AFINITOR 10 MG 30 TAB

Purchase this product now and earn 19,100 Points!

Description

AFINITOR 10 MG 30 TAB

Afinitor

Afinitor treats hormone receptor-positive, HER2/neu negative advanced breast cancer, in combination with exemestane, in postmenopausal women without symptomatic visceral disease after recurrence or progression following a non-steroidal aromatase inhibitor.

 

ACTIVE INGREDIENT

Each tablet contains 10 mg everolimus.

 

Description of Afinitor

White to slightly yellow, elongated tablets of approximately 15.1 mm in length and 6.0 mm in width, with a bevelled edge and no score, engraved with “UHE” on one side and “NVR” on the other.

 

Therapeutic indications of Afinitor 

 

  • Hormone receptor-positive advanced breast cancer

Afinitor treats hormone receptor-positive, HER2/neu negative advanced breast cancer, in combination with exemestane, in postmenopausal women without symptomatic visceral disease after recurrence or progression following a non-steroidal aromatase inhibitor.

  • Neuroendocrine tumours of pancreatic origin

Afinitor treats unresectable or metastatic, well- or moderately-differentiated neuroendocrine tumours of pancreatic origin in adults with progressive disease.

  • Neuroendocrine tumours of gastrointestinal or lung origin

Afinitor treats unresectable or metastatic, well-differentiated (Grade 1 or Grade 2) non-functional neuroendocrine tumours of gastrointestinal or lung origin in adults with progressive disease.

  • Renal cell carcinoma

Afinitor treats patients with advanced renal cell carcinoma, whose disease has progressed on or after treatment with VEGF-targeted therapy.

 

Posology and method of administration

  • Physicians should supervise and intiate the treatment with Afinitor  in the use of anticancer therapies.
  • For the different dose regimens Afinitor is available as 2.5 mg, 5 mg and 10 mg tablets.
  • The dose is 10 mg everolimus once daily. Treatment should continue as long as clinical benefit presents or until unacceptable toxicity occurs.
  • If you miss a dose, the patient should not take an additional dose, but take the next prescribed dose as usual.
  • Dose adjustment due to adverse reactions
  • Management of severe and or intolerable adverse reactions may require dose reduction and/or temporary interruption of Afinitor therapy. For adverse reactions of Grade 1, physicians need to do dose adjustment. If dose reduction occurs, the dose is 5 mg daily and must not be lower than 5 mg daily.

 

Drug Interactions

Everolimus is a substrate of CYP3A4, and also a substrate and moderate inhibitor of PgP. Therefore, absorption and subsequent elimination of everolimus may be influenced by products that affect CYP3A4 and/or PgP. In vitro, everolimus is a competitive inhibitor of CYP3A4 and a mixed inhibitor of CYP2D6.

 CYP3A4 and PgP inhibitors increasing everolimus concentrations

Substances that are inhibitors of CYP3A4 or PgP may increase everolimus blood concentrations by decreasing metabolism or the efflux of everolimus from intestinal cells.

 CYP3A4 and PgP inducers decreasing everolimus concentrations

Substances that are inducers of CYP3A4 or PgP may decrease everolimus blood concentrations by increasing metabolism or the efflux of everolimus from intestinal cells.

 

Special Populations

Pregnancy

There are no adequate data from the use of everolimus in pregnant women. Studies in animals have shown reproductive toxicity effects including embryotoxicity and foetotoxicity. The potential risk for humans is unknown.

Pregnant Women shouldn’t take everolimus during pregnancy and in women of childbearing potential not using contraception.

 

Breast-feeding

In human breast milk, everolimus presents. Additionally, in rats, everolimus and/or its metabolites readily pass into the milk. Therefore, women taking everolimus should not breast-feed during treatment and for 2 weeks after the last dose.

 

Fertility

The potential for everolimus to cause infertility in male and female patients is unknown, however amenorrhoea (secondary amenorrhoea and other menstrual irregularities) and associated luteinising hormone (LH)/follicle stimulating hormone (FSH) imbalance has been observed in female patients. Based on non-clinical findings, male and female fertility may be compromised by treatment with everolimus.

 

Hepatic impairment

The safety, tolerability and pharmacokinetics of everolimus were evaluated in two single oral dose studies of Afinitor tablets in 8 and 34 subjects with impaired hepatic function relative to subjects with normal hepatic function.

In the first study, the average AUC of everolimus in 8 subjects with moderate hepatic impairment (Child-Pugh B) was twice that found in 8 subjects with normal hepatic function.

In the second study of 34 subjects with different impaired hepatic function compared to normal subjects, there was a 1.6-fold, 3.3-fold and 3.6-fold increase in exposure for subjects with mild (Child-Pugh A), moderate (Child-Pugh B) and severe (Child-Pugh C) hepatic impairment, respectively.

Simulations of multiple dose pharmacokinetics support the dosing recommendations in subjects with hepatic impairment based on their Child-Pugh status.

Based on the results of the two studies, you must do dose adjustment for patients with hepatic impairment.

 

Renal impairment

In a population pharmacokinetic analysis of 170 patients with advanced solid tumors, has no significant influence of creatinine clearance (25-178 ml/min) on CL/F of everolimus. Post-transplant renal impairment (creatinine clearance range 11-107 ml/min) did not affect the pharmacokinetics of everolimus in transplant patients.

 

Elderly patients

In a population pharmacokinetic evaluation in cancer patients, has no significant influence of age (27-85 years) on oral clearance of everolimus.

 

Ethnicity

Oral clearance (CL/F) is similar in Japanese and Caucasian cancer patients with similar liver functions. Based on analysis of population pharmacokinetics, CL/F is on average 20% higher in black transplant patients.

 

Pharmacodynamic properties

Pharmacotherapeutic group: Antineoplastic agents, other antineoplastic agents, protein kinase inhibitors.

 

Mechanism of action

Everolimus is a selective mTOR (mammalian target of rapamycin) inhibitor. mTOR is a key serine-threonine kinase, the activity of which is upregulated in a number of human cancers. Everolimus binds to the intracellular protein FKBP-12, forming a complex that inhibits mTOR complex-1 (mTORC1) activity. Inhibition of the mTORC1 signalling pathway interferes with the translation and synthesis of proteins by reducing the activity of S6 ribosomal protein kinase (S6K1) and eukaryotic elongation factor 4E-binding protein (4EBP-1) that regulate proteins involved in the cell cycle, angiogenesis and glycolysis. Everolimus reduces levels of vascular endothelial growth factor (VEGF), which potentiates tumour angiogenic processes. Everolimus is a potent inhibitor of the growth and proliferation of tumour cells, endothelial cells, fibroblasts and blood-vessel-associated smooth muscle cells and reduces glycolysis in solid tumours in vitro and in vivo.

 

SIDE EFFECTS
  • Infections are very common
  • Blood and lymphatic system disorders like anemia are very common.
  • Thrombocytopenia, neutropenia, leukopenia, lymphopenia.
  • Metabolism and nutrition disorders like decreased appetite, hyperglycemia and hypercholestrimia,  hypertriglyceridaemia, hypophosphataemia, diabetes mellitus.
  • Gastrointestinal disorders like diarrhea, stomatitis and nausea.
  • Vomiting dry mouth and abdominal pain are also common.

 

Patient Leaflet 

 

 

Reviews (0)

Reviews

There are no reviews yet.

Be the first to review “AFINITOR 10 MG 30 TAB”

Your email address will not be published. Required fields are marked *

Shopping Cart
Don`t copy text!
Scroll to Top
🏷️ WANT A COUPON
Give us a review on Google or Facebook
Google Review

Facebook Review
and Subscribe now to get free discount coupon code. Don't miss out

    SUBSCRIBE