Evergraf 0.25mg belongs to anti-neoplastic agent; it comes under mTOR kinase inhibitor (single transduction inhibitor).
Evergraf 0.25mg is an immunosuppressive macrolide.
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patient who fail to respond the tablet letrozole or anastrozole therapy, would be treated with Rapact. Evergraf 0.25mg is used in advanced stage of breast cancer.
Evergraf 0.25mg involved in the treatment of some neuroendocrine tumors like pancreatic, gastrointestinal or lung cancer.
Renal cell cancer
patient treating with Evergraf 0.25mg after the failure of treatment with Sunitinib or Sorafenib.
Evergraf 0.25mg also used in the condition of;
Heart, liver, kidney transplantation
Other carcinoid tumors.
Mechanism of action
Evergraf is prohibitor of mammalian target of rapamycin (mTOR), a serine threonine kinase.
Evergraf bind with intercellular protein (FKBP-12), leads to inhibitory complex formation with mTOR complex 1 (mTORC1) this leads to inhibition of mTOR kinase activity.
Evergraf decreased the effect of S6 ribosomal protein kinase (S6K1) and eukaryotic elongation factor 4E binding protein (4E-BP1) which are essential for protein synthesis.
mTOR inhibited by Evergraf lead to reduce cell multiplication and angiogenesis.
The peak plasma concentration of Evergraf reached within 1 to 2 hours after administration.
The blood plasma ratio of Evergraf occurs over the range of 5 to 5000ng/ml.
On oral administration, Evergraf is metabolized into six main metabolites;
Two hydrolytic ring opened product
Phosphatidylcholine conjugate of Rapact.
Evergraf is a substrate of CYP3A4 and PgP.
Evergraf is mixed inhibitor of CYP2D6 substrate dextromethorphan
Evergraf inhibits the metabolism of CYP3A4.
The 80% of the drug eliminated through feces. The half-life time of drug Evergraf is approximately 30 hours.
Dosage and administration
The recommended dose of the Tablet Evergraf is 10mg should be taken as a single dose in all carcinogenic condition, except organ transplantation.
Organ transplant: 0.75mg orally twice daily.
Brain/intracranial tumor: 4.5mg/m2 orally once a day (for both pediatric and adult dose)
Hepatic impairment: dose reduced to 7.5mg once daily followed by 5mg as a single dose.
Evergrafis in tablet form. It should be administered orally at same time every day.
Evergrafshould be taken with or without food.
Evergraftablets should not crush or broken.
The over dosage of Evergraf 0.25mg is rarely occur, in case of over dosage patient must be provide with supportive measures. The acute toxicity of Everolimus over dosage should be monitored.
The side effects of Evergraf 0.25mg tablets are predicted by the terms of their onset, duration, and severity
Side effects of Evergraf 0.25mg is preventable and it is minimized :
Mouth sores, Mucositis, Stomatitis or esophagitis, Infection, Rash, itching or dry skin, Fatigue, Diarrhea, Edema, Stomach pain, Nausea, vomiting, Fever, Weakness or asthenia, Headache.
Blood test abnormalities
Hypercholesterolemia, High triglycerides, High blood sugar level, Low calcium, Low phosphate, Low blood counts, Liver problems, Kidney problems.
Cough, Loss appetite, Shortness of breath, Hypertension, Bleeding problems, Joint pain, Muscle pain, Loss of fertility.
Before going to start the Evergraf 0.25mg therapy, doctor should consult with patient whether they are taking any medicines like;
Any kind of immunization or vaccine
Care should be taken in pregnancy condition.
Some list of medications should not be taken with Tablet Rapact, they will interact with Evergraf 0.25mg to produce serious ill;
Angiotensin converting enzyme inhibitors: Evergraf 0.25mg increases the adverse effect of ACE inhibitors.
Anti-hepaciviral increase the serum concentration of Evergraf 0.25mg