OralTherapeutic flag

Tamoxifen

CAS 10540-29-1

Tamoxifen (CAS 10540-29-1) is a Phase 4 pharmaceutical compound with 65 bioactivity targets and 1,598 adverse event associations.

SOURCE NLM DailyMed
Label records
0
SOURCE EMBL-EBI ChEMBL
Bioactivity
77
SOURCE DrugCentral
Adverse signals
1,598
SOURCE IUPHAR/BPS
PubMed IDs
32
SOURCE EMBL-EBI ChEMBL B25820EEF0F0

Compound Identity

Matched identifiers and naming fields for the pharmaceutical compound record.

Primary Name
Tamoxifen
CAS Number
10540-29-1
UNII
094ZI81Y45
InChIKey
NKANXQFJJICGDU-QPLCGJKRSA-N
ChEMBL ID
CHEMBL83
Molecule Type
Small molecule
Source Match
EMBL-EBI ChEMBL (INCHIKEY)
Synonyms and normalized names
Tamoxifen Citrate
black box warningoraltherapeutic flag
SOURCE EMBL-EBI ChEMBL B25820EEF0F0

Clinical Development Phase

Highest clinical development phase rendered from the matched compound identifier rows.

Phase 4 (Approved)
Approved or marketed human pharmaceutical use is represented in the source phase field.
ChEMBL CHEMBL83 | Small molecule
SOURCE EMBL-EBI ChEMBL 77 bioactivity rows

Bioactivity & Target Interactions

Target-level activity records with assay counts, activity type, and measured value where present.

TargetActivity ValueAssaysOrganism
- IC50 14827.782802850355 nM 420 -
- AC50 18384.081714285716 nM 105 -
- GI50 8070.906190476191 nM 63 -
- Potency 25652.495402298853 nM 60 -
- Ki 4102.770931034483 nM 58 -
- EC50 19281.505 nM 22 -
- IC50 6.5175 ug.mL-1 16 -
- MIC 38.18181818181818 ug.mL-1 11 -
- GI50 10 ug.mL-1 1 -
- Kd 1 nM 1 -
Adenosine receptor A1
GPCR
Ki 4.858 - Homo sapiens
Sodium/potassium-transporting ATPase subunit alpha-2
Ion channel
IC50 4.807 - Sus scrofa
Beta-1 adrenergic receptor
GPCR
Ki 5.001 - Homo sapiens
Prostaglandin G/H synthase 2
Enzyme
IC50 4.46 - Homo sapiens
Prostaglandin G/H synthase 1
Enzyme
IC50 5.357 - Homo sapiens
Mu-type opioid receptor
GPCR
Ki 5.146 - Homo sapiens
D(1A) dopamine receptor
GPCR
Ki 5.372 - Homo sapiens
D(2) dopamine receptor
GPCR
Ki 5.335 - Homo sapiens
Adenosine receptor A2a
GPCR
Ki 5.4 - Homo sapiens
Alpha-2A adrenergic receptor
GPCR
Ki 6.139 - Homo sapiens
Sigma non-opioid intracellular receptor 1
Membrane receptor
Ki 7.5 - Homo sapiens
Potassium voltage-gated channel subfamily H member 2
Ion channel
IC50 5.8 - Homo sapiens
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase
Enzyme
Ki 8.301 - Homo sapiens
Multidrug resistance protein 1
Transporter
Ki 7 - Homo sapiens
Sodium-dependent serotonin transporter
Transporter
Ki 5.907 - Homo sapiens
Sodium-dependent noradrenaline transporter
Transporter
Ki 5.836 - Homo sapiens
5-hydroxytryptamine receptor 1A
GPCR
Ki 5.158 - Homo sapiens
5-hydroxytryptamine receptor 2A
GPCR
Ki 5.863 - Homo sapiens
5-hydroxytryptamine receptor 2B
GPCR
Ki 5.877 - Homo sapiens
5-hydroxytryptamine receptor 2C
GPCR
Ki 6.618 - Homo sapiens
5-hydroxytryptamine receptor 6
GPCR
Ki 5.98 - Homo sapiens
Alpha-2B adrenergic receptor
GPCR
Ki 5.794 - Homo sapiens
D(3) dopamine receptor
GPCR
Ki 6.439 - Homo sapiens
Histamine H2 receptor
GPCR
Ki 5.034 - Homo sapiens
Muscarinic acetylcholine receptor M1
GPCR
Ki 6.167 - Homo sapiens
Muscarinic acetylcholine receptor M2
GPCR
Ki 5.557 - Homo sapiens
Muscarinic acetylcholine receptor M3
GPCR
Ki 6.201 - Homo sapiens
Muscarinic acetylcholine receptor M4
GPCR
Ki 6.173 - Homo sapiens
Muscarinic acetylcholine receptor M5
GPCR
Ki 5.731 - Homo sapiens
Aldehyde oxidase
Enzyme
IC50 5.658 - Homo sapiens
Beta-3 adrenergic receptor
GPCR
Ki 5.238 - Homo sapiens
Sodium-dependent dopamine transporter
Transporter
Ki 5.835 - Homo sapiens
Adenosine receptor A3
GPCR
Ki 5.679 - Homo sapiens
Nuclear receptor subfamily 1 group I member 2
Nuclear hormone receptor
Ki 7.456 - Homo sapiens
D(4) dopamine receptor
GPCR
Ki 5.407 - Homo sapiens
Alpha-1D adrenergic receptor
GPCR
Ki 5.611 - Homo sapiens
Kappa-type opioid receptor
GPCR
Ki 5.204 - Homo sapiens
Estrogen receptor
Nuclear hormone receptor
Ki 7.51 - Homo sapiens
Progesterone receptor
Nuclear hormone receptor
IC50 6.89 - Homo sapiens
Delta-type opioid receptor
GPCR
Ki 5.328 - Homo sapiens
SOURCE DrugCentral 80 associations

Adverse Event Associations

DrugCentral / FAERS disproportionality signal rows matched to this compound.

Reaction PTDrug AE LLRMedDRA
Metastases to bone 753 2218.542 10027452
Malignant neoplasm progression 1053 1784.654 10051398
Metastases to liver 495 1194.816 10027457
Metastases to lung 311 760.029 10027458
Breast cancer recurrent 183 636.496 10006198
Metastases to lymph nodes 225 597.144 10027459
Breast cancer metastatic 217 586.99 10055113
Disease progression 548 432.1 10061818
Neoplasm progression 289 420.169 10061309
Breast cancer 254 387.542 10006187
Osteonecrosis of jaw 208 268.244 10064658
Metastases to central nervous system 150 265.721 10059282
Metastasis 116 259.581 10062194
PIK3CA-activated mutation 62 230.597 10081234
Metastases to spine 88 220.463 10027468
Hot flush 194 188.818 10060800
Tumour marker increased 76 183.863 10048621
Uterine polyp 57 178.739 10046811
Endometrial hyperplasia 47 175.717 10014755
Bone lesion 81 166.055 10061728
Metastases to pleura 53 159.248 10027463
Bone disorder 118 158.832 10005956
Metastases to skin 53 156.255 10027465
Carbohydrate antigen 15-3 increased 45 144.234 10051415
Osteonecrosis 125 135.474 10031264
Metastases to the mediastinum 38 133.136 10027469
Hormone receptor positive breast cancer 34 131 10083234
Hepatic lesion 68 129.577 10061998
Pseudocirrhosis 35 126.042 10076501
Metastases to peritoneum 56 119.941 10051676
Neuropathy peripheral 275 119.227 10029331
Sarcoma uterus 19 113.379 10039497
Endometrial hypertrophy 26 109.969 10014756
Bone pain 151 106.516 10006002
Endometrial cancer 43 105.153 10014733
Acute myeloid leukaemia 106 102.343 10000880
Second primary malignancy 77 100.864 10039801
Contraindicated product administered 6 98.175 10078504
Hysteroscopy 17 97.337 10050125
Tonsillar disorder 34 95.862 10053477
Uterine cancer 45 94.732 10046766
Breast mass 55 93.287 10006272
Invasive ductal breast carcinoma 49 89.296 10073095
Pulmonary mass 95 88.514 10056342
Lymphoedema 67 88.373 10025282
Device related thrombosis 37 85.325 10077455
Nail disorder 64 83.164 10028694
Systemic lupus erythematosus 7 81.099 10042945
Blood uric acid decreased 28 79.27 10005860
Therapeutic product effect decreased 9 79.257 10082201

Association rows are source-linked signal records, not incidence rates or clinical causality claims.

SOURCE IUPHAR/BPS 7 interactions

IUPHAR Ligand-Target Data

Curated ligand-target interaction rows with action, affinity, and literature identifiers.

TargetAction AffinityPubMed
Estrogen receptor-α
ESR1
Agonist 7.820000171661377 pKi 9048584
Estrogen receptor-α
ESR1
Antagonist 7.800000190734863 pKi 9048584
Estrogen receptor-β
ESR2
Agonist 7.16 pKi 9048584
Estrogen receptor-β
ESR2
Antagonist 7.17 pKi 9048584
GPER
GPER1
Full agonist 6.0 pKi 15539556
Maxi Cl - Activator - -
VRAC Channel blocker - -
SOURCE PharmGKB 60 phenotype rows

Pharmacogenomics

Drug-gene phenotype annotations and evidence levels from PharmGKB-mapped rows.

CYP2D6 (PA128) CYP2D6 poor metabolizers
CYP2D6 poor metabolizers are not associated with decreased risk of Hot Flashes when treated with tamoxifen as compared to CYP2D6 normal metabolizers.
Evidence: -; PMID 22735900
CYP19A1 (PA27091) rs4646
Genotype AA is associated with decreased response to anastrozole, letrozole or tamoxifen in women with Breast Neoplasms and Menopause as compared to genotypes AC + CC.
Evidence: -; PMID 25793413
CYP19A1 (PA27091) rs4646
Genotype AA is associated with increased response to anastrozole, letrozole or tamoxifen in women with Breast Neoplasms as compared to genotypes AC + CC.
Evidence: -; PMID 25793413
CYP2C9 (PA126) CYP2C9*1, CYP2C9*2
CYP2C9 *2 is not associated with increased risk of Recurrence when treated with tamoxifen in women with Breast Neoplasms as compared to CYP2C9 *1.
Evidence: -; PMID 18024866
CYP2D6 (PA128) rs3892097
Genotype TT is associated with increased disease free survival when treated with tamoxifen in people with Breast Neoplasms as compared to genotypes CC + CT.
Evidence: -; PMID 17244352
CYP2D6 (PA128) rs3892097
Genotype TT is associated with decreased severity of hot flashes when treated with tamoxifen in people with Breast Neoplasms as compared to genotypes CC + CT.
Evidence: -; PMID 16361630
LRMDA (PA134899373) rs10509373
Allele C is associated with decreased recurrence-free survival when treated with tamoxifen in women with Breast Neoplasms as compared to allele T.
Evidence: -; PMID 22180457
CYP2D6 (PA128) CYP2D6*1, CYP2D6*10
CYP2D6 *10/*10 is associated with increased risk of Recurrence when treated with tamoxifen in women with Breast Neoplasms as compared to CYP2D6 *1/*1 + *1/*10.
Evidence: -; PMID 18294285
ABCB1 (PA267) rs2032582
Allele C is not associated with increased or decreased recurrence-free survival time when treated with tamoxifen as compared to allele A.
Evidence: -; PMID 20124171
ABCB1 (PA267) rs3213619
Allele A is not associated with increased or decreased recurrence-free survival time when treated with tamoxifen as compared to allele G.
Evidence: -; PMID 20124171
ABCC2 (PA116) rs3740065
Genotype AA is not associated with increased or decreased plasma levels of endoxifen or 4-hydroxytamoxifen in recipients of tamoxifen as compared to genotype GG.
Evidence: -; PMID 20124171
CYP3A5 (PA131) CYP3A5 haplotype
CYP3A5 poor metabolizer and intermediate metabolizer genotypes are not associated with concentrations of tamoxifen in women with Breast Neoplasms.
Evidence: -; PMID 29436156
ESR1 (PA156) rs9340799
Genotype GG is associated with decreased in total cholesterol in postmenopausal woman and increase in triglycerides and decrease in high density lipoprotein in premenopausal women when treated with tamoxifen as compared to genotypes AA + AG.
Evidence: -; PMID 17713466
ESR2 (PA27886) rs4986938
Genotype CC is associated with increased triglycerides in postmenopausal woman when treated with tamoxifen as compared to genotype TT.
Evidence: -; PMID 17713466
CYP2D6 (PA128) rs3892097
Genotype TT is associated with decreased relapse free time when treated with tamoxifen in people with Breast Neoplasms as compared to genotypes CC + CT.
Evidence: -; PMID 16361630
CYP3A (PA27114),"CYP3A5 (PA131)" rs776746
Allele T is not associated with survival when treated with tamoxifen in people with Breast Neoplasms as compared to allele C.
Evidence: -; PMID 16361630
CYP2D6 (PA128) rs1065852
Allele A is associated with increased risk of recurrence when treated with tamoxifen in people with Breast Neoplasms as compared to allele G.
Evidence: -; PMID 18024866
CYP2D6 (PA128) rs3892097
Allele C is associated with increased risk of recurrence when treated with tamoxifen in people with Breast Neoplasms as compared to allele T.
Evidence: -; PMID 18024866
CYP2D6 (PA128) rs28371725
Allele T is associated with increased risk of recurrence when treated with tamoxifen in people with Breast Neoplasms as compared to allele C.
Evidence: -; PMID 18024866
CYP2C19 (PA124) rs12248560
Allele T is associated with decreased risk of Recurrence when treated with tamoxifen in people with Breast Neoplasms as compared to genotype CC.
Evidence: -; PMID 18024866
RRAS2 (PA34862) rs11023197
Allele A is associated with increased frequency of relapse when treated with tamoxifen in people with Breast Neoplasms as compared to allele G.
Evidence: -; PMID 19047159
CYP2C19 (PA124) CYP2C19*1, CYP2C19*2
CYP2C19 *2 is associated with increased response to tamoxifen in women with Breast Neoplasms as compared to CYP2C19 *1.
Evidence: -; PMID 21830868
CYP2C19 (PA124) CYP2C19*1, CYP2C19*17
CYP2C19 *17 is associated with decreased response to tamoxifen in women with Breast Neoplasms as compared to CYP2C19 *1.
Evidence: -; PMID 21830868
CYP2D6 (PA128) CYP2D6*1, CYP2D6*4
CYP2D6 *4 is not associated with response to antineoplastic agents and tamoxifen in women with Breast Neoplasms as compared to CYP2D6 *1.
Evidence: -; PMID 21830868
ESR1 (PA156) rs9340799
Genotype GG is not associated with tamoxifen-induced changes in levels of total cholesterol, triglycerides, and high-density lipoprotein (HDL) cholesterol when treated with tamoxifen as compared to genotypes AA + AG.
Evidence: -; PMID 20827267
IGF1 (PA29697) rs6214
Allele T is not associated with risk of Recurrence when treated with tamoxifen in women with Breast Neoplasms as compared to allele C.
Evidence: -; PMID 23459444
CYP3A4 (PA130) rs2740574
Genotype CT is associated with increased risk of Endometrial Neoplasms when treated with tamoxifen in people with Breast Neoplasms as compared to genotype TT.
Evidence: -; PMID 17434921
IGFBP3 (PA29705) rs2854744
Allele T is not associated with risk of Recurrence when treated with tamoxifen in women with Breast Neoplasms as compared to allele G.
Evidence: -; PMID 23459444
IGF1 (PA29697) rs2946834
Allele A is not associated with risk of Recurrence when treated with tamoxifen in women with Breast Neoplasms as compared to allele G.
Evidence: -; PMID 23459444
CYP2C19 (PA124) CYP2C19*1, CYP2C19*17
CYP2C19 *17 is not associated with increased event-free survival when treated with tamoxifen in women with Breast Neoplasms as compared to CYP2C19 *1.
Evidence: -; PMID 21961651
SOURCE NLM RxNorm 6 name rows

Drug Names / RxNorm

Normalized drug-name vocabulary rows, RxCUIs, and source abbreviations.

NameRxCUI TypeSource
TAMOXIFEN 10324 SU MTHSPL
Tamoxifen 10324 SU MTHSPL
Tamoxifen Citrate 40137 SU MTHSPL
TAMOXIFEN CITRATE 40137 SU MTHSPL
tamoxifen 10324 IN RXNORM
tamoxifen citrate 40137 PIN RXNORM
SOURCE SIDER 80 side-effect rows

Side Effects

SIDER side-effect terms mapped to the drug or same-CAS compound identity.

Side EffectDrug Name MedDRA TypeConcept ID
Abdominal cramps tamoxifen LLT C0000729
Abdominal discomfort tamoxifen PT C0232487
Abdominal pain tamoxifen PT C0000737
Abdominal pain tamoxifen LLT C0000737
Abdominal pain tamoxifen PT C0000737
Accidental exposure to product tamoxifen PT C3544060
Accidental ingestion tamoxifen LLT C0857807
Accidental injury tamoxifen LLT C0151736
Acute coronary syndrome tamoxifen PT C0948089
Adenocarcinoma tamoxifen LLT C0001418
Adenocarcinoma tamoxifen PT C0001418
Alanine aminotransferase increased tamoxifen LLT C0151905
Alanine aminotransferase increased tamoxifen PT C0151905
Alopecia tamoxifen LLT C0002170
Alopecia tamoxifen PT C0002170
Alopecia tamoxifen LLT C0002170
Alopecia tamoxifen PT C0002170
Amenorrhoea tamoxifen LLT C0002453
Amenorrhoea tamoxifen PT C0002453
Anaemia tamoxifen LLT C0002871
Anaemia tamoxifen PT C0002871
Angina pectoris tamoxifen LLT C0002962
Angina pectoris tamoxifen PT C0002962
Angioedema tamoxifen LLT C0002994
Angioedema tamoxifen PT C0002994
Angioedema tamoxifen LLT C0002994
Angioedema tamoxifen PT C0002994
Ankle edema tamoxifen LLT C0235439
Anorexia tamoxifen LLT C0003123
Anxiety tamoxifen LLT C0003467
Anxiety tamoxifen PT C0003467
Appetite absent tamoxifen LLT C1971624
Arrhythmia tamoxifen LLT C0003811
Arrhythmia tamoxifen PT C0003811
Arthralgia tamoxifen LLT C0003862
Arthralgia tamoxifen PT C0003862
Arthritis tamoxifen LLT C0003864
Arthritis tamoxifen PT C0003864
Arthropathy tamoxifen LLT C0022408
Arthropathy tamoxifen PT C0022408
Aspartate aminotransferase increased tamoxifen LLT C0151904
Aspartate aminotransferase increased tamoxifen PT C0151904
Asthenia tamoxifen LLT C0004093
Asthenia tamoxifen PT C0004093
Asthenia tamoxifen PT C0004093
Back pain tamoxifen LLT C0004604
Back pain tamoxifen PT C0004604
Benign neoplasm tamoxifen LLT C0086692
Benign neoplasm tamoxifen PT C0086692
Blindness tamoxifen LLT C0456909
Blindness tamoxifen PT C0456909
Blindness tamoxifen LLT C0456909
Blindness tamoxifen PT C0456909
Blister tamoxifen LLT C0005758
Blister tamoxifen PT C0005758
Blood bilirubin increased tamoxifen LLT C0311468
Blood bilirubin increased tamoxifen PT C0311468
Blood creatinine increased tamoxifen PT C0235431
Blood triglycerides increased tamoxifen PT C0853692
Bone pain tamoxifen LLT C0151825
Bone pain tamoxifen PT C0151825
Breast cancer male tamoxifen LLT C0238033
Breast cancer male tamoxifen PT C0238033
Breast feeding tamoxifen LLT C0006147
Breast feeding tamoxifen PT C0006147
Breast neoplasm tamoxifen LLT C1458155
Breast neoplasm tamoxifen PT C1458155
Breast pain tamoxifen LLT C0024902
Breast pain tamoxifen PT C0024902
Bronchitis tamoxifen LLT C0006277
Bronchitis tamoxifen PT C0006277
Cardiovascular disorder tamoxifen LLT C0007222
Cardiovascular disorder tamoxifen PT C0007222
Cataract tamoxifen LLT C0086543
Cataract tamoxifen PT C0086543
Cataract tamoxifen PT C0086543
Cataract specified tamoxifen LLT C0151547
Chest pain tamoxifen LLT C0008031
Chest pain tamoxifen PT C0008031
Cholestasis tamoxifen LLT C0008370
SOURCE Rendered pharma page rows FAQPage JSON-LD

Frequently Asked Questions

Short answers generated only from the same visible source-linked rows on this page.

What is Tamoxifen used for in pharmaceutical contexts?

Tamoxifen (CAS 10540-29-1) is rendered as a pharmaceutical compound from the matched source rows; no DailyMed product-name rows are present in this page query.

What are the known adverse events for Tamoxifen?

Tamoxifen has 1,598 DrugCentral/FAERS adverse event associations. Rendered reaction terms include Metastases to bone, Malignant neoplasm progression, Metastases to liver, Metastases to lung, Breast cancer recurrent. Signal rows are source-linked records and should not be read as incidence rates or causality conclusions.

Is Tamoxifen also used in cosmetics?

No same-CAS cosmetics profile is rendered from the ingredients-table cross-reference for Tamoxifen.

What clinical phase is Tamoxifen in?

Tamoxifen is rendered with ChEMBL max phase 4 (approved).

What bioactivity targets are documented for Tamoxifen?

Tamoxifen has 77 bioactivity rows in this page query. Rendered target entries include Adenosine receptor A1, Sodium/potassium-transporting ATPase subunit alpha-2, Beta-1 adrenergic receptor, Prostaglandin G/H synthase 2, Prostaglandin G/H synthase 1.