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Exemestane

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Molecule Summary

Uses
Breast Cancer
Therapy
Anti-Neoplastic
Side Effects
Hot Flashes, Joint Pain, Tiredness, Sweating
3 Step Quality
Assurance
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NPPA
Regulated

Molecule Description

Exemestane contains exemestane, an irreversible steroidal aromatase inhibitor used to treat hormone-dependent breast cancer in postmenopausal women. It is used for advanced breast cancer that has progressed after tamoxifen and as adjuvant hormonal therapy for early breast cancer after an initial course of tamoxifen. It works by blocking the aromatase enzyme, reducing the body's production of oestrogen and thereby limiting oestrogen stimulation of hormone-sensitive breast cancer cells. Exemestane is intended for postmenopausal women and should not be used in women who are premenopausal. Because it lowers oestrogen levels, it can reduce bone mineral density and increase fracture risk. Your doctor may assess bone health before and during treatment, particularly if you have osteoporosis or other risk factors. Exemestane is taken by mouth, preferably after a meal, as food increases its absorption. Take it exactly as prescribed and do not change or stop the dose without medical advice. Common side effects include hot flushes, joint and muscle pain, fatigue, headache, dizziness, sweating, and nausea. Tell your doctor if you develop jaundice, severe skin reactions, unusual bruising or bleeding, new bone pain, or fractures. Before starting treatment, tell your doctor about liver or kidney problems and all medicines, supplements, and herbal products you take, as some medicines may reduce the effectiveness of exemestane. Exemestane should not be used during pregnancy or breastfeeding. If pregnancy is possible, discuss appropriate contraception with your doctor. Use caution when driving if you experience dizziness or fatigue.

Uses

  • Treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.
  • Adjuvant (follow-on) treatment of postmenopausal women with oestrogen-receptor positive or unknown early breast cancer, following an initial course of adjuvant tamoxifen therapy.

Contraindications

When should one not use Exemestane

  • If you have a known hypersensitivity to exemestane or any ingredient of this medicine.

Side effects

Common side effects of this drug are:

  • Low white blood cell count (leucopenia)
  • Insomnia
  • Headache, dizziness
  • Hot flushes
  • Abdominal pain, nausea
  • Excessive sweating (hyperhidrosis)
  • Joint and musculoskeletal pain
  • General pain, fatigue
  • Raised liver enzymes, blood bilirubin, and alkaline phosphatase (seen on blood tests)
  • Low platelet count (thrombocytopenia)
  • Loss of appetite
  • Carpal tunnel syndrome, tingling sensations (paraesthesia)
  • Vomiting, diarrhoea, constipation, indigestion
  • Hair loss (alopecia), rash, hives, itching
  • Bone fracture, osteoporosis
  • Swelling of the limbs (peripheral oedema), weakness (asthenia)
  • Hypersensitivity reactions
  • Rare Side Effects
  • Excessive sleepiness (somnolence)
  • Hepatitis, cholestatic hepatitis
  • Acute generalised exanthematous pustulosis (a severe skin reaction)
  • Decreased lymphocyte count

Precautions and Warnings

Pregnancy

Pregnancy

No. Exemestane exposure during pregnancy, or even within one month before conception, can cause harm to the baby. If you have the potential to become pregnant, use effective contraception during treatment and for one month after your last dose, and tell your doctor immediately if you become pregnant or suspect you might be.

Breast Feeding

Breast Feeding

It is not known whether exemestane passes into breast milk, but due to the potential harm to the nursing infant breastfeeding is not recommended during treatment with Exemestane and for one month after the last dose.

Driving

Driving

Exemestane can have a moderate effect on your ability to drive or use machinery, as it has been associated with drowsiness, sleepiness, weakness and dizziness. If you experience these effects, avoid driving or operating machinery.

Alcohol

Alcohol

Discuss alcohol use with your doctor, particularly if you have any liver problems.

Other General Warnings

Other General Warnings

Talk to your doctor if
  • You are still having menstrual periods or are unsure of your menopausal status, as Exemestane is only for use in postmenopausal women.
  • You have liver or kidney problems.
  • You have osteoporosis or risk factors for osteoporosis, as this medicine can reduce bone density and increase fracture risk.
  • You have a rare hereditary condition such as fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency, as this medicine contains sucrose.
  • You have had allergic reactions to preservatives in medicines, as this tablet contains methyl parahydroxybenzoate, which may rarely, and possibly with delay, cause allergic reactions.
  • You are taking any oestrogen-containing medicine, as it should not be combined with Exemestane.
  • You develop yellowing of the skin or eyes, severe skin rash or blistering, or any signs of a severe allergic reaction.
  • You notice unusual bruising, bleeding or symptoms of low blood counts such as frequent infections.
  • You are pregnant, breastfeeding or could become pregnant.
  • Take Exemestane after a meal to help your body absorb it better.
  • Keep all scheduled appointments, including any bone density assessments your doctor recommends.
  • Report hot flushes, joint pain or fatigue to your doctor if they become severe or hard to manage. Supportive treatment may help.
  • Report any yellowing of the skin or eyes, dark urine or severe skin rash to your doctor promptly.
  • Watch for unusual bruising or bleeding and report it to your doctor.
  • Do not take oestrogen-containing medicines, including certain hormone therapies, while on this medicine.
  • Inform all your healthcare providers that you are taking this medication before any other medical or dental procedure.

Mode of Action

How Does It Work?

Exemestane contains exemestane, an irreversible, steroidal aromatase inhibitor. In postmenopausal women, oestrogen is produced mainly by the conversion of androgens into oestrogens through the aromatase enzyme in body tissues outside the ovaries. Exemestane blocks this enzyme, substantially reducing oestrogen levels throughout the body. Because many breast cancers depend on oestrogen to grow, this oestrogen deprivation is an effective and selective way to treat hormone-dependent breast cancer in postmenopausal women.

Interactions

Interactions with other medicines

  • Rifampicin: A strong inducer of the CYP3A4 enzyme. It has been shown to significantly reduce exemestane levels in the body and may reduce how well this medicine works.
  • Anticonvulsant medicines such as phenytoin and carbamazepine: These are also CYP3A4 inducers and may reduce the efficacy of Exemestane in the same way as rifampicin.
  • Herbal preparations containing St. John's Wort (Hypericum perforatum): These induce CYP3A4 and may reduce the efficacy of Exemestane.

Interactions with food items

Taking Exemestane with food increases the amount of medicine absorbed into the body, so it is recommended to take it after a meal.

Dosage

Overdose

If an overdose is suspected, seek medical attention immediately. You will be monitored closely and be provided with symptomatic management of the side effects.

Missed a Dose

If you miss a dose of Exemestane, take it as soon as you remember unless it is close to your next dose. In that case, skip the missed dose and continue your normal schedule. Do not take a double dose to make up for a missed one. Contact your doctor if you are unsure.

Frequently Asked Questions (FAQs)

Exemestane works by lowering oestrogen produced outside the ovaries. In premenopausal women, the ovaries continue to produce oestrogen independently of this pathway, so the medicine would not work as intended and is not approved for this use. Your doctor may check hormone levels to confirm your menopausal status.

Exemestane lowers oestrogen, and oestrogen helps maintain bone density. Over time, this can reduce bone mineral density and increase fracture risk, so your doctor may recommend a bone density assessment, especially if you have osteoporosis or risk factors for it.

Exemestane is used for the conditions listed in the Uses section of this page. Your doctor will decide whether it is suitable for your cancer type and stage.

No. Do not stop, delay or change your treatment on your own, even if you feel well. Stopping early can make the treatment less effective. Always speak to your doctor first.

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