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Aromasin® [Exemestane]

Pfizer
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2019-09-19
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Clinical Pharmacology

Aromasin® - inhibiting the synthesis of estrogen, antitumor.

Blocks aromatase and stops the synthesis of estrogen (without affecting the production of other steroid hormones, such as cortisol and aldosterone).

Irreversible steroid aromatase inhibitor, similar in structure to the natural substance androstenedione. In postmenopausal women, estrogens are produced predominantly by the conversion of androgens into estrogens by the action of the aromatase enzyme in peripheral tissues. Blocking the formation of estrogen by inhibiting aromatase is an effective and selective treatment for hormone-dependent breast cancer in postmenopausal women. The mechanism of action of the drug Aromazin® is due to the fact that it irreversibly binds to the active fragment of the enzyme, causing its inactivation.

In postmenopausal women, Aromazin® reliably decreases the serum estrogen concentration starting at a dose of 5 mg, and the maximum reduction (> 90%) is achieved with doses of 10-25 mg. In postmenopausal patients with a diagnosis of breast cancer who received 25 mg of the drug daily, the overall level of the enzyme aromatase in the body decreased by 98%.

Exemestane does not possess progestogenic and estrogenic activity. Only insignificant androgenic activity is detected, mainly when used in high doses.

Aromasin® does not affect the biosynthesis of cortisol and aldosterone in the adrenal glands, which confirms the selectivity of the drug. In this regard, there is no need for replacement therapy with glucocorticoids and mineralocorticoids.

With the use of the drug, even in low doses, there is a slight increase in the content of LH and FSH in the serum, which is characteristic of drugs of this pharmacological group and probably develops on the basis of feedback at the pituitary level: a decrease in the concentration of estrogen stimulates the secretion of gonadotropins in the pituitary gland also postmenopausal women.

Pharmacokinetics

Suction

After oral administration, exemestane is rapidly absorbed, mainly from the digestive tract. The absolute bioavailability of the drug has not been established. It is assumed that it is limited by the extensive effect of the first passage through the liver. With a single dose of the drug in a dose of 25 mg Cmax in plasma it is 17 ng / ml and is reached in 2 hours. Simultaneous food intake increases the bioavailability of the drug by 40%.

The pharmacokinetic parameters of exemestane are linear.

Distribution

Communication with plasma proteins is approximately 90%. Exemestane and its metabolites do not bind to red blood cells. With repeated use of unpredictable cumulation of exemestane is not observed.

Metabolism

The process of biotransformation of exemestane is carried out by oxidation of the methylene group at 6 position under the action of the isoenzyme CYP3A4 and / or reduction of the 17-keto group under the action of aldoketoreductase with subsequent conjugation. The metabolites of exemestane are either inactive or less active in relation to the inhibition of aromatase than the parent compound.

Removal

Final t1/2 approximately 24 hours. Approximately equal amounts of exemestane (about 40%) are excreted in the urine and feces during the week. From 0.1 to 1% is excreted in the urine unchanged.

Pharmacokinetics in special clinical situations

A pronounced relationship between systemic exposure of the drug and age has not been established.

In patients with severe renal failure (CC <30 ml="" min="" systemic="" exposure="" to="" exemestane="" is="" 2="" times="" higher="" but="" dose="" adjustment="" not="" required="" p="">

In patients with moderate or severe hepatic impairment systemic exposure to exemestane is 2–3 times higher, but dose adjustment is not required.

Indications

  • Common breast cancer in women in natural or induced postmenopause with the progression of the disease on the background of anti-estrogen therapy, as well as with the progression of the disease after repeated use of various types of hormonal therapy;
  • adjuvant treatment of early breast cancer in postmenopausal women with estrogen-positive receptors or with an unknown receptor status, after completion of a 2–3-year initial adjuvant therapy with tamoxifen, to reduce the risk of recurrence (remote or regional), as well as contralateral breast cancer .

Composition

1 tablet contains:

Active substances: exemestane 25 mg;

Excipients: mannitol, hypromellose, polysorbate 80, crospovidone, hydrated colloidal silicon dioxide, microcrystalline cellulose, sodium carboxymethyl starch, magnesium stearate;

The composition of the sugar shell: hypromellose, simethicone emulsion, macrogol 6000, magnesium carbonate, titanium dioxide, methyl p-hydroxybenzoate, polyvinyl alcohol, sucrose.

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Aromasin® [Exemestane]

Dosage and Administration

For oral use. For adults and elderly patients The recommended dose is 25 mg 1 time per day, preferably after a meal.

For early breast cancer, drug treatment is recommended to continue until the total duration of the successive adjuvant hormone therapy reaches 5 years. Treatment of patients with advanced breast cancer is long. If there are signs of progression of a tumor disease or if a contralateral breast cancer appears, treatment with Aromasin should be stopped.

When liver or kidney failure dose adjustment is not required.

Not recommended use the drug in children.

Adverse reactions

From the digestive system: very often nausea; often - anorexia, abdominal pain, vomiting, constipation, dyspepsia, diarrhea.

From the central and peripheral nervous system: very often - insomnia, headache; often - depression, dizziness, carpal tunnel syndrome.

Since the cardiovascular system: very often - tides.

Dermatological reactions: very often - sweating; often - rash, alopecia.

From the musculoskeletal system: very often - joint and musculoskeletal pains.

Other: very often - increased fatigue; often - pain of unspecified localization, peripheral edema or swelling of the legs.

Approximately 20% of patients (especially patients with baseline lymphopenia) experienced a periodic decrease in the number of lymphocytes. However, the average number of lymphocytes in these patients did not change significantly over time, and there was no concomitant increase in the incidence of viral infections.

Sometimes there was an increase in liver enzymes and alkaline phosphatase, mainly in patients with metastases to the liver and bone, as well as in the presence of other liver lesions (it is not established whether these changes are related to the drug intake or not).

Carefully: should use the drug in violation of the liver or kidneys

Drug interactions

Preparations containing estrogen, while being used with Aromasin, completely level its pharmacological action.

Exemestane is metabolized by CYP3A4 and aldoketoreductases and does not inhibit any of the major CYP isoenzymes. Specific inhibition of CYP3A4 by ketoconazole does not have a significant effect on the pharmacokinetics of exemestane. Despite the established pharmacokinetic interaction of exemestane with rifampicin, a strong inducer of CYP3A4, the pharmacological activity of Aromasin (estrogen suppression) remains unchanged, therefore, dose adjustment is not required.

Pregnancy and Lactation

Aromazin® is contraindicated for use during pregnancy and lactation.

Special instructions

Aromasin® should not be administered to women with premenopausal endocrine status, therefore, in cases where it is clinically justified, the postmenopausal status should be confirmed by determining the level of LH, FSH and estradiol.

Aromasin® should not be administered simultaneously with drugs containing estrogen.

Impact on the ability to drive vehicles and other mechanisms that require high concentration of attention

Patients should be warned about the possibility of drowsiness, asthenia and dizziness during the treatment with Aromasin. If these symptoms occur, it is recommended that patients refrain from driving and other potentially hazardous activities that require increased concentration and psychomotor reactions.

Overdosage

Symptoms: a single dose of the drug that could cause life-threatening symptoms has not been established. The use of exemestane in a single dose of up to 800 mg in healthy women and in a daily dose of up to 600 mg in postmenopausal women with advanced breast cancer was well tolerated.

Treatment: there are no specific antidotes.If necessary, symptomatic therapy should be carried out, as well as regular monitoring of vital functions and careful monitoring.

  • Brand name: Aromasin®
  • Active ingredient: Exemestane
  • Dosage form: Sugar-coated pills.
  • Manufacturer: Pfizer
  • Country of Origin: USA

Studies and clinical trials of Exemestane (Click to expand)

  1. Cost-effectiveness analysis of exemestane compared with megestrol in patients with advanced breast carcinoma
  2. Derivatives of Exemestane — Synthesis and Evaluation of Aromatase Inhibition.
  3. An overview of the pharmacology and pharmacokinetics of the newer generation aromatase inhibitors anastrozole, letrozole, and exemestane
  4. Cost-effectiveness of switching to exemestane versus continued tamoxifen as adjuvant therapy for postmenopausal women with primary breast cancer
  5. Exemestane versus anastrozole as front-line endocrine therapy in postmenopausal patients with hormone receptor-positive, advanced breast cancer : Final results from the Spanish Breast Cancer Group 2001-03 phase 2 randomized trial
  6. Determination of plasma levels of exemestane (FCE 24304), a new irreversible aromatase inhibitor, using liquid chromatography/thermospray mass spectrometry
  7. A liquid chromatography-tandem mass spectrometry method for the simultaneous determination of exemestane and its metabolite 17-dihydroexemestane in human plasma
  8. Enhanced bioavailability of exemestane via proliposomes based transdermal delivery
  9. Determination of exemestane, a new aromatase inhibitor, in plasma by high-performance liquid chromatography with ultraviolet detection
  10. Proliposomes of exemestane for improved oral delivery: Formulation and in vitro evaluation using PAMPA, Caco-2 and rat intestine
  11. Alternative oral exemestane formulation: Improved dissolution and permeation
  12. Efficacy of exemestane, a new generation of aromatase inhibitor, on sex differentiation in a gonochoristic fish
  13. Combined chemical and microbiological synthesis of exemestane from sitosterol
  14. Development and validation of a sensitive liquid chromatography/tandem mass spectrometry method for the determination of exemestane in human plasma
  15. LC–MS–MS determination of exemestane in human plasma with heated nebulizer interface following solid-phase extraction in the 96 well plate format
  16. Identification of the aromatase inhibitors anastrozole and exemestane in human urine using liquid chromatography/tandem mass spectrometry
  17. Analysis of exemestane and 17β-hydroxyexemestane in human urine by gas chromatography/mass spectrometry: development and validation of a method using MO-TMS derivatives
  18. Toxic hepatitis secondary to oral administration of exemestane
  19. Durable clinical benefit with exemestane in leptomeningeal metastasis of breast cancer
  20. The effects of degree of hepatic or renal impairment on the pharmacokinetics of exemestane in postmenopausal women
  21. Exemestane: the dawn of a new era in breast cancer treatment
  22. The effect of exemestane and tamoxifen on bone health within the Tamoxifen Exemestane Adjuvant Multinational (TEAM) trial: a meta-analysis of the US, German, Netherlands, and Belgium sub-studies
  23. Bilateral oophorectomy combined with exemestane treating advanced refractory breast cancer

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