An Expert Monograph on Anastrozole (DB01217): Pharmacology, Clinical Efficacy, and Safety Profile

1.0 Executive Summary and Drug Identification

1.1 Overview

Anastrozole is a potent, selective, non-steroidal, third-generation aromatase inhibitor (AI) that represents a cornerstone in the endocrine management of hormone-sensitive malignancies.[1] Its primary clinical application is the treatment of hormone receptor-positive (HR+) breast cancer in postmenopausal women, where it functions by profoundly suppressing systemic estrogen levels.[1] By inhibiting the key enzyme responsible for estrogen biosynthesis in peripheral tissues, Anastrozole deprives HR+ cancer cells of their primary mitogenic stimulus.

First approved for medical use in the United States in 1995, Anastrozole has established a superior efficacy and distinct safety profile compared to the long-standing standard of care, the selective estrogen receptor modulator (SERM) tamoxifen.[1] This has positioned it, along with other third-generation AIs, as a first-line endocrine therapy of choice in the postmenopausal setting. Its global significance is underscored by its inclusion on the World Health Organization's List of Essential Medicines.[4] Marketed under the brand name Arimidex® and widely available as a generic, it was the 179th most commonly prescribed medication in the United States in 2022, reflecting its extensive clinical use.[4]

1.2 Identification and Chemical Properties

Precise identification of a pharmaceutical agent is critical for research, clinical practice, and regulatory affairs. The following table consolidates the key identifiers and physicochemical properties of Anastrozole from multiple authoritative sources, providing a definitive reference for the compound.

Table 1: Key Drug Identifiers and Chemical Properties