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Exemestane

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Also known as AromasinExemestanoFCE-24304FCE24304NSC-758907PNU-155971SID26719821SID49681613SID144205052SID170464628C0164716

Summary

Exemestane (CHEMBL1200374) is an approved small-molecule EC 1.14.14.14 (aromatase) inhibitor (ATC L02BG06) targeting CYP19A1; indicated across 17 conditions including breast carcinoma and neoplasm; with CIViC clinical evidence for 4 variant-indication associations (e.g. ESR2 underexpression beta-1 in breast cancer).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L02BG06
  • Targets: 1 (CYP19A1)
  • Indications: 17 conditions
  • Clinical trials: 237
  • Precision-oncology evidence (CIViC): 4 variant–indication associations
  • Chemistry: 296.4 Da · C20H24O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1200374
NameExemestane
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID60198
ChEBICHEBI:4953
ATCL02BG06
Molecular formulaC20H24O2
Molecular weight296.4
InChIKeyBFYIZQONLCFLEV-DAELLWKTSA-N

SMILES: C[C@]12CC[C@H]3[C@H]([C@@H]1CCC2=O)CC(=C)C4=CC(=O)C=C[C@]34C

IUPAC name: (8R,9S,10R,13S,14S)-10,13-dimethyl-6-methylidene-7,8,9,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-3,17-dione

ChEBI definition: A 17-oxo steroid that is androsta-1,4-diene-3,17-dione in which the hydrogens at position 6 are replaced by a double bond to a methylene group. A selective inhibitor of the aromatase (oestrogen synthase) system, it is used in the treatment of advanced breast cancer.

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

Other ChEBI roles (chemical / environmental): environmental contaminant, xenobiotic.

Also known as: Aromasin, Exemestane, Exemestano, FCE-24304, FCE24304, NSC-758907, PNU-155971, SID26719821, SID49681613, EXEMESTANE, exemestane, SID144205052

Patent coverage: 17,299 distinct patent families (72,530 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
CYP19A1CYP19A1Inhibition7.60%P11511

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Aromatase, Glucocorticoid receptor, Progesterone receptor, 5-hydroxytryptamine receptor 2A, Kappa-type opioid receptor, Androgen receptor, Aromatase, Bile salt export pump.

Bioactivity

ChEMBL activities: 19 potent at pChembl ≥ 5 of 22 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
CYP19A19.02Ki0.95nMCHEMBL_ACT_25029270
CYP19A17.99Ki10.2nMCHEMBL_ACT_16432268
CYP19A17.82IC5015nMCHEMBL_ACT_24713144
CYP19A17.64IC5023nMCHEMBL_ACT_23277440
CYP19A17.58Ki26nMCHEMBL_ACT_16432267
CYP19A17.58Ki26nMCHEMBL_ACT_19204487
CYP19A17.58Ki26nMCHEMBL_ACT_19269806
P224437.52IC5030nMCHEMBL_ACT_29176244
CYP19A17.37IC5042.5nMCHEMBL_ACT_18102381
CYP19A17.3IC5050.1nMCHEMBL_ACT_12155939
CYP19A17.3IC5050nMCHEMBL_ACT_15190295
CYP19A17.3IC5050.1nMCHEMBL_ACT_24742461
CYP19A16.64IC50230nMCHEMBL_ACT_16432446
CYP19A16.05IC50900nMCHEMBL_ACT_15190285
CYP19A15.73IC501850nMCHEMBL_ACT_29176246
OPRK15.62AC502406nMCHEMBL_ACT_25128994
P152075.3AC505040nMCHEMBL_ACT_25187178
NR3C15.17AC506760nMCHEMBL_ACT_25175422
HTR2A5.16AC506963nMCHEMBL_ACT_25173450

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

17 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
neoplasm4MONDO:0005070EFO:0000616
breast neoplasm4MONDO:0021100EFO:0003869
male breast carcinoma3MONDO:0005628EFO:0006861
ductal breast carcinoma in situ3MONDO:0005023EFO:0000432
ovarian cancer3MONDO:0008170MONDO:0008170
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
breast carcinoma in situ2MONDO:0004658MONDO:0004658
endometrium neoplasm2MONDO:0021251MONDO:0011962
atypical endometrial hyperplasia2MONDO:0006096EFO:1000098
triple-negative breast carcinoma2MONDO:0005494EFO:0005537
granulosa cell tumor2MONDO:0006036MONDO:0020541
lymphoma1MONDO:0005062EFO:0000574
lung neoplasm1MONDO:0021117MONDO:0008903

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

Clinical trials

Total trials: 237.

Phase distribution

PhaseTrials
PHASE299
PHASE366
Not specified27
PHASE123
PHASE1/PHASE211
PHASE49
PHASE2/PHASE32

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00649090PHASE4COMPLETEDA Study to Evaluate the Safety of Adjuvant Treatment With Exemestane Following Previous Treatment With Tamoxifen in Postmenopausal Women With Estrogen Sensitive Primary Breast Cancer
NCT01176916PHASE4COMPLETEDAromasin® Interventional Study Of Early Invasive Breast Cancer Patients In China
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
NCT01743560PHASE4COMPLETEDAn Open Label Study of Postmenopausal Women With Oestrogen Receptor Positive Locally Advanced or Metastatic Breast Cancer Treated With Everolimus (RAD001) With Exemestane, With Exploratory Epigenetic Marker Analysis
NCT02248571PHASE4COMPLETEDPatient Preference for Everolimus in Combination With Exemestane or Capecitabine in Combination With Bevacizumab
NCT02467686PHASE4UNKNOWNBreast Cancer, Sexuality and Black Cohosh
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
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
NCT02115282PHASE3ACTIVE_NOT_RECRUITINGExemestane With or Without Entinostat in Treating Patients With Recurrent Hormone Receptor-Positive Breast Cancer That is Locally Advanced or Metastatic
NCT02344472PHASE3ACTIVE_NOT_RECRUITINGDetect V / CHEVENDO (Chemo vs. Endo)
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
NCT04906395PHASE3ACTIVE_NOT_RECRUITINGOvarian Suppression Evaluating Subcutaneous Leuprolide Acetate in Breast Cancer
NCT04975308PHASE3ACTIVE_NOT_RECRUITINGA Study of Imlunestrant, Investigator’s Choice of Endocrine Therapy, and Imlunestrant Plus Abemaciclib in Participants With ER+, HER2- Advanced Breast Cancer
NCT05306340PHASE3ACTIVE_NOT_RECRUITINGA Study Evaluating the Efficacy and Safety of Giredestrant Plus Everolimus Compared With the Physician’s Choice of Endocrine Therapy Plus Everolimus in Participants With Estrogen Receptor-Positive, HER2-Negative, Locally Advanced or Metastatic Breast Cancer (evERA 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
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
NCT05827081PHASE3RECRUITINGPhase IIIb Study of Ribociclib + ET in Early 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
NCT06223698PHASE3NOT_YET_RECRUITINGOptimizing Extended Adjuvant Endocrine Therapy in Patients With Breast Cancer
NCT06380751PHASE3RECRUITINGSaruparib (AZD5305) Plus Camizestrant Compared With CDK4/6 Inhibitor Plus Endocrine Therapy or Plus Camizestrant in HR-Positive, HER2-Negative (IHC 0, 1+, 2+/ ISH Non-amplified), BRCA1, BRCA2, or PALB2m Advanced Breast Cancer
NCT06492616PHASE3RECRUITINGA Study of Elacestrant Versus Standard Endocrine Therapy in Women and Men With ER+,HER2-, Early Breast Cancer With High Risk of Recurrence
NCT06680921PHASE3RECRUITINGA Study of SIM0270 Combined With Everolimus vs. Treatment of Physician’s Choice in Patients With ER+/HER2- Advanced Breast Cancer (SIMRISE)
NCT07024173PHASE3RECRUITINGA Phase 3 Study of HRS-8080 Versus Treatment Chosen by Physicians in Locally Advanced and Metastatic Breast Cancer
NCT07062965PHASE3RECRUITINGA Study to Learn About the Study Medicine Called PF-07248144 in Combination With Fulvestrant in People With HR-positive, HER2-negative Advanced or Metastatic Breast Cancer Who Progressed After a Prior Line of Treatment.
NCT07174336PHASE3RECRUITINGA Study of Tersolisib (LY4064809/STX-478) With Other Anti-Cancer Treatments in Participants With Advanced Breast Cancer With a Genetic Change (PIK3CA)
NCT07190443PHASE3RECRUITINGAdjuvant Abemaciclib for Locoregional Recurrence of HR-positive, HER2-negative Breast Cancer (JCOG2313, AURA)
NCT07349069PHASE3RECRUITINGA Phase III Trial Comparing HRS-8080 With Standard Endocrine Therapy in Patients With Intermediate or High Risk Early Breast Cancer
NCT07391774PHASE3NOT_YET_RECRUITINGTesting Whether Hormone Therapy With Ribociclib is as Effective as Chemotherapy Followed by Hormone Therapy With Ribociclib for the Treatment of High Anatomic Stage Breast Cancer With Low Recurrence Risk, The RxFINE-Low Trial
NCT00002777PHASE3COMPLETEDExemestane Compared With Tamoxifen in Treating Women With Locally Recurrent or Metastatic Breast Cancer
NCT00003418PHASE3UNKNOWNExemestane Compared With Tamoxifen in Treating Postmenopausal Women With Primary Breast Cancer
NCT00016432PHASE3COMPLETEDExemestane in Treating Postmenopausal Women With Resected Stage I, Stage II, or Stage IIIA Breast Cancer Who Have Completed 5 Years of Tamoxifen

Clinical evidence (CIViC)

Variant × indication × effect (4 predictive associations from 4 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
ESR2 underexpression beta-1Breast CancerSensitivity/ResponseExemestane + TamoxifenCIViC BEID9612
IGF1R OverexpressionBreast CancerSensitivity/ResponseExemestane + MetforminCIViC BEID10138
PGR ExpressionBreast CancerSensitivity/ResponseExemestane + TamoxifenCIViC BEID502
STK11 F354LBreast CancerSensitivity/ResponseEverolimus + ExemestaneCIViC BEID5568

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 13 clinical and 63 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
ANASTROZOLEChEMBLPhase 4 (approved)CYP19A1
CLOTRIMAZOLEChEMBLPhase 4 (approved)CYP19A1
ESTRONEChEMBLPhase 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