What is aromatase inhibitors used for?
Aromatase inhibitors (AIs) lower estrogen levels by stopping an enzyme in fat tissue (called aromatase) from changing other hormones into estrogen. (Estrogen can fuel the growth of breast cancer cells.) These drugs don't stop the ovaries from making estrogen.Dec 16, 2021
Who should take aromatase inhibitors?
Aromatase inhibitor research has demonstrated improved survival in postmenopausal women, postmenopausal women with metastasis, and premenopausal women under the age of 35 with ovarian ablation. Aromatase inhibitors are also effective in the preventative setting.
Which aromatase inhibitor is best for breast cancer?
These third-generation aromatase inhibitors (letrozole/Femara (Novartis Pharmaceuticals, Basel, Switzerland) and anastrozole/Arimidex (AstraZeneca, Pharmaceuticals, Macclesfield, Cheshire, UK)), have recently demonstrated superior efficacy compared with tamoxifen as initial therapy for early breast cancer improving ...Mar 1, 2011
Can men take aromatase inhibitors for breast cancer?
These drugs stop estrogen production by blocking an enzyme (aromatase) in fat tissue that converts male hormones from the adrenal glands into estrogen. Aromatase inhibitors are taken daily as pills. They have been very effective in treating breast cancer in women, but they have not been well-studied in men.Apr 27, 2018
What are examples of aromatase inhibitors?
Examples of aromatase inhibitors include: Femara (letrozole) Arimidex (anastrozole) Aromasin (exemestane)Aug 5, 2016
What is adjuvant aromatase inhibitor therapy?
Background: Aromatase inhibitors (AIs) are standard hormone therapy (HT) for the adjuvant treatment of postmenopausal endocrine-sensitive early breast cancer.
What is Arimistane used for?
Arimistane is used for weight loss, to improve athletic performance, to reduce sexual problems, and for other uses, but there is no good scientific evidence to support its use. Arimistane might also be unsafe.
What is anastrozole used for?
Anastrozole is used to treat early hormone receptor-positive breast cancer. It is also used for first-line treatment of hormone receptor-positive or hormone receptor-unknown advanced or metastatic (cancer that has spread) breast cancer.Feb 1, 2022
What are the 3 aromatase inhibitors?
Arimidex (chemical name: anastrozole)Aromasin (chemical name: exemestane)Femara (chemical name: letrozole)Jan 13, 2022
What do estrogen blockers do for males?
Medications. Medications used as estrogen blockers include: Aromatase inhibitors (AI): This medication can increase testosterone, along with other hormones, by inhibiting the ability of androgens to be converted to estradiol in the body. This decreases the overall level of estrogen in the body.Feb 24, 2022
What is anastrozole used for in males?
We conclude that the aromatase inhibitor anastrozole increases androgen production and normalizes serum testosterone levels in older men with mild hypogonadism. Serum estradiol levels are reduced but generally remain within the normal range for men.
What is the function of aromatase?
Aromatase is an enzyme involved in the conversion of androgen (such as testosterone) to estrogen (such as 17β-estradiol). It is also a very effective therapeutic target for the treatment of endocrine-responsive breast cancer.Aug 13, 2015
How long does aromatase inhibitor last?
Aromatase inhibitors are prescribed for 5-10 years. The length of this treatment along with side effects can make it tough to complete treatment. Dealing with menopausal symptoms related to hormone therapy can be hard. Talk with your health care provider about ways to ease these and other side effects.
What are the side effects of aromatase inhibitors?
Side Effects of Aromatase Inhibitors. Possible side effects of aromatase inhibitors include muscle pain, joint pain and menopausal symptoms (such as hot flashes). Aromatase inhibitors also cause a loss of bone density. You’ll get a baseline measure of your bone density so changes in your bone density can be monitored.
What hormones are needed for breast cancer?
Hormone receptor-positive breast cancers need estrogen and/or progesterone (female hormones) to grow. Aromatase inhibitors lower estrogen levels in the body by blocking aromatase, an enzyme that converts other hormones into estrogen.
How long does breast cancer treatment last?
Breast cancer treatment is most effective when all parts of the treatment plan are followed as prescribed. Aromatase inhibitors are prescribed for 5-10 years. The length of this treatment along with side effects can make it tough to complete treatment.
Do aromatase inhibitors work in premenopausal women?
Aromatase Inhibitors and Ovarian Suppression. Aromatase inhibitors don’t normally work in premenopausal women because their ovaries are still making estrogen.
Is aromatase inhibitor a risk reduction drug?
Aromatase inhibitors have been studied in the risk reduction setting. Findings from randomized controlled trials have shown the aromatase inhibitors exemestane and anastrozole may lower the risk of developing breast cancer in postmenopausal women at high risk [ 113-114 ].
Can aromatase inhibitors be used for breast cancer?
In general, aromatase inhibitors are only used to treat breast cancer in postmenopausal women. However, some premenopausal women may take an aromatase inhibitor when combined with ovarian suppression. Ovarian suppression prevents the ovaries from making estrogen, so a woman becomes postmenopausal.
What are aromatase inhibitors?
Aromatase inhibitors use two distinct mechanisms to block the action of aromatase and thereby reduce estrogen production. Type I inhibitors such as exemestane and formestane (Lentaron) are androgen-like compounds that bind irreversibly to the substrate-complex, causing permanent inactivation of the enzyme. [8,9] This could potentially lead to prolonged estrogen deprivation even after the drug is cleared. These drugs are also known as aromatase inactivators. Type II inhibitors such as aminoglutethimide, letrozole, and anastrozole are nonsteroidal compounds that reversibly bind to the heme-iron component of the aromatase enzyme, thereby inhibiting the conversion of androgen to estrogen in an indirect fashion. [8]
What is the ATAC trialists group?
The ATAC Trialists Group: Pharmacokineticsof anastrozole and tamoxifen alone,and in combination, during adjuvant endocrinetherapy for early breast cancer in postmenopausalwomen: A sub-protocol of the “Arimidexand tamoxifen alone or in combination” ( ATAC) trial. Br J Cancer 85:317-324, 2001.
What is the ATAC trial?
The ATAC trial is the only adjuvant trial of a new aromatase inhibitor that has been published so far. [5] This large multinational double-blind placebo-controlled trial began in July 1996 and ended accrual in March 2000. The aim of the trial was to compare the efficacy and sideeffect profile of 5 years of anastrozole (1 mg po qd), tamoxifen (20 mg po qd), and the combination of tamoxifen and anastrozole in the management of postmenopausal women with earlystage breast cancer.
What is the survival rate for breast cancer?
Despite these promising statistics, the 15-year survival rate for breast cancer is still only about 60%. [2] . These data highlight the need for innovative therapies such as the new generation of aromatase inhibitors, including anastrozole (Arimidex), exemestane (Aromasin), and letrozole (Femara).
Is letrozole anastrozole or exemestane?
All three aromatase inhibitors- letrozole (2.5 mg/d), anastro zole (1 mg/d), and exemestane (25 mg/d)- have been approved by the US Food and Drug Administration (FDA) as second-line hormonal therapy in postmenopausal women with estrogen-responsive disease. In randomized trials comparing letrozole, anastrozole, or exemestane to megestrol acetate in women who had received tamoxifen, time to progression and overall survival were as good, if not slightly better, with the newer drugs. [24-29] Similar results were observed in a randomized trial comparing letrozole with aminoglutethimide. [30]
Does letrozole suppress estrogen?
Biochemical studies show that letrozole and anastrozole can significantly suppress both tissue and plasma concentrations of estrogen and its derivatives. [42,43] Postmenopausal women with ER-positive locally advanced breast cancer who receive 3 to 4 months of anastrozole, letrozole, or exemestane therapy have shown a decrease in tumor volume of between 75% and 90%. [42,44-47] In a small randomized trial comparing 1 or 10 mg of anastrozole daily over a 3-month period, 15 of the 17 patients who would have required a mastectomy achieved the option of breast-conserving surgery. [45]
Is aminoglutethimide an adjuvant?
Aminoglutethim ide was the first aromatase inhibitor to be evaluated in the adjuvant setting. In a multicenter trial in the United Kingdom, 354 women with node-positive breast cancer were randomized to receive either aminoglutethimide (250 mg po qid) and hydrocortisone (20 mg po bid) or placebo for 2 years after surgical treatment. Aminoglutethimide appeared to be superior to placebo for disease-free survival in the 4-year interim analysis, but no difference in disease-free or overall survival was observed at a median follow-up of 8.1 years. [37]
What is aromatase inhibitor?
Ongoing Research. Aromatase inhibitors are a class of drug used to prevent cancer recurrence in postmenopausal women with estrogen receptor-positive breast cancer. These medications also are prescribed for premenopausal women in combination with ovarian suppression therapy and for men with breast cancer who are unable to take tamoxifen.
How long does it take for aromatase inhibitors to slow down bone loss?
Treatment with tamoxifen for two to five years before aromatase inhibitors may slow down the rate of bone loss.
What is Femara used for?
Treatment of advanced cancer if it progresses with tamoxifen. Femara is indicated for use as: 8 . Adjuvant therapy for early-stage breast cancer. Second-line adjuvant therapy for early-stage breast cancer after tamoxifen has been used for five years. First-line treatment for advanced breast cancer.
What are the side effects of aromatase inhibitors?
The common short-term side effects associated with all three aromatase inhibitors include: Hot flashes. Joint pain 4 . Muscle pain.
Is aromatase good for premenopausal women?
There is growing evidence that aromatase may benefit more than just postmenopausal women. A number of studies shown that the drugs may be beneficial in premenopausal women whose ovaries have suppressed with gonadotropin-releasing hormone agonists (GnHRa) .
Can you take Arimidex with food?
Aromatase inhibitors are delivered in tablet form and prescribed as a once-daily dose. 4 Arimidex and Femara can be taken with or without food. Aromasin should be taken after a meal as fat in food aids in the drug's absorption.
Can you use aromatase inhibitors while on tamoxifen?
An aromatase inhibitor may also be recommended in women who have advanced cancer that progresses while on tamoxifen. Each individual aromatase inhibitor has its own specific indications. Second-line adjuvant therapy for early-stage breast cancer after tamoxifen has been used for two to three years.
Technical Summary
We have developed exemestane-based vinyl diazo compounds that act as aromatase inhibitors to be used in the treatment of cancer, particularly breast and ovarian cancer. Exemestane is structurally related to androstenedione and acts as an irreversible, steroidal aromatase inactivator.
Developmental Stage & Potential Market
Additional testing is underway to investigate the stereoselectivity of the insertion site.
To take aromatase inhibitors...or not?
I had breast cancer diagnosed (thanks to a mammogram) in June 2011, had 2 ops in July/Aug to remove the lump (1st one they didnt know if they had taken a wide enough area...turned out they had!) and all lymph glands, followed by 6 Chemo treatments (Taxotere / FEC) and 4 weeks of Radiotherapy, all finishing around March 2012.
Re: To take aromatase inhibitors...or not?
hi sugarpuff, i too had same cancer as you picked up almost three years ago with mamagram refused chem fec but had three weeks radiotherapy then put on arimidex for five years was in total agony and im a very tough cookie my oncologist said try to persevere i did so for a year life was awful as i live alone and love gardening couldnt pick kettle up some days pain in my feet hands shoulders neck hips knees and no sleep as keep waking up with numb tingling fingers i said cant take anymore so she then put me on exemerstane that was not so bad for a couple of months but now im in agony again my surgeon said when i see her again which will be august to ask for tamoxifen to be honest i dont think any are any different i just hope after five years it all stops no one seems to know i call it a living hell, sorry i cant be more helpful i dread each day as this is not quality of life.
To take aromatase inhibitors...or not?
Hi....this is now 2020 and hoping to reach sugarpuff as I could have written her post. I have been on femera for just over two and a half years and basically have come to a grinding halt. Wrist tendinitis in both wrists, De Quervains tendinitis in both thumbs and tendon problems in some fingers.
To take aromatase inhibitors...or not?
Hi I had a lumpectomy and full lymph gland removal in April 2020 and was given Letrozole to take for 10 years. I am only into just over a month and already my hair is falling out in handfuls, my skin has aged terribly, have pins and needles in my feet and hands, cannot sleep at all, if I get 2 hours per night that's a gift.
To take aromatase inhibitors...or not?
Hi finished taking chemo exactly a year ago on - Letrozole. No SEs to start but they have built up over time. Frozen shoulder carpal tunnel syndrome sweats ... horrible, But we MUST take them . They are so effective that now prescribed for 10 not 5 years we are not ' cured' we need these drugs to keep us cancer=free.
To take aromatase inhibitors...or not?
I understand completely where you are coming from but living for 10 years (and I will not be far off 80 when this is up) with this horrible drug is causing me severe depression. Before I was diagnosed with cancer I was active, vibrant with a **** for life, on a good diet, not overweight, in the gym 3 to 4 times a week.
To take aromatase inhibitors...or not?
i do understand but you need to speak to your onc before doing anything. My figure is also 6 per cent but that is the difference it makes in long-term survival ie mortality not recurrence which AIs can stop by up to 50 per cent.