Tamoxifen
Highest phase reached
Approved
Drug type
Small molecule
First approval year
1977
- First approval year
- 1977
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Tamoxifen
- Molecular weight
- 371.52
- Structure (SMILES)
- CC/C(=C(\c1ccccc1)c1ccc(OCCN(C)C)cc1)c1ccccc1
- ici 47699
- ICI-47699
- mammaton
- Mammaton
- novaldex
- Novaldex
- nsc 727681
- NSC-727681
- tamoplex
- Tamoplex
- tamoxifen
- Tamoxifen
- TAMOXIFEN [HSDB]
- TAMOXIFEN [IARC]
- tamoxifen [INN]
- TAMOXIFEN [MI]
- TAMOXIFEN [VANDF]
- Tamoxifen [WHO-DD]
- tamoxifen hsdb
- tamoxifen iarc
- tamoxifen inn
- tamoxifen mi
- tamoxifen vandf
- tamoxifen who dd
- tamoxifene
And 3 more, listed on the interactive page.
- ATC classification codes
- L02BA01
Sources for recorded values
- CAS registry numbers
- 10540-29-1
- ChEMBL ID
- CHEMBL83
- InChIKey
- NKANXQFJJICGDU-QPLCGJKRSA-N
- PubChem compound IDs
- 2733526
- RxNorm IDs (RxCUI)
- 10324
- FDA ingredient codes (UNII)
- 094ZI81Y45
- Applicant
- ASTRAZENECA
- Approval date
- 30 Dec 1977
- Application number
- NDA017970
- First in class
- No
- Orphan designation
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- United States (FDA)
- Approved
- Pharmacology name
- tamoxifen
- Type
- Synthetic organic
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Activator
- Action type
- ACTIVATOR
- Target
- Maxi Cl-
- Gene symbol
- Maxi Cl-
- Action
- Agonist
- Action type
- Agonist
- Target
- Estrogen receptor-α
- Gene symbol
- ESR1
- Protein identifier
- P03372
- Median affinity
- 7.82
- Affinity units
- pKi
- Primary target
- Yes
- Action
- Agonist
- Action type
- Agonist
- Target
- Estrogen receptor-β
- Gene symbol
- ESR2
- Protein identifier
- Q92731
- Median affinity
- 7.16
- Affinity units
- pKi
- Action
- Antagonist
- Action type
- Antagonist
- Target
- Estrogen receptor-α
- Gene symbol
- ESR1
- Protein identifier
- P03372
- Median affinity
- 7.8
- Affinity units
- pKi
- Primary target
- Yes
- Action
- Antagonist
- Action type
- Antagonist
- Target
- Estrogen receptor-β
- Gene symbol
- ESR2
- Protein identifier
- Q92731
- Median affinity
- 7.17
- Affinity units
- pKi
- Action
- Channel blocker
- Action type
- Channel blocker
- Target
- VRAC
- Gene symbol
- VRAC
- Action
- Full agonist
- Action type
- FULL_AGONIST
- Target
- GPER
- Gene symbol
- GPER1
- Protein identifier
- Q99527
- Median affinity
- 6
- Affinity units
- pKi
Open Targets mechanisms
- Mechanism
- Estrogen receptor alpha modulator
- Action type
- MODULATOR
- Target
- Estrogen receptor
DrugCentral mechanisms
- Action type
- MODULATOR
- Gene symbol
- ESR1
- Protein identifier
- P03372
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Adenoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000232
- Subject identifier
- D000236
- Condition
- Urinary Bladder Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000294
- Subject identifier
- D001749
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Lymphoma, Large B-Cell, Diffuse
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000403
- Subject identifier
- D016403
- Condition
- Carcinoma, Intraductal, Noninfiltrating
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000432
- Subject identifier
- D002285
- Condition
- Glioblastoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Hyperplasia
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000536
- Subject identifier
- D006965
- Condition
- Hypertension
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000537
- Subject identifier
- D006973
- Condition
- Infertility
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000545
- Subject identifier
- D007246
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Osteosarcoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000637
- Subject identifier
- D012516
- Condition
- HIV Infections
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000764
- Subject identifier
- D015658
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0001075
- Subject identifier
- D010051
- Condition
- Uterine Cervical Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001416
- Subject identifier
- D002583
- Condition
- Coronary Disease
- Highest recorded phase
- 3
- Condition identifier
- EFO:0001645
- Subject identifier
- D003327
- Condition
- Brain Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003833
- Subject identifier
- D001932
- Condition
- Pain
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003843
- Subject identifier
- D010146
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003869
- Subject identifier
- D001943
- Condition
- Hepatitis C, Chronic
- Highest recorded phase
- 1
- Condition identifier
- EFO:0004220
- Subject identifier
- D019698
- Condition
- Infertility, Male
- Highest recorded phase
- 2
- Condition identifier
- EFO:0004248
- Subject identifier
- D007248
- Condition
- Breast Neoplasms, Male
- Highest recorded phase
- 3
- Condition identifier
- EFO:0006861
- Subject identifier
- D018567
- Condition
- Neoplasm Metastasis
- Highest recorded phase
- 3
- Condition identifier
- EFO:0009708
- Subject identifier
- D009362
- Condition
- Fallopian Tube Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:1000251
- Subject identifier
- D005185
- Condition
- Myocardial Ischemia
- Highest recorded phase
- 3
- Condition identifier
- EFO:1001375
- Subject identifier
- D017202
- Condition
- Neuroendocrine Tumors
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001901
- Subject identifier
- D018358
And 16 more, listed on the interactive page.
- Condition identifier
- EFO_0000232
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000280
- Condition identifier
- EFO_0000294
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000305
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000403
- Condition identifier
- EFO_0000432
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000536
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000545
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0001416
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003860
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003869
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003895
- Highest recorded phase
- 2
- Condition identifier
- EFO_0004220
- Highest recorded phase
- 1
- Condition identifier
- EFO_0006861
- Highest recorded phase
- 3
- Condition identifier
- EFO_0009870
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000251
- Highest recorded phase
- 3
- Condition identifier
- EFO_1000649
- Condition identifier
- EFO_1000650
- Condition identifier
- EFO_1001366
- Highest recorded phase
- 3
- Condition identifier
- EFO_1001901
- Highest recorded phase
- 2
- Condition identifier
- GO_0042697
- Highest recorded phase
- 3
- Condition identifier
- HP_0000771
- Highest recorded phase
- 2
- Condition identifier
- HP_0000789
- Highest recorded phase
- 2
- Condition identifier
- HP_0031217
- Highest recorded phase
- 3
And 61 more, listed on the interactive page.
- Warning
- Black Box Warning
- Effect
- carcinogenicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- immune system toxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- neurotoxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- respiratory toxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- vascular toxicity
- Country
- United States
- Event
- acquired gene mutation
- Reports
- 15
- Reporting signal score
- 43.8069
- Event
- adenocarcinoma
- Reports
- 18
- Reporting signal score
- 47.9343
- Event
- adnexa uteri mass
- Reports
- 10
- Reporting signal score
- 40.9104
- Event
- blood creatinine decreased
- Reports
- 25
- Reporting signal score
- 67.5914
- Event
- blood lactate dehydrogenase increased
- Reports
- 31
- Reporting signal score
- 37.9816
- Event
- blood uric acid decreased
- Reports
- 21
- Reporting signal score
- 87.9505
- Event
- bone lesion
- Reports
- 20
- Reporting signal score
- 46.6506
- Event
- breast cancer
- Reports
- 207
- Reporting signal score
- 519.47
- Event
- breast cancer female
- Reports
- 21
- Reporting signal score
- 42.706
- Event
- breast cancer metastatic
- Reports
- 190
- Reporting signal score
- 778.883
- Event
- breast cancer recurrent
- Reports
- 83
- Reporting signal score
- 330.23
- Event
- breast mass
- Reports
- 20
- Reporting signal score
- 41.6821
- Event
- carbohydrate antigen 15-3 increased
- Reports
- 26
- Reporting signal score
- 113.342
- Event
- device related thrombosis
- Reports
- 12
- Reporting signal score
- 37.8565
- Event
- disease progression
- Reports
- 204
- Reporting signal score
- 309.401
- Event
- disease recurrence
- Reports
- 39
- Reporting signal score
- 45.9528
- Event
- drug intolerance
- Reports
- 68
- Reporting signal score
- 35.7677
- Event
- endometrial cancer
- Reports
- 16
- Reporting signal score
- 42.1509
- Event
- endometriosis
- Reports
- 22
- Reporting signal score
- 58.2017
- Event
- eosinophil percentage increased
- Reports
- 21
- Reporting signal score
- 78.8376
- Event
- hepatic lesion
- Reports
- 35
- Reporting signal score
- 97.3945
- Event
- hot flush
- Reports
- 73
- Reporting signal score
- 96.0584
- Event
- invasive ductal breast carcinoma
- Reports
- 30
- Reporting signal score
- 81.9775
- Event
- invasive lobular breast carcinoma
- Reports
- 11
- Reporting signal score
- 38.5327
- Event
- lower limb fracture
- Reports
- 26
- Reporting signal score
- 44.1469
And 34 more, listed on the interactive page.
- NCT00000529
- NCT00001436
- NCT00002707
- NCT00003906
- NCT00005822
- NCT00053339
- NCT00066703
- NCT00066807
- NCT00152178
- NCT00171704
- NCT00201851
- NCT00206492
- NCT00232661
- NCT00241449
- NCT00286117
- NCT00287534
- NCT00290654
- NCT00291759
- NCT00293540
- NCT00295100
- NCT00295646
- NCT00309478
- NCT00309491
- NCT00412022
- NCT00433589
And 150 more, listed on the interactive page.
- Dose
- 20-40mg
- How often
- Once daily
- Hydrogen bond acceptors
- 2
- Hydrogen bond donors
- 0
- Polar surface area
- 12.47
- Calculated partition coefficient (ALogP)
- 6
- Calculated partition coefficient (XLogP)
- 7.1
- Prodrug
- Yes
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 8
- Heavy atoms
- 28
- Molecular formula
- C26H29NO
- Monoisotopic mass
- 371.224914549
- Natural product
- No
- Recorded assays
- 7,648
- Active assays
- 1,429
- Confirmatory
- Other
- Screening
- Summary
- Estrogen Antagonists
- Antineoplastic Agents, Hormonal
- Selective Estrogen Receptor Modulators
- Bone Density Conservation Agents
These details could not be displayed.
Related records
Trials (261)
- A Multicenter Trial Assessing the Efficacy and Safety of tamOxifen Plus LY2228820 in Advanced or Metastatic Breast Cancer Progressing on aromatasE Inhibitors
- A Phase 2 Single-Arm Open-Label Pilot Trial Evaluating Zanidatamab (ZW25) in Patients With Early Stage HER2/Neu Positive (HER2+) Breast Cancer (BC)
- A Phase 2 Study of the IDO Inhibitor Epacadostat Versus Tamoxifen for Subjects With Biochemical-recurrent-only EOC, PPC or FTC Following Complete Remission With First-line Chemotherapy
- A Phase I Study of OncoLAR® (Registered Trademark) (NSC 685403) With/Without Tamoxifen in Patients With Osteosarcoma
- A Phase Ib Dose Escalation Study of the Combination of LEE011 With Letrozole and Dose Expansion of LEE011 With Hormonal Therapy for the Treatment of Pre-(With Goserelin) and Postmenopausal Women With Hormone Receptor Positive, HER2-negative, Advanced Breast Cancer
- A Phase II Study of ZD1839 and Tamoxifen in Patients With Epithelial Ovarian Carcinoma, Cancer of the Fallopian Tube or the Peritoneum Refractory to Platinum- and Taxane-based Therapy
- A Pilot Clinical Trial to Evaluate the Biological Activity of Fulvestrant in Breast Ductal Carcinoma in Situ (DCIS)
- A Pilot Study of Varying Doses of Tamoxifen in the Setting of Genetic Polymorphisms of CYP2D6
- A Precision Medicine Approach (SMMART-ACT) for the Treatment of Patients With Advanced Sarcoma, Prostate, Breast, Ovarian or Pancreatic Cancer
- A Study Evaluating Megestrol Acetate Modulation in Hormone Receptor Positive Advanced Breast Cancer
- A 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)
- A Study for Safety and Effectiveness of IMC-A12 by Itself or Combined With Antiestrogens to Treat Breast Cancer
- A Study of Abemaciclib (LY2835219) Plus Tamoxifen or Abemaciclib Alone in Women With Metastatic Breast Cancer
- A Study of Camizestrant in ER+/HER2- Early Breast Cancer After at Least 2 Years of Standard Adjuvant Endocrine Therapy
- A Study of Elacestrant Versus Standard Endocrine Therapy in Women and Men With ER+,HER2-, Early Breast Cancer With High Risk of Recurrence
- A Study of Imlunestrant (LY3484356) in Premenopausal Women With Estrogen Receptor-Positive (ER+) Human Epidermal Growth Factor Receptor 2 Negative (HER2-) Early Breast Cancer
- A Study of Imlunestrant Versus Standard Endocrine Therapy in Participants With Early Breast Cancer
- A Study of LY2228820 in Participants With Advanced Cancer
- A Study of LY2835219 (Abemaciclib) in Combination With Therapies for Breast Cancer That Has Spread
- A Study of Maprotiline in Combination With Tamoxifen and Temozolomide for Recurrent Glioblastoma
Approved for (2)
In development for (66)
- Adenoma Phase 2
- Amyotrophic lateral sclerosis Phase 2
- Barrett esophagus Phase 1
- Bipolar disorder Phase 2
- Bladder papillary urothelial carcinoma Phase 2
- Brain neoplasm Phase 1
- Brain stem glioma Phase 2
- Breast adenocarcinoma Phase 3
- Breast cancer Phase 3
- Breast carcinoma Phase 3
- Breast neoplasm Phase 3
- Centronuclear myopathy Phase 1
- Cervical adenocarcinoma Phase 2
- Cervical squamous cell carcinoma Phase 2
- Chronic hepatitis C virus infection Phase 1
- Coronary artery disorder Phase 3
- COVID-19 Phase 2
- Cryptococcal meningitis Phase 2
- Cystic neoplasm Phase 1
- Desmoid tumor Phase 2