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Small MoleculeApproved

Anastrozole (Arimidex)

an-AS-troh-zole

Research profile · How we handle evidence

Category

Small Molecule

Compound type

Phase / Status

Approved

FDA approved for breast cancer. Off-label use in some hormonal contexts is widespread.

Standard Dose

0.5-1mg EOD to daily

Every other day or daily

Half-life

46-48 hours

Plasma elimination

Route(s)

OR

Oral

Research Stage

Market Approved

Regulatory approval granted; post-market monitoring ongoing.

Overview

Anastrozole helps lower estrogen by blocking aromatase. When estrogen is reduced, some people may experience fewer estrogen-related side effects, but overly low estrogen can also cause problems. Use should be clinician-guided when applicable.

Plain-language summary

Anastrozole helps lower estrogen by blocking aromatase. When estrogen is reduced, some people may experience fewer estrogen-related side effects, but overly low estrogen can also cause problems. Use should be clinician-guided when applicable.

Administration Routes

  • Oral

Also known as

AdexArimidexAIAnastroAromatase inhibitorRimi

Mechanisms

1

Competitively inhibits aromatase (CYP19A1), reducing conversion of androgens to estrogens. Non-steroidal and does not directly bind hormone receptors as an estrogen.

Detailed mechanism

Competitively inhibits aromatase (CYP19A1), blocking conversion of androgens to estrogens. Modulates enzyme activity to reduce estrogen production at the molecular level.

Safety

Side effects

  • Joint pain or stiffness (possible with low estrogen)
  • Bone density concerns with longer-term use
  • Fatigue or mood changes in some users
  • Libido changes when estrogen is suppressed
  • Hot flashes (possible)
  • Cardiometabolic risks may vary with individual factors

Reported benefits

  • Reduces estradiol levels
  • May reduce estrogen-related symptoms
  • Helps manage aromatization when clinically indicated
  • Extensive historical clinical use in oncology

Safety profile

Well-characterized safety profile from clinical use. Hormone suppression needs individualized monitoring, and bone-health considerations may apply.

Clinical trials

Completed clinical trials leading to FDA approval.

Structure

View 3D structure

Verified structure

Anastrozole (Arimidex)

Exact 2D structure can be rendered from a PubChem-backed canonical SMILES string.

Verified via PubChemMatched by casNumber
Source: PubChemLookup: 120511-73-1InChIKey YBBLVLTVTVSKRW-UHFFFAOYSA-N
Chemical Formula
C17H19N5
Molecular Weight
293.37 g/mol
CAS Number
120511-73-1
InChIKey
YBBLVLTVTVSKRW-UHFFFAOYSA-N

Stack Context

Stacks with

TestosteroneNolvadexHCG

References

  1. 1

    Anastrozole alone or in combination with tamoxifen versus tamoxifen alone for adjuvant treatment of postmenopausal women with early breast cancer: first ATAC trial results (Lancet)

    2002

    View source
  2. 2

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

    2010

    View source
  3. 3

    Anastrozole versus tamoxifen in postmenopausal women with hormone receptor-positive early breast cancer: meta-analysis of combined data from two RCTs (Eur J Cancer)

    2013

    View source

This profile summarizes research literature for education only. It is not medical advice, and it does not diagnose, treat, or recommend a dose. Consult a qualified professional before changing a protocol.

Research-driven insights.Evidence-based decisions.