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Hormone · Profile

Anastrozole

Arimidex · AI · Aromatase Inhibitor

Hormone ManagementApproved
MW
293.4g/mol
Formula
C17H19N5

Anastrozole is a third-generation aromatase inhibitor primarily used in the management of hormone receptor-positive breast cancer in postmenopausal women. Researchers primarily study anastrozole to evaluate its efficacy and safety compared to other treatments, particularly tamoxifen. Key findings from the ATAC trial indicate that anastrozole significantly prolongs disease-free survival and reduces the risk of recurrence and distant metastases compared to tamoxifen, with a lower incidence of certain side effects. Current research continues to explore its long-term outcomes and potential applications in other contexts, highlighting its clinical relevance in oncology.

Overview

Übersicht

Anastrozole is a synthetic, non-steroidal aromatase inhibitor primarily used in the management of hormone receptor-positive breast cancer. It belongs to the chemical class of triazoles and is marketed under the brand name Arimidex. Anastrozole is produced synthetically and is not an endogenous compound. Researchers have extensively studied its role in hormone management, particularly in postmenopausal women with breast cancer. The primary physiological role of anastrozole is to inhibit the aromatase enzyme, which is responsible for the conversion of androgens to estrogens. This reduction in estrogen levels is beneficial in treating estrogen receptor-positive breast cancer, as it limits the growth of cancer cells that rely on estrogen. Researchers have observed that anastrozole is more effective than tamoxifen in improving disease-free survival and reducing recurrence in breast cancer patients. Anastrozole acts by binding to the aromatase enzyme, thereby inhibiting the conversion of androgens to estrogens. This action decreases circulating estrogen levels, which in turn reduces the growth stimulus for estrogen-dependent breast cancer cells. The pharmacokinetic properties of anastrozole include a half-life of approximately 50 hours, allowing for once-daily oral dosing. It is metabolized primarily in the liver and has good oral bioavailability. Clinically, anastrozole is used as an adjuvant treatment for hormone receptor-positive breast cancer in postmenopausal women. It is approved by regulatory agencies such as the FDA and is considered a standard of care in this setting. Researchers continue to explore its use in other hormone-related conditions.

Chemical profile

Chemische Struktur

Chemical structure of Anastrozole
FormelC17H19N5
Molekulargewicht293.4g/mol
CAS-Nummer120511-73-1
PubChem CID2187
Mechanism

Wirkmechanismus

Anastrozole acts on the aromatase enzyme, inhibiting its activity and thus preventing the conversion of androgens to estrogens. This results in a significant reduction in circulating estrogen levels, which is crucial for limiting the growth of estrogen-dependent breast cancer cells.

Mechanism

Signalweg

Anastrozole is a selective aromatase inhibitor that reduces estrogen synthesis by inhibiting the aromatase enzyme, which converts androgens (androstenedione and testosterone) into estrogens (estrone and estradiol) in peripheral tissues. This reduction in estrogen levels leads to decreased activation of estrogen receptors (ERα and ERβ) in hormone receptor-positive breast cancer cells, inhibiting estrogen-dependent signaling pathways such as the PI3K/Akt and MAPK pathways, ultimately resulting in reduced cell proliferation and tumor growth. The precise molecular mechanisms underlying the long-term effects of anastrozole on breast cancer recurrence and survival are still being elucidated.

Half-Life & Pharmacokinetics

POOral

Approximately 50 hours

Anastrozole is well-absorbed orally, and its long half-life supports once-daily dosing.

Storage

Temperature

Store at room temperature (15-30C)

Light

Protect from light

Form

Stable in tablet form

Notes

Ensure packaging is intact to maintain efficacy.

Solubility

Löslichkeit

Anastrozole is poorly soluble in water but soluble in organic solvents such as ethanol.

Legal Status

🇩🇪DE

Verschreibungspflichtig (prescription only), not a controlled substance under BtMG.

🇺🇸US

FDA approved for breast cancer treatment, prescription only.

🇦🇺AU

TGA Schedule 4 (prescription only medicine).

🇬🇧UK

Prescription only medicine (POM) as per MHRA guidelines.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

Open Questions

Offene Forschungsfragen

Current evidence is limited regarding the long-term safety and efficacy of anastrozole in diverse populations, particularly in younger patients and those with varying comorbidities. Further research is needed to explore the mechanisms underlying the increased incidence of fractures and arthralgia associated with anastrozole, as well as to clarify the potential carryover benefits of anastrozole beyond the initial treatment period. Additionally, larger randomized controlled trials are necessary to assess the comparative effectiveness of anastrozole versus other emerging therapies in specific subgroups, such as those with different hormone receptor statuses or genetic backgrounds.

64 Research Publications

9,291

Total Citations

39

Human/RCT

6.5

Avg. Influence

2025

Latest

Sort
Filter
#01

Results of the ATAC (Arimidex, Tamoxifen, Alone or in Combination) trial after completion of 5 years' adjuvant treatment for breast cancer.

Howell A, et al. · Lancet (London, England)

HumanInfluence76.0
2347
Researchers observed that anastrozole significantly prolonged disease-free survival and reduced distant metastases compared to tamoxifen in postmenopausal women with localized hormone-receptor-positive breast cancer.

Key findings

  1. 01Anastrozole led to fewer cancer recurrences than tamoxifen.
  2. 02Patients on anastrozole experienced fewer side effects, particularly gynecological issues.
  3. 03Anastrozole reduced the occurrence of distant metastases and contralateral breast cancers.
#02

Effect of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer: 10-year analysis of the ATAC trial.

Cuzick Jack, et al. · The Lancet. Oncology · 2010

HumanInfluence36.0
1533
The study demonstrated that anastrozole provides superior long-term efficacy compared to tamoxifen in disease-free survival and time to recurrence for postmenopausal women with hormone-receptor-positive early-stage breast cancer.

Key findings

  1. 01Anastrozole improved disease-free survival compared to tamoxifen.
  2. 02Patients on anastrozole had longer times before cancer recurrence.
  3. 03Serious side effects were less common with anastrozole than tamoxifen.
#03

Anastrozole is superior to tamoxifen as first-line therapy for advanced breast cancer in postmenopausal women: results of a North American multicenter randomized trial. Arimidex Study Group.

HumanInfluence17.0
1009
Researchers observed that anastrozole provides a significant increase in time to progression compared to tamoxifen in postmenopausal women with advanced breast cancer, with fewer adverse events.
#04

Anastrozole versus tamoxifen as first-line therapy for advanced breast cancer in 668 postmenopausal women: results of the Tamoxifen or Arimidex Randomized Group Efficacy and Tolerability study.

HumanInfluence17.0
868
Researchers observed that anastrozole was equivalent to tamoxifen in efficacy for advanced breast cancer, with a lower incidence of thromboembolic events and vaginal bleeding in postmenopausal women.
#05

Relationship between quantitative estrogen and progesterone receptor expression and human epidermal growth factor receptor 2 (HER-2) status with recurrence in the Arimidex, Tamoxifen, Alone or in Combination trial.

HumanInfluence2.0
438
Researchers observed that quantitative expression of estrogen and progesterone receptors did not identify patients who would benefit differentially from anastrozole compared to tamoxifen in terms of time to recurrence.
#06

Anastrozole, a potent and selective aromatase inhibitor, versus megestrol acetate in postmenopausal women with advanced breast cancer: results of overview analysis of two phase III trials. Arimidex Study Group.

HumanInfluence4.0
403
The study demonstrated that anastrozole is well tolerated and as effective as megestrol acetate in postmenopausal women with advanced breast cancer who progressed after tamoxifen treatment.
#07

Comparison of anastrozole versus tamoxifen as preoperative therapy in postmenopausal women with hormone receptor-positive breast cancer: the Pre-Operative "Arimidex" Compared to Tamoxifen (PROACT) trial.

HumanInfluence8.0
364
The study demonstrated that anastrozole is an effective preoperative therapy for postmenopausal women with hormone receptor-positive breast cancer, leading to clinically beneficial tumor downstaging.
#08

Influence of anastrozole (Arimidex), a selective, non-steroidal aromatase inhibitor, on in vivo aromatisation and plasma oestrogen levels in postmenopausal women with breast cancer.

HumanInfluence5.0
350
Researchers observed that anastrozole effectively inhibits in vivo aromatization and significantly reduces plasma estrogen levels in postmenopausal women with breast cancer.
#09

Potent Cell-Cycle Inhibition and Upregulation of Immune Response with Abemaciclib and Anastrozole in neoMONARCH, Phase II Neoadjuvant Study in HR+/HER2- Breast Cancer.

Hurvitz Sara A, et al. · Clinical cancer research : an official journal of the American Association for Cancer Research · 2020

HumanInfluence11.0
180
Researchers observed that the combination of abemaciclib and anastrozole resulted in significant cell-cycle arrest and enhanced immune activation in postmenopausal women with HR+/HER2- early breast cancer.

Key findings

  1. 01Abemaciclib combined with anastrozole led to a significant decrease in cell growth.
  2. 0258% to 68% of patients achieved complete cell-cycle arrest with the combination therapy.
  3. 03The treatment showed biological and clinical activity with manageable side effects.
#10

Arimidex: a potent and selective fourth-generation aromatase inhibitor.

AnimalInfluence8.0
164
The study demonstrated that anastrozole is a potent and selective aromatase inhibitor with a favorable pharmacokinetic profile in humans.

Clinical Trials (25)

Preclinical
Phase I
Phase II
Phase III
Approved

25

Total Trials

8,951

Total Enrolled

Non-interventional Study to Evaluate Arimidex in Postmenopausal Women With Advanced Breast Cancer

NCT00562458COMPLETED
Sponsor

AstraZeneca

Enrollment

200

Started

2006

Advanced Breast Cancer

Arimidex Therapy Compliance Electronic Monitoring System

NCT00936442COMPLETED
Sponsor

AstraZeneca

Enrollment

104

Started

2009

Primary outcome

Overall adherence to anastrozole

Breast Cancer

Bone Geometry and Muscle Density Changes in Postmenopausal Women and Breast Cancer Patients Prescribed Anastrozole

NCT00421447COMPLETED
Sponsor

Hamilton Health Sciences Corporation

Enrollment

58

Started

2007

Breast Cancer

Anastrozole Biphosphonate Study in Postmenopausal Women With Hormone-Receptor-Positive Early Breast Cancer

NCT00082277Phase 4COMPLETED
Sponsor

AstraZeneca

Enrollment

237

Started

2004

Primary outcome

The change from baseline in lumbar spine (L1-L4) bone mineral density (BMD)

Breast Cancer

A Prospective,Open-label Study of Anastrozole in Post-menopausal Women With Hormone Sensitive Advanced Breast Cancer

NCT00544986Phase 4COMPLETED
Sponsor

AstraZeneca

Started

2005

Primary outcome

1. Tolerability(safety) 2.Efficacy (a) Time to tumor progression TTP (b) Objective Response (OR) Rate (c) Symptom Evaluation

Breast Cancer

Anastrozole in Preventing Breast Cancer in Postmenopausal Women at Increased Risk of Breast Cancer

NCT00078832Phase 3COMPLETED
Sponsor

Queen Mary University of London

Enrollment

3,864

Started

2003

Primary outcome

Development of histologically confirmed breast cancer, both invasive and non-invasive with median follow-up at 5 years

Breast Cancer

Different Durations of Adjuvant Anastrozole Therapy After 2 to 3 Years Tamoxifen Therapy in Breast Cancer

NCT00301457Phase 3COMPLETED
Sponsor

Maastricht University Medical Center

Enrollment

1,914

Started

2006

Primary outcome

To assess the disease free survival (DFS) with 6 years of adjuvant anastrozole compared with 3 years of adjuvant anastrozole in postmenopausal hormone sensitive breast cancer patients, subsequent to 2 to 3 years of adjuvant tamoxifen

Breast Cancer

A Global Study to Compare the Effects of Fulvestrant and Arimidex in a Subset of Patients With Breast Cancer.

NCT01602380Phase 3COMPLETED
Sponsor

AstraZeneca

Enrollment

462

Started

2012

Primary outcome

Comparison of Progression-Free Survival (PFS) in Patients Treated With Fulvestrant With Those Treated With Anastrozole

Hormone Receptor Positive Breast Cancer

Ribociclib in Hormone Receptor-positive, HER2-negative Early Breast Cancer With Residual Disease After Neoadjuvant Chemotherapy

NCT07400523Phase 3NOT_YET_RECRUITING
Sponsor

Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University

Enrollment

446

Started

2026

Primary outcome

3-year invasive disease-free survival

Breast Cancer

A Study of SHR6390 in Combination With Letrozole or Anastrozole in Patients With HR Positive and HER2 Negative Advanced Breast Cancer

NCT03966898Phase 3UNKNOWN
Sponsor

Jiangsu HengRui Medicine Co., Ltd.

Enrollment

426

Started

2019

Primary outcome

Investigator-assessed PFS

Advanced Breast Cancer

Study of Arimidex and Radiotherapy Sequencing

NCT01402193Phase 3UNKNOWN
Sponsor

Fudan University

Enrollment

220

Started

2011

Primary outcome

Level of TGF-β1

Breast Cancer

Aromatase Inhibitors in the Treatment of Male Infertility

NCT00440180Phase 3TERMINATED
Sponsor

University of Utah

Enrollment

20

Started

2007

Primary outcome

Pregnancy Rate

ObesityOligospermia

Arimidex Multicenter Trial in Growth Hormone (GH) Deficient Boys

NCT00133354Phase 2/3COMPLETED
Sponsor

Nemours Children's Clinic

Enrollment

53

Started

2001

Primary outcome

The primary measure of efficacy is change in predicted adult height based on rate of bone age advancement.

Hypopituitarism

Bay98-7196, Dose Finding / POC Study

NCT02203331Phase 2COMPLETED
Sponsor

Bayer

Enrollment

319

Started

2014

Primary outcome

Absolute Change in Mean Pain of the 7 Days With Worst EAPP From Baseline (Last 28 Days Before Randomization) to End of Treatment (Last 28 Days of Treatment Period, Days 57-84) as Measured on NRS by Question 1 of ESD

Endometriosis

Capecitabine in Combination With Aromatase Inhibitor Versus Aromatase Inhibitors, in Hormonal Receptor Positive Recurrent or Metastatic Breast Cancer Patients, Randomized Controlled Study

NCT04012918Phase 2UNKNOWN
Sponsor

Ain Shams University

Enrollment

124

Started

2018

Primary outcome

Progress-free survival

Metastatic Breast Cancer

Molecular Analyses to Predict Pathways of Endocrine Resistance Following Short Term Neoadjuvant Endocrine Treatment in Patients With Hormone Receptor-Positive HER2-negative Breast Cancer

NCT06361940Phase 2RECRUITING
Sponsor

Medical College of Wisconsin

Enrollment

100

Started

2024

Primary outcome

Change from baseline in the number of subjects with increased HER-1 receptor tyrosine kinases protein expression in tumors.

Breast Cancer

Partial Double-Blind, Placebo-Controlled Study to Assess the Effect of Anastrozole on the Endometrium in Healthy Volunteers

NCT00467493Phase 2COMPLETED
Sponsor

Meditrina Pharmaceuticals

Enrollment

64

Started

2007

Primary outcome

Endometrial thickness as measured by transvaginal ultrasound, safety

Menstruation Disorders

Effects of Aromatase Inhibition Versus Testosterone in Older Men With Low Testosterone: Randomized-Controlled Trial.

NCT00104572Phase 2COMPLETED
Sponsor

National Institute on Aging (NIA)

Enrollment

44

Started

2004

Primary outcome

Effect of Testosterone Gel vs. Anastrozole on Bone Mineral Density

HypogonadismDiabetesSarcopeniaOsteoporosisDepression

Precision Treatment of Recurrent/Metastatic Salivary Gland Carcinoma Guided by Molecular Typing

NCT06145308Phase 2RECRUITING
Sponsor

Peking Union Medical College

Enrollment

39

Started

2023

Primary outcome

ORR

Salivary Gland CarcinomaPrecision Therapy

Estradiol Suppression for the Treatment of Metastatic Breast Cancer in Premenopausal Women

NCT00186121Phase 2COMPLETED
Sponsor

Stanford University

Enrollment

35

Started

2000

Primary outcome

Objective Response Rate (ORR)

Breast Cancer

Neoadjuvant Dalpiciclib Plus Aromatase Inhibitors in Luminal B/HER2-negative Breast Cancer (DANCER)

NCT05640778Phase 2UNKNOWN
Sponsor

Second Affiliated Hospital, School of Medicine, Zhejiang University

Enrollment

30

Started

2022

Primary outcome

Complete cell cycle arrest(CCCA, defined as ki67≤2.7%)rate at 2 weeks of treatment

Luminal B/HER2-negative Breast Cancer

Akt Inhibitor MK-2206 and Anastrozole With or Without Goserelin Acetate in Treating Patients With Stage II-III Breast Cancer

NCT01776008Phase 2TERMINATED
Sponsor

National Cancer Institute (NCI)

Enrollment

16

Started

2013

Primary outcome

Pathological Complete Response Rate

Estrogen Receptor PositiveHER2/Neu NegativeRecurrent Breast CarcinomaStage IIA Breast CancerStage IIB Breast CancerStage IIIA Breast CancerStage IIIB Breast CancerStage IIIC Breast Cancer

Combination Chemotherapy and Peripheral Stem Cell Transplantation in Treating Women With Metastatic Breast Cancer

NCT00004906Phase 2COMPLETED
Sponsor

Hackensack Meridian Health

Started

1999

Breast Cancer

This Study in Patients With Different Types of Cancer (Solid Tumours) Aims to Find a Safe Dose of Xentuzumab in Combination With Abemaciclib With or Without Hormonal Therapies. The Study Also Tests How Effective These Medicines Are in Patients With Lung and Breast Cancer

NCT03099174Phase 1COMPLETED
Sponsor

Boehringer Ingelheim

Enrollment

133

Started

2017

Primary outcome

[Cohort A, B, C & D] Maximum Tolerated Dose (MTD) of Xentuzumab

NeoplasmsBreast Neoplasms

Impact of Estradiol Addback

NCT01862835Phase 1COMPLETED
Sponsor

Mayo Clinic

Enrollment

43

Started

2013

Primary outcome

BioStatistical Analysis

Normal Healthy Volunteers

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This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer