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long term side effects of letrozole

long term side effects of letrozole


In 2010, it is estimated that more than 200,000 women will be newly diagnosed with invasive breast cancer in the United States, making it the most commonly diagnosed cancer in women. The majority of women are post-menopausal at the time of diagnosis. Adjuvant endocrine manipulations reduce the risk of breast cancer-related recurrence and death in women with hormone receptor-positive disease. The introduction of aromatase inhibitors (AIs) to the adjuvant treatment of postmenopausal women with hormone receptor-positive breast cancer has significantly changed the management of the disease. These agents are commonly used instead of or in sequence with tamoxifen because of the demonstrated improvement in disease-free survival compared to tamoxifen alone .

How Letrozole Works:

Hormones are chemical substances that are produced by glands in the body, which enter the bloodstream and cause effects in other tissues.  For example, the hormone testosterone made in the testicles and is responsible for male characteristics such as deepening voice and increased body hair.  The use of hormone therapy to treat cancer is based on the observation that receptors for specific hormones that are needed for cell growth are on the surface of some tumor cells.  Hormone therapies work by stopping the production of a certain hormone, blocking hormone receptors, or substituting chemically similar agents for the active hormone, which cannot be used by the tumor cell.  The different types of hormone therapies are categorized by their function and/or the type of hormone that is effected.

Letrozole is an aromatase inhibitor.  This means it blocks the enzyme aromatase (found in the body's muscle, skin, breast and fat), which is used to convert androgens (hormones produced by the adrenal glands) into estrogen. In the absence of estrogen, tumors dependent on this hormone for growth will shrink.

Note:  We strongly encourage you to talk with your health care professional about your specific medical condition and treatments. The information contained in this website is meant to be helpful and educational, but is not a substitute for medical advice. 

Letrozole and breast cancer

Elimination of estrogen production can be achieved by aromatase inhibitors. These inhibitors antagonize the conversion of androgens into estrogen by targeting the aromatase enzyme and have been increasingly used to inhibit estrogen production in breast cancers.6 Compounds that inhibit aromatase have been developed from the first- to the third-generation inhibitors, and letrozole (Femara®; Novartis Pharmaceuticals Basel, Switzerland) is a third-generation aromatase inhibitor with high selectivity. Specifically, because aromatase in peripheral tissues provides the major source of estrogens in postmenopausal women, and letrozole inhibits aromatase activity in these tissues by >99% in vivo,8 letrozole is most widely used in advanced, recurrent, or metastatic breast cancers in postmenopausal patients. In premenopausal women, high levels of estrogens are produced primarily from the ovaries, where compensatory feedback loops for gonadotropin production dampen the effectiveness of letrozole.


Before starting Letrozole treatment, make sure you tell your doctor about any other medications you are taking (including prescription, over-the-counter, vitamins, herbal remedies, etc.). 

Inform your health care professional if you are pregnant or may be pregnant prior to starting this treatment. Pregnancy category D (Letrozole may be hazardous to the fetus.  Women who are pregnant or become pregnant must be advised of the potential hazard to the fetus).

Letrozole is indicated for post-menopausal women. Do not conceive a child (get pregnant) while taking Letrozole. Barrier methods of contraception, such as condoms, are recommended. Discuss with your doctor when you may safely become pregnant or conceive a child after therapy.


Although most women in this study took adjuvant endocrine therapy as prescribed, many endured a range of side effects, often without seeking help. Advice, support and monitoring for adherence are not routinely offered in conventional follow-up settings. Women deserve more opportunity to discuss the pros, cons and impact of long-term adjuvant endocrine therapy. New service models are needed to support adherence, enhance quality of life and ultimately improve survival. These should ideally be community based, in order to promote self-management in the longer term.

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