Evertor containing an active ingredient known as Everolimus which is intercedes with cancer cell growth and slows down its process.
Evertor tablets are not used as curable medicine, which is used to slow their spreading in to the body.
Trade name: Evertor
Active component: Everolimus
Pack: 10 tablets in a strip
Category: Anti-neoplastic drug
Evertor prescribing information;
Evertor tablets are mainly indicated in;
Everolimus is also used in various advanced stage cancer in stomach, intestines or pancreas.
Everolimus is an mTOR prohibitor, binds at high compatibility to FK506 binding protein 12, through producing drug complex that prohibits the effective of mTOR.
This prohibition decrease the activity of effectors downstream, which may causes blockage of cell progression from G1 into S phase, subsequently causes cell growth arrest and apoptosis
The peak plasma concentration time of Everolimus reaches within 1 to 2 hours.
The effect of food with Evertor is given below;
With heavy meal: Reduction of systemic exposure to Evertor 10mg, and the peak blood plasma concentration by 54%.
The blood plasma ratio of Evertor with the range of 5 to 5000ng/ml is 17% to 73%.
Evertor human plasma protein bound with the range of 74%.
The metabolism of Everolimus is occurred in liver, which is a substrate of CYP3A4.
The metabolites of Everolimus;
Three monohydroxylated metabolite,
Two hydrolytic rings opened products, &
Phosphatidylcholine conjugate of Everolimus.
The terminal half life period of Everolimus is relatively 30 hours
The major route of elimination;
5% in urine; the parent compound has been detected in urine or feces.
When to take the drug Evertor;
Evertor tablets should be administered with or without food.
Dosage regimen of Evertor;
In breast cancer, renal cell cancer, pancreatic cancer, Neuro endocrine cancer:
The recommended dosage is 10mg should be taken as a single dose.
In Brain or intracranial cancer:
The recommended dosage of Evertor is 4.5mg/m2 orally as a single dose.
The usual pediatric dosage of Evertor in brain or intracranial tumor is 4.5mg/m2 should be taken orally as a single dose.
Evertor caused side effects;
Lymphomas & other malignancy
Kidney graft thrombosis
Hepatic artery thrombosis
Interstitial lung disease
New commencement of diabetes
Drug – Drug interaction;
Evertor is metabolized hepatically, a substrate of CYP3A4.
Evertor combined with strong inhibitor of CYP3A4, or P-gp, leads to cause decreasing the efflux of Everolimus and increase the plasma concentration of Everolimus.
Evertor with strong CYP3A4 inducers, causes increasing the exposure of Everolimus.
Co administration of Evertor with cyclosporine causes increasing the AUC level of Everolimus frequently.
Evertor tablet is combined with ketaconazole or other CYP3A4 inhibitors causes increasing the plasma concentration and AUC of Everolimus.
Concomitant of Evertor with erythromycin causes increasing in AUC of Everolimus.
Co administration of Evertor with verapamil leads to increasing the plasma concentration of Everolimus.
Co administration of Evertor with Atorvastatin or pravastatin causes rhabdomyolysis, due ti increasing concentration of lipid lowering agents.
Evertor with rifampicin causes decreasing the AUC of Everolimus
Moderate inhibitors of CYP3A4 & P-gp coadminstered with Evertor leads to cause increasing the plasma concentration of Everolimus.
Octreotide is co administered with Evertor causes increasing the Cmin value of Octreotide.
Food drug interaction;
Grape fruit juice may elevate the blood levels and effect of Everolimus.
Patients, who are receiving Evertor therapy, should not intake the grape fruit or grape fruit juice.
Orange fruit is not conventionally to interact.
Some anaphylactic reaction occurs, if patients are contraindicated to the components present in the Evertor tablets.
Increased exposure of skin cancers, patient may protect from UV light
Patients receiving Evertor have high risk of acquiring various infections related to bacteria, virus, and fungi.
Anti-microbial agents are preferred for the suspected patients.
Hepatic artery thrombosis
In liver transplant patients, Evertor therapy should not be recommended.
Renal function should be monitored frequently; caution should be taken while using Evertor in renal impaired patients.
This may occurred in the patients receiving concomitantly Evertor with Angiotensin converting enzyme agents
Patient getting Evertor with lipid lowering drugs causes increasing in plasma concentration of these drugs causes hyperlipidaemia
Interstitial lung disease: Occurred in Evertor therapy
Thrombocytopenia: Using Evertor with cyclosporine causes thrombocytopenia
Outbreak of diabetes: Blood glucose level should be monitored
Embryo fetal toxicity: Causes fetal damage using Evertor in pregnancy condition
Immunization: Using live vaccines in Evertor therapy
Hereditary disorders: In the conditions like galactose intolerance, glucose-galactose malabsorption, Evertor should not be used may results in diarrhea & malabsorption.
Interact with grape juice: Causes increasing blood levels of Everolimus; avoid these concomitant.
Pregnancy and lactation;
Pregnancy category of Everolimus C
Evertor is used only by the patients after knowing the benefits to the mother outweighs the risk to fetus.
Breast feeding should not be suggested
Storage and handling;
Evertor tablet should be kept at 25oC
Keep the tablet 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.
The over dosage of Everolimus 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.