Anastrozole, sold under the brand name Arimidex among others, is an medication used in addition to other treatments for breast cancer.[ Specifically it is used for hormone receptor-positive breast cancer.][ It has also been used to prevent breast cancer in those at high risk.][ It is taken orally.]
Common side effects of anastrozole include , mood changes, joint pain, and nausea.[ Severe side effects include an increased risk of heart disease and osteoporosis.][ Use during pregnancy may harm the baby.][ Anastrozole is in the aromatase-inhibiting family of medications.][ It works by blocking the biosynthesis of in the body, and hence has effects.][
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Anastrozole was patented in 1987 and was approved for medical use in 1995.[ In 2023, it was the 194th most commonly prescribed medication in the United States, with more than 2million prescriptions.]
Medical uses
Breast cancer
Anastrozole is used in the treatment and prevention of breast cancer in women.[ ] After more than 5 years the group that received anastrozole had better results than the tamoxifen group.
Early puberty
Anastrozole is used at a dosage of 0.5 to 1 mg/day in combination with the antiandrogen bicalutamide in the treatment of peripheral precocious puberty, for instance due to familial male-limited precocious puberty (testotoxicosis) and McCune–Albright syndrome, in boys.
Available forms
Anastrozole is available in the form of 1 mg oral tablets.
Contraindications
of anastrozole include hypersensitivity to anastrozole or any other component of anastrozole formulations, pregnancy, and breastfeeding.
Side effects
Common of anastrozole (≥10% incidence) include ,
asthenia, arthritis, pain, arthralgia, hypertension, depression, nausea and vomiting, rash, osteoporosis, , back pain, insomnia, headache, bone pain, peripheral edema, coughing, dyspnea, pharyngitis, and lymphedema.
Interactions
Anastrozole is thought to have clinically negligible inhibitory effects on the cytochrome P450 CYP1A2, CYP2A6, CYP2D6, CYP2C8, CYP2C9, and CYP2C19.
Anastrozole does not affect circulating levels of tamoxifen or its major metabolite N-desmethyltamoxifen.
Pharmacology
Pharmacodynamics
Anastrozole works by reversibly binding to the aromatase enzyme, and through competitive inhibition blocks the conversion of to in peripheral (extragonadal) tissues.
Pharmacokinetics
The bioavailability of anastrozole in humans is unknown, but it was found to be well-absorbed in animals.
Active efflux of anastrozole by P-glycoprotein at the blood–brain barrier has been found to limit the central nervous system penetration of anastrozole in rodents, whereas this was not the case with letrozole and vorozole.
The metabolism of anastrozole is by N-dealkylation, hydroxylation, and glucuronidation.
Chemistry
Anastrozole is a nonsteroidal benzyl compound triazole.
History
Anastrozole was patented by Imperial Chemical Industries (ICI) in 1987 and was approved for medical use, specifically the treatment of breast cancer, in 1995.
Society and culture
Generic names
Anastrozole is the generic drug of the drug and its , , , and .
Brand names
Anastrozole is primarily sold under the brand name Arimidex.
Availability
Anastrozole is available widely throughout the world.
Research
Anastrozole is surprisingly ineffective at treating gynecomastia, in contrast to selective estrogen receptor modulators like tamoxifen.
Anastrozole was under development for the treatment of female infertility but did not complete development and hence was never approved for this indication.
An anastrozole and levonorgestrel vaginal ring (developmental code name BAY 98–7196) was under development for use as a hormonal contraceptive and treatment for endometriosis. Development was discontinued in November 2018, and the formulation was never marketed.
Anastrozole increases testosterone levels in males and has been studied as an alternative method of androgen replacement therapy in men with hypogonadism.
