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Letrozole

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Also known as CGS 20267CGS-20267FemaraLetrozolNSC-759652SID11112889SID124882709SID144213877SID144204270C0164571Letrazole

Summary

Letrozole (CHEMBL1444) is an approved small-molecule antineoplastic agent (ATC L02BG04) targeting CYP19A1; indicated across 51 conditions including breast carcinoma and breast neoplasm; with CIViC clinical evidence for 6 variant-indication associations (e.g. ERBB2 Amplification in breast cancer).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L02BG04
  • Targets: 1 (CYP19A1)
  • Indications: 51 conditions
  • Clinical trials: 562
  • Precision-oncology evidence (CIViC): 6 variant–indication associations
  • Chemistry: 285.3 Da · C17H11N5

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1444
NameLetrozole
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID3902
ChEBICHEBI:6413
ATCL02BG04
Molecular formulaC17H11N5
Molecular weight285.3
InChIKeyHPJKCIUCZWXJDR-UHFFFAOYSA-N

SMILES: C1=CC(=CC=C1C#N)C(C2=CC=C(C=C2)C#N)N3C=NC=N3

IUPAC name: 4-[(4-cyanophenyl)-(1,2,4-triazol-1-yl)methyl]benzonitrile

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

Also known as: CGS 20267, CGS-20267, Femara, Letrozol, Letrozole, NSC-759652, letrozole, SID11112889, LETROZOLE, SID124882709, SID144213877, SID144204270

Patent coverage: 19,893 distinct patent families (81,122 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
CYP19A1CYP19A1Inhibition7.90%P11511

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Cytochrome P450 11B1, mitochondrial, Thyrotropin receptor, Aromatase, Cytochrome P450 11B2, mitochondrial, Cytochrome P450 3A4, Cytochrome P450 2C19, Aromatase.

Bioactivity

ChEMBL activities: 57 potent at pChembl ≥ 5 of 59 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
CYP19A110.7Ki0.02nMCHEMBL_ACT_8060203
CYP19A19.15IC500.7nMCHEMBL_ACT_24742445
CYP19A19.15IC500.7nMCHEMBL_ACT_25000926
CYP19A19.05IC500.89nMCHEMBL_ACT_15742048
CYP19A19.05IC500.89nMCHEMBL_ACT_2574553
CYP19A19.05IC500.89nMCHEMBL_ACT_3124020
CYP19A19IC501nMCHEMBL_ACT_23277441
CYP19A19IC501nMCHEMBL_ACT_8055533
CYP19A18.96IC501.1nMCHEMBL_ACT_13965551
CYP19A18.74IC501.8nMCHEMBL_ACT_25477383
CYP19A18.74IC501.8nMCHEMBL_ACT_25885532
CYP19A18.72IC501.9nMCHEMBL_ACT_18364270
CYP19A18.72IC501.9nMCHEMBL_ACT_18899072
CYP19A18.72IC501.9nMCHEMBL_ACT_19075255
CYP19A18.7IC502nMCHEMBL_ACT_24713143
CYP19A18.7IC502nMCHEMBL_ACT_8060182
CYP19A18.66IC502.18nMCHEMBL_ACT_19480222
CYP19A18.66IC502.18nMCHEMBL_ACT_19480249
CYP19A18.66Ki2.2nMCHEMBL_ACT_2247869
CYP19A18.55IC502.8nMCHEMBL_ACT_13884359
CYP19A18.55IC502.8nMCHEMBL_ACT_24663728
CYP19A18.55IC502.8nMCHEMBL_ACT_25002591
CYP19A18.48IC503.3nMCHEMBL_ACT_15636415
CYP19A18.47IC503.4nMCHEMBL_ACT_13510532
CYP19A18.4IC504nMCHEMBL_ACT_16587929
CYP19A18.4IC504nMCHEMBL_ACT_24377186
CYP19A18.38IC504.2nMCHEMBL_ACT_6222867
CYP19A18.28IC505.3nMCHEMBL_ACT_15236575
CYP19A18.28IC505.3nMCHEMBL_ACT_16756993
CYP19A18.21IC506.1nMCHEMBL_ACT_2247780
CYP19A18.1IC508nMCHEMBL_ACT_25861477
CYP19A18.1IC508nMCHEMBL_ACT_6354694
CYP19A18IC509.9nMCHEMBL_ACT_12155937
CYP19A18IC509.95nMCHEMBL_ACT_18486410
CYP19A18IC5010nMCHEMBL_ACT_19201327
CYP19A18IC5010nMCHEMBL_ACT_20638467
CYP19A18IC5010nMCHEMBL_ACT_25056470
CYP19A17.94IC5011.5nMCHEMBL_ACT_2567491
CYP19A17.94IC5011.5nMCHEMBL_ACT_3290694
CYP19A17.78IC5016.53nMCHEMBL_ACT_12684597
CYP19A17.75IC5018nMCHEMBL_ACT_6219414
CYP19A17.58IC5026nMCHEMBL_ACT_24886567
CYP19A17.58IC5026nMCHEMBL_ACT_25905279
CYP19A17.44IC5036nMCHEMBL_ACT_12629296
CYP19A17.44IC5036.2nMCHEMBL_ACT_14531456
CYP19A17.3IC5049.5nMCHEMBL_ACT_18368644
CYP19A17.28IC5052.48nMCHEMBL_ACT_1845847
CYP19A16.55IC50279nMCHEMBL_ACT_25892891
P224436.54IC50290nMCHEMBL_ACT_29176242
CYP11B25.85IC501420nMCHEMBL_ACT_12629232
CYP11B15.58IC502620nMCHEMBL_ACT_12629264
CYP3A45.3Potency5012nMCHEMBL_ACT_5010152
CYP3A45.3Potency5012nMCHEMBL_ACT_5078523
CYP3A45.3AC505012nMCHEMBL_ACT_6049032
TSHR5.1Potency7943nMCHEMBL_ACT_3911916
CYP2C195.1Potency7943nMCHEMBL_ACT_4016309
CYP2C195.1AC507943nMCHEMBL_ACT_6052104

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

9 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

IndicationPhaseMONDOEFO
breast carcinoma4MONDO:0004989EFO:0000305
breast neoplasm4MONDO:0021100EFO:0003869
neoplasm4MONDO:0005070EFO:0000616
hereditary breast ovarian cancer syndrome3MONDO:0003582Orphanet:145
ductal breast carcinoma in situ3MONDO:0005023EFO:0000432
ovarian carcinoma3MONDO:0005140EFO:0001075
endometrial carcinoma3MONDO:0002447EFO:1001512
ovarian cancer3MONDO:0008170MONDO:0008170
endometrium neoplasm3MONDO:0021251MONDO:0011962

31 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)PhaseMONDOEFO
infertility disorder3MONDO:0005047EFO:0000545
polycystic ovary syndrome3MONDO:0008487EFO:0000660
spermatogenic failure3MONDO:0004983EFO:0000279
osteoporosis3MONDO:0005298EFO:0003882
hypogonadism3MONDO:0002146MONDO:0018555
ovarian hyperstimulation syndrome3MONDO:0011972MONDO:0011972
leiomyosarcoma2MONDO:0005058EFO:0000564
cervical adenocarcinoma2MONDO:0005153EFO:0001416
endometriosis2MONDO:0005133EFO:0001065
tumor of uterus2MONDO:0021353EFO:0003859
fallopian tube carcinoma2MONDO:0006206EFO:1000251
inflammatory breast carcinoma2MONDO:0006804EFO:1000984
carcinoma2MONDO:0004993EFO:0000313
breast lobular carcinoma2MONDO:0000552EFO:0008509
adenomyosis2MONDO:0010888EFO:1001757
peritoneal neoplasm2MONDO:0006901MONDO:0002087
fallopian tube neoplasm2MONDO:0021092MONDO:0002158
uterine cancer2MONDO:0002715MONDO:0002715
anovulation2MONDO:0002775MONDO:0002775
invasive lobular breast carcinoma2MONDO:0005051EFO:0000553
angiosarcoma2MONDO:0016982EFO:0003968
triple-negative breast carcinoma2MONDO:0005494EFO:0005537
lymphangioleiomyomatosis2MONDO:0011705MONDO:0011705
male infertility2MONDO:0005372EFO:0004248
Hermansky-Pudlak syndrome2MONDO:0019312MONDO:0019312
uterine corpus leiomyoma1MONDO:0007886EFO:0000731
mesothelioma1MONDO:0005065EFO:0000588
non-small cell lung carcinoma1MONDO:0005233EFO:0003060
non-Hodgkin lymphoma1MONDO:0018908EFO:0005952
endometrioid adenocarcinoma1MONDO:0005026EFO:0000466
ectopic pregnancy1MONDO:0000755HP:0031456

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

Clinical trials

Total trials: 562.

Phase distribution

PhaseTrials
PHASE2202
PHASE3117
Not specified81
PHASE150
PHASE449
PHASE1/PHASE228
PHASE2/PHASE321
EARLY_PHASE114

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05161195PHASE4ACTIVE_NOT_RECRUITINGRoll-over Study to Allow Continued Access to Ribociclib
NCT05183828PHASE4RECRUITINGEffect of HSD3B1 (1245C) Gene Mutation on Treatment of Stage I-III Breast Cancer
NCT05206448PHASE4ACTIVE_NOT_RECRUITINGRandomized Controlled Trial of Combined Letrozole and Clomid (CLC II) Versus Letrozole Alone for Women With Anovulation
NCT05341817PHASE4RECRUITINGThe Use of Letrozole or Mifepristone for Pretreatment of Medical Termination of Pregnancy
NCT06143631PHASE4RECRUITINGPrescription of Letrozole for Uterine Myoma
NCT06354439PHASE4RECRUITINGUse of Letrozole for Ectopic Pregnancy
NCT06985186PHASE4NOT_YET_RECRUITINGDoes The Addition Of Letrozole To Ultra-Long GnRH Agonists Help Adenomyosis Patients in ART? The AURA Trial
NCT07160855PHASE4RECRUITINGLetrozole Plus Misoprostol Versus Misoprostol Alone for Treating Women With Missed Miscarriage
NCT00014638PHASE4COMPLETEDLetrozole in Treating Postmenopausal Women With Metastatic Breast Cancer
NCT00171847PHASE4TERMINATEDStudy of the Efficacy and Safety of Letrozole Combined With Trastuzumab in Patients With Metastatic Breast Cancer
NCT00237133PHASE4COMPLETEDTreatment of Locally Advanced Breast Cancer With Letrozole in Postmenopausal Women
NCT00237224PHASE4COMPLETEDOpen Label Study of Postmenopausal Women With ER and /or PgR Positive Breast Cancer Treated With Letrozole
NCT00241046PHASE4TERMINATEDLetrozole in the Treatment of 1st and 2nd Line Hormone Receptor Positive Breast Cancer: Pre-therapeutic Risk Assessment
NCT00375752PHASE4TERMINATEDEfficacy and Safety of Letrozole vs. Letrozole Plus Zoledronic Acid as Endocrine Therapy Before Surgery in Postmenopausal Patients With Breast Cancer
NCT00478504PHASE4COMPLETEDLetrozole Versus Clomifene Citrate for Ovulation Induction
NCT00688909PHASE4COMPLETEDRheumatological Evaluation of Anastrozole and Letrozole as Adjuvant Treatment in Post-menopausal Women With Breast Cancer
NCT00804960PHASE4WITHDRAWNDoes Letrozole Improve the Outcomes and/or Reduce the Cost of IVF-ET Cycles?
NCT01035099PHASE4COMPLETEDRCT of Fixed vs Titrated Letrozole in Breast Cancer Patient Undergoing IVF
NCT01046578PHASE4COMPLETEDAromatase Inhibitor Effects on Ovarian Function During the Follicular and Early Luteal Phase in Women
NCT01072318PHASE4UNKNOWNExtended Adjuvant Treatment With Letrozole in Breast Cancer Who Complete 5 Years of Toremifene
NCT01127295PHASE4COMPLETEDPharmacology of Adjuvant Hormonotherapy in Breast Cancer
NCT01315912PHASE4COMPLETEDDosage Optimization for Letrozole Treatment
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
NCT01908556PHASE4UNKNOWNEvaluation of Predictive Factors Regarding the Effectivity of Aromatase Inhibitor Therapy (PreFace)
NCT01999569PHASE4COMPLETEDThe Role of Estrogen in Luteinizing Hormone Surge and Ovulation
NCT02097680PHASE4COMPLETEDInfluence of Aromatase Inhibition on Hepatic- and Cardiac Function in Severe Obese Men
NCT02137538PHASE4COMPLETEDAromatase Inhibitor Growth Study: Letrozole vs. Anastrozole
NCT02470741PHASE4COMPLETEDPilot of Letrozole for Uterine Myomas
NCT02661932PHASE4COMPLETEDFertility Preservation in Breast Cancer Patients
NCT02670304PHASE4COMPLETEDPreventive Application of Letrozole Decrease Incidence of Early Onset of OHSS
NCT02679755PHASE4COMPLETEDPalbociclib In Combination With Letrozole As Treatment Of Post-Menopausal Women With HR+, HER2- Advanced Breast Cancer
NCT02703649PHASE4COMPLETEDAdministration of Single High Dose Letrozole for Ovulation Induction
NCT02802865PHASE4COMPLETEDCombined Letrozole and Clomid in Women With Infertility and PCOS
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
NCT03901170PHASE4UNKNOWNDoes Letrozole Improve Pregnancy Outcome in Fresh Embryo Transfer IVF/ICSI Cycle?
NCT04002635PHASE4WITHDRAWNLetrozole for Frozen Embryo Transfer (FET) in Patients With Polycystic Ovary Syndrome (PCOS)
NCT04289805PHASE4TERMINATEDControlled Ovarian Stimulation in Newly Diagnosed Breast Cancer PatiEnts (fAMHOPE)
NCT04321551PHASE4WITHDRAWNHormone Secretion in Transgender Males
NCT04331197PHASE4UNKNOWNBMI Effect on the Response to Ovulation Induction in Letrozole vs Clomid
NCT04364581PHASE4UNKNOWNEndometrial Preparation by Short Course of Letrozole Before Hysteroscopic Removal of Endocavitary Lesions
NCT04590482PHASE4UNKNOWNLetrozole Pretreatment With Misoprostol Induction of Abortion in First Trimester Missed Abortion
NCT04834791PHASE4COMPLETEDLetrozole Versus Gonadotropins in Clomiphene Citrate Resistance
NCT05168865PHASE4WITHDRAWNLetrozole Versus Hormonal Preparation in Frozen Cycles of PCOS Patients.
NCT05198141PHASE4COMPLETEDEvaluation of Different Doses of Letrozole in Ectopic Pregnancy
NCT05205837PHASE4TERMINATEDA Randomized, Double-blinded, Clinical, Placebo-controlled Trial on the Effects of Therapy With Letrozole and hUman Choriongonadotropin in Male Hypogonadism Induced by Illicit Use of Anabolic Androgenic Steroids- The LUCAS Trial
NCT05809024PHASE4UNKNOWNSelect the Appropriate Population for Adding CDK4/6i to Neoadjuvant Endocrine Therapy
NCT06181305PHASE4UNKNOWNEndometrial Preparation in Frozen Embryo Transfer Cycles
NCT00310180PHASE3ACTIVE_NOT_RECRUITINGHormone Therapy With or Without Combination Chemotherapy in Treating Women Who Have Undergone Surgery for Node-Negative Breast Cancer (The TAILORx Trial)
NCT01064635PHASE3ACTIVE_NOT_RECRUITINGLetrozole in Treating Breast Cancer in Postmenopausal Women With Stage I, II, or III Breast Cancer Previously Treated With Tamoxifen (GIM4)
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
NCT02221999PHASE2/PHASE3ACTIVE_NOT_RECRUITINGWeekly Paclitaxel and Cisplatin to Treat Hormone Receptor Positive and Triple Negative Breast Cancer Patients
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
NCT03011684PHASE3RECRUITINGFertility Preservation Using Tamoxifen and Letrozole in Estrogen Sensitive Tumors Trial
NCT03458221PHASE2/PHASE3RECRUITINGSignal TrAnsduction Pathway Activity Analysis in OVarian cancER
NCT04095364PHASE3ACTIVE_NOT_RECRUITINGLetrozole With or Without Paclitaxel and Carboplatin in Treating Patients With Stage II-IV Ovarian, Fallopian Tube, or Primary Peritoneal Cancer
NCT04111978PHASE3RECRUITINGMAintenance Therapy With Aromatase Inhibitor in Epithelial Ovarian Cancer (MATAO)
NCT04158362PHASE3ACTIVE_NOT_RECRUITINGEndocrine Therapy With Abemaciclib or Chemotherapy as Initial Metastatic Treatment in ER+/HER2- Breast Cancer
NCT04546009PHASE3ACTIVE_NOT_RECRUITINGA Study Evaluating the Efficacy and Safety of Giredestrant Combined With Palbociclib Compared With Letrozole Combined With Palbociclib in Participants With Estrogen Receptor-Positive, HER2-Negative Locally Advanced or Metastatic Breast Cancer (persevERA Breast Cancer)
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)
NCT05316935PHASE2/PHASE3RECRUITINGGnRHa + Letrozole in Non-obese Progestin-insensitive Endometrial Cancer and Atypical Hyperplasia Patients
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
NCT05601700PHASE3RECRUITINGLetrozole for Estrogen/Progesterone Receptor Positive Low-grade Serous Epithelial Ovarian Cancer (LEPRE Trial)
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
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)
NCT05909397PHASE3ACTIVE_NOT_RECRUITINGVepdegestrant (ARV-471/PF-07850327) + Palbociclib vs Letrozole + Palbociclib in ER(+)/HER2(-) Advanced Breast Cancer
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
NCT06072781PHASE3RECRUITINGA Study of Avutometinib (VS-6766) + Defactinib (VS-6063) in Recurrent Low-Grade Serous Ovarian Cancer
NCT06223698PHASE3NOT_YET_RECRUITINGOptimizing Extended Adjuvant Endocrine Therapy in Patients With Breast Cancer
NCT06244745PHASE3RECRUITINGEffects of Letrozole During the Luteal Phase After Controlled Ovarian Stimulation in Oocyte Donors.
NCT06379113PHASE2/PHASE3RECRUITINGGnRHa + Letrozole in Obese Progestin-insensitive Endometrial Cancer Patients
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
NCT06390904PHASE2/PHASE3ACTIVE_NOT_RECRUITINGGnRHa + Letrozole in Obese Progestin-insensitive Endometrial Atypical Hyperplasia Patients
NCT06405178PHASE3NOT_YET_RECRUITINGAdjuvant Therapy With Letrozole in Induction of Ovulation With Polycystic Ovarian Syndrome
NCT06405243PHASE3NOT_YET_RECRUITINGMyoinositol, L-arginine and Chromium With Letrozole for Ovulation Induction in Polycystic Ovarian Syndrome Patients
NCT06492616PHASE3RECRUITINGA Study of Elacestrant Versus Standard Endocrine Therapy in Women and Men With ER+,HER2-, Early Breast Cancer With High Risk of Recurrence
NCT06507618PHASE3RECRUITINGPre-Operative Window of ET to Inform RT Decisions (POWER II)
NCT06757634PHASE3RECRUITINGPhase 3 Study of Gedatolisib as First-Line Treatment for Patients With HR-Positive, HER2-Negative Advanced Breast Cancer (VIKTORIA-2)
NCT06760637PHASE3ACTIVE_NOT_RECRUITINGStudy of PF-07220060 With Letrozole in Adults With HR-positive HER2-negative Breast Cancer Who Have Not Received Anticancer Treatment for Advanced/Metastatic Disease
NCT06790693PHASE3RECRUITINGA Study Evaluating the Efficacy and Safety of Inavolisib Plus CDK4/6 Inhibitor and Letrozole vs Placebo + CDK4/6i and Letrozole in Participants With Endocrine-Sensitive PIK3CA-Mutated, Hormone Receptor-Positive, HER2-Negative Advanced Breast Cancer
NCT07019363PHASE3RECRUITINGCDK4/6 Inhibitors Combined With Standard Adjuvant Endocrine Therapy in High-Risk, HR+/HER2+ Early Breast Cancer Patients(CHESS)
NCT07024173PHASE3RECRUITINGA Phase 3 Study of HRS-8080 Versus Treatment Chosen by Physicians in Locally Advanced and Metastatic Breast Cancer
NCT07085767PHASE3RECRUITINGPalazestrant in Combination With Ribociclib for the First-line Treatment of ER+/HER2- Advanced Breast Cancer
NCT07174336PHASE3RECRUITINGA Study of Tersolisib (LY4064809/STX-478) With Other Anti-Cancer Treatments in Participants With Advanced Breast Cancer With a Genetic Change (PIK3CA)
NCT07319429PHASE2/PHASE3RECRUITINGRefining Fertility-sparing Treatment in Endometrial Carcinoma Based on Molecular Classification
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
NCT07492641PHASE3RECRUITINGBGB-43395 Plus Letrozole Versus CDK4/6i Plus Letrozole for Patients With Advanced or Metastatic HR+/HER2- Breast Cancer Who Have Not Received Prior Treatment for Advanced or Metastatic Disease

Clinical evidence (CIViC)

Variant × indication × effect (6 predictive associations from 6 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
ERBB2 AmplificationBreast CancerSensitivity/ResponseLapatinib + LetrozoleCIViC AEID11248
ESR1 OverexpressionBreast CancerSensitivity/ResponsePalbociclib + LetrozoleCIViC BEID1541
FGFR1 Amplification AND ZNF703 AmplificationBreast CancerResistanceRibociclib + LetrozoleCIViC BEID12531
CDKN2A LossHer2-receptor Negative Breast CancerSensitivity/ResponseLetrozole + PalbociclibCIViC CEID1765
ESR1 D538GBreast CancerSensitivity/ResponseLetrozole + PalbociclibCIViC CEID4814
PIK3CA P447_L455delEstrogen-receptor Positive Breast CancerSensitivity/ResponseLetrozole + AlpelisibCIViC CEID9575

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 19 clinical and 86 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
EXEMESTANEChEMBLPhase 4 (approved)CYP19A1
FLUCONAZOLEChEMBLPhase 4 (approved)CYP19A1
FLUOROURACILChEMBLPhase 4 (approved)CYP19A1
KETOCONAZOLEChEMBLPhase 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
v1.1.4
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