High Purity 98% Anticancer Pharmaceutical Raw Powder Everolimus CAS 159351-69-6 with good price

Everolimus More Info

Everolimus is a potent mTOR (mechanistic target of rapamycin) inhibitor used both as an immunosuppressant and an anticancer agent.

Mechanism of Action

Everolimus binds with high affinity to the intracellular protein FK506 binding protein-12 (FKBP-12), forming a complex that inhibits the serine/threonine kinase activity of mTOR complex 1 (mTORC1). This inhibition blocks mTOR’s downstream signaling pathways, which are crucial for cell growth, proliferation, angiogenesis, and metabolism. Specifically, everolimus:
Prevents progression of cells from the G1 phase to the S phase of the cell cycle, inducing cell growth arrest and apoptosis.
Inhibits hypoxia-inducible factor (HIF-1α), leading to reduced vascular endothelial growth factor (VEGF) expression, thereby decreasing tumor angiogenesis.
Reduces glucose uptake and overall cell proliferation.
In transplantation, everolimus suppresses the immune system by inhibiting T-cell activation and proliferation, reducing the risk of organ rejection.

Applications

Everolimus is approved for multiple indications:
Oncology:
Advanced renal cell carcinoma (kidney cancer) resistant to other treatments.
Advanced hormone receptor-positive, HER2-negative breast cancer in postmenopausal women (in combination with exemestane).
Progressive or metastatic pancreatic, gastrointestinal, or lung neuroendocrine tumors.
Subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis complex (TSC) in patients unsuitable for surgery.
TSC-associated renal angiomyolipoma (kidney tumors).
TSC-associated partial-onset seizures in adults and children aged 2 years and older.
Off-label uses include carcinoid tumors, Hodgkin lymphoma, and Waldenström macroglobulinemia.
Transplantation:
Prevention of organ rejection after kidney or liver transplantation, typically used with other immunosuppressants like cyclosporine and steroids.
Cardiovascular:
Used in drug-eluting stents to prevent restenosis by inhibiting vascular smooth muscle proliferation.

Routes of Administration

Oral: Everolimus is administered orally as tablets or tablets for oral suspension. It is usually taken once daily for cancer or TSC-related indications, and twice daily when used for transplant rejection prevention.

Pharmacokinetics

Absorption: Peak plasma concentrations occur 1 to 2 hours after oral dosing. The drug exhibits dose-proportional pharmacokinetics between 5 mg and 10 mg doses; higher doses show less than proportional increases in peak concentration but proportional increases in overall exposure (AUC).
Distribution: Everolimus is widely distributed in tissues.
Metabolism: Primarily metabolized by CYP3A4 enzymes in the liver.
Elimination: Excreted mainly via feces, with a half-life supporting once or twice daily dosing.
Steady-state: Achieved within approximately two weeks of daily dosing.

Safety and Side Effects

Common Side Effects: Stomatitis (mouth sores), infections, rash, fatigue, diarrhea, edema (swelling), anemia, nausea, hyperlipidemia, cough, and peripheral edema.
Serious Side Effects:
Increased risk of infections due to immunosuppression.
Non-infectious pneumonitis.
Severe hypersensitivity reactions.
Impaired wound healing.
Increased risk of bleeding.
Potential for renal impairment.
Elevated blood sugar and lipid levels.
Contraindications and Precautions:
Use with caution in patients with liver impairment.
Pregnancy category D: may cause fetal harm.
Avoid live vaccines during treatment.
Monitor for drug interactions, especially with CYP3A4 inhibitors or inducers.
Monitoring: Regular blood counts, liver and kidney function tests, lipid profiles, and signs of infection are recommended.

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