Fulvestrant
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2002
- First approval year
- 2002
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Fulvestrant
- Molecular weight
- 606.78
- Structure (SMILES)
- C[C@]12CC[C@@H]3c4ccc(O)cc4C[C@@H](CCCCCCCCC[S+]([O-])CCCC(F)(F)C(F)(F)F)[C@H]3[C@@H]1CC[C@@H]2O
- faslodex
- Faslodex
- fulvestrant mylan
- Fulvestrant mylan
- abemaciclib fulvestrant
- Faslodex
- Faslodex (Fulvestrant)
- Faslodex (Reference)
- faslodex 500mg
- fulvestrant
- Fulvestrant
- FULVESTRANT
- fulvestrant (Faslodex)
- FULVESTRANT [EMA EPAR]
- FULVESTRANT [EP MONOGRAPH]
- fulvestrant [INN]
- FULVESTRANT [JAN]
- FULVESTRANT [MART.]
- FULVESTRANT [MI]
- FULVESTRANT [ORANGE BOOK]
- FULVESTRANT [USAN]
- FULVESTRANT [USP IMPURITY]
- FULVESTRANT [USP MONOGRAPH]
- FULVESTRANT [USP-RS]
- FULVESTRANT [VANDF]
- Fulvestrant [WHO-DD]
- fulvestrant 500 mg
- Fulvestrant 500 mg
- Fulvestrant 500g
And 27 more, listed on the interactive page.
- ATC classification codes
- L02BA03
Sources for recorded values
- CAS registry numbers
- 129453-61-8
- ChEMBL ID
- CHEMBL1358
- InChIKey
- VWUXBMIQPBEWFH-WCCTWKNTSA-N
- PubChem compound IDs
- 104741
- RxNorm IDs (RxCUI)
- 282357
- FDA ingredient codes (UNII)
- 22X328QOC4
- Applicant
- ASTRAZENECA
- Approval date
- 25 Apr 2002
- Application number
- NDA021344
- Status
- Authorised
- Status date
- 9 Mar 2004
- Authorisation date
- 9 Mar 2004
- Approved indications
- Faslodex is indicated as monotherapy for the treatment of estrogen receptor positive, locally advanced or metastatic breast cancer in postmenopausal women: not previously treated with endocrine therapy, or with disease relapse on or after adjuvant antiestrogen therapy, or disease progression on antiestrogen therapy. in combination with palbociclib for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic breast cancer in women who have received prior endocrine therapy. In pre- or perimenopausal women, the combination treatment with palbociclib should be combined with a luteinizing hormone releasing hormone (LHRH) agonist.
- Product number
- EMEA/H/C/000540
- Authorisation holder
- AstraZeneca AB
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 1
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Breast Neoplasms
European medicines record
- Patents
- 3
- Designations
- 0
- Earliest recorded loss of exclusivity
- 17 May 2034
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- fulvestrant
- Type
- Synthetic organic
- Drug name stem
- -estr-; -estrant
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Parenteral
- Action
- Antagonist
- Action type
- Antagonist
- Target
- Estrogen receptor-α
- Gene symbol
- ESR1
- Protein identifier
- P03372
- Median affinity
- 8.98
- Affinity units
- pKi
- Primary target
- Yes
- Action
- Antagonist
- Action type
- Antagonist
- Target
- Estrogen receptor-β
- Gene symbol
- ESR2
- Protein identifier
- Q92731
- Median affinity
- 8.86
- Affinity units
- pKi
- Primary target
- Yes
- Mechanism
- Estrogen receptor alpha antagonist
- Action type
- Antagonist
- Target
- Estrogen receptor
- Protein identifier
- P03372
- Mechanism
- Estrogen receptor degrader
- Action type
- DEGRADER
- Target
- Estrogen receptor
- Protein identifier
- P03372
- Action
- Full agonist
- Action type
- FULL_AGONIST
- Target
- GPER
- Gene symbol
- GPER1
- Protein identifier
- Q99527
- Median affinity
- 7
- Affinity units
- pKi
- Mechanism
- Estrogen receptor alpha antagonist
- Action type
- Antagonist
- Target
- Estrogen receptor
- Mechanism
- Estrogen receptor degrader
- Action type
- DEGRADER
- Target
- Estrogen receptor
- Action type
- Antagonist
- Gene symbol
- ESR1
- Protein identifier
- P03372
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Antagonist
- Gene symbol
- ESR2
- Protein identifier
- Q92731
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000181
- Subject identifier
- D002294
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Carcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000313
- Subject identifier
- D002277
- Condition
- Carcinoma, Intraductal, Noninfiltrating
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000432
- Subject identifier
- D002285
- Condition
- Carcinoma, Lobular
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000553
- Subject identifier
- D018275
- Condition
- Lymphoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Mesothelioma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000588
- Subject identifier
- D008654
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000673
- Subject identifier
- D011471
- Condition
- Small Cell Lung Carcinoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000702
- Subject identifier
- D055752
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001075
- Subject identifier
- D010051
- Condition
- Hypertension, Pulmonary
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001361
- Subject identifier
- D006976
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003869
- Subject identifier
- D001943
- Condition
- Lymphoma, Non-Hodgkin
- Highest recorded phase
- 1
- Condition identifier
- EFO:0005952
- Subject identifier
- D008228
- Condition
- Carcinoma, Ductal
- Highest recorded phase
- 1
- Condition identifier
- EFO:0006318
- Subject identifier
- D044584
- Condition
- Endometrial Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0007532
- Subject identifier
- D016889
- Condition
- Urinary Bladder Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0008528
- Subject identifier
- D001749
- Condition
- Neoplasm Metastasis
- Highest recorded phase
- 3
- Condition identifier
- EFO:0009708
- Subject identifier
- D009362
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:1000294
- Subject identifier
- D001943
- Condition
- Sarcoma, Endometrial Stromal
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000919
- Subject identifier
- D018203
- Condition
- Genital Neoplasms, Female
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001331
- Subject identifier
- D005833
- Condition
- Endometrial Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001512
- Subject identifier
- D016889
- Condition
- Puberty, Precocious
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0000088
- Subject identifier
- D011629
And 10 more, listed on the interactive page.
- Condition identifier
- EFO_0000305
- Condition identifier
- EFO_0000313
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000574
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000673
- Highest recorded phase
- 2
- Condition identifier
- EFO_0001361
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003869
- Condition identifier
- EFO_0007532
- Highest recorded phase
- 2
- Condition identifier
- EFO_0009782
- Highest recorded phase
- 2
- Condition identifier
- EFO_0009870
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001331
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001512
- Highest recorded phase
- 2
- Condition identifier
- HP_0000023
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0000088
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0000521
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001416
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002158
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002447
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002715
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002974
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003060
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004989
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0004990
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 2
And 36 more, listed on the interactive page.
- Event
- abdominal lymphadenopathy
- Reports
- 26
- Reporting signal score
- 82.9577
- Event
- bone lesion
- Reports
- 39
- Reporting signal score
- 84.7168
- Event
- bone pain
- Reports
- 118
- Reporting signal score
- 105.2
- Event
- breast cancer
- Reports
- 296
- Reporting signal score
- 606.243
- Event
- breast cancer metastatic
- Reports
- 399
- Reporting signal score
- 1,599.68
- Event
- breast cancer recurrent
- Reports
- 80
- Reporting signal score
- 249.066
- Event
- carbohydrate antigen 15-3 increased
- Reports
- 56
- Reporting signal score
- 240.623
- Event
- disease progression
- Reports
- 300
- Reporting signal score
- 332.791
- Event
- fatigue
- Reports
- 505
- Reporting signal score
- 109.561
- Event
- hepatic lesion
- Reports
- 53
- Reporting signal score
- 125.357
- Event
- hyperglycaemia
- Reports
- 93
- Reporting signal score
- 85.4895
- Event
- invasive lobular breast carcinoma
- Reports
- 24
- Reporting signal score
- 82.8923
- Event
- leukopenia
- Reports
- 151
- Reporting signal score
- 126.304
- Event
- malignant neoplasm progression
- Reports
- 1,201
- Reporting signal score
- 3,405.31
- Event
- metastases to bone
- Reports
- 571
- Reporting signal score
- 2,055.07
- Event
- metastases to central nervous system
- Reports
- 64
- Reporting signal score
- 107.838
- Event
- metastases to chest wall
- Reports
- 25
- Reporting signal score
- 103.978
- Event
- metastases to liver
- Reports
- 464
- Reporting signal score
- 1,579.32
- Event
- metastases to lung
- Reports
- 185
- Reporting signal score
- 532.1
- Event
- metastases to lymph nodes
- Reports
- 147
- Reporting signal score
- 447.913
- Event
- metastases to peritoneum
- Reports
- 38
- Reporting signal score
- 103.764
- Event
- metastases to pleura
- Reports
- 47
- Reporting signal score
- 179.241
- Event
- metastases to skin
- Reports
- 58
- Reporting signal score
- 216.449
- Event
- metastases to spine
- Reports
- 52
- Reporting signal score
- 153.917
- Event
- metastasis
- Reports
- 62
- Reporting signal score
- 141.761
And 8 more, listed on the interactive page.
- NCT00006903
- NCT00010153
- NCT00012025
- NCT00057941
- NCT00065325
- NCT00075764
- NCT00082810
- NCT00093002
- NCT00099437
- NCT00138125
- NCT00146601
- NCT00201864
- NCT00206414
- NCT00234403
- NCT00241449
- NCT00253422
- NCT00256698
- NCT00259090
- NCT00274469
- NCT00305448
- NCT00313170
- NCT00327769
- NCT00328120
- NCT00357110
- NCT00405938
And 258 more, listed on the interactive page.
- Dose
- 500 mg (two 5 mL injections) or 250 mg (one 5 mL injection in hepatic impairment)
- Route
- Intramuscular
- How often
- Days 1, 15, 29, and once monthly thereafter
Conditions of use
- Administer slowly (1 to 2 minutes)
- Hydrogen bond acceptors
- 3
- Hydrogen bond donors
- 2
- Polar surface area
- 63.52
- Calculated partition coefficient (ALogP)
- 8.68
- Calculated partition coefficient (XLogP)
- 9.2
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 2
- Rotatable bonds
- 14
- Heavy atoms
- 41
- Molecular formula
- C32H47F5O3S
- Monoisotopic mass
- 606.31660734
- Natural product
- No
- 0143-9022
- 0310-0720
- 0781-3532
- 0781-9055
- 16714-070
- 16729-436
- 25021-471
- 43598-262
- 55150-394
- 62332-650
- 63323-715
- 68001-484
- 68001-522
- 68001-626
- 68462-317
- 70700-284
- 70860-211
- 71288-555
- 83634-203
- 83831-159
- 70121-1463
- 70710-1688
- 70771-1626
- 71731-6121
- Recorded assays
- 2,068
- Active assays
- 292
- Confirmatory
- Other
- Screening
- Summary
- Antineoplastic Agents, Hormonal
- Estrogen Receptor Antagonists
These details could not be displayed.
Related records
Trials (466)
- "Neo-Adjuvant Treatment With Palbociclib: Effect on Ki67 and Apoptosis Before, During and After Treatment "
- (VELA) Study of BLU-222 in Advanced Solid Tumors
- [177Lu]Lu-NeoB in Combination With Ribociclib and Fulvestrant in Participants With ER+, HER2- and GRPR+ Advanced Breast Cancer
- 1303GCC: Trastuzmab & Pertuzumab With Hormonal Therapy or Chemotherapy in Women Aged 60 and Over.
- A Biomarker Study of Palbociclib + Fulvestrant for Second, and Third Line of Postmenopausal Women With hr+/her2- Advanced Breast Cancer
- A Clinical Study of JS105 in Combination With Other Anti-tumor Therapies in Patients With Solid Tumors
- A Clinical Trial to Compare Efficacy and Tolerability of Atorvastatin in Addition to Endocrine Treatment With Focus on Mechanisms of Resistance to Endocrine Treatment (Fulvestrant/Aromatase Inhibitors) in Patients With Advanced Breast Cancer
- A Clinical Trial to Compare Efficacy and Tolerability of Faslodex With Arimidex in Patients With Advanced Breast Cancer
- A Clinical Trial to Compare Efficacy and Tolerability of Fulvestrant 250mg, 250mg (Plus 250mg Loading Regimen) and 500mg
- A Clinical Trial to Compare Efficacy and Tolerability of Fulvestrant 250mg, 250mg Plus 250mg Loading Regimen and 500mg
- A Dose Escalation Study Evaluating the Safety and Tolerability of GDC-0032 in Participants With Locally Advanced or Metastatic Solid Tumors or Non-Hodgkin's Lymphoma (NHL) and in Combination With Endocrine Therapy in Locally Advanced or Metastatic Hormone Receptor-Positive Breast Cancer
- A Global Study to Compare the Effects of Fulvestrant and Arimidex in a Subset of Patients With Breast Cancer.
- A Multicenter Clinical Study of Apatinib Mesylate Combined With Doctor's Choice for Advanced Breast Cancer
- A Phase 1 Study of ATV-1601 in Patients With Advanced Cancer That Have AKT1 E17K Mutations
- A Phase 1 Study of BMS-986500 as Monotherapy or Combination Therapy in Advanced Solid Tumors
- A Phase 1 Study of LY2835219 In Participants With Advanced Cancer
- A Phase 1/2 Trial of TER-2013 in Patients With Solid Tumors Harboring AKT/PI3K/PTEN Pathway Alterations
- A Phase 1b Study of T-DXd Combinations in HER2-low Advanced or Metastatic Breast Cancer
- A Phase 3 Study of HRS-8080 Versus Treatment Chosen by Physicians in Locally Advanced and Metastatic Breast Cancer
- A Phase I/II Study of XZP-3287 in Metastasis Solid Tumors
Approved for (6)
- Breast cancer
- Breast carcinoma
- Breast neoplasm
- Cancer
- HER2 positive breast carcinoma
- Neoplasm
In development for (28)
- Breast ductal adenocarcinoma Phase 1
- Carcinoma Phase 2
- Colorectal cancer Phase 1
- Ductal breast carcinoma in situ Phase 2
- Endometrial cancer Phase 2
- Endometrial carcinoma Phase 2
- Endometrioid stromal sarcoma Phase 2
- Exocrine pancreatic carcinoma Phase 1
- Female reproductive organ cancer Phase 2
- Head and neck squamous cell carcinoma Phase 1
- Hereditary breast ovarian cancer syndrome Phase 1
- Invasive lobular breast carcinoma Phase 3
- Lung cancer Phase 2
- Lymphoma Phase 1
- McCune-Albright syndrome Phase 2
- Mesothelioma Phase 1
- Non-Hodgkin lymphoma Phase 1
- Non-small cell lung carcinoma Phase 2
- Ovarian cancer Phase 2
- Ovarian carcinoma Phase 2
Targets (1)
- ESR1 Estrogen receptor alpha antagonist; Estrogen receptor degrader