrics (under 1 year or BSA < 0.58 m²): Contraindicated for SEGA :contentReference[oaicite:44]{index=44}.

A full evaluation must be done before initiating therapy to assess risks from comorbid conditions, other drugs, and organ function.

Storage of AFINITOR 10mg

Maintaining the medication’s integrity requires proper storage:

• Temperature: Store at 20–25 °C (68–77 °F), with excursions permitted between 15–30 °C (59–86 °F) :contentReference[oaicite:45]{index=45}.
• Packaging: Keep tablets in original blister pack until use; protect from light and moisture :contentReference[oaicite:46]{index=46}.
• Discarding: Do not use after expiry date; properly dispose of used/blistered tablets in accordance with local guidelines :contentReference[oaicite:47]{index=47}.
• Safety: Keep out of reach of children and pets :contentReference[oaicite:48]{index=48}.

Following these guidelines helps preserve therapeutic efficacy and patient safety.