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Exeplex – The Aromatase Inhibitor

Exeplex or Exemestane is an oral steroidal aromatase inhibitor or an aromatase inactivator that can prevent the estrogen hormone-induced breast cancer among the postmenstrual women. Like other estrogen inhibitors, it also blocks estrogen from synthesizing. This is used in hormonal therapy as well. In 2005, FDA in the USA had approved the component for using on specific conditions. The hormone receptor-positive breast cancer can be properly treated with the use of Exeplex.


The best of the use for Exeplex is in treating cancer among the patients. The estrogen receptor is able to provide the best effective care for the patients after receiving Tamoxifen for a couple of years. Premenopausal women’s breast cancer requires hormone-receptor-positive therapy to prevent the hormonal surge in terms of affecting the treatment process. The drug is perfect for premenopausal women, including pregnant and lactating mothers.


The oral pill of Exeplex is taken through the mouth. The anti-cancer medication can be effective for treating the patients along with other Aromasin drugs. Single-dose of the drug is at least 32-fold or 800mg, while continuous therapy can be of about 24-fold or 600mg, which would be perfectly tolerated. Animal studies may consider the drug as 2000 to 4000-fold.

The dosage can be consumed (as per common prescriptions) 50mg PO q/day. However, the breast cancer treatment may continue for a couple or more years with 25mg PO q/day, which may be increased with time as the cancerous tumours grow. It is supposed to consume the component after having meals.


Exeplex as ER-positive breast cancer medication is proper medication for treating the post-menstrual women. This is an irreversible steroidal aromatase inactivator of type 1 with a structurally natural substrate of 4-androstenedione, as it acts as a false substrate for the aromatase enzyme. It is also known as suicide inhibition.

On pharmacokinetics, it can be said that Exeplex is absorbed from the gut with strong first-pass effect in the liver. The hepatic contractions may be effective towards the users. The liver enzyme known as CYP3A4 oxidizes the methylidene group in position 6, while the 17-Keto group is reduced by Aldo-keto reductases. About 40% of the component is excreted by urine and 40% by faeces. The terminal half-life of the component is 24-hours.

Chemically the component stands as 6-methylideneandrosta-1, 4-diene-3, 17-Dione. This makes Exeplex a steroid, which appears to structurally similar to 4-androstenedione.


Performance enhancement, along with treating the cancerous factors can be considered as a prime feature of Exeplex. Other than that the problems may follow the post-therapy process are –

  • Hot flashes
  • Hair loss
  • Muscle pain
  • Tiredness
  • Anxiety
  • Diarrhoea
  • Bone fracture
  • Dark urine
  • Vaginal bleeding
  • Mood swing
  • Yellowing eyes/skin

It is important not to use birth control pills during the period of consuming Exeplex. The component is considered as a hazard-free component as the milking mothers can use it. However, allergic reactions and more things should be checked out to prevent problems.


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