Afinitor 10 mg (Everolimus)

Adult dose

This medicine should be taken once daily at the same time each day, consistently either with food or on an empty stomach. Swallow the tablet whole with a glass of water; do not chew or crush it. If the tablet is difficult to swallow, place it in water (approximately 30 mL) and stir well until fully dispersed (approximately 7 minutes), then drink it immediately. After drinking, rinse the cup with the same amount of water and drink all of the rinse water to ensure that the full dose is taken. Treatment with this medicine should be initiated by a physician experienced in the use of anticancer therapy. Treatment should continue for as long as clinical benefit is observed or until unacceptable toxicity occurs. 1. Breast cancer, neuroendocrine tumors, renal cell carcinoma, and renal angiomyolipoma associated with tuberous sclerosis complex (TSC) Adult patients The recommended dose of this medicine is 10 mg orally once daily. 2. Subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis complex (TSC) The dose is individualized based on body surface area (BSA, m2) using the Dubois formula. (W; body weight (kg), H; height (cm)) BSA = (W0.425 x H0.725) x 0.007184 Starting dose and trough blood concentration The recommended starting dose of this medicine for the treatment of patients with SEGA associated with TSC is 4.5 mg/m2. (Administer the nearest dose (n) tablet.) The dose may be adjusted by combining this medicine with other strengths to achieve the total dose. The dose should be titrated to achieve a trough blood concentration of 5-15 ng/mL. The dose should be titrated in increments of 2.5 mg to achieve a trough blood concentration associated with an optimal clinical response. When titrating the dose, consider efficacy, safety, concomitant medications, and the current trough blood concentration. Dose titration can be calculated using a simple proportion: New everolimus dose = current dose x (target concentration/current concentration) For example, for a patient whose dose is 2.5 mg based on current BSA and whose steady-state concentration is 4 ng/mL, the new everolimus dose to achieve a trough concentration of at least 5 ng/mL (e.g., 8 ng/mL) is 5 mg (an increase of 2.5 mg from the current daily dose). The trough blood concentration should be assessed within 1-2 weeks after a dose change. If the adjusted dose is not a multiple of 2.5 mg, administer the nearest dose. Dose monitoring The whole-blood concentration of everolimus should be assessed approximately 1-2 weeks after treatment initiation or a dose change. Assess SEGA volume approximately 3 months after starting this medicine, and adjust the dose based on changes in SEGA volume, the corresponding trough blood concentration, and tolerability. Once a stable dose has been achieved, monitor the trough blood concentration every 3-6 months in patients whose BSA has changed, and every 6-12 months in patients with stable BSA. 3. Dose adjustment (1) Adverse reactions: If severe or intolerable adverse drug reactions occur, temporary dose reduction or interruption of treatment may be required. If dose reduction is necessary, approximately 50% of the previously administered dose is recommended. If reducing the dose below the lowest dose of one tablet of this medicine, consider administration every 2 days. Elderly patients (65 years of age or older) No dose adjustment is necessary in elderly patients. Patients with renal impairment No dose adjustment is necessary in patients with renal impairment. Patients with hepatic impairment - Breast cancer, neuroendocrine tumors, renal cell carcinoma, and renal angiomyolipoma associated with tuberous sclerosis complex (TSC): • Mild hepatic impairment (Child-Pugh A): The recommended dose is 7.5mg once daily. If not tolerated, the dose may be reduced to 5mg. • Moderate hepatic impairment (Child-Pugh B): The recommended dose is 5mg once daily. If not tolerated, the dose may be reduced to 2.5mg. • Severe hepatic impairment (Child-Pugh C): Administration is not recommended. Administer only if the therapeutic benefit outweighs the risk, and do not exceed 2.5mg once daily. The dose should be adjusted if the patient's hepatic status (Child-Pugh) changes during treatment. - Subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis complex (TSC) (1) Patients 18 years of age or older • Mild hepatic impairment (Child-Pugh A): The recommended dose is 75% of the dose calculated based on BSA. (Administer the nearest dose (1 tablet).) • Moderate hepatic impairment (Child-Pugh B): The recommended dose is 50% of the dose calculated based on BSA. (Administer the nearest dose (1 tablet).) • Severe hepatic impairment (Child-Pugh C): Administration is not recommended. The whole-blood trough concentration of everolimus should be measured 1 - 2 weeks after starting treatment or after a change in hepatic status (Child-Pugh). The dose should be titrated to achieve a trough concentration of 5-15ng/mL. The dose should be adjusted if the patient's hepatic status (Child-Pugh) changes during treatment.

Child dose

- Breast cancer, neuroendocrine tumors, renal cell carcinoma, and renal angiomyolipoma associated with tuberous sclerosis complex (TSC): The safety and efficacy of this medicine have not been established in pediatric patients under 18 years of age. - Subependymal giant cell astrocytoma (SEGA) associated with TSC: The recommended dose of this medicine for pediatric patients 1 year of age and older is the same as that for adult patients. - SEGA associated with TSC: This medicine is not recommended for patients under 1 year of age with TSC-associated SEGA or for patients under 18 years of age with TSC-associated SEGA who have hepatic impairment, as it has not been studied in these patients. (2) Patients under 18 years of age This medicine is not recommended for patients under 18 years of age with TSC-associated SEGA who have hepatic impairment.

This medication may cause non-infectious pneumonia, which leads to inflammation in the lungs. Symptoms such as difficulty breathing, coughing, and hypoxia should be reported to a doctor immediately. Additionally, this drug suppresses the immune system, making it easier to contract various infections such as bacterial, viral, and fungal infections; rapid treatment is necessary if infection symptoms appear. During the course of this medication, allergic reactions may occur, and immediate consultation with medical professionals should take place if symptoms such as difficulty breathing, skin rashes, or swelling of the face or neck develop. Oral ulcers and stomatitis can be common, so it is important to maintain oral hygiene and avoid mouthwashes with irritating ingredients. Kidney function may decline, so regular blood tests to monitor renal status are necessary. Blood sugar and lipid levels may increase, thus periodic monitoring of blood glucose and cholesterol levels is required. Blood counts may decrease, requiring monitoring via blood tests. There are many drug interactions; thus, caution is necessary, especially when taken with certain antifungals, antibiotics, calcium channel blockers, and foods like grapefruit or grapefruit juice. Patients with poor liver function should avoid using this medicine, or adjust the dosage with the advice of a doctor if necessary. Live vaccine vaccinations should be avoided while taking this medication, and women who are pregnant or may become pregnant should consult a doctor before use. Breastfeeding women should not take this medication and should avoid breastfeeding for at least 2 weeks after taking it. This medication may affect reproductive ability, thus effective contraceptive methods should be used during and for a certain period after taking it. There is no specific antidote for overdose, so appropriate supportive care is required based on symptoms. Lastly, keep this medication out of the reach of children and store it in its original container to prevent misuse.

Non-infectious pneumonia, hypoxia, pleural effusion, cough, dyspnea, pneumonia, bacterial infection, aspergillosis, candidiasis, pneumocystis pneumonia, viral infection, septic shock, sepsis, respiratory failure, liver failure, anaphylaxis, flushing, chest pain, vascular edema, stomatitis, oral ulcer, oral mucositis, acute kidney failure, elevated serum creatinine, proteinuria, hyperglycemia, hypercholesterolemia, hypertriglyceridemia, decreased hemoglobin, lymphopenia, neutropenia, thrombocytopenia, rash, fatigue, diarrhea, nausea, decreased appetite, anemia, taste disturbance, peripheral edema, asthenia, pruritus, weight loss, epistaxis, headache, thrombocytopenia, dyspnea, hemorrhage, hypophosphatemia, hypertension, increased aspartate aminotransferase, increased alanine aminotransferase, diabetes mellitus, insomnia, taste alteration, congestive heart failure, deep venous thrombosis, hemoptysis, pulmonary embolism, acute respiratory distress syndrome, dry mouth, abdominal pain, oral pain, dyspepsia, dysphagia, dry skin, nail disorder, rash, angioedema, arthralgia, increased daytime urination, menstrual irregularities, amenorrhea, fever, mucosal inflammation, noncardiac chest pain, impaired wound healing, weight loss, elevated serum creatinine, nasopharyngitis, upper respiratory infection, urinary tract infection, sinusitis, pharyngitis, otitis media, cellulitis, streptococcal pharyngitis, viral gastroenteritis, gingivitis, herpes zoster, viral bronchitis, aggression, hypersensitivity, lymphedema, constipation, abdominal distension, gastritis, acne, alopecia, rhabdomyolysis, menorrhagia, ovarian cyst, vaginal bleeding, delayed menstruation, increased serum lactate dehydrogenase, increased serum luteinizing hormone, increased serum follicle-stimulating hormone, duodenal ulcer hemorrhage, skin ulcer, hematuria, sputum disorders, leg pain, hypercalcemia, hyponatremia, leukocytosis, hypothyroidism, melena, ocular hemorrhage, altered mental status, interstitial lung disease, hemoptysis, malignancy, pulmonary toxicity, sensory disturbance, pulmonary tuberculosis, pulmonary edema, thrombocytopenia, decreased serum uric acid, urticaria, dizziness, skin hyperpigmentation, dermatotoxicity, hypothyroidism, seizures, hyperuricemia, myalgia, eyelid edema, paralysis, peripheral neuropathy, epigastric discomfort, decreased glomerular filtration rate, blurred vision, heart failure, facial edema, otitis externa, communication disorders, generalized edema, rhinitis, chapped lips, decreased serum sodium, decreased serum albumin, elevated serum creatinine

This medication should be stored in a tightly closed container to prevent exposure to air or moisture, maintaining a temperature between 1 and 30 degrees Celsius. Additionally, it is important to store it out of direct sunlight to preserve the drug's efficacy.

Appearance

White to pale yellowish rectangular tablets

Package unit

30 tablets (10 tablets/PTP packaging x 3)