Drug Index

Everolimus

 
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Mechanism :

Everolimus is a macrolide immunosuppressant and a mechanistic target of rapamycin (mTOR) inhibitor which has antiproliferative and antiangiogenic properties, and also reduces lipoma volume in patients with angiomyolipoma.
Reduces protein synthesis and cell proliferation by binding to the FK binding protein-12 (FKBP-12), an intracellular protein, to form a complex that inhibits activation of mTOR) serine-threonine kinase activity.


Indication :

• Tuberous sclerosis complex-associated partial-onset seizures

• Tuberous sclerosis complex-associated subependymal giant cell astrocytoma

• Neuroendocrine tumors: Progressive pancreatic neuroendocrine tumors (PNET)

• Renal cell carcinoma

• Liver and renal transplantation


Contraindications :

Clinically significant hypersensitivity to everolimus, other rapamycin derivatives, or any component of the formulation.


Dosing :

Tuberous sclerosis complex-associated partial-onset seizures:

Oral: Initial 5 mg/m2 once daily; continue until disease progression or unacceptable toxicity.

Tuberous sclerosis complex-associated subependymal giant cell astrocytoma:

Oral: 4.5 mg/m2 once daily; continue until disease progression or unacceptable toxicity.


Adverse Effect :

Stomatitis, constipation, infections, asthenia, fatigue, cough, diarrhea, rash, anemia, nausea, anorexia, edema, peripheral, dyspnea, pyrexia, vomiting, headache, epistaxis, decreased lymphocytes, increased glucose, pneumonitis, pruritus, dry skin, menstrual irregularities, hypertension, hemorrhage, tachycardia, congenital heart failure.


Interaction :

Angiotensin-Converting Enzyme Inhibitors: Everolimus may enhance the adverse/toxic effect of Angiotensin-Converting Enzyme Inhibitors.
Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents.
CYP3A4 Inducers: May decrease the serum concentration of Everolimus.
CYP3A4 Inhibitors: May increase the serum concentration of Everolimus.
Efavirenz: May decrease the serum concentration of Everolimus.
Vaccines (Live): Immunosuppressants may enhance the adverse/toxic effect of Vaccines (Live). Avoid use of live organism vaccines with immunosuppressants; live-attenuated vaccines should not be given for at least 3 months after immunosuppressants.


07/21/2019 21:47:20 Everolimus
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