120511-73-1

Description

Anastrozole is a hormone treatment medication known for lowering estrogen levels in the body, particularly in postmenopausal women with hormone-dependent breast cancer. Chemically identified as 2,2-[5-(1H-1,2,4-triazol-1-ylmethyl)-1,3-phenylene]bis(2-methylpropiononitrile), it is a third-generation aromatase inhibitor with the trade name ARIMIDEX®.

Uses

Widely used in breast cancer treatment, Anastrozole is indicated for early-stage, hormone receptor-positive breast cancer in postmenopausal women. It has shown effectiveness in reducing the risks of breast cancer recurrence and metastasis when compared to tamoxifen. The medication is well-tolerated, with the primary adverse effect being an increased risk of bone fractures during the treatment period. Anastrozole has linear pharmacokinetics, is metabolized in the liver, and is unlikely to cause clinically significant drug interactions.

Function

Functioning as a competitive and selective inhibitor of aromatase, Anastrozole prevents the conversion of testosterone into estradiol and androstenedione into estrone. This inhibition occurs through competitive binding of aromatase to the hemegroup of cytochrome P450, reducing estrogen biosynthesis in peripheral tissues and the breast.

The synthesis of Anastrozole involves a four-step process, and it has been used in various research applications. Classified as readily biodegradable and moderately mobile in soils, Anastrozole is a potent and highly selective aromatase inhibitor used as second-line therapy in postmenopausal breast cancer treatment after tamoxifen.

Chemical Properties

Crystalline Solid. soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide. The solubility of anastrozole in these solvents is approximately 20, 13, and 14 mg/ml.

Originator

Zeneca (United Kingdom)

Definition

ChEBI: Anastrozole is a 1,2,4-triazole compound having a 3,5-bis(2-cyano-2-propyl)benzyl group at the 1-position. It has a role as an antineoplastic agent and an EC 1.14.14.14 (aromatase) inhibitor. It is a member of triazoles and a nitrile.

Brand name

Arimidex (AstraZeneca).

Therapeutic Function

Antitumor

Biological Activity

Potent and highly selective aromatase (CYP19) inhibitor (IC 50 = 15nM) that has no discernible effect on adrenocorticoid hormone synthesis. Reduces plasma estrogen levels and exhibits antitumor activity in vivo . Orally active.

Biochem/physiol Actions

Anastrozole, which contains a triazole functional group, reversibly binds to the cytochrome P-450 component of aromatase. Binding interferes with the catalytic properties of aromatase, which results in inhibition of estrogen synthesis.

Drug interactions

Potentially hazardous interactions with other drugs Oestrogen-containing therapies: avoid concomitant administration as would negate pharmacological action. Tamoxifen: avoid concomitant administration.