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Fulvestrant

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Also known as FaslodexFulvestrant mylanICI 182,780ICI-182780NSC-759879ZD-9238ZD9238FluvestrantSID90341164SID29215034SID144204490SID170464917SID144213958SID144209802

Summary

Fulvestrant (CHEMBL1358) is an approved small-molecule antineoplastic agent (ATC L02BA03) targeting GPER1, ESR1, and ESR2; indicated across 35 conditions including breast carcinoma and breast neoplasm; with CIViC clinical evidence for 56 variant-indication associations (e.g. AKT1 E17K in her2-receptor negative breast cancer).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L02BA03
  • Targets: 3 (GPER1, ESR1, ESR2)
  • Indications: 35 conditions
  • Clinical trials: 427
  • Precision-oncology evidence (CIViC): 56 variant–indication associations
  • Chemistry: 606.8 Da · C32H47F5O3S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1358
NameFulvestrant
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID104741
ChEBICHEBI:31638
ATCL02BA03
Molecular formulaC32H47F5O3S
Molecular weight606.8
InChIKeyVWUXBMIQPBEWFH-WCCTWKNTSA-N

SMILES: C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2O)[C@@H](CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F

IUPAC name: (7R,8R,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol

ChEBI definition: A 3-hydroxy steroid that is 17β-estradiol in which the 7α hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer.

Pharmacological roles (ChEBI): antineoplastic agent, estrogen receptor antagonist, estrogen antagonist.

Also known as: Faslodex, Fulvestrant, Fulvestrant mylan, ICI 182,780, ICI-182780, NSC-759879, ZD-9238, ZD9238, fulvestrant, Fluvestrant, SID90341164, FULVESTRANT

Patent coverage: 13,857 distinct patent families (56,655 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 56,372 (100%) of the total. 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
GPER1GPERFull agonist70.2%Q99527
ESR1Estrogen receptor-αAntagonist8.981.7%P03372
ESR2Estrogen receptor-βAntagonist8.860.2%Q92731

Broader ChEMBL bioactivity targets: 13 (assay-derived). Sample: Glucocorticoid receptor, Bile acid receptor, Estrogen receptor, Progesterone receptor, Estrogen receptor, NAD-dependent protein deacylase sirtuin-5, mitochondrial, Peroxisome proliferator-activated receptor gamma, Beta-lactamase TEM, Bifunctional epoxide hydrolase 2, Estrogen receptor beta.

Bioactivity

ChEMBL activities: 79 potent at pChembl ≥ 5 of 81 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
ESR110.22IC500.06nMCHEMBL_ACT_18049258
ESR110.2IC500.06nMCHEMBL_ACT_15740553
ESR19.7EC500.2nMCHEMBL_ACT_25568142
ESR19.68IC500.21nMCHEMBL_ACT_1449889
PGR9.68IC500.21nMCHEMBL_ACT_15740517
ESR19.6IC500.25nMCHEMBL_ACT_23232648
ESR19.52IC500.3nMCHEMBL_ACT_18063454
ESR29.52IC500.3nMCHEMBL_ACT_24910974
ESR19.49IC500.32nMCHEMBL_ACT_20665411
ESR19.4EC500.4nMCHEMBL_ACT_15616081
ESR19.4EC500.4nMCHEMBL_ACT_18954324
ESR19.38EC500.42nMCHEMBL_ACT_25477469
ESR19.33IC500.47nMCHEMBL_ACT_281424
ESR19.3IC500.5nMCHEMBL_ACT_25568138
ESR19.24IC500.57nMCHEMBL_ACT_27458015
ESR19.22Ki0.6nMCHEMBL_ACT_25920318
ESR19.18Ki0.67nMCHEMBL_ACT_1280519
ESR29.18EC500.67nMCHEMBL_ACT_25477483
ESR19.12Ki0.76nMCHEMBL_ACT_1280517
ESR19.11IC500.78nMCHEMBL_ACT_19211884
ESR19.09IC500.81nMCHEMBL_ACT_15740572
ESR19.08IC500.84nMCHEMBL_ACT_20665472
ESR29.05IC500.9nMCHEMBL_ACT_25568140
ESR19IC501nMCHEMBL_ACT_18049117
ESR19IC501nMCHEMBL_ACT_24910941
ESR18.98Ki1.04nMCHEMBL_ACT_1152801
ESR18.92IC501.2nMCHEMBL_ACT_18049295
ESR18.92IC501.2nMCHEMBL_ACT_18113395
ESR28.86Ki1.39nMCHEMBL_ACT_1152802
ESR18.85EC501.4nMCHEMBL_ACT_19211891

Target pathways

Aggregated over 3 target gene(s): GPER1, ESR1, ESR2.

Top Reactome pathways

20 total, by targets touching each:

PathwayTargetsGenes
PIP3 activates AKT signaling2ESR1, ESR2
Constitutive Signaling by Aberrant PI3K in Cancer2ESR1, ESR2
Nuclear Receptor transcription pathway2ESR1, ESR2
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling2ESR1, ESR2
ESR-mediated signaling2ESR1, ESR2
Extra-nuclear estrogen signaling2ESR1, ESR2
Nuclear signaling by ERBB41ESR1
Peptide ligand-binding receptors1GPER1
SUMOylation of intracellular receptors1ESR1
G alpha (i) signalling events1GPER1
Ovarian tumor domain proteases1ESR1
TFAP2 (AP-2) family regulates transcription of growth factors and their receptors1ESR1
RUNX1 regulates estrogen receptor mediated transcription1ESR1
RUNX1 regulates transcription of genes involved in WNT signaling1ESR1
Regulation of RUNX2 expression and activity1ESR1
Estrogen-dependent gene expression1ESR1
GPER1 signaling1GPER1
Mitochondrial unfolded protein response (UPRmt)1ESR1
Developmental Lineage of Mammary Gland Luminal Epithelial Cells1ESR1
Developmental Lineage of Mammary Gland Alveolar Cells1ESR1

Dominant GO biological processes

GO termTargets
positive regulation of transcription by RNA polymerase II3
cellular response to estradiol stimulus3
signal transduction3
positive regulation of cytosolic calcium ion concentration2
negative regulation of gene expression2
nuclear receptor-mediated steroid hormone signaling pathway2
steroid hormone receptor signaling pathway2
negative regulation of transcription by RNA polymerase II2
regulation of DNA-templated transcription2
regulation of transcription by RNA polymerase II2
estrogen receptor signaling pathway2
positive regulation of DNA-templated transcription2
obsolete positive regulation of DNA-binding transcription factor activity2
cellular response to oxygen-containing compound2
positive regulation of protein phosphorylation1

Indications & clinical

Indications

35 indications (6 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
HER2 positive breast carcinoma4MONDO:0006244EFO:1000294
invasive lobular breast carcinoma3MONDO:0005051EFO:0000553
prostate adenocarcinoma2MONDO:0005082EFO:0000673
pulmonary arterial hypertension2MONDO:0015924EFO:0001361
carcinoma2MONDO:0004993EFO:0000313
ductal breast carcinoma in situ2MONDO:0005023EFO:0000432
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
endometrial carcinoma2MONDO:0002447EFO:1001512
female reproductive organ cancer2MONDO:0001416EFO:1001331
endometrioid stromal sarcoma2MONDO:0006745EFO:1000919
ovarian cancer2MONDO:0008170MONDO:0008170
lung neoplasm2MONDO:0021117MONDO:0008903
precocious puberty2MONDO:0000088MONDO:0000088
endometrium neoplasm2MONDO:0021251MONDO:0011962
polyostotic fibrous dysplasia2MONDO:0008274MONDO:0018919
ovarian carcinoma2MONDO:0005140EFO:0001075
uterine corpus cancer2MONDO:0006003EFO:0007532
systemic lupus erythematosus2MONDO:0007915MONDO:0007915
head and neck squamous cell carcinoma1MONDO:0010150EFO:0000181
lymphoma1MONDO:0005062EFO:0000574
mesothelioma1MONDO:0005065EFO:0000588
non-Hodgkin lymphoma1MONDO:0018908EFO:0005952
urothelial carcinoma1MONDO:0040679EFO:0008528
hereditary breast ovarian cancer syndrome1MONDO:0003582Orphanet:145
breast ductal adenocarcinoma1MONDO:0005590EFO:0006318
small cell lung carcinoma1MONDO:0008433EFO:0000702
exocrine pancreatic carcinoma1MONDO:0005192EFO:0002618
colorectal neoplasm1MONDO:0005335MONDO:0005575

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

Clinical trials

Total trials: 427.

Phase distribution

PhaseTrials
PHASE2189
PHASE184
PHASE371
PHASE1/PHASE250
Not specified18
PHASE49
PHASE2/PHASE34
EARLY_PHASE12

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05161195PHASE4ACTIVE_NOT_RECRUITINGRoll-over Study to Allow Continued Access to Ribociclib
NCT05362760PHASE4RECRUITINGCombination of Abemaciclib and Endocrine Therapy in Hormone Receptor Positive HER2 Negative Locally Advanced or Metastatic Breast Cancer With Focus on Digital Side Effect Management
NCT02447328PHASE4COMPLETEDA Single Arm, Tolerability and Safety Phase IV Study of Fulvestrant(Faslodex® ) as 2nd Line and Later Therapy in Postmenopausal Women With Locally Advanced or Metastatic Breast Cancer
NCT03220178PHASE4TERMINATEDImpact of eHealth-support on Quality of Life in Metastatic Breast Cancer Patients Treated With Palbociclib and Endocrine Therapy
NCT03591549PHASE4UNKNOWNFulvestrant in Metastatic Breast Cancer
NCT04031885PHASE4TERMINATEDA Study of Abemaciclib (LY2835219) in Combination With Fulvestrant Compared to Chemotherapy in Women With HR Positive, HER2 Negative Metastatic Breast Cancer
NCT04707196PHASE4COMPLETEDA Study of Abemaciclib in Indian Women With Advanced Breast Cancer
NCT05191914PHASE4UNKNOWNClinical Study of Fulvestrant Combined With Chidamide in the Treatment of Hormone Receptor-positive Advanced Breast Cancer Resistant to CDK4/6 Inhibitors
NCT05631795PHASE4COMPLETEDStudy to Assess the Safety of Alpelisib Plus Fulvestrant, in Men and Post-menopausal Women With HR-positive, HER2-negative, Advanced Breast Cancer (aBC) With PIK3CA Mutation, Whose Disease Progressed on or After Endocrine Treatment
NCT00099437PHASE3ACTIVE_NOT_RECRUITINGComparison of Fulvestrant (FASLODEX™) 250 mg and 500 mg in Postmenopausal Women With Oestrogen Receptor Positive Advanced Breast Cancer Progressing or Relapsing After Previous Endocrine Therapy.
NCT01953588PHASE3ACTIVE_NOT_RECRUITINGFulvestrant and/or Anastrozole in Treating Postmenopausal Patients With Stage II-III Breast Cancer Undergoing Surgery
NCT02107703PHASE3ACTIVE_NOT_RECRUITINGA Study of Abemaciclib (LY2835219) Combined With Fulvestrant in Women With Hormone Receptor Positive HER2 Negative 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
NCT03425838PHASE3ACTIVE_NOT_RECRUITINGEndocrine Therapy Plus CDK4/6 in First or Second Line for Hormone (SONIA) Receptor Positive Advanced Breast Cancer
NCT04191499PHASE2/PHASE3ACTIVE_NOT_RECRUITINGA Study Evaluating the Efficacy and Safety of Inavolisib + Palbociclib + Fulvestrant vs Placebo + Palbociclib + Fulvestrant in Participants With PIK3CA-Mutant, Hormone Receptor-Positive, HER2-Negative, Locally Advanced or Metastatic Breast Cancer
NCT04263298PHASE3RECRUITINGFulvestrant Versus Capecitabine as Maintenance Therapy After First-line Chemotherapy in Patients With HR+/HER2- Metastatic Breast Cancer
NCT04305496PHASE3ACTIVE_NOT_RECRUITINGCapivasertib+Fulvestrant vs Placebo+Fulvestrant as Treatment for Locally Advanced (Inoperable) or Metastatic HR+/HER2- Breast Cancer
NCT04650581PHASE3ACTIVE_NOT_RECRUITINGFulvestrant and Ipatasertib for Advanced HER-2 Negative and Estrogen Receptor Positive (ER+) Breast Cancer Following Progression on First Line CDK 4/6 Inhibitor and Aromatase Inhibitor
NCT04862663PHASE3RECRUITINGCapivasertib + CDK4/6i + Fulvestrant for Advanced/Metastatic HR+/HER2- Breast Cancer (CAPItello-292)
NCT04975308PHASE3ACTIVE_NOT_RECRUITINGA Study of Imlunestrant, Investigator’s Choice of Endocrine Therapy, and Imlunestrant Plus Abemaciclib in Participants With ER+, HER2- Advanced Breast Cancer
NCT05038735PHASE3ACTIVE_NOT_RECRUITINGStudy to Assess the Efficacy and Safety of Alpelisib Plus Fulvestrant in Participants With HR-positive (HR+), HER2-negative, Advanced Breast Cancer After Treatment With a CDK4/6 Inhibitor and an Aromatase Inhibitor.
NCT05063786PHASE3ACTIVE_NOT_RECRUITINGTrastuzumab + Alpelisib +/- Fulvestrant vs Trastuzumab + CT in Patients With PIK3CA Mutated Previously Treated HER2+ Advanced BrEasT Cancer (ALPHABET)
NCT05077449PHASE3ACTIVE_NOT_RECRUITINGA Study of XZP-3287 in Combination With Fulvestrant in Patients With Advanced Breast Cancer
NCT05169567PHASE3ACTIVE_NOT_RECRUITINGAbemaciclib (LY2835219) Plus Fulvestrant Compared to Placebo Plus Fulvestrant in Previously Treated 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)
NCT05365178PHASE3ACTIVE_NOT_RECRUITINGTo Evaluate the Efficacy and Safety of TQB3616 in Combination With Fulvestrant Versus Placebo in Combination With Fulvestrant in Previously Untreated Hormone-receptor (HR)-Positive, Human Epidermal Growth Factor Receptor 2 (HER2)-Negative Advanced Breast Cancer
NCT05501886PHASE3ACTIVE_NOT_RECRUITINGGedatolisib Plus Fulvestrant With or Without Palbociclib vs Standard-of-Care for the Treatment of Patients With Advanced or Metastatic HR+/HER2- Breast Cancer (VIKTORIA-1)
NCT05646862PHASE3ACTIVE_NOT_RECRUITINGA Study Evaluating the Efficacy and Safety of Inavolisib Plus Fulvestrant Compared With Alpelisib Plus Fulvestrant in Participants With HR-Positive, HER2-Negative, PIK3CA Mutated, Locally Advanced or Metastatic Breast Cancer Post CDK4/6i and Endocrine Combination Therapy
NCT05654623PHASE3ACTIVE_NOT_RECRUITINGA Study to Learn About a New Medicine Called Vepdegestrant (ARV-471, PF-07850327) in People Who Have Advanced Metastatic Breast Cancer
NCT06016738PHASE3RECRUITINGOP-1250 (Palazestrant) vs. Standard of Care for the Treatment of ER+/HER2- Advanced Breast Cancer
NCT06065748PHASE3RECRUITINGA Study to Evaluate Efficacy and Safety of Giredestrant Compared With Fulvestrant (Plus a CDK4/6 Inhibitor), in Participants With ER-Positive, HER2-Negative Advanced Breast Cancer Resistant to Adjuvant Endocrine Therapy (pionERA 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
NCT06447623PHASE3RECRUITINGApatinib Combined With cdk4/6i in First-line Treatment for HR+/HER2- SNF4 Subtype Breast Cancer
NCT06506955PHASE2/PHASE3ENROLLING_BY_INVITATIONFutibatinib in Patients Previously Enrolled in an Antecedent Futibatinib as Monotherapy or Combination Therapy.
NCT06635447PHASE3ACTIVE_NOT_RECRUITINGCapivasertib+Fulvestrant asTreatment for Locally Advanced(Inoperable) or Metastatic HR+/HER2- Breast Cancer in Chinese Patients
NCT06680921PHASE3RECRUITINGA Study of SIM0270 Combined With Everolimus vs. Treatment of Physician’s Choice in Patients With ER+/HER2- Advanced Breast Cancer (SIMRISE)
NCT06757634PHASE3RECRUITINGPhase 3 Study of Gedatolisib as First-Line Treatment for Patients With HR-Positive, HER2-Negative Advanced Breast Cancer (VIKTORIA-2)
NCT06764186PHASE3ACTIVE_NOT_RECRUITINGA Phase IIIB Study to Evaluate the Use of Capivasertib in Combination With Fulvestrant in Patients With Advanced Breast Cancer Who Have Relapsed/Progressed on ET and CDK4/6 Inhibitor Reflecting Real World Clinical Practice in Spain

Clinical evidence (CIViC)

Variant × indication × effect (56 predictive associations from 56 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
AKT1 E17KHer2-receptor Negative Breast CancerSensitivity/ResponseCapivasertib + FulvestrantCIViC AEID12181
ESR1 MutationBreast CarcinomaSensitivity/ResponseAromatase Inhibitor + Fulvestrant + Imlunestrant RegimenCIViC AEID12600
PIK3CA C420RBreast CancerSensitivity/ResponseAlpelisib + FulvestrantCIViC AEID11275
PIK3CA C420RHer2-receptor Negative Breast CancerSensitivity/ResponseCapivasertib + FulvestrantCIViC AEID12183
PIK3CA E453K OR PIK3CA E453Q OR PIK3CA E453A OR PIK3CA E453D OR PIK3CA E453G OR PIK3CA E453VBreast CancerSensitivity/ResponseFulvestrant + Inavolisib + PalbociclibCIViC AEID12540
PIK3CA E542KHer2-receptor Negative Breast CancerSensitivity/ResponseFulvestrant + CapivasertibCIViC AEID12184
PIK3CA E542KBreast CancerSensitivity/ResponseFulvestrant + AlpelisibCIViC AEID7315
PIK3CA E542K OR PIK3CA E542Q OR PIK3CA E542A OR PIK3CA E542D OR PIK3CA E542G OR PIK3CA E542R OR PIK3CA E542VBreast CancerSensitivity/ResponsePalbociclib + Inavolisib + FulvestrantCIViC AEID12535
PIK3CA E545AHer2-receptor Negative Breast CancerSensitivity/ResponseFulvestrant + CapivasertibCIViC AEID12185
PIK3CA E545DHer2-receptor Negative Breast CancerSensitivity/ResponseCapivasertib + FulvestrantCIViC AEID12186
PIK3CA E545GHer2-receptor Negative Breast CancerSensitivity/ResponseFulvestrant + CapivasertibCIViC AEID12189
PIK3CA E545KHer2-receptor Negative Breast CancerSensitivity/ResponseFulvestrant + CapivasertibCIViC AEID12188
PIK3CA E545K OR PIK3CA E545A OR PIK3CA E545G OR PIK3CA E545DBreast CancerSensitivity/ResponseFulvestrant + AlpelisibCIViC AEID7468
PIK3CA E545K OR PIK3CA E545Q OR PIK3CA E545A OR PIK3CA E545G OR PIK3CA E545V OR PIK3CA E545D OR PIK3CA E545L OR PIK3CA E545RBreast CancerSensitivity/ResponsePalbociclib + Inavolisib + FulvestrantCIViC AEID12534
PIK3CA E545QHer2-receptor Negative Breast CancerSensitivity/ResponseFulvestrant + CapivasertibCIViC AEID12187
PIK3CA G1049RHer2-receptor Negative Breast CancerSensitivity/ResponseCapivasertib + FulvestrantCIViC AEID12198
PIK3CA G1049S OR PIK3CA G1049R OR PIK3CA G106V OR PIK3CA G106R OR PIK3CA G1049A OR PIK3CA G106S OR PIK3CA G106A OR PIK3CA G106D OR PIK3CA G118D OR PIK3CA G1049C OR PIK3CA G1049DBreast CancerSensitivity/ResponsePalbociclib + Inavolisib + FulvestrantCIViC AEID12537
PIK3CA H1047LHer2-receptor Negative Breast CancerSensitivity/ResponseCapivasertib + FulvestrantCIViC AEID12197
PIK3CA H1047RHer2-receptor Negative Breast CancerSensitivity/ResponseFulvestrant + CapivasertibCIViC AEID12196
PIK3CA H1047R OR PIK3CA H1047Y OR PIK3CA H1047LBreast CancerSensitivity/ResponseFulvestrant + AlpelisibCIViC AEID7318
PIK3CA H1047R OR PIK3CA H1047Y OR PIK3CA H1047L OR PIK3CA H1047D OR PIK3CA H1047I OR PIK3CA H1047N OR PIK3CA H1047P OR PIK3CA H1047Q OR PIK3CA H1047TBreast CancerSensitivity/ResponsePalbociclib + Inavolisib + FulvestrantCIViC AEID12533
PIK3CA H1047YHer2-receptor Negative Breast CancerSensitivity/ResponseCapivasertib + FulvestrantCIViC AEID12195
PIK3CA M1043IHer2-receptor Negative Breast CancerSensitivity/ResponseCapivasertib + FulvestrantCIViC AEID12194
PIK3CA M1043VHer2-receptor Negative Breast CancerSensitivity/ResponseFulvestrant + CapivasertibCIViC AEID12193
PIK3CA MutationBreast CancerSensitivity/ResponseAlpelisib + FulvestrantCIViC AEID7313
PIK3CA Mutation OR PTEN Mutation OR AKT1 MutationBreast CancerSensitivity/ResponseCapivasertib + FulvestrantCIViC AEID12020
PIK3CA N345KHer2-receptor Negative Breast CancerSensitivity/ResponseCapivasertib + FulvestrantCIViC AEID12182
PIK3CA N345K OR PIK3CA N345D OR PIK3CA N345H OR PIK3CA N345I OR PIK3CA N345S OR PIK3CA N345T OR PIK3CA N345YBreast CancerSensitivity/ResponsePalbociclib + Inavolisib + FulvestrantCIViC AEID12538
PIK3CA Q546EHer2-receptor Negative Breast CancerSensitivity/ResponseFulvestrant + CapivasertibCIViC AEID12190
PIK3CA Q546E OR PIK3CA Q546RBreast CancerSensitivity/ResponseFulvestrant + AlpelisibCIViC AEID7316

+26 more predictive associations (showing top 30 by level).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 1 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.

178 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
ESTRADIOLChEMBL + PubChemPhase 4 (approved)ESR1, ESR2, GPER1
RaloxifeneChEMBL + PubChemPhase 4 (approved)ESR1, ESR2, GPER1
TamoxifenChEMBL + PubChemPhase 4 (approved)ESR1, ESR2, GPER1
BAZEDOXIFENEChEMBLPhase 4 (approved)ESR1, ESR2
BITHIONOLChEMBLPhase 4 (approved)ESR1, ESR2
CISPLATINChEMBLPhase 4 (approved)ESR1, ESR2
DIETHYLSTILBESTROLChEMBLPhase 4 (approved)ESR1, ESR2
ELACESTRANTChEMBLPhase 4 (approved)ESR1, ESR2
ESTETROLChEMBLPhase 4 (approved)ESR1, ESR2
ESTRIOLChEMBLPhase 4 (approved)ESR1, ESR2
ESTRONEChEMBLPhase 4 (approved)ESR1, ESR2
ETHINYL ESTRADIOLChEMBLPhase 4 (approved)ESR1, ESR2
HEXACHLOROPHENEChEMBLPhase 4 (approved)ESR1, ESR2
LASOFOXIFENEChEMBLPhase 4 (approved)ESR1, ESR2
MEDROXYPROGESTERONEChEMBLPhase 4 (approved)ESR1, ESR2
MIFEPRISTONEChEMBLPhase 4 (approved)ESR1, ESR2
PHENOLPHTHALEINChEMBLPhase 4 (approved)ESR1, ESR2
SPIRONOLACTONEChEMBLPhase 4 (approved)ESR1, ESR2
ACOLBIFENEChEMBLPhase 3ESR1, ESR2
AFIMOXIFENEChEMBLPhase 3ESR1, ESR2
AMCENESTRANTChEMBLPhase 3ESR1, ESR2
ARZOXIFENEChEMBLPhase 3ESR1, ESR2
BENSERAZIDEChEMBLPhase 3ESR1, ESR2
ALFATRADIOLChEMBLPhase 2ESR1, ESR2
AUS-131ChEMBLPhase 2ESR1, ESR2
BRILANESTRANTChEMBLPhase 2ESR1, ESR2
DAIDZEINChEMBLPhase 2ESR1, ESR2
ERTEBERELChEMBLPhase 2ESR1, ESR2
GENISTEINChEMBLPhase 2ESR1, ESR2
GTX-758ChEMBLPhase 2ESR1, ESR2
IDOXIFENEChEMBLPhase 2ESR1, ESR2
LEVORMELOXIFENEChEMBLPhase 2ESR1, ESR2
MOXESTROLChEMBLPhase 2ESR1, ESR2
PIPENDOXIFENEChEMBLPhase 2ESR1, ESR2
PRINABERELChEMBLPhase 2ESR1, ESR2
STALLIMYCINChEMBLPhase 2ESR1, ESR2
BosentanPubChemApprovedESR1, ESR2
DihydroergotaminePubChemApprovedESR1, ESR2
FidaxomicinPubChemApprovedESR1, ESR2
PropoxyphenePubChemApprovedESR1, ESR2
PyrazinamidePubChemApprovedESR1, ESR2
ACETOPHENAZINEChEMBLPhase 4 (approved)ESR1
ALECTINIBChEMBLPhase 4 (approved)ESR1
APOMORPHINEChEMBLPhase 4 (approved)ESR1
ARIPIPRAZOLEChEMBLPhase 4 (approved)ESR1
ASPIRINChEMBLPhase 4 (approved)ESR1
AZTREONAMChEMBLPhase 4 (approved)ESR1
BELINOSTATChEMBLPhase 4 (approved)ESR1
BENZBROMARONEChEMBLPhase 4 (approved)ESR1
BEXAROTENEChEMBLPhase 4 (approved)ESR1
BISACODYLChEMBLPhase 4 (approved)ESR1
BROMOCRIPTINEChEMBLPhase 4 (approved)ESR1
BUTOCONAZOLEChEMBLPhase 4 (approved)ESR1
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)ESR1
CASPOFUNGINChEMBLPhase 4 (approved)ESR1
CEFADROXILChEMBLPhase 4 (approved)ESR1
CEFEPIMEChEMBLPhase 4 (approved)ESR1
CEFTAZIDIMEChEMBLPhase 4 (approved)ESR1
CERIVASTATINChEMBLPhase 4 (approved)ESR1
CHLOROTRIANISENEChEMBLPhase 4 (approved)ESR1

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