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Atlas / Drug / Anastrozole

Anastrozole

drug
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Also known as AnastrozolArimidexICI D1033ICI-D1033NastrosaNSC-719344NSC-759855Rvg-106400ZD-1033ZD1033AnastrosolSID174007355SID170464923SID144205791SID26719808SID144213873C0164598Anastrazole

Summary

Anastrozole (CHEMBL1399) is an approved small-molecule antineoplastic agent (ATC L02BG03) targeting CYP19A1; indicated across 28 conditions including breast carcinoma and breast neoplasm.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L02BG03
  • Targets: 1 (CYP19A1)
  • Indications: 28 conditions
  • Clinical trials: 281
  • Chemistry: 293.4 Da · C17H19N5

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1399
NameAnastrozole
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID2187
ChEBICHEBI:2704
ATCL02BG03
Molecular formulaC17H19N5
Molecular weight293.4
InChIKeyYBBLVLTVTVSKRW-UHFFFAOYSA-N

SMILES: CC(C)(C#N)C1=CC(=CC(=C1)CN2C=NC=N2)C(C)(C)C#N

IUPAC name: 2-[3-(2-cyanopropan-2-yl)-5-(1,2,4-triazol-1-ylmethyl)phenyl]-2-methylpropanenitrile

ChEBI definition: A 1,2,4-triazole compound having a 3,5-bis(2-cyano-2-propyl)benzyl group at the 1-position.

Pharmacological roles (ChEBI): antineoplastic agent, EC 1.14.14.14 (aromatase) inhibitor.

Also known as: Anastrozol, Anastrozole, Arimidex, ICI D1033, ICI-D1033, Nastrosa, NSC-719344, NSC-759855, Rvg-106400, ZD-1033, ZD1033, anastrozole

Patent coverage: 21,199 distinct patent families (89,972 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
CYP19A1CYP19A1Inhibition7.820%P11511

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Aromatase, 3’,5’-cyclic-AMP phosphodiesterase 4D, UDP-glucuronosyltransferase 1A4, Aromatase.

Bioactivity

ChEMBL activities: 14 potent at pChembl ≥ 5 of 15 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
CYP19A19.89Ki0.13nMCHEMBL_ACT_8060204
CYP19A18.82IC501.5nMCHEMBL_ACT_15742061
CYP19A18.82IC501.5nMCHEMBL_ACT_18577011
CYP19A18.82IC501.5nMCHEMBL_ACT_3124021
CYP19A18.44IC503.6nMCHEMBL_ACT_16620058
CYP19A18.1IC508nMCHEMBL_ACT_24713141
CYP19A18.1IC508nMCHEMBL_ACT_8060183
CYP19A18IC5010nMCHEMBL_ACT_2567490
CYP19A17.92IC5012nMCHEMBL_ACT_10833619
CYP19A17.82IC5015.14nMCHEMBL_ACT_1845884
CYP19A17.82IC5015nMCHEMBL_ACT_3290679
CYP19A16.22IC50600nMCHEMBL_ACT_1675998
P224435.41IC503930nMCHEMBL_ACT_29176243
UGT1A45.33IC504720nMCHEMBL_ACT_15457540

Target pathways

Aggregated over 1 target gene(s): CYP19A1.

Top Reactome pathways

3 total, by targets touching each:

PathwayTargetsGenes
Estrogen biosynthesis1CYP19A1
Endogenous sterols1CYP19A1
Defective CYP19A1 causes AEXS1CYP19A1

Dominant GO biological processes

GO termTargets
negative regulation of chronic inflammatory response1
steroid biosynthetic process1
estrogen biosynthetic process1
androgen catabolic process1
obsolete syncytium formation1
female gonad development1
negative regulation of macrophage chemotaxis1
sterol metabolic process1
female genitalia development1
mammary gland development1
response to estradiol1
uterus development1
prostate gland growth1
testosterone biosynthetic process1
positive regulation of estradiol secretion1

Indications & clinical

Indications

28 indications (5 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
breast carcinoma4MONDO:0004989EFO:0000305
breast neoplasm4MONDO:0021100EFO:0003869
neoplasm4MONDO:0005070EFO:0000616
invasive lobular breast carcinoma3MONDO:0005051EFO:0000553
ductal breast carcinoma in situ3MONDO:0005023EFO:0000432
gynecomastia disorder3MONDO:0001571HP:0000771
ovarian cancer3MONDO:0008170MONDO:0008170
Klinefelter syndrome3MONDO:0006823EFO:1001006
pulmonary arterial hypertension2MONDO:0015924EFO:0001361
carcinoma2MONDO:0004993EFO:0000313
endometriosis2MONDO:0005133EFO:0001065
metabolic syndrome X2MONDO:0011565EFO:0000195
hypopituitarism2MONDO:0005152EFO:0001380
triple-negative breast carcinoma2MONDO:0005494EFO:0005537
male breast carcinoma2MONDO:0005628EFO:0006861
precocious puberty2MONDO:0000088MONDO:0000088
hypogonadism2MONDO:0002146MONDO:0002146
anovulation2MONDO:0002775MONDO:0002775
polyostotic fibrous dysplasia2MONDO:0008274MONDO:0018919
endometrial carcinoma1MONDO:0002447EFO:1001512
endometrium neoplasm1MONDO:0021251MONDO:0011962
Kallmann syndrome1MONDO:0018800MONDO:0018800
breast disorder1MONDO:0002657EFO:0009483
hypertensive disorder0MONDO:0005044EFO:0000537

4 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 281.

Phase distribution

PhaseTrials
PHASE2112
PHASE377
Not specified42
PHASE126
PHASE415
PHASE1/PHASE26
EARLY_PHASE12
PHASE2/PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05161195PHASE4ACTIVE_NOT_RECRUITINGRoll-over Study to Allow Continued Access to Ribociclib
NCT00082277PHASE4COMPLETEDAnastrozole Biphosphonate Study in Postmenopausal Women With Hormone-Receptor-Positive Early Breast Cancer
NCT00323479PHASE4COMPLETEDArthralgia During Anastrozole Therapy for Breast Cancer
NCT00537771PHASE4COMPLETEDLiver Safety Under Upfront Arimidex vs Tamoxifen
NCT00544986PHASE4COMPLETEDA Prospective,Open-label Study of Anastrozole in Post-menopausal Women With Hormone Sensitive Advanced Breast Cancer
NCT01553903PHASE4COMPLETEDFeasibility Study for the Determination of Oxysterols in Patients With Breast Cancer Receiving Hormonal Therapy With Tamoxifen or Not
NCT01612871PHASE4COMPLETEDCirculating miRNAs as Biomarkers of Hormone Sensitivity in Breast Cancer
NCT01769781PHASE4COMPLETEDAnastrazole Plus GnRH-agonist in the Treatment of Endometriosis Recurrence
NCT02089854PHASE4UNKNOWNAdjuvant Endocrine Therapy for Estrogen Receptor-beta Positive Triple Negative Breast Cancer
NCT02137538PHASE4COMPLETEDAromatase Inhibitor Growth Study: Letrozole vs. Anastrozole
NCT02959853PHASE4COMPLETEDAromatase Inhibitors and Weight Loss in Severely Obese Hypogonadal Male Veterans (Pilot)
NCT03220178PHASE4TERMINATEDImpact of eHealth-support on Quality of Life in Metastatic Breast Cancer Patients Treated With Palbociclib and Endocrine Therapy
NCT03238703PHASE4WITHDRAWNEndocrine Therapy in Treating Patients With HER2 Negative, Low Risk Breast Cancer
NCT03490513PHASE4COMPLETEDAromatase Inhibitors and Weight Loss in Severely Obese Men With Hypogonadism
NCT06253702PHASE4COMPLETEDBrain Blood Flow Responses to Stress: Sex Differences
NCT00310180PHASE3ACTIVE_NOT_RECRUITINGHormone Therapy With or Without Combination Chemotherapy in Treating Women Who Have Undergone Surgery for Node-Negative Breast Cancer (The TAILORx Trial)
NCT01272037PHASE3ACTIVE_NOT_RECRUITINGTamoxifen Citrate, Letrozole, Anastrozole, or Exemestane With or Without Chemotherapy in Treating Patients With Invasive RxPONDER Breast Cancer
NCT01674140PHASE3ACTIVE_NOT_RECRUITINGS1207 Hormone Therapy With or Without Everolimus in Treating Patients With Breast Cancer
NCT01953588PHASE3ACTIVE_NOT_RECRUITINGFulvestrant and/or Anastrozole in Treating Postmenopausal Patients With Stage II-III Breast Cancer Undergoing Surgery
NCT02246621PHASE3ACTIVE_NOT_RECRUITINGA Study of Nonsteroidal Aromatase Inhibitors Plus Abemaciclib (LY2835219) in Postmenopausal Women With Breast Cancer
NCT02344472PHASE3ACTIVE_NOT_RECRUITINGDetect V / CHEVENDO (Chemo vs. Endo)
NCT02763566PHASE3ACTIVE_NOT_RECRUITINGA Study of Abemaciclib (LY2835219) in Participants With Breast Cancer
NCT02947685PHASE3ACTIVE_NOT_RECRUITINGRandomized, Open Label, Clinical Study of the Targeted Therapy, Palbociclib, to Treat Metastatic Breast Cancer
NCT04134598PHASE3ACTIVE_NOT_RECRUITINGExclUsive endocRine Therapy Or Radiation theraPy for Women Aged ≥70 Years Early Stage Breast Cancer
NCT04158362PHASE3ACTIVE_NOT_RECRUITINGEndocrine Therapy With Abemaciclib or Chemotherapy as Initial Metastatic Treatment in ER+/HER2- Breast Cancer
NCT04584853PHASE3ACTIVE_NOT_RECRUITINGPreOperative Endocrine Therapy for Individualised Care With Abemaciclib
NCT04711252PHASE3ACTIVE_NOT_RECRUITINGA 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
NCT04852887PHASE3RECRUITINGDe-Escalation of Breast Radiation Trial for Hormone Sensitive, HER-2 Negative, Oncotype Recurrence Score Less Than or Equal to 18 Breast Cancer (DEBRA)
NCT04906395PHASE3ACTIVE_NOT_RECRUITINGOvarian Suppression Evaluating Subcutaneous Leuprolide Acetate in Breast Cancer
NCT04964934PHASE3ACTIVE_NOT_RECRUITINGPhase III Study to Assess AZD9833+ CDK4/6 Inhibitor in HR+/HER2-MBC With Detectable ESR1m Before Progression (SERENA-6)
NCT05257395PHASE3ACTIVE_NOT_RECRUITINGA Study of XZP-3287 in Combination With Letrozole/Anastrozole in Patients With Advanced Breast Cancer
NCT05512364PHASE3RECRUITINGElacestrant for Treating ER+/HER2- Breast Cancer Patients With ctDNA Relapse (TREAT ctDNA)
NCT05514054PHASE3ACTIVE_NOT_RECRUITINGA Study of Imlunestrant Versus Standard Endocrine Therapy in Participants With Early Breast Cancer
NCT05586802PHASE3RECRUITINGSex Steroids Balance for Metabolic and Reproductive Health in Klinefelter Syndrome
NCT05645536PHASE3ENROLLING_BY_INVITATIONSafety Extension Study for Subjects With HR+, HER2- Breast Cancer for Subjects Who Have Completed the OVELIA Study
NCT05774951PHASE3RECRUITINGA Study of Camizestrant in ER+/HER2- Early Breast Cancer After at Least 2 Years of Standard Adjuvant Endocrine Therapy
NCT05780567PHASE3ACTIVE_NOT_RECRUITINGClinical Study on Adjuvant Therapy of TQB3616 Combined With Endocrine Therapy Compared With Placebo Combined With Endocrine Therapy in Patients With Breast Cancer
NCT05891093PHASE3RECRUITINGEfficacy and Safety of Fluzoparib Combined With Adjuvant Endocrine Therapy for HR+/HER2- SNF3-subtype Early Breast Cancer (BCTOP-L-A01)
NCT05952557PHASE3RECRUITINGAn Adjuvant Endocrine-based Therapy Study of Camizestrant (AZD9833) in ER+/HER2- Early Breast Cancer (CAMBRIA-2)
NCT06016738PHASE3RECRUITINGOP-1250 (Palazestrant) vs. Standard of Care for the Treatment of ER+/HER2- Advanced Breast Cancer

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 18 clinical and 121 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

40 molecules share ≥1 primary target. Top 40 by shared-target count:

MoleculeSourceStatusShared targets
AMINOGLUTETHIMIDEChEMBLPhase 4 (approved)CYP19A1
CLOTRIMAZOLEChEMBLPhase 4 (approved)CYP19A1
ESTRONEChEMBLPhase 4 (approved)CYP19A1
EXEMESTANEChEMBLPhase 4 (approved)CYP19A1
FLUCONAZOLEChEMBLPhase 4 (approved)CYP19A1
FLUOROURACILChEMBLPhase 4 (approved)CYP19A1
KETOCONAZOLEChEMBLPhase 4 (approved)CYP19A1
LETROZOLEChEMBLPhase 4 (approved)CYP19A1
MICONAZOLEChEMBLPhase 4 (approved)CYP19A1
NIMESULIDEChEMBLPhase 4 (approved)CYP19A1
OSILODROSTATChEMBLPhase 4 (approved)CYP19A1
POSACONAZOLEChEMBLPhase 4 (approved)CYP19A1
TESTOLACTONEChEMBLPhase 4 (approved)CYP19A1
TESTOSTERONEChEMBLPhase 4 (approved)CYP19A1
DOCONEXENTChEMBLPhase 3CYP19A1
ENDOXIFENChEMBLPhase 3CYP19A1
ICOSAPENTChEMBLPhase 3CYP19A1
QUERCETINChEMBLPhase 3CYP19A1
RESVERATROLChEMBLPhase 3CYP19A1
2-METHOXYESTRADIOLChEMBLPhase 2CYP19A1
AZALANSTATChEMBLPhase 2CYP19A1
DAIDZEINChEMBLPhase 2CYP19A1
DEXFADROSTATChEMBLPhase 2CYP19A1
DOCOSAPENTAENOIC ACIDChEMBLPhase 2CYP19A1
FADROZOLEChEMBLPhase 2CYP19A1
FLAVONEChEMBLPhase 2CYP19A1
FORMESTANEChEMBLPhase 2CYP19A1
GENISTEINChEMBLPhase 2CYP19A1
IROSUSTATChEMBLPhase 2CYP19A1
LIAROZOLEChEMBLPhase 2CYP19A1
LINOLEIC ACIDChEMBLPhase 2CYP19A1
LUTEOLINChEMBLPhase 2CYP19A1
OLEIC ACIDChEMBLPhase 2CYP19A1
PINOCEMBRINChEMBLPhase 2CYP19A1
PLOMESTANEChEMBLPhase 2CYP19A1
ROGLETIMIDEChEMBLPhase 2CYP19A1
STANOLONEChEMBLPhase 2CYP19A1
URSOLIC ACIDChEMBLPhase 2CYP19A1
VOROZOLEChEMBLPhase 2CYP19A1
FulvestrantPubChemApprovedCYP19A1

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot