Cipla Everolimus Rolimus 5mg

[Drug Name]

Generic Name: Everolimus Tablets

Brand Name: Everolimus Tablets (Afinitor)

English Name: Everolimus Tablets

Full Pinyin Code: YiWeiMoSiPian (FeiNiTuo)

[Main Ingredient] Everolimus.

[Composition]

Chemical Name: 40-O-(2-hydroxyethyl)-rapamycin

Molecular Formula: C53H83NO14

[Description] This product is a white or slightly yellowish tablet.

[Indications/Therapeutic Uses]

Renal Cell Carcinoma: Everolimus is indicated for patients with advanced renal cell carcinoma, particularly those whose disease has progressed following prior treatment with sunitinib or sorafenib. By inhibiting the mTOR signaling pathway, it blocks the growth, proliferation, and angiogenesis of tumor cells, thereby exerting an anti-tumor effect and extending the patient's progression-free survival.

Pancreatic Neuroendocrine Tumors: For unresectable, locally advanced, or metastatic pancreatic neuroendocrine tumors—specifically when tumor growth is evident or symptoms are present—everolimus serves as an effective treatment option. It controls the metabolism and proliferation of tumor cells, stabilizes the disease, improves the patient's quality of life, and extends survival time.

Gastrointestinal or Lung Neuroendocrine Tumors: Everolimus may be used to treat unresectable, locally advanced, or metastatic neuroendocrine tumors of gastrointestinal or pulmonary origin. For these tumors, which originate from neuroendocrine cells, everolimus modulates cellular signaling to inhibit tumor growth and dissemination, thereby providing an effective therapeutic intervention for patients.

Breast Cancer: Everolimus, in combination with exemestane, is indicated for the treatment of advanced breast cancer in postmenopausal women with estrogen receptor-positive (ER+) and human epidermal growth factor receptor 2-negative (HER2-) disease, particularly in patients whose disease has progressed following treatment with letrozole or anastrozole. It helps overcome resistance to endocrine therapy by inhibiting the mTOR pathway and blocking the downstream signaling of estrogen receptors, thereby suppressing the growth of tumor cells. Tuberous Sclerosis Complex (TSC)-associated Subependymal Giant Cell Astrocytoma (SEGA): For patients with TSC accompanied by SEGA who do not require immediate surgical intervention, Everolimus may be used for treatment. It inhibits the abnormal cell proliferation associated with TSC, reduces tumor volume, alleviates symptoms, and lowers the need for—as well as the risks associated with—surgery.

TSC-associated Renal Angiomyolipoma: Everolimus may be used to treat TSC-associated renal angiomyolipoma in patients who do not require immediate surgical intervention. It inhibits the growth of tumor cells, controls tumor progression, reduces tumor-related complications, preserves renal function, and improves the patient's quality of life.

[Specifications] 5 mg × 10 tablets

[Dosage and Administration]

Administration

Everolimus is generally administered orally. It is available in various tablet strengths (1 mg, 2.5 mg, 5 mg, and 10 mg) and should be swallowed whole; tablets must not be chewed or crushed. For patients unable to swallow tablets, the tablets may be dispersed in water or apple juice; stir gently until fully dispersed, then consume immediately.

Dosage

Advanced Renal Cell Carcinoma; Pancreatic Neuroendocrine Tumors; Gastrointestinal or Lung Neuroendocrine Tumors

The recommended dosage is 10 mg once daily. It should be taken at the same time each day, with or without food.

Breast Cancer

When used in combination with Exemestane, the recommended dosage of Everolimus is also 10 mg once daily.

TSC-associated Subependymal Giant Cell Astrocytoma (SEGA)

The initial dosage is determined based on body surface area (BSA), typically 4.5 mg/m² once daily. Dosage adjustments should be made based on drug trough concentrations, with a target trough concentration range of 5–10 ng/mL.

TSC-associated Renal Angiomyolipoma

The recommended initial dosage is 10 mg once daily. Dose adjustment should also be guided by trough concentrations, with a target trough concentration of 5–10 ng/mL.

Dose Adjustment

Renal Impairment: No dose adjustment is required for patients with mild renal impairment; for patients with moderate renal impairment, the recommended starting dose is 5 mg/day; for patients with severe renal impairment or those undergoing dialysis, the recommended starting dose is 2.5 mg/day, which may subsequently be adjusted based on individual tolerability and therapeutic response.

Hepatic Impairment: For patients with mild hepatic impairment, the recommended starting dose is 7.5 mg/day; for patients with moderate hepatic impairment, the recommended starting dose is 5 mg/day; use in patients with severe hepatic impairment is not recommended unless the potential benefits outweigh the risks.

Adverse Reactions: If adverse reactions occur during treatment, it may be necessary to temporarily interrupt administration, reduce the dose, or permanently discontinue the drug. In the event of non-hematologic adverse reactions, depending on severity, a dose reduction to 5 mg/day or 2.5 mg/day may be considered; in the event of hematologic adverse reactions, dose adjustment or temporary interruption of treatment is also required based on the specific clinical situation.

[Adverse Reactions] 1. Advanced RCC: The most common adverse reactions (incidence ≥30%) are stomatitis, infections, asthenia, fatigue, cough, and diarrhea. 2. SEGA: The most common adverse reactions (incidence ≥30%) are stomatitis, upper respiratory tract infection, sinusitis, otitis media, and pyrexia.

[Contraindications] Hypersensitivity to everolimus, to other rapamycin derivatives, or to any component of the excipients.

[Precautions] 1. Non-infectious Pneumonitis: Monitor for clinical symptoms or radiologic changes; fatal cases have occurred. Manage by reducing the dose or discontinuing the drug until symptoms resolve, and consider the use of corticosteroids. 2. Infections: Increased risk of infection, some of which have been fatal. Monitor for signs and symptoms, and treat promptly. 3. Oral Ulceration: Oral ulcers, stomatitis, and oral mucositis are common. Management includes the use of alcohol-free or peroxide-free mouthwashes and topical treatments. 4. Laboratory Test Changes: Elevations in serum creatinine, blood glucose, and lipids may occur. Decreases in hemoglobin, neutrophils, and platelets may also occur. Monitor renal function, blood glucose, lipids, and hematologic parameters prior to treatment and periodically thereafter. 5. Immunizations: Avoid live vaccines and close contact with individuals who have recently received live vaccines. 6. Use in Pregnancy: Fetal harm may occur when administered to pregnant women. Advise women of the potential risk to the fetus. Please read the package insert carefully and use strictly according to physician's instructions.

[Pediatric Use] Not established.

[Geriatric Use] Not established.

[Use in Pregnant and Lactating Women] Discontinue the drug or discontinue breastfeeding, taking into account the importance of the drug to the mother.

[Drug Interactions] 1. Strong CYP3A4 Inhibitors: Avoid concomitant use. 2. Moderate CYP3A4 and/or PgP Inhibitors: If concomitant use is necessary, use with caution and reduce the dosage of AFINITOR. 3. Strong CYP3A4 Inducers: Avoid concomitant use. If concomitant use cannot be avoided, increase the dosage of AFINITOR.

[Overdosage] Not established.

[Pharmacology and Toxicology] Not established.

[Pharmacokinetics] Not established.

[Storage] Keep tightly closed.

[Packaging] 10 tablets per box.

[Shelf Life] 24 months.

Product Specifications

Product Name: Cipla Afinitor (Everolimus Tablets) 5mg x 10 Tablets | Everolimus Rolimus 5mg

Common Name: Afinitor

Composition: The main active ingredient of this product is Everolimus.

Dosage Form: Tablets

Specification: 5mg x 10 tablets

Manufacturer: Cipla Pharmaceuticals

Indications: Everolimus is indicated for the treatment of the following patients:

Renal Cell Carcinoma: Everolimus is indicated for patients with advanced renal cell carcinoma, particularly those whose disease has progressed despite prior treatment with sunitinib or sorafenib. It exerts its anti-tumor effects—thereby extending patients' progression-free survival—by inhibiting the mTOR signaling pathway, thereby blocking the growth, proliferation, and angiogenesis of tumor cells.

Pancreatic Neuroendocrine Tumors: For unresectable, locally advanced, or metastatic pancreatic neuroendocrine tumors, Everolimus serves as an effective treatment option when tumor growth is evident or symptoms arise. It regulates the metabolism and proliferation of tumor cells, stabilizes the disease, improves patients' quality of life, and extends survival duration.

Gastrointestinal or Lung Neuroendocrine Tumors: Everolimus is indicated for the treatment of unresectable, locally advanced, or metastatic neuroendocrine tumors of gastrointestinal or pulmonary origin. For these tumors, which originate from neuroendocrine cells, Everolimus modulates cellular signaling to inhibit tumor growth and dissemination, thereby providing an effective therapeutic modality for patients.

Breast Cancer: Everolimus, in combination with Exemestane, is used to treat advanced breast cancer in postmenopausal women with estrogen receptor-positive (ER+) and human epidermal growth factor receptor 2-negative (HER2-) disease—particularly in patients whose disease has progressed following treatment with Letrozole or Anastrozole. It helps overcome resistance to endocrine therapy by inhibiting the mTOR pathway and blocking downstream signaling from estrogen receptors, thereby suppressing the growth of tumor cells.

Tuberous Sclerosis Complex-Associated Subependymal Giant Cell Astrocytoma (SEGA): For patients with Tuberous Sclerosis Complex (TSC) who also present with a subependymal giant cell astrocytoma (SEGA), Everolimus may be used to treat those for whom immediate surgical intervention is not required. It inhibits the abnormal cellular proliferation associated with TSC, reduces tumor volume, alleviates symptoms, and mitigates the need for—as well as the risks associated with—surgery.

Tuberous Sclerosis Complex-Associated Renal Angiomyolipoma: Everolimus is indicated for the treatment of renal angiomyolipomas associated with Tuberous Sclerosis Complex (TSC) in patients for whom immediate surgical intervention is not required. It inhibits the growth of tumor cells, controls tumor progression, reduces tumor-related complications, preserves renal function, and improves patients' quality of life. Dosage and Administration:

Administration

Everolimus is generally administered orally and is available in various tablet strengths, including 1 mg, 2.5 mg, 5 mg, and 10 mg. The tablets should be swallowed whole; they must not be chewed or crushed. For patients unable to swallow tablets, the tablets may be dispersed in water or apple juice; stir gently until completely dispersed, then consume immediately.

Dosage

Advanced Renal Cell Carcinoma, Pancreatic Neuroendocrine Tumors, Gastrointestinal or Lung Neuroendocrine Tumors

The recommended dose is 10 mg once daily, taken at the same time each day. It may be taken with or without food.

Breast Cancer

When Everolimus is used in combination with Exemestane, the recommended dose of Everolimus is also 10 mg once daily.

Subependymal Giant Cell Astrocytoma (SEGA) associated with Tuberous Sclerosis Complex (TSC)

The initial dose is determined based on body surface area (BSA), generally 4.5 mg/m² once daily. Dosage adjustments should be made based on trough concentrations, with a target trough concentration of 5–10 ng/mL.

Renal Angiomyolipoma associated with Tuberous Sclerosis Complex (TSC)

The recommended initial dose is 10 mg once daily. Dosage adjustments should likewise be made based on trough concentrations, with a target trough concentration of 5–10 ng/mL.

Dosage Adjustment

Renal Impairment: No dosage adjustment is required for patients with mild renal impairment. For patients with moderate renal impairment, the recommended starting dose is 5 mg/day. For patients with severe renal impairment or those undergoing dialysis, the recommended starting dose is 2.5 mg/day; subsequent adjustments may be made based on individual tolerability and therapeutic response.

Hepatic Impairment: For patients with mild hepatic impairment, the recommended starting dose is 7.5 mg/day. For patients with moderate hepatic impairment, the recommended starting dose is 5 mg/day. Use in patients with severe hepatic impairment is not recommended unless the potential benefits outweigh the risks.

Adverse Reactions: If adverse reactions occur during treatment, it may be necessary to temporarily interrupt administration, reduce the dosage, or permanently discontinue the medication. In the event of non-hematologic adverse reactions, depending on the severity, a dose reduction to 5 mg/day or 2.5 mg/day may be considered; in the event of hematologic adverse reactions, the dose should also be adjusted or treatment suspended based on the specific circumstances.