> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/anastrozole-327e05a9-e5b7-41d1-a335-bd8a46453b55
> Record changed: 2026-10-13

# Anastrozole

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1399)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1399)

First approval year

1995

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1399)

## Development status

**First approval year**

1995

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1399)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1399)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1399)

**Drug name**

Anastrozole

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1399)

**Molecular weight**

293.37

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1399)

**Structure (SMILES)**

CC(C)(C#N)c1cc(Cn2cncn2)cc(C(C)(C)C#N)c1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1399)

### Brand names (6)

- anastrozole
- Anastrozole
- arimidex
- Arimidex
- nastrosa
- Nastrosa

### Other names (69)

- 1 3 benzenediacetonitrile alpha alpha alpha alpha tetramethyl 5 1h 1 2 4 triazol 1 ylmethyl
- 1,3-BENZENEDIACETONITRILE,.ALPHA.,.ALPHA.,.ALPHA.',.ALPHA.'-TETRAMETHYL-5-(1H-1,2,4-TRIAZOL-1-YLMETHYL)-
- abemaciclib and letrozole anastrozole
- Anastozole (Arimidex)
- Anastrazole (Arimidex)
- anastrazole (Arimidex®)
- anastrozol
- Anastrozol
- anastrozole
- Anastrozole
- anastrozole (Arimidex)
- Anastrozole (Arimidex)
- Anastrozole (Arimidex®)
- Anastrozole (ARIMIDEX™)
- Anastrozole (Aromatase Inhibitor)
- Anastrozole (Teva Pharmaceuticals USA)
- ANASTROZOLE \[EP MONOGRAPH\]
- ANASTROZOLE \[HSDB\]
- anastrozole \[INN\]
- ANASTROZOLE \[JAN\]
- ANASTROZOLE \[MART.\]
- ANASTROZOLE \[MI\]
- ANASTROZOLE \[ORANGE BOOK\]
- ANASTROZOLE \[USAN\]
- ANASTROZOLE \[USP IMPURITY\]

And 44 more, listed on the interactive page.

## Identifiers

**ATC classification codes**

- L02BG03

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1399)

**CAS registry numbers**

- 120511-73-1

**ChEMBL ID**

CHEMBL1399

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1399)

**InChIKey**

YBBLVLTVTVSKRW-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1399)

**PubChem compound IDs**

- 2187

**RxNorm IDs (RxCUI)**

- 84857

**FDA ingredient codes (UNII)**

- 2Z07MYW1AZ

## Regulatory information

### United States

**Applicant**

ANI PHARMS

**Approval date**

27 Dec 1995

**Application number**

NDA020541

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

**Availability**

Prescription only

## Pharmacology

### Drug classification

**Pharmacology name**

anastrozole

**Type**

Synthetic organic

**Drug name stem**

\-rozole

**Approval recorded by Guide to Pharmacology**

Yes

#### Administration routes

- Oral

### Mechanisms of action (2)

- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
CYP19A1

**Gene symbol**  
CYP19A1

**Protein identifier**  
P11511

**Median affinity**

7.82

**Affinity units**  
pIC50

**Primary target**  
Yes
- **Mechanism**  
Cytochrome P450 19A1 inhibitor

**Action type**  
Inhibitor

**Target**  
Aromatase

**Protein identifier**  
P11511

### Open Targets mechanisms

- **Mechanism**  
Cytochrome P450 19A1 inhibitor

**Action type**  
Inhibitor

**Target**  
Aromatase

### DrugCentral mechanisms

- **Action type**  
Inhibitor

**Gene symbol**  
CYP19A1

**Protein identifier**  
P11511

**Organism**  
Homo sapiens

**Target development level**  
Clinical

### Investigated indications (28)

- **Condition**  
Metabolic Syndrome

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000195

**Subject identifier**  
D024821
- **Condition**  
Breast Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0000305

**Subject identifier**  
D001943
- **Condition**  
Carcinoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000313

**Subject identifier**  
D002277
- **Condition**  
Carcinoma, Intraductal, Noninfiltrating

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000432

**Subject identifier**  
D002285
- **Condition**  
Hypertension

**Highest recorded phase**

0.5

**Condition identifier**  
EFO:0000537

**Subject identifier**  
D006973
- **Condition**  
Carcinoma, Lobular

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000553

**Subject identifier**  
D018275
- **Condition**  
Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369
- **Condition**  
Endometriosis

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0001065

**Subject identifier**  
D004715
- **Condition**  
Hypertension, Pulmonary

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0001361

**Subject identifier**  
D006976
- **Condition**  
Hypopituitarism

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0001380

**Subject identifier**  
D007018
- **Condition**  
Breast Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0003869

**Subject identifier**  
D001943
- **Condition**  
Triple Negative Breast Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0005537

**Subject identifier**  
D064726
- **Condition**  
Breast Neoplasms, Male

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0006861

**Subject identifier**  
D018567
- **Condition**  
Breast Diseases

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0009483

**Subject identifier**  
D001941
- **Condition**  
Aging

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0022597

**Subject identifier**  
D000375
- **Condition**  
Klinefelter Syndrome

**Highest recorded phase**  
3

**Condition identifier**  
EFO:1001006

**Subject identifier**  
D007713
- **Condition**  
Endometrial Neoplasms

**Highest recorded phase**  
1

**Condition identifier**  
EFO:1001512

**Subject identifier**  
D016889
- **Condition**  
Gynecomastia

**Highest recorded phase**  
3

**Condition identifier**  
HP:0000771

**Subject identifier**  
D006177
- **Condition**  
Puberty, Precocious

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0000088

**Subject identifier**  
D011629
- **Condition**  
Hypogonadism

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0002146

**Subject identifier**  
D007006
- **Condition**  
Anovulation

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0002775

**Subject identifier**  
D000858
- **Condition**  
Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
MONDO:0004992

**Subject identifier**  
D009369
- **Condition**  
Breast Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
MONDO:0007254

**Subject identifier**  
D001943
- **Condition**  
Ovarian Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0008170

**Subject identifier**  
D010051
- **Condition**  
Endometrial Neoplasms

**Highest recorded phase**  
1

**Condition identifier**  
MONDO:0011962

**Subject identifier**  
D016889

And 3 more, listed on the interactive page.

### Open Targets indications (56)

- **Condition identifier**  
EFO\_0000195

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000305
- **Condition identifier**  
EFO\_0000313

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000432

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000537
- **Condition identifier**  
EFO\_0000616
- **Condition identifier**  
EFO\_0001065

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0001361

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0003869

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0004714

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0009483
- **Condition identifier**  
EFO\_0009870

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_1000307
- **Condition identifier**  
EFO\_1001006

**Highest recorded phase**  
3
- **Condition identifier**  
HP\_0000771

**Highest recorded phase**  
3
- **Condition identifier**  
HP\_0000789

**Highest recorded phase**  
3
- **Condition identifier**  
HP\_0000855

**Highest recorded phase**  
2
- **Condition identifier**  
HP\_0002829
- **Condition identifier**  
HP\_0012743
- **Condition identifier**  
MONDO\_0000088

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0002146

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0002447

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0004379

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0004953
- **Condition identifier**  
MONDO\_0004989

**Highest recorded phase**  
4

And 31 more, listed on the interactive page.

### Reported adverse events (26)

- **Event**  
alopecia

**Reports**  
639

**Reporting signal score**

501.004
- **Event**  
arthralgia

**Reports**  
1,387

**Reporting signal score**

766.594
- **Event**  
bone pain

**Reports**  
484

**Reporting signal score**

555.235
- **Event**  
breast cancer

**Reports**  
743

**Reporting signal score**  
1,384.6
- **Event**  
breast cancer metastatic

**Reports**  
702

**Reporting signal score**  
2,425.01
- **Event**  
breast cancer recurrent

**Reports**  
220

**Reporting signal score**

663.174
- **Event**  
carbohydrate antigen 15-3 increased

**Reports**  
97

**Reporting signal score**

362.44
- **Event**  
carpal tunnel syndrome

**Reports**  
53

**Reporting signal score**

84.4647
- **Event**  
disease progression

**Reports**  
797

**Reporting signal score**

790.879
- **Event**  
fatigue

**Reports**  
1,443

**Reporting signal score**

266.103
- **Event**  
hot flush

**Reports**  
580

**Reporting signal score**

830.111
- **Event**  
malignant neoplasm progression

**Reports**  
1,690

**Reporting signal score**  
3,447.45
- **Event**  
metastases to bone

**Reports**  
932

**Reporting signal score**  
2,763.91
- **Event**  
metastases to liver

**Reports**  
747

**Reporting signal score**  
2,063.58
- **Event**  
metastases to lung

**Reports**  
363

**Reporting signal score**

887.657
- **Event**  
metastases to lymph nodes

**Reports**  
274

**Reporting signal score**

702.82
- **Event**  
metastases to skin

**Reports**  
85

**Reporting signal score**

255.825
- **Event**  
metastases to spine

**Reports**  
119

**Reporting signal score**

319.107
- **Event**  
nasal disorder

**Reports**  
30

**Reporting signal score**

77.7688
- **Event**  
neoplasm progression

**Reports**  
787

**Reporting signal score**  
1,695.49
- **Event**  
neutropenia

**Reports**  
1,377

**Reporting signal score**  
1,390.24
- **Event**  
osteopenia

**Reports**  
58

**Reporting signal score**

106.355
- **Event**  
pik3ca-activated mutation

**Reports**  
95

**Reporting signal score**

399.89
- **Event**  
tonsillar disorder

**Reports**  
28

**Reporting signal score**

87.7008
- **Event**  
trigger finger

**Reports**  
44

**Reporting signal score**

125.292

And 1 more, listed on the interactive page.

### Trial references (203)

- NCT00004900  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00004900)
- NCT00004906  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00004906)
- NCT00005908  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00005908)
- NCT00049062  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00049062)
- NCT00053898  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00053898)
- NCT00053911  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00053911)
- NCT00057941  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00057941)
- NCT00066378  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00066378)
- NCT00066573  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00066573)
- NCT00072462  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00072462)
- NCT00075764  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00075764)
- NCT00077025  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00077025)
- NCT00077168  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00077168)
- NCT00078832  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00078832)
- NCT00081510  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00081510)
- NCT00082277  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00082277)
- NCT00126360  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00126360)
- NCT00128843  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00128843)
- NCT00186121  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00186121)
- NCT00206414  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00206414)
- NCT00217399  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00217399)
- NCT00217659  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00217659)
- NCT00232661  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00232661)
- NCT00235937  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00235937)
- NCT00244959  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00244959)

And 178 more, listed on the interactive page.

## Dosing

**Dose**

1mg

**Route**

Oral

**How often**

Once daily

### Conditions of use

- Take with or without food

## Chemical properties

**Hydrogen bond acceptors**

5

**Hydrogen bond donors**

0

**Polar surface area**

78.29

**Calculated partition coefficient (ALogP)**

2.93

**Calculated partition coefficient (XLogP)**

2.1

**Prodrug**

No

**Chirality**

Achiral

**Inorganic**

No

**Rule-of-five violations**

0

**Rotatable bonds**

4

**Heavy atoms**

22

**Molecular formula**

C17H19N5

**Monoisotopic mass**

293.16404563

**Natural product**

Yes

## National Drug Codes

- 0093-7536
- 16729-035
- 23155-857
- 24979-725
- 42291-016
- 42291-085
- 43063-383
- 50268-075
- 51991-620
- 59651-236
- 60687-112
- 62135-490
- 62559-670
- 63187-080
- 65841-743
- 68001-155
- 68382-209
- 72189-415
- 72189-682
- 72789-008
- 72789-342
- 72789-575
- 76420-004
- 82804-162
- 87063-224

And 15 more, listed on the interactive page.

## Evidence counts

**Recorded assays**

3,012

**Active assays**

52

### Active assay types (4)

- Confirmatory
- Other
- Screening
- Summary

## Pharmacologic actions

- Antineoplastic Agents, Hormonal  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D018931.html)
- Aromatase Inhibitors  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D047072.html)

## Biological measurements

### Observed measurements

#### Oral bioavailability

**Median**

84

**Mean**

84

**Minimum**

84

**Maximum**

84

**Unit**

%

**Assays**

1

**Standard deviation**

0

**Summary method**

median

**Censored results excluded**

0

**Other units excluded**

0

**Unknown units excluded**

0

#### Measurement types

- F

## Related records

### Trials (303)

- 3 Years of Anastrozole vs. no Treatment as Extended Adjuvant Therapy for Postmenopausal Women With Breast Cancer
- A Clinical Study of Darcilil Combined With AI Combined With Pyrrotinib in the Treatment of TPBC
- A Clinical Trial to Compare Efficacy and Tolerability of Faslodex With Arimidex in Patients With Advanced Breast Cancer
- A Comparative Study of AZD9833 Plus Palbociclib Versus Anastrozole Plus Palbociclib in Patients With ER-Positive HER2 Negative Breast Cancer Who Have Not Received Any Systemic Treatment for Advanced Disease
- A Global Study to Compare the Effects of Fulvestrant and Arimidex in a Subset of Patients With Breast Cancer.
- A Neoadjuvant Study of Abemaciclib (LY2835219) in Postmenopausal Women With Hormone Receptor Positive, HER2 Negative Breast Cancer
- A Open Study of Metronomic Oral Vinorelbine in Combination With Aromatase Inhibitors for the Treatment of Postmenopausal Women With Hormone Receptor Positive,HER2-negative, Advanced Breast Cancer Who Received no Prior Therapy for Advanced Disease
- A Pharmacokinetic and Randomized Trial of Neoadjuvant Treatment With Anastrozole Plus AZD0530 in Postmenopausal Patients With Hormone Receptor Positive Breast Cancer
- A Phase 1b Study of T-DXd Combinations in HER2-low Advanced or Metastatic Breast Cancer
- A Phase 3 Study of HRS-8080 Versus Treatment Chosen by Physicians in Locally Advanced and Metastatic Breast Cancer
- A Phase I/II Study of XZP-3287 in Metastasis Solid Tumors
- [A Phase III Trial Comparing HRS-8080 With Standard Endocrine Therapy in Patients With Intermediate or High Risk Early Breast Cancer](https://trialight.com/data/trial/a-phase-iii-trial-comparing-hrs-8080-with-standard-endocrine-e2a57990-1f83-4ce5-bd36-8e94a49c52ad.md)
- A Prospective,Open-label Study of Anastrozole in Post-menopausal Women With Hormone Sensitive Advanced Breast Cancer
- A Retrospective Real-world Study of Abemaciclib in HR+ Breast Cancer
- A Study Evaluating Megestrol Acetate Modulation in Hormone Receptor Positive Advanced Breast Cancer
- A Study for Safety and Effectiveness of IMC-A12 by Itself or Combined With Antiestrogens to Treat Breast Cancer
- A Study of Abemaciclib (LY2835219) in Participants With Breast Cancer
- A Study of Abemaciclib (LY2835219) in Participants With Non-Small Cell Lung Cancer or Breast Cancer
- A Study of Avutometinib (VS-6766) + Defactinib (VS-6063) in Recurrent Low-Grade Serous Ovarian Cancer
- [A Study of Camizestrant in ER+/HER2- Early Breast Cancer After at Least 2 Years of Standard Adjuvant Endocrine Therapy](https://trialight.com/data/trial/a-study-of-camizestrant-in-er-her2-early-breast-cancer-after-2e9eb478-c398-409a-a2cc-81da5599f650.md)

### Approved for (5)

- [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md)
- Breast carcinoma
- [Breast neoplasm](https://trialight.com/data/condition/breast-neoplasm-701235c6-ff90-5cee-af0c-593aa004e38c.md)
- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md)
- Neoplasm

### In development for (23)

- Anovulation Phase 2
- [Breast disorder](https://trialight.com/data/condition/breast-disorder-c24c48eb-9ec6-54b1-80b7-1e9cec90eba4.md) Phase 1
- [Carcinoma](https://trialight.com/data/condition/carcinoma-575e4c82-5fa5-5455-b1b7-30972eca1a2f.md) Phase 2
- Ductal breast carcinoma in situ Phase 3
- [Endometrial cancer](https://trialight.com/data/condition/endometrial-cancer-4da2a0bc-7943-502b-a698-cc2beccbed8c.md) Phase 1
- [Endometrial carcinoma](https://trialight.com/data/condition/endometrial-carcinoma-d0794a04-ff16-5af6-8fb7-7b3d6bd6c537.md) Phase 1
- [Endometriosis](https://trialight.com/data/condition/endometriosis-3a5471b6-6d24-50b8-b1e6-8803dd78b0db.md) Phase 2
- Female breast carcinoma Phase 3
- Gynecomastia disorder Phase 3
- [Hypertensive disorder](https://trialight.com/data/condition/hypertensive-disorder-6d786557-b9e8-5afc-80f3-89a1995f9da5.md) Early phase 1
- Hypogonadism Phase 2
- Hypogonadotropic hypogonadism Phase 2
- Hypopituitarism Phase 2
- Invasive lobular breast carcinoma Phase 3
- Kallmann syndrome Phase 1
- Klinefelter syndrome Phase 3
- Male breast carcinoma Phase 2
- McCune-Albright syndrome Phase 2
- Metabolic syndrome X Phase 2
- [Ovarian cancer](https://trialight.com/data/condition/ovarian-cancer-f64f2018-55a5-553a-8960-76cb4906aa17.md) Phase 3

### Other linked conditions (1)

- Invasive breast carcinoma

### Targets (1)

- [CYP19A1](https://trialight.com/data/target/cyp19a1-9682b33b-ed66-55a7-8155-bf00584059c7.md) Cytochrome P450 19A1 inhibitor

---

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