Afinitor Everolimus Tablets

1. Indications and Usage
Advanced Renal Cell Carcinoma (RCC):
Indicated for the treatment of advanced RCC in patients treated previously with sunitinib or sorafenib.
Neuroendocrine Tumors (NETs):
Indicated for the treatment of adult patients with progressive, well-differentiated pancreatic NETs.
Tuberous Sclerosis Complex (TSC):
Indicated for the treatment of TSC-associated subependymal giant cell astrocytoma (SEGA) and renal angiomyolipoma.
Breast Cancer:
Indicated in combination with exemestane for hormone receptor-positive, HER2-negative advanced breast cancer.
2. Dosage and Administration
Recommended Dosage:
Standard Regimen: 10 mg once daily.
TSC-SEGA Regimen: Initial dose based on body surface area (typically 4.5 mg/m² once daily).
Administration: Administer orally at the same time each day, either consistently with food or consistently without food.
Handling:
Swallow whole with water; do not chew or crush.
3. Mechanism of Action
mTOR Inhibition:
Everolimus is a selective mTOR inhibitor.
Physiological Effect:
It binds to the intracellular protein FKBP-12 to form a complex that inhibits the mTOR kinase, thereby downregulating protein synthesis and proliferation of tumor cells and endothelial cells.
4. Safety and Warnings
Non-Infectious Pneumonia:
Everolimus may cause non-infectious pneumonitis, which can be fatal. Monitor for respiratory symptoms.
Metabolic Abnormalities:
Hyperglycemia, hyperlipidemia, and hypertriglyceridemia may occur. Monitor blood glucose and lipid profiles.
Infections:
May increase susceptibility to bacterial, fungal, or viral infections.
5. Adverse Reactions
Most Common:
Stomatitis (mouth sores), rash, infections, fatigue, diarrhea, nausea, edema, anorexia, and cough.
6. Drug Interactions
CYP3A4 and P-gp Inhibitors:
Avoid strong inhibitors (e.g., ketoconazole) as they significantly increase everolimus exposure. Dose reduction is required for moderate inhibitors (e.g., erythromycin).
CYP3A4 Inducers:
Avoid strong inducers (e.g., rifampin) as they decrease everolimus exposure and efficacy.
Live Vaccines:
Avoid live vaccines during treatment.
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Everolimus.
Storage:
Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F).