Advacan 0.25 Tablet

Description of Advacan 0.25  (Everolimus 0.25mg) tablet

Advacan 0.25 is an oral anticancer preparation consisting of 0.25mg everolimus, a selective inhibitor of the mammalian target of rapamycin (mTOR) signalling pathway. Unlike other cytotoxic chemotherapeutic agents, which destroy cells with the highest rate of proliferation without being specific to them, everolimus is a type of drug that selectively inhibits the mTOR cascade, which is a key regulator of cellular functions in terms of growth, proliferation, and survival. This pathway is inhibited, thus suppressing the growth of the neoplastic cells, which is capable of inhibiting the development of tumours. Everolimus is mainly used in the treatment of malignancies with hyperactivity of the mTOR pathway because of its mechanism of action.

Indications of Advacan 0.25 (Everolimus 0.25mg) tablet

List of common indications of everolimus includes the following HER2 negative Breast cancer of the advanced hormone receptor type (usually in combination therapy). High grade renal cell carcinoma. Tumours of the pancreatic neuroendocrine. and Certain neoplasms of the brain like subependymal giant cell astrocytoma, which is linked to tuberculosis sclerosis complex. Tumours at the other end of the tuberous sclerosis complex-associated pathology. The agent is most often chosen in cases of disease advancement after initial therapy or in case of targeted therapy with better advantage compared to traditional cytotoxic chemotherapy.

Mechanism of action of Advacan 0.25 (Everolimus 0.25mg) tablet

Everolimus is intracellularly bound to immunophilin FKBP12 to create a complex which directly inhibits mechanistic target of rapamycin complex 1 (mTORC1). This suppression suppresses protein synthesis, cell multiplication, angiogenesis, and cell metabolism. Blocking of this complex interferes with the proliferation and development of tumour cells including the vascular development, slowing down tumour growth and facilitating an effective control of diseases.

How to consume Advacan 0.25 (Everolimus 0.25mg) tablet

Everolimus is to be taken orally, but once per day, at the same time. The drug can be administered with and without food but it is necessary to have consistent schedule. The tablet should not be crushed, chewed, or cut down as this must be taken whole with water. To individualize tolerability and adverse effect profile, dosage changes might be required. The patients are to strictly follow the recommendation of the oncologist.

Side Effects of Advacan 0.25 (Everolimus 0.25mg) tablet

1. Common side effects

• Oral ulcerations
• Fatigue
• Cutaneous rash
• Mild anemia
• Appetite gets lower

2. Serious side effects

• Hyperglycemia
• Renal functional impairment
• Haemorrhagic life-threatening events

3. Rare side effects

• Heart-related cases (myocardial infarct for example)
• Anaphylactic reactions
• Hepatic dysfunction

Safety Advice for Advacan 0.25 (Everolimus 0.25mg) tablet

Regular clinical follow-up cannot be done away with during the treatment process. Haemoglobin counts, parameters of hepatic and renal functions, and glycemic status need to be periodically measured.

Breastfeeding: Limited information is available regarding the use of this medicine in patients during breastfeeding. But on animal studies it shows a harmful effect on fetus, so it is better to avoid during breastfeeding.

Pregnancy: The use of this medicine is considered unsafe because this medicine may cause harmful effect on the fetus. Kindly consult with your doctor for further information.

Alcohol: There must be a reduction in taking alcohol since it might give higher risk of some impacts.

Liver: Patients having liver problems should use with care.

Lungs: If some lung disease is already there, it must be talked with your doctor before you start.

Kidney: Patients having kidney problems should use with care.

Driving: Tiredness and feeling dizzy can be possible, so machines and driving must be done with care.

Interaction of Advacan 0.25 (Everolimus 0.25mg) tablet

• Drug-Drug Interaction:

Ketoconazole × Everolimus 

Ketoconazole is a strong inhibitor of cytochrom 3A4 (CYP3A4), which leads to an outstanding increase in everolimus plasma concentrations. There is a comorbid drug interaction which is linked with increased toxicity and is clinically expressed in the form of stomatitis, opportunistic infections, and pneumonitis.

Itraconazole × Everolimus 

Itraconazole suppresses Everolimus metabolism, which causes greater systemic exposure, which increases the adverse events risk.

Clarithromycin × Everolimus 

Clarithromycin inhibits CYP3A4, which has the potential of increasing the levels of Everolimus and thereby increasing the possibility of toxicity occurrence.

Rifampicin × Everolimus 

On the other hand, a strong CYP3A4 inducer like rifampicin can lower the plasma concentration of everolimus, and this will increase its adverse effects on its efficacy.

Phenytoin × Everolimus 

Phenytoin causes hepatic enzymes, which may lower the levels of Everolimus and also undermine the oncologic effect.

• Drug-Food Interaction:

Citrus Grapefruit and Grapefruit Juice. 

Citrus fruits, in particular grapefruit and grapefruit juice, include active ingredients that are highly potent decreases CYP3A4 activity in the intestines and cause increased everolimus plasma concentrations and an increased risk of severe adverse events.

High-Fat Meals 

Everolimus can be given with or without a meal though it is important to stick to a regular dosage schedule. Giving of a drug in conjunction with high-fat food may twerk the drug absorption slightly, which may influence plasma levels. The patients are therefore advised to stick to similar conditions of dosing regularly in order to maintain steady levels of the drugs.

• Drug-Disease Interaction:

Severe  Infections. 

Everolimus acts as immunosuppressant due to T-cell activation inhibition thus predisposing the resurgence of already existing bacterial, viral, or fungal infections. Therefore, therapy should not be started in uncontrolled infections in patients.

Pulmonary Disorders 

Considering its immunosuppressive effects, one should avoid exposing patients to those who have active infections. Clinical manifestations which are clinically significant such as persistent cough, fever, dyspnea, or severe fatigue are warning signs and should be reported immediately. It is recommended that patients should clarify or consult the services of a specialist with their treating clinician when such symptoms emerge

Diabetes Mellitus 

Everolimus is linked to hyperglycemia and diabetes mellitus exacerbation. Blood glucose level is supposed to be checked regularly especially among diabetic patients.

Hepatic Impairment 

Since the Everolimus is subjected to hepatic metabolism, hepatic dysfunction can lead to systemic drug exposure.

Renal Impairment 

Though being hepatically metabolised mostly, Everolimus can still affect the renal functioning. Renal parameters should be assessed periodically.

Hyperlipidemia 

Everolimus can increase the level of serum cholesterol and triglycerides, thus, regular lipid screening is justified during treatment.

Bone Marrow Suppression 

Everolimus has a pharmacologic profile that has the possibility of causing anaemia, thrombocytopenia, and leukopenia. Close observation should be done among patients with pre-existing bone marrow suppression.

Dosage of Advacan 0.25 (Everolimus 0.25mg) tablet

The clinician can adjust the dose depending on how the patient is feeling, his/her hepatic function, and the therapeutic effects in the control of the disease. Severe adverse events such as stomatitis, infectious processes or pulmonary complications may require dose adjustments.

Storage of Advacan 0.25 (Everolimus 0.25mg) tablets 

Tablets of everolimus should be kept in an ambient room temperature and should not be exposed to too much heat and moisture. The pills are to be kept in their original package until the time of administration and kept safely, where children do not have access.

Missed Dose to Advacan 0.25 (Everolimus 0.25mg) tablets

If you miss one tablet, just use planned next dose on the regular schedule. Taking two tablets together to replace a missed one is not required. Do not try to increase your next dose for this.

Other General Information of Advacan 0.25 (Everolimus 0.25mg) tablets 

Patients should be made to stay hydrated and have a well-balanced diet during the course of treatment. Regular cheque-ups and lab tests are to be conducted to assess the haematological levels, hepatic status, renal status, and glycaemic status. Since Everolimus is immunosuppressive in nature, the patient should not be in contact with people, who have active illnesses. Persistent cough, fever, dyspnoea, or intense fatigue are atypical clinical manifestations, and their emergence should be reported promptly. Patients should refer to the treating clinician in order to get further clarity or specialized medical advice.

FAQs about Advacan 0.25 (Everolimus 0.25mg) tablet

1. Is it possible that Everolimus affects glycaemic control?

Yes, the Everolimus can increase the level of glucose in the blood. Glycaemic measurements of patients with pre-existing diabetes also should be monitored on a regular basis during therapy.

2. Does Everolimus have any interaction with concomitant anticancer agents?

No, it is often combined with regimens, depending on the particular malignancy. All patients are expected to report all concomitant pharmacotherapies to their physician.

3. So what is to be done in the case of overdose?

In case of an overdose, medical attention has to be sought immediately.

4. Does Everolimus qualify as a standard chemotherapeutic agent?

Everolimus is not a conventional cytotoxic chemotherapeutic, rather it is a targeted agent, which is an mTOR inhibitor.

5. Is it acceptable to terminate therapy when the symptoms improve?

The withdrawal can never be made without the order of a physician, even when the symptoms are relieved, as early withdrawal can jeopardise the effect of treatment.

Fact Box of Advacan 0.25 (Everolimus 0.25mg) tablet:

Field	Details
Generic/Molecule Name	Everolimus
Therapeutic Class	Anti-neoplastic agent
Pharmacological Class	mTOR inhibitor
Dosage form	Tablet
Habit forming	No
Indication	Advanced breast cancer, Renal cell carcinoma, Neuroendocrine tumors, Tuberous sclerosis complex.

 

References

• FDA Prescribing Information – Afinitor (Everolimus)
  https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/022334s058lbl.pdf
• European Medicines Agency (EMA) – Afinitor Summary of Product Characteristics
  https://www.ema.europa.eu/en/documents/product-information/afinitor-epar-product-information_en.pdf
• DrugBank Online – Everolimus (DB01590)
  https://go.drugbank.com/drugs/DB01590
• National Cancer Institute (NCI) – Everolimus
  https://www.cancer.gov/about-cancer/treatment/drugs/everolimus