Evertor

Evertor 5mg belongs to anti-neoplastic agent; it comes under mTOR kinase inhibitor (single transduction inhibitor). Evertor 5mg is an immunosuppressive macrolide.

Everolimus

Evertor

5mg

Biocon





Evertor used for

Breast cancer
patient who fail to respond the tablet letrozole or anastrozole therapy, would be treated with Evertor. Evertor 5mg is used in advanced stage of breast cancer.

Neuroendocrine tumors
Evertor 5mg involved in the treatment of some neuroendocrine tumors like pancreatic, gastrointestinal or lung cancer.

Renal cell cancer
patient treating with Evertor 5mg after the failure of treatment with Sunitinib or Sorafenib.

Evertor also used in the condition of: Heart, liver, kidney transplantation Waldenstrom macroglobulinemia Other carcinoid tumors

Mechanism of action

Evertor is prohibitor of mammalian target of rapamycin (mTOR), a serine threonine kinase.
Evertor bind with intercellular protein (FKBP-12), leads to inhibitory complex formation with mTOR complex 1 (mTORC1) this leads to inhibition of mTOR kinase activity.
Evertor 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 Evertor lead to reduce cell multiplication and angiogenesis.



Pharmacokinetics

The peak plasma concentration of Evertor reached within 1 to 2 hours after administration.

The blood plasma ratio of Evertor occurs over the range of 5 to 5000ng/ml.

On oral administration, Evertor is metabolized into six main metabolites;
Three monohydroxylated
Two hydrolytic ring opened product
Phosphatidylcholine conjugate of Evertor.
Evertor is a substrate of CYP3A4 and PgP.
Evertor is mixed inhibitor of CYP2D6 substrate dextromethorphan
Evertor inhibits the metabolism of CYP3A4.

The 80% of the drug eliminated through feces. The half-life time of drug Evertor is approximately 30 hours.




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drug
Brand Evertor
Ingredients Everolimus
Strength 5mg
Manufactured Biocon
Rating


Dosage and administration

The recommended dose of the Tablet Evertor 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.
Evertor is in tablet form. It should be administered orally at same time every day.
Evertor should be taken with or without food.
Evertor tablets should not crush or broken.

Over dosage

The over dosage of Evertor 5mg 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.

SIDE EFFECTS

The side effects of Evertor tablets are predicted by the terms of their onset, duration, and severity Side effects of Evertor 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.

Less common

Cough, Loss appetite, Shortness of breath, Hypertension, Bleeding problems, Joint pain, Muscle pain, Loss of fertility.

Precautions

Before going to start the Evertor 5mg therapy, doctor should consult with patient whether they are taking any medicines like;
Aspirin
Any kind of immunization or vaccine
Care should be taken in pregnancy condition.

Drug interaction

Some list of medications should not be taken with Tablet Evertor, they will interact with Evertor 5mgto produce serious ill;
Angiotensin converting enzyme inhibitors: Evertor 5mg increases the adverse effect of ACE inhibitors.
Anti-diabetic agents
Anti-hepaciviral increase the serum concentration of Evertor 5mg
Amphetamine/dextroamphetamine
Aspirin
Lorazepam
Amoxicillin/clavulanate
Sulfamethoxazole/trimethaprim
Vitamin D
Fish oil
Fluconazole
Atorvastatin
Paracetamol
Clopidogrel
Pantoprazole
Sorafenib
Sunitinib.



Evertor 5mg is contraindicated to sirolimus and other rapamycin derivatives, to produce anaphylactic reactions.

Evertor 5mg should not use in pregnancy conditions and for breastfeeding mothers.
Pregnancy category: C
Evertor 5mg causes harm or any malformation in unborn babies.

Evertor 5mg should be stored in room temperature
Keep away from moisture, heat and light.

In case of missed dose, patients must consult with medical practitioner and follow the instructions given by them.
On the other hand, the missed dose should be avoid and follow the regular dosing schedule.

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