Everolimus: Brands, Price & Uses in Bangladesh

Everolimus is an oral mTOR (mammalian target of rapamycin) inhibitor with two broad categories of approved use: certain cancers/tumor conditions, and prevention of organ transplant rejection (in a lower-dose formulation used with other immunosuppressants).

Established / FDA-approved oncology and tumor indications

• Hormone receptor-positive, HER2-negative advanced breast cancer in postmenopausal women, in combination with exemestane, after failure of letrozole or anastrozole.
• Advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib.
• Progressive, well-differentiated, non-functional neuroendocrine tumors (NET) of gastrointestinal, lung, or pancreatic origin that are unresectable, locally advanced, or metastatic.
• Renal angiomyolipoma associated with tuberous sclerosis complex (TSC), not requiring immediate surgery.
• Subependymal giant cell astrocytoma (SEGA) associated with TSC that requires therapeutic intervention but is not amenable to curative surgical resection (a dispersible tablet formulation is used in younger children).
• Adjunctive treatment of TSC-associated partial-onset seizures, in patients 2 years of age and older.

Established use requiring combination therapy (transplant rejection prophylaxis)

• Prophylaxis of organ rejection in adult kidney transplant recipients at low-to-moderate immunologic risk, used in combination with reduced-dose cyclosporine, basiliximab induction, and corticosteroids.
• Prophylaxis of organ rejection in adult liver transplant recipients, used with reduced-dose tacrolimus and corticosteroids (not started within the first month after liver transplant because of an increased risk of hepatic artery thrombosis).
• Prophylaxis of organ rejection in adult heart transplant recipients, used with reduced-dose cyclosporine and corticosteroids.

Note: the transplant-rejection indication uses a different, lower-dose product/trough-target than the oncology indications; the two uses are not interchangeable.

Oncology / tumor indications (adult, tablet form, standard strengths)

TSC-associated SEGA and partial-onset seizures (dispersible or standard tablet, weight/body-surface-area based)

• SEGA: starting dose approximately 4.5 mg/m² once daily, subsequently titrated to achieve a trough blood concentration of 5-15 ng/mL, based on therapeutic drug monitoring.
• Partial-onset seizures (age 2 years and older): starting dose approximately 5 mg/m² once daily (lower in patients also taking strong CYP3A4 inducers), titrated to a target trough of 5-15 ng/mL.

Organ transplant rejection prophylaxis (lower-strength tablet, used with other immunosuppressants)

• Typically initiated at a low dose (e.g., 0.75 mg twice daily in combination regimens) and subsequently adjusted based on measured whole-blood trough concentrations, in combination with reduced-dose calcineurin inhibitor and corticosteroids, per the transplant team's protocol.

Hepatic impairment (oncology indications)

Administration

Take at the same time each day, consistently either with or without food, and swallow tablets whole with a glass of water; do not chew or crush standard tablets. Dispersible tablets must not be swallowed whole and should be dispersed in water as directed by the pharmacist/physician immediately before administration. Dose adjustments for adverse reactions (e.g., pausing, reducing dose) should follow physician instructions. Take exactly as prescribed; do not stop, change the dose, or skip doses without consulting the prescribing physician, given the narrow therapeutic window and need for blood level monitoring in transplant use.

Adverse effects of Everolimus vary somewhat by indication but commonly include:

• Very common: mouth sores/stomatitis, fatigue, diarrhea, nausea, decreased appetite, rash, peripheral edema, headache, cough, fever.
• Metabolic: hyperglycemia, hyperlipidemia (elevated cholesterol/triglycerides), which may require monitoring and treatment.
• Hematologic: anemia, low white blood cell counts (increasing infection risk), low platelet counts.
• Respiratory: non-infectious pneumonitis (cough, shortness of breath, may require dose interruption or corticosteroids) — see Precautions and Warnings.
• Infections: increased susceptibility to bacterial, fungal, viral, and opportunistic infections due to immunosuppressive effect — see Precautions and Warnings.
• Renal: increased creatinine, proteinuria.
• Skin/mucosal: rash, dry skin, nail disorders, acneiform dermatitis.
• Less common but serious: angioedema, impaired wound healing, and (in transplant patients specifically) renal artery/vein thrombosis risk in the early post-transplant period — see Precautions and Warnings.

Report any new or worsening symptoms, especially breathing difficulty, unusual bleeding, signs of infection, or swelling of the face/throat, to a physician promptly.