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Letrozole

Breast Neoplasms

DRUG STATUS

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Approvals

US(FDA), UK(BNF)

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Essential Medicine

YES

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Teratogenicity

Unlisted

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Pharmaceutical Class

Aromatase Inhibitor

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Drug Ingredient

Letrozole

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Summary

  • Letrozole is a medication used to treat hormone receptor-positive breast cancer in postmenopausal women. It can also be used after other treatments, like tamoxifen, to prevent the cancer from returning.

  • Letrozole is a nonsteroidal aromatase inhibitor. It works by reducing estrogen synthesis in the body, which helps slow the growth of hormone-fueled breast cancer.

  • The usual dose of Letrozole for adults is one 2.5 mg pill taken once a day, with or without food.

  • Common side effects of Letrozole include hot flashes, nausea, joint pain, and shortness of breath. Other effects like fatigue, dizziness, and weight increase have also been reported.

  • Letrozole should not be taken by pregnant women as it can harm the baby. It can also cause tiredness and dizziness, so caution is advised when driving or using machinery. Letrozole can sometimes weaken bones, so your doctor may need to monitor your bone health.

Indications and Purpose

What is Letrozole used for?

Letrozole is a medicine for women who have gone through menopause and have breast cancer. It's used when the cancer's growth is fueled by hormones or when it's unclear if hormones play a role. It can treat advanced breast cancer that has spread, and it can also be used after surgery for early-stage breast cancer to help prevent the cancer from returning. Sometimes, it's used for a longer time after another medicine called tamoxifen. 

How does Letrozole work?

Letrozole is a medicine that's quickly absorbed into the body. It breaks down slowly into harmless substances and is mostly removed through the kidneys in urine. Most of the drug is found in the urine. It takes about 2 days for half of the drug to leave your body, and it takes several weeks to reach a stable level in your blood. Two liver enzymes, CYP3A4 and CYP2A6, help break it down.

Is Letrozole effective?

Letrozole is a medication used to treat breast cancer in postmenopausal women. It works best in cancers that are fueled by hormones. It can be used after other treatments like tamoxifen, even for a long time (up to 5 years after tamoxifen), to help prevent the cancer from returning. It's also used to treat advanced or spread breast cancer in these women. Studies show it's effective for many years. 

How does one know if Letrozole is working?

The effectiveness is monitored through regular medical evaluations, imaging studies, and assessments of disease-free survival​

Directions for Use

What is the usual dose of Letrozole?

For grown-ups, the usual dose of letrozole is one small pill (2.5 mg) once a day. It doesn't matter if you take it with or without food. 

How do I take Letrozole?

Take one 2.5mg Letrozole pill each day. It doesn't matter if you take it with or without food. 

For how long do I take Letrozole?

The duration of letrozole therapy varies depending on the indication:

  • Adjuvant Treatment of Early Breast Cancer: Median treatment duration is 5 years.
  • Extended Adjuvant Treatment: Median duration is also around 5 years.
  • Advanced Breast Cancer: Continue treatment until tumor progression is observed​

How long does it take for Letrozole to start working?

Letrozole significantly reduces estrogen levels within 2 to 3 days of starting treatment.

How should I store Letrozole?

Store letrozole at room temperature, between 20°C to 25°C (68°F to 77°F

Warnings and Precautions

Who should avoid taking Letrozole?

Letrozole is a medicine that shouldn't be taken by pregnant women because it can harm the baby. Women who can get pregnant need to use birth control during and for three weeks after taking it. It can sometimes weaken bones, so doctors will need to check on that. It can also cause tiredness and dizziness, so be careful driving or using machines. Your cholesterol might go up, so that needs checking too. If you have serious liver problems, you might need a lower dose. 

Can I take Letrozole with other prescription drugs?

Taking Letrozole with tamoxifen lowers the amount of Letrozole in the bloodstream, but it doesn't seem to affect how well Letrozole works if you take it after tamoxifen. Other drugs like cimetidine and warfarin don't appear to interact significantly with Letrozole. There's not much information about how Letrozole interacts with other cancer drugs. 

Can I take Letrozole with vitamins or supplements?

There is no specific information on interactions with vitamins or supplements. Consult a healthcare provider before combining.

Can Letrozole be taken safely while pregnant?

Letrozole is contraindicated in pregnancy due to its potential to cause fetal harm. It has been associated with spontaneous abortions and congenital defects​

Can Letrozole be taken safely while breastfeeding?

Women who are breastfeeding shouldn't take the medication letrozole because it could seriously harm their babies. There's no information on how it affects babies who are breastfed, so it's best to avoid any risk. Breastfeeding should also be stopped for at least three weeks after finishing the medication. 

Is Letrozole safe for the elderly?

Older people with metastatic breast cancer taking common treatments didn't show more problems or less benefit than younger people in studies. While bone density might decrease, doctors should watch for that. Even in long-term treatment, older patients (many over 65, some over 75) did just as well as younger patients.

Is it safe to exercise while taking Letrozole?

Exercise is generally safe but monitor for fatigue or bone-related side effects like fractures or pain​.

Is it safe to drink alcohol while taking Letrozole?

No specific interaction is noted, but alcohol may exacerbate side effects like dizziness or fatigue.