Anastrozole is a medicine approved for adjuvant drug therapy of hormone-dependent breast cancer in postmenopausal women. This substance is from a group of active substances called aromatase inhibitors.

Synthesis of Anastrozol

Anastrozol is commercially synthesized from dibromomesitylene in a four step process. In the first stage of the synthesis, nucleophilic substitution occurs, in which β-dibromesitylene reacts with potassium cyanide using a phase transfer catalyst to form the corresponding dinitrile. This is followed by exhaustive methylation with methyl iodide. In the last step of the chemical synthesis reaction of Anastrozola with N-bromosuccinimide, the corresponding benzyl bromide derivative is obtained by radical bromination, which in the last step is converted to anastrozole with 1,2,4-triazole in basic medium.

What side effects may occur?

  • Headache
  • high tide
  • Nausea
  • Skin rash
  • joint pain
  • Joint stiffness
  • joint inflammation
  • Osteoporosis (bone loss)
  • Powerlessness or weakness
  • Loss of appetite
  • Lipid metabolism disorders with high cholesterol (hypercholesterolemia)
  • Drowsiness
  • carpal tunnel syndrome
  • Diarrhea
  • Vomit
  • Elevated alkaline phosphatase
  • Elevated liver values ​​(ALAT, AST)
  • Hair loss with alopecia (alopecia)
  • Allergic skin hypersensitivity (allergic dermatitis)
  • Pain in the bones
  • Muscle pain
  • Dry mucous membrane in the vaginal area
  • vaginal bleeding
  • Disorder of feelings and perception (sensory disorder)
  • paresthesia
  • Loss of taste (ageusia)
  • taste disorder
  • High levels of calcium in the blood (hypercalcemia), with or without an increase in parathyroid hormone (parathyroid hormone) levels
  • Elevated liver values ​​(GGT)
  • Increased bile pigment (bilirubin) in the blood
  • Inflammation of the liver
  • Urticaria (urticaria)

Mechanism of action

The central action of anastrozole is based on highly effective inhibition of the aromatase enzyme. This enzyme catalyzes the conversion of androgens to estrone and estrogen-type estradiol. Persistent inhibition of aromatase results in a permanent decrease in estrogen levels in the bloodstream as anastrozole continues to act. For a malignant tumor – breast cancer – there are fewer and fewer hormones for growth, further growth of tumor tissue is possible. This leads to a very effective suppression of the growth of the cancerous ulcer and thus initially also to the protection of the surrounding breast tissue from infiltration and destruction by the breast cancer. The pharmacological feature of Anastrozola should be especially noted: on the one hand, it does not have a steroid structure, and on the other hand, it reversibly inhibits aromatase. This is a crucial difference from the active ingredient exemestane, which acts as an irreversible aromatase inhibitor.

Another feature of the effectiveness of Anastrozola is its targeted direct effect on the tumor, as it also inhibits aromatase in malignant tissue. That allows you to fight breast cancer much more accurately and effectively. Anastrozole is also very effective: a single dose of 1 mg of the active substance reduces estrogen levels by 70% in 7 days and up to 80% in 14 days. Anastrozole does not have an estrogenic, androgenic or progestogenic effect.

Use in sports

An increased level of female sex hormones, such as estrogen, has a certain inhibitory effect on high athletic performance. The action of estrogen leads to a significant increase in the accumulation of water and fat. When using an anastrozole inhibitor, this effect can be significantly reduced. Anastrozol inhibits aromatase, resulting in a rapid drop in estrogen levels and greatly reduces effects such as water retention and fat accumulation.