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Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 29.10.2020

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Synonym(s)

6-methylidenandrosta-1,4-diene-3,17-dione; CAS number: 107868-30-4; (e) Exemestane

Definition
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Exemestan (molecular formula: C20H24O2; half-life of two days) is an active substance from the group of steroidal aromatase inhibitors. The structure of the Exemestan is similar to that of the natural substrate androstendione. Exemestane inhibits estrogen production by irreversibly blocking the conversion of androgens to estrone and estradiol in non-ovarian tissues. By blocking the aromatases, the remaining oestrogen production in and after menopause decreases significantly. Exemestan lowers the estrogen level to 5 to 10 % of the initial value and shows a. A daily administration of 25 mg causes a reduction of the total aromatase activity by up to 98 %.

Exemestan has no gestagenic, androgenic or estrogenic effect.

Undesirable effects
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The most common side effects that may occur during treatment with Exemestan include

Very common side effects (in more than 1 treated person out of 10)

  • Hot flushes and blushes
  • Tiredness
  • Headaches
  • Nausea
  • Depressions
  • Insomnia
  • muscle and joint pain
  • frequent side effects (in 1 to 10 treated persons out of 100)
  • Loss of appetite
  • Depressions
  • Swindle
  • Carpal tunnel syndrome
  • Abdominal pain
  • Exantheme
  • Effluvium
  • Cutaneous vasculitis (Santoro S et al. 2011)
  • Increase in blood lipid levels

Preparations
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Aromasin®+ Generics

Literature
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  1. Goss PE et al (2013) Exemestane versus anastrozole in postmenopausal women with early breast cancer: NCIC CTG MA.27--a randomized controlled phase III trial. J Clin Oncol 31:1398-1404.
  2. Johnston SR et al (2013) Fulvestrant plus anastrozole or placebo versus exemestane alone after progression on non-steroidal aromatase inhibitors in postmenopausal patients with hormone-receptor-positive locally advanced or metastatic breast cancer (SoFEA): a composite, multicentre, phase 3 randomised trial. Lancet Oncol 14:989-998.
  3. Santoro S et al (2011) Aromatase inhibitor-induced skin adverse reactions: exemestane- related cutaneous vasculitis. J Eur Acad Dermatol Venereol 25:596-598.
  4. Yardley DA et al (2013) Everolimus plus exemestane in postmenopausal patients with HR(+) breast cancer: BOLERO-2 final progression-free survival analysis. Adv Ther 30:870-884.

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Last updated on: 29.10.2020