User:Din.a/sandbox

Anastrozole is a type of new generation endocrine therapy used to treat breast cancer. Specifically, it is an aromatase inhibitor pill for to stop estrogen production. It is used by patients with hormone receptor-positive breast cancer or those at high risk for developing cancer.

It was first approved by the FDA in 1995 and then again in 2000 as a first-line treatment. Common side effects include vasodilation, nausea, pain in the bone. Use during pregnancy is known to harm the baby.

Mechanism of action
Anastrozole is part of the aromatase inhibitor family which means it reversibly binds to the aromatase enzyme. and through competitive inhibition blocks the conversion of androgens to estrogens in peripheral (extra-gonadal) tissues. In short it works by blocking the production of estrogen.

Market production
It is a pill taken orally, commonly referred to by under the trade name Arimidex among others. Anastrozole was patented in 1987 and approved for medical use in 1995. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. Anastrozole is available as a generic medication. The wholesale cost in the developing world is about 1.92 to 30.60 USD a month.[6] In the United States, the wholesale cost is about 3.81 USD per month.[7]

Breast Cancer
Newer endocrine therapies have developed in the recent years because of Tamoxifen, which was the originally most popular and thought to be the most effective drug, built up resistance in patients (Ohno).

The ATAC trial was of localized breast cancer and women received either anastrozole, tamoxifen, or both for five years, followed by five years of follow-up. After more than 5 years the group that received anastrozole had better results than the tamoxifen group. The trial suggested that anastrozole is the preferred medical therapy for postmenopausal women with localized breast cancer, which is estrogen receptor (ER) positive. Another study found that the risk of recurrence was reduced by 40%, but was associated with an increased risk of bone fractures. The study concluded that ER positive patients benefited from switching from tamoxifen to anastrozole in patients who have completed 2 years' adjuvant tamoxifen. A more recent trial found that anastrozole significantly reduced the incidence of breast cancer in postmenopausal women relative to placebo, and while there were side effects related to estrogen deprivation observed, the researchers concluded that this was probably not related to the treatment. Lead author Jack Cuzick was quoted by the BBC as saying, "This class of drugs is more effective than previous drugs such as tamoxifen and crucially, it has fewer side effects," adding that he thought there was now enough evidence to support offering the drug.

Combination Therapy
A correlation study in 2002 found that Anastrozole is more effective alone than when used in combination with Tamoxifen Fulvestrant and Anastrozole were given in combination therapy trials, which found the combination therapy to be more effective than each medication alone, or when given sequentially. Currently, there is no clinical evidence to show that Anastrozole in combination with Fulvestrant had a clinical advantage over anastrozole monotherapy in patients with a history of previous adjuvant anti-estrogen exposure.

Side Effects
Common side effects are an altered mood, coughing, hot flashes, and nausea. Many reports of general, bone, joint and back pain have been seen. More severe side effects are vasodilation, osteoporosis and, bone loss An increased risk for heart disease and bone fracture is also recorded.

In Females
Recent studies have begun using aromatase inhibitors to treat other female diseases, such as endometriosis. There has been positive feedback that indicate that it allows for better control in late-stage disease.

In men
AnastrozoAnastrozole has been tested for reducing estrogens, including estradiol, in men. Excess estradiol in men can cause benign prostatic hyperplasia, gynecomastia, and symptoms of hypogonadism. It can also contribute to increased risk of stroke, heart attack, chronic inflammation, prostate enlargement and prostate cancer. Some athletes and body builders use anastrozole as part of their steroid cycle to reduce and prevent symptoms of excess estrogen--gynecomastia, emotional lability and water retention. Study data suggest dosages of 0.5 mg to 1 mg a day reduce serum estradiol by approximately 50% in men, which differs in postmenopausal women. Anastrozole has also proven to be efficient in increasing testosterone production in elderly males. This opens the potential for Anastrozole to be used as an androgen replacement therapy in the future.

In children
Anastrozole may be used off-label in children with precocious puberty, or children with pubertal gynecomastia. Aromatase inhibitors, in combination with an antiandrogen are effective in preventing bone age advancement and virilization in boys with FMPP. Following the onset of puberty, the epiphyseal plate begins to close due to an increased amount of estrogen production escaping local metabolism and spreading to the circulatory system. It is shown to help slow this process, and increase adult height prediction in adolescent males treated with protein-based peptide hormones for the treatment of growth hormone deficiency.