Identification

Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Logo pink
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.
#DrugBankUpdates
Name
Fulvestrant
Accession Number
DB00947  (APRD00654)
Type
Small Molecule
Groups
Approved, Investigational
Description

Fulvestrant is a drug treatment of hormone receptor (HR)-positive metastatic breast cancer in post-menopausal women with disease progression following anti-estrogen therapy. It is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor. While it is used as monotherapy for the treatment of breast cancers, it is also used in combination with alpelisib for the treatment of HR-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer

Structure
Thumb
Synonyms
  • (7α,17β)-7-{9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl}estra-1(10),2,4-triene-3,17-diol
  • Fulvestrant
External IDs
ICI 182,780 / ICI 182780 / ICI-182780 / ZD-9238 / ZD9238
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
FaslodexInjection50 mg/1mLIntramuscularAstraZeneca Pharmaceuticals LP2010-11-01Not applicableUs
FaslodexInjection, solution250 mg/5mlIntramuscularAstra Zeneca Ab2004-03-10Not applicableEu
FaslodexSolution50 mgIntramuscularAstra Zeneca2004-06-14Not applicableCanada
FaslodexInjection, solution250 mg/5mlIntramuscularAstra Zeneca Ab2004-03-10Not applicableEu
FulvestrantInjection250 mg/5mLIntramuscularActavis Pharma, Inc.2019-08-22Not applicableUs
FulvestrantInjection, solution50 mg/1mLIntramuscularFresenius Kabi USA, LLC2019-05-20Not applicableUs
Fulvestrant InjectionSolutionIntramuscularMylan PharmaceuticalsNot applicableNot applicableCanada
Fulvestrant InjectionSolutionIntramuscularSandoz Canada Incorporated2019-02-01Not applicableCanada
Fulvestrant InjectionSolutionIntramuscularAccord Healthcare IncNot applicableNot applicableCanada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-fulvestrantSolutionIntramuscularApotex CorporationNot applicableNot applicableCanada
FulvestrantInjection50 mg/1mLIntramuscularGlenmark Pharmaceuticals Inc., USA2019-08-22Not applicableUs
FulvestrantInjection50 mg/1mLIntramuscularSandoz Inc2019-05-29Not applicableUs
FulvestrantInjection, solution50 mg/1mLIntramuscularSagent Pharmaceuticals2019-08-01Not applicableUs
FulvestrantInjection, solution250 mg/5mLIntramuscularAmneal Pharmaceuticals LLC2019-03-04Not applicableUs
FulvestrantInjection50 mg/1mLIntramuscularAstraZeneca Pharmaceuticals LP2019-10-08Not applicableUs
FulvestrantInjection50 mg/1mLIntramuscularMylan Institutional LLC2019-09-09Not applicableUs
Teva-fulvestrant InjectionSolutionIntramuscularTEVA Canada Limited2019-01-15Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Categories
UNII
22X328QOC4
CAS number
129453-61-8
Weight
Average: 606.78
Monoisotopic: 606.316607362
Chemical Formula
C32H47F5O3S
InChI Key
VWUXBMIQPBEWFH-WCCTWKNTSA-N
InChI
InChI=1S/C32H47F5O3S/c1-30-17-15-26-25-12-11-24(38)21-23(25)20-22(29(26)27(30)13-14-28(30)39)10-7-5-3-2-4-6-8-18-41(40)19-9-16-31(33,34)32(35,36)37/h11-12,21-22,26-29,38-39H,2-10,13-20H2,1H3/t22-,26-,27+,28+,29-,30+,41?/m1/s1
IUPAC Name
(1S,3aS,3bR,4R,9bS,11aS)-11a-methyl-4-[9-(4,4,5,5,5-pentafluoropentanesulfinyl)nonyl]-1H,2H,3H,3aH,3bH,4H,5H,9bH,10H,11H,11aH-cyclopenta[a]phenanthrene-1,7-diol
SMILES
[H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@]1([H])C3=CC=C(O)C=C3C[C@@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)[C@@]21[H]

Pharmacology

Indication

For the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy, as monotherapy or in combination with other antineoplastic agents.

Associated Conditions
Pharmacodynamics

Fulvestrant for intramuscular administration is an estrogen receptor antagonist without known agonist effects.

Mechanism of action

Fulvestrant competitively and reversibly binds to estrogen receptors present in cancer cells and achieves its anti-estrogen effects through two separate mechanisms. First, fulvestrant binds to the receptors and downregulates them so that estrogen is no longer able to bind to these receptors. Second, fulvestrant degrades the estrogen receptors to which it is bound. Both of these mechanisms inhibit the growth of tamoxifen-resistant as well as estrogen-sensitive human breast cancer cell lines.

TargetActionsOrganism
AEstrogen receptor alpha
antagonist
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

Learn more
Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

Learn more
Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

Learn more
Absorption
Not Available
Volume of distribution
  • 3 to 5 L/kg
Protein binding

99% (mainly VLDL, LDL, and HDL)

Metabolism

Metabolism of fulvestrant appears to involve combinations of a number of possible biotransformation pathways analogous to those of endogenous steroids, including oxidation, aromatic hydroxylation, conjugation with glucuronic acid and/or sulphate at the 2, 3 and 17 positions of the steroid nucleus, and oxidation of the side chain sulphoxide. Identified metabolites are either less active or exhibit similar activity to fulvestrant in antiestrogen models. Studies using human liver preparations and recombinant human enzymes indicate that cytochrome P-450 3A4 (CYP 3A4) is the only P-450 isoenzyme involved in the oxidation of fulvestrant; however, the relative contribution of P-450 and non-P-450 routes in vivo is unknown.

Route of elimination

Fulvestrant was rapidly cleared by the hepatobiliary route with excretion primarily via the feces (approximately 90%). Renal elimination was negligible (less than 1%).

Half life

40 days

Clearance
Not Available
Toxicity

There is no clinical experience with overdosage in humans.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AdenineThe metabolism of Fulvestrant can be decreased when combined with Adenine.
AmitriptylineThe metabolism of Fulvestrant can be decreased when combined with Amitriptyline.
AtazanavirThe metabolism of Fulvestrant can be decreased when combined with Atazanavir.
CarbamazepineThe metabolism of Fulvestrant can be increased when combined with Carbamazepine.
DacomitinibThe metabolism of Fulvestrant can be decreased when combined with Dacomitinib.
Darbepoetin alfaThe risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Fulvestrant.
DasabuvirThe metabolism of Fulvestrant can be decreased when combined with Dasabuvir.
DeferasiroxThe metabolism of Fulvestrant can be decreased when combined with Deferasirox.
DesogestrelThe metabolism of Fulvestrant can be increased when combined with Desogestrel.
EfavirenzThe metabolism of Fulvestrant can be increased when combined with Efavirenz.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

    Learn more
  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
Not Available

References

General References
  1. Kansra S, Yamagata S, Sneade L, Foster L, Ben-Jonathan N: Differential effects of estrogen receptor antagonists on pituitary lactotroph proliferation and prolactin release. Mol Cell Endocrinol. 2005 Jul 15;239(1-2):27-36. [PubMed:15950373]
  2. Kabos P, Borges VF: Fulvestrant: a unique antiendocrine agent for estrogen-sensitive breast cancer. Expert Opin Pharmacother. 2010 Apr;11(5):807-16. doi: 10.1517/14656561003641982. [PubMed:20151846]
  3. Bross PF, Cohen MH, Williams GA, Pazdur R: FDA drug approval summaries: fulvestrant. Oncologist. 2002;7(6):477-80. [PubMed:12490735]
External Links
Human Metabolome Database
HMDB0015082
KEGG Drug
D01161
PubChem Compound
17756771
PubChem Substance
46508664
ChemSpider
94553
BindingDB
50169743
ChEBI
31638
ChEMBL
CHEMBL1358
Therapeutic Targets Database
DAP000319
PharmGKB
PA164747170
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Fulvestrant
ATC Codes
L02BA03 — Fulvestrant
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
Download (520 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingBasic ScienceAdvanced Metastatic Breast Cancer1
1Active Not RecruitingOtherPharmacokinetics1
1Active Not RecruitingTreatmentAdvanced or Metastatic Breast Cancer / Advanced Solid Malignancies / AKT1 / Cervical Cancers / Endometrial Cancers / ER Positive / ER+ / HER2 Positive / HER2+ / Ovarian Cancer / Pharmacodynamics / Pharmacokinetics / PIK3CA / PTEN / Safety and Tolerability / Tumour Response1
1Active Not RecruitingTreatmentAdvanced Solid Tumors With an Alteration of the PIK3CA Gene / Estrogen Receptor Positive Breast Cancer1
1Active Not RecruitingTreatmentAdvanced Solid Tumors / Breast Cancer / Ovarian Cancer1
1Active Not RecruitingTreatmentAdvanced and Metastatic Breast Cancer1
1Active Not RecruitingTreatmentCancer, Advanced1
1Active Not RecruitingTreatmentCancer, Advanced / Lung Cancer Non-Small Cell Cancer (NSCLC) / Mesothelioma, Malignant / Metastatic Breast Cancer (MBC) / Metastatic Cancers / Non-Hodgkin's Lymphoma (NHL)1
1Active Not RecruitingTreatmentHormone Receptor Positive, HER2-negative, Advanced Breast Cancer1
1Active Not RecruitingTreatmentNon-Hodgkin's Lymphoma (NHL) / Non-Hodgkin's Lymphoma, Solid Cancers / Solid Cancers1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceNormal Healthy Volunteers1
1CompletedOtherHealthy Volunteers1
1CompletedOtherSolid Malignancies1
1CompletedTreatmentAdvanced Breast Cancer1
1CompletedTreatmentAdvanced Solid Malignancies / Breast Cancer - ER+, HER2 - / Breast Cancer - ER+, HER2-, PIK3CA Gene Mutation1
1CompletedTreatmentBreast Cancer2
1CompletedTreatmentEstrogen Receptor Positive / Invasive Breast Carcinoma / Recurrent Breast Carcinoma / Stage IV Breast Cancer / Stage IV Breast Cancer AJCC v6 and v71
1CompletedTreatmentEstrogen Receptor Positive / Progesterone Receptor Positive / Recurrent Breast Carcinoma / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
1CompletedTreatmentEstrogen Receptor-Positive Breast Cancer / Recurrent Breast Cancer / Stage IV Breast Cancer1
1CompletedTreatmentMalignant Lymphomas / Tumors, Solid1
1CompletedTreatmentPostmenopausal Women With ER+ HER2- Primary Breast Cancer1
1Not Yet RecruitingTreatmentAdvanced Breast Cancer / BRCA1 Mutations / BRCA2 Mutation / Locally Advanced Breast Cancer (LABC) / Metastatic Breast Cancer (MBC)1
1Not Yet RecruitingTreatmentAnatomic Stage III Breast Cancer AJCC v8 / Anatomic Stage IIIA Breast Cancer AJCC v8 / Anatomic Stage IIIB Breast Cancer AJCC v8 / Anatomic Stage IIIC Breast Cancer AJCC v8 / Anatomic Stage IV Breast Cancer AJCC v8 / Estrogen Receptor Positive / HER2/Neu Negative / Invasive Breast Carcinoma / Prognostic Stage III Breast Cancer AJCC v8 / Prognostic Stage IIIA Breast Cancer AJCC v8 / Prognostic Stage IIIB Breast Cancer AJCC v8 / Prognostic Stage IIIC Breast Cancer AJCC v8 / Prognostic Stage IV Breast Cancer AJCC v8 / Recurrent Breast Carcinoma1
1RecruitingOtherBreast Cancer1
1RecruitingTreatmentAdvanced Solid Tumors / Breast Cancer / Prostate Cancer1
1RecruitingTreatmentAdvanced or Metastatic Breast Cancer1
1RecruitingTreatmentBreast Cancer3
1RecruitingTreatmentBreast Cancer / Tumors, Solid1
1RecruitingTreatmentHER2-Negative Breast Cancer / Metastatic Epithelial Ovarian Cancer / Metastatic Hormone-Receptor-Positive (HR+) Breast Cancer1
1RecruitingTreatmentHormone Receptor Positive Breast Cancer / Human Epidermal Growth Factor 2 Negative Carcinoma of Breast / Metastatic Breast Cancer (MBC)1
1RecruitingTreatmentMalignancies / Tumors, Solid1
1RecruitingTreatmentMetastatic Breast Cancer (MBC)1
1RecruitingTreatmentNeoplasms, Breast1
1RecruitingTreatmentNeoplasms / Neoplasms, Breast1
1TerminatedTreatmentAdvanced Estrogen Receptor Positive HER2- Breast Cancer1
1TerminatedTreatmentBreast Cancer1
1WithdrawnTreatmentNon Small Cell Lung Carcinoma (NSCLC)1
1, 2Active Not RecruitingTreatmentBreast Cancer1
1, 2Active Not RecruitingTreatmentEstrogen Receptor Positive Breast Cancer1
1, 2CompletedTreatmentER+ Breast Cancer / FGFR Inhibition, Pharmacokinetics, Biomarkers1
1, 2Not Yet RecruitingTreatmentAnatomic Stage IV Breast Cancer AJCC v8 / Breast Carcinoma Metastatic in the Brain / Estrogen Receptor Positive / HER2/Neu Negative / Metastatic Breast Carcinoma / Metastatic Malignant Neoplasm in the Brain / One to five years postmenopausal / Prognostic Stage IV Breast Cancer AJCC v81
1, 2Not Yet RecruitingTreatmentAnatomic Stage IV Breast Cancer AJCC v8 / ERBB2 Gene Amplification Negative / Estrogen Receptor Positive / HER2/Neu Negative / Hormone Receptor Positive Breast Carcinoma / Metastatic Breast Carcinoma / Progesterone Receptor Positive / Prognostic Stage IV Breast Cancer AJCC v8 / Progressive Disease / Recurrent Breast Carcinoma1
1, 2RecruitingTreatmentAdvanced Breast Cancer1
1, 2RecruitingTreatmentAdvanced Solid Malignancies1
1, 2RecruitingTreatmentBreast Cancer1
1, 2RecruitingTreatmentBreast Cancer / Carcinoma, Ductal, Breast / Neoplasms, Breast1
1, 2RecruitingTreatmentNeoplasms, Breast1
1, 2TerminatedTreatmentBreast Cancer1
1, 2TerminatedTreatmentER-positive Breast Cancer / Her2-Positive Breast Cancer1
1, 2WithdrawnTreatmentColorectal Cancers1
1, 2WithdrawnTreatmentHead and Neck Squamous Cell Carcinoma (HNSCC)1
1, 2WithdrawnTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1, 2WithdrawnTreatmentOvarian Cancer1
1, 2WithdrawnTreatmentTransitional Cell Carcinoma1
2Active Not RecruitingOtherNeoplasms, Breast1
2Active Not RecruitingTreatmentBreast Cancer7
2Active Not RecruitingTreatmentBreast Cancer Invasive Nos1
2Active Not RecruitingTreatmentBreast Cancer / Hormone Receptor Positive Tumor / Human Epidermal Growth Factor 2 Negative Carcinoma of Breast1
2Active Not RecruitingTreatmentEndometrial Cancers / Recurrent Uterine Corpus Carcinoma / Stage III Uterine Corpus Cancer / Stage III Uterine Corpus Cancer AJCC v7 / Stage IV Uterine Corpus Cancer / Stage IV Uterine Corpus Cancer AJCC v71
2Active Not RecruitingTreatmentEstrogen Receptor Positive / Recurrent Breast Carcinoma / Stage III Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
2Active Not RecruitingTreatmentEstrogen Receptor-Positive Breast Cancer / HER2-Negative Breast Cancer / Progesterone Receptor-positive Breast Cancer / Recurrent Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
2Active Not RecruitingTreatmentHER-2 Positive Breast Cancer / Hormone Receptor Positive Tumor1
2Active Not RecruitingTreatmentMcCune-Albright Syndrome / Puberty, Precocious1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)3
2Active Not RecruitingTreatmentNeoplasms, Breast2
2Active Not RecruitingTreatmentStage IV Lung Cancer1
2CompletedTreatmentAdvanced Breast Cancer2
2CompletedTreatmentAdvanced Breast Cancer / Metastatic Breast Cancer (MBC)2
2CompletedTreatmentBreast Cancer14
2CompletedTreatmentBreast Cancer / Neoplasms, Breast1
2CompletedTreatmentEndometrial Carcinoma1
2CompletedTreatmentEstrogen Receptor-Positive Breast Cancer / Progesterone Receptor-positive Breast Cancer / Recurrent Breast Cancer / Stage IV Breast Cancer1
2CompletedTreatmentEstrogen Receptor-Positive Breast Cancer / Recurrent Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
2CompletedTreatmentLung Cancers1
2CompletedTreatmentMetastatic Breast Cancer (MBC)6
2CompletedTreatmentNeoplasms, Breast2
2CompletedTreatmentOvarian Cancer1
2CompletedTreatmentProstate Cancer1
2CompletedTreatmentProstate Cancer / Prostatic Neoplasms1
2CompletedTreatmentPulmonary Arterial Hypertension (PAH)1
2CompletedTreatmentSystemic Lupus Erythematosus (SLE)1
2Not Yet RecruitingTreatmentBreast Cancer / HR+/HER2-negative Breast Cancer / Metastasis1
2Not Yet RecruitingTreatmentFGFR2 Amplification / Metastatic Breast Cancer (MBC)1
2Not Yet RecruitingTreatmentNeoplasms, Breast1
2RecruitingBasic ScienceBreast Cancer1
2RecruitingOtherAdvanced Breast Cancer1
2RecruitingOtherLobular Breast Carcinoma / Malignant Neoplasm of Stomach1
2RecruitingTreatmentAdenocarcinoma of Endometrium1
2RecruitingTreatmentAdenosarcoma of Uterus / Endometrial Cancers / Leiomyosarcoma Uterus / Sarcoma, Endometrial Stromal / Serous Ovarian Tumor / Sex Cord Stromal Tumor1
2RecruitingTreatmentAdvanced Breast Cancer / Breast Cancer / Hormone Receptor Positive Tumor / Human Epidermal Growth Factor 2 Negative Carcinoma of Breast1
2RecruitingTreatmentAnatomic Stage IV Breast Cancer AJCC v8 / Estrogen Receptor Positive / HER2/Neu Negative / Metastatic Breast Carcinoma / Metastatic Malignant Neoplasm in the Bone / Progesterone Receptor Positive / Prognostic Stage IV Breast Cancer AJCC v81
2RecruitingTreatmentBreast Cancer9
2RecruitingTreatmentBreast Cancer Metastatic3
2RecruitingTreatmentBreast Cancer, PI3K, Alpelisib1
2RecruitingTreatmentBreast Cancer / Cancer of the Breast / Carcinoma, Breast / Malignant Tumor of Breast1
2RecruitingTreatmentBreast Cancer / Cancer of the Breast / Neoplasms, Breast1
2RecruitingTreatmentBreast Cancer / Her2-Positive Breast Cancer1
2RecruitingTreatmentCarcinoma, Breast / Metastatic Breast Cancer (MBC)1
2RecruitingTreatmentA Germline or Somatic BRCA Mutation, or a Deleterious Alteration of Other Genes Involved in Homologous Recombination Repair (HRR) or in MSI Status / ER-positive and HER2-negative Metastatic or Locally Advanced Breast Cancer1
2RecruitingTreatmentEstrogen Receptor Negative / Estrogen Receptor Positive / Estrogen Receptor Status / HER2/Neu Negative / Invasive Breast Carcinoma / One to five years postmenopausal / Stage III Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
2RecruitingTreatmentEstrogen Receptor Positive Breast Cancer1
2RecruitingTreatmentEstrogen Receptor and/or Progesterone Receptor Positive / HER2/Neu Negative / Stage IA Breast Cancer / Stage IB Breast Cancer / Stage IIA Breast Cancer / Stage IIB Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
2RecruitingTreatmentEstrogen Receptor-Positive Breast Cancer / HER2/Neu Negative / Stage IV Breast Cancer AJCC v6 and v71
2RecruitingTreatmentEstrogen Receptor-positive (ER+)/Human Epidermal Growth Factor Receptor (HER2)-Negative Locally Advanced or Metastatic Breast Cancer1
2RecruitingTreatmentFemale Breast Carcinoma / Female Ductal Carcinoma In Situ1
2RecruitingTreatmentFibrolamellar Carcinoma / Malignant Solid Tumours / Tumors, Solid1
2RecruitingTreatmentLocally Advanced or Metastatic Breast Cancer1
2RecruitingTreatmentMalignancies / Neoplasms1
2RecruitingTreatmentMalignant Neoplasms of Female Genital Organs1
2RecruitingTreatmentMetastatic Breast Cancer (MBC)4
2RecruitingTreatmentNeoplasms1
2RecruitingTreatmentNeoplasms, Breast2
2TerminatedTreatmentBreast Cancer4
2TerminatedTreatmentCarcinoma, Breast1
2TerminatedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Postmenopausal Women1
2TerminatedTreatmentMetastatic Breast Cancer (MBC)4
2TerminatedTreatmentNeoplasms, Breast4
2TerminatedTreatmentNon Small Cell Lung Carcinoma (NSCLC)1
2TerminatedTreatmentProstate Cancer1
2Unknown StatusTreatmentBreast Cancer3
2Unknown StatusTreatmentBreast Cancer Nos Premenopausal / Estrogen Receptor Positive Tumor / Metastatic Breast Cancer (MBC)1
2Unknown StatusTreatmentMetastatic Breast Cancer (MBC)1
2WithdrawnTreatmentBreast Cancer1
2WithdrawnTreatmentBreast Cancer Metastatic1
2WithdrawnTreatmentEstrogen Receptor Positive / HER2/Neu Negative / Progesterone Receptor Positive / Stage IV Breast Cancer AJCC v6 and v71
2, 3Active Not RecruitingTreatmentHormone Receptor Positive HER-2 Negative Breast Cancer / HR+ HER2 Negative Breast Cancer1
2, 3CompletedTreatmentTumors, Solid1
3Active Not RecruitingTreatmentAdvanced Breast Cancer / Antineoplastic Agents / Antineoplastic Agents, Hormonal / Breast Diseases / Estrogen Receptor Antagonists / Fulvestrant / Hormone Antagonists / Hormones, Hormone Substitutes, and Hormone Antagonists / Molecular Mechanisms of Pharmacological Action / Neoplasms / Neoplasms by Site / Neoplasms, Breast / Pharmacologic Actions / Therapeutic Uses1
3Active Not RecruitingTreatmentBreast Cancer5
3Active Not RecruitingTreatmentEstrogen Receptor Positive / HER2 Positive Breast Carcinoma / HER2/Neu Negative / Progesterone Receptor Positive / Recurrent Breast Carcinoma / Stage IIIB Breast Cancer / Stage IIIB Breast Cancer AJCC v7 / Stage IIIC Breast Cancer / Stage IIIC Breast Cancer AJCC v7 / Stage IV Breast Cancer / Stage IV Breast Cancer AJCC v6 and v71
3Active Not RecruitingTreatmentEstrogen Receptor-Positive Breast Cancer / HER2-Negative Breast Cancer / Invasive Ductal Breast Carcinoma / Invasive Lobular Breast Carcinoma / Recurrent Breast Cancer / Stage II Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
3Active Not RecruitingTreatmentHormone Receptor Positive Breast Cancer1
3Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)3
3CompletedTreatmentAdvanced Breast Cancer2
3CompletedTreatmentBreast Cancer5
3CompletedTreatmentBreast Cancer / Metastasis1
3CompletedTreatmentLocally Advanced Breast Cancer (LABC) / Metastatic Breast Cancer (MBC)1
3CompletedTreatmentProgression-free Survival1
3Not Yet RecruitingTreatmentCancer Metastatic1
3RecruitingDiagnosticMetastatic Breast Cancer (MBC)1
3RecruitingTreatmentBreast Cancer2
3RecruitingTreatmentBreast Cancer / HER 2 Negative Breast Cancer / Hormone Receptor Positive Tumor1
3RecruitingTreatmentBreast Cancer / Hormone Receptor Positive Tumor / Human Epidermal Growth Factor 2 Negative Carcinoma of Breast / Locally Advanced Malignant Neoplasm / Metastatic Breast Cancer (MBC)1
3RecruitingTreatmentBreast Neoplasm Female2
3RecruitingTreatmentEstrogen Receptor Positive Breast Cancer / HER-2 Positive Breast Cancer1
3RecruitingTreatmentMetastatic Breast Cancer (MBC)2
3RecruitingTreatmentNeoplasms, Breast1
3SuspendedTreatmentBreast Cancer1
3TerminatedTreatmentBreast Cancer2
3TerminatedTreatmentMetastatic Breast Cancer (MBC) / Metastatic Breast Cancer HR+, HER2-1
3Unknown StatusTreatmentBreast Cancer2
4Active Not RecruitingOtherLocally Advanced or / Metastatic Breast Cancer (MBC)1
4Not Yet RecruitingTreatmentMetastatic Breast Cancer (MBC)1
4RecruitingTreatmentMetastatic Breast Cancer (MBC)2
4RecruitingTreatmentNeoplasms, Breast1
Not AvailableCompletedNot AvailableBreast Cancer2
Not AvailableCompletedNot AvailableMalignant Neoplasm of Breast Stage IV1
Not AvailableCompletedTreatmentMetastatic Breast Cancer (MBC)1
Not AvailableRecruitingNot AvailableHR+ HER2- Men, Pre/Postmenopausal Advanced Breast Cancer / HR+ HER2- Postmenopausal Advanced Breast Cancer1
Not AvailableRecruitingNot AvailableMetastatic Breast Cancer (MBC)1
Not AvailableRecruitingTreatmentBreast Cancer1
Not AvailableUnknown StatusTreatmentBreast Cancer1

Pharmacoeconomics

Manufacturers
  • Astrazeneca pharmaceuticals lp
Packagers
  • AstraZeneca Inc.
  • Vetter Pharma Fertigung GmbH and Co. KG
Dosage forms
FormRouteStrength
InjectionIntramuscular50 mg/1mL
Injection, solutionIntramuscular250 mg/5ml
SolutionIntramuscular50 mg
InjectionIntramuscular250 mg/5mL
Injection, solutionIntramuscular50 mg/1mL
SolutionIntramuscular
Prices
Unit descriptionCostUnit
Faslodex 125 mg/2.5 ml syringe240.83USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2351004No2003-02-182021-01-08Canada
US6774122Yes2004-08-102021-07-09Us
US7456160Yes2008-11-252021-07-09Us
US8329680Yes2012-12-112021-07-09Us
US8466139Yes2013-06-182021-07-09Us
US10188663No2019-01-292034-02-14Us
US9271990No2016-03-012034-05-17Us
US9833459No2017-12-052034-02-14Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP8.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00672 mg/mLALOGPS
logP6.54ALOGPS
logP7.57ChemAxon
logS-5ALOGPS
pKa (Strongest Acidic)10.32ChemAxon
pKa (Strongest Basic)-0.88ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area57.53 Å2ChemAxon
Rotatable Bond Count15ChemAxon
Refractivity155.34 m3·mol-1ChemAxon
Polarizability65.88 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9217
Caco-2 permeable-0.5095
P-glycoprotein substrateSubstrate0.722
P-glycoprotein inhibitor INon-inhibitor0.6251
P-glycoprotein inhibitor IINon-inhibitor0.967
Renal organic cation transporterNon-inhibitor0.7568
CYP450 2C9 substrateNon-substrate0.7667
CYP450 2D6 substrateNon-substrate0.7737
CYP450 3A4 substrateSubstrate0.6945
CYP450 1A2 substrateNon-inhibitor0.6842
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.658
CYP450 3A4 inhibitorInhibitor0.7959
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6701
Ames testNon AMES toxic0.6318
CarcinogenicityNon-carcinogens0.75
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6310 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6158
hERG inhibition (predictor II)Inhibitor0.7955
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Details
1. Estrogen receptor alpha
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Zinc ion binding
Specific Function
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissu...
Gene Name
ESR1
Uniprot ID
P03372
Uniprot Name
Estrogen receptor
Molecular Weight
66215.45 Da
References
  1. Curran M, Wiseman L: Fulvestrant. Drugs. 2001;61(6):807-13; discussion 814. [PubMed:11398912]
  2. Elkak AE, Mokbel K: Pure antiestrogens and breast cancer. Curr Med Res Opin. 2001;17(4):282-9. [PubMed:11922402]
  3. Dow KH: Existing and emerging endocrine therapies for breast cancer. Cancer Nurs. 2002 Apr;25 Suppl 2:6S-11S. [PubMed:12080538]
  4. Bundred N, Howell A: Fulvestrant (Faslodex): current status in the therapy of breast cancer. Expert Rev Anticancer Ther. 2002 Apr;2(2):151-60. [PubMed:12113237]
  5. Morris C, Wakeling A: Fulvestrant ('Faslodex')--a new treatment option for patients progressing on prior endocrine therapy. Endocr Relat Cancer. 2002 Dec;9(4):267-76. [PubMed:12542403]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  7. Kabos P, Borges VF: Fulvestrant: a unique antiendocrine agent for estrogen-sensitive breast cancer. Expert Opin Pharmacother. 2010 Apr;11(5):807-16. doi: 10.1517/14656561003641982. [PubMed:20151846]
  8. McKeage K, Curran MP, Plosker GL: Fulvestrant: a review of its use in hormone receptor-positive metastatic breast cancer in postmenopausal women with disease progression following antiestrogen therapy. Drugs. 2004;64(6):633-48. [PubMed:15018596]
  9. Jones SE, Pippen J: Effectiveness and tolerability of fulvestrant in postmenopausal women with hormone receptor-positive breast cancer. Clin Breast Cancer. 2005 Apr;6 Suppl 1:S9-14. [PubMed:15865850]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
The FDA label for Fluvesrant indicates that this enzyme action is unlikely to be involved in any drug interactions. No dose adjustments are recommended.
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Robertson JF, Harrison M: Fulvestrant: pharmacokinetics and pharmacology. Br J Cancer. 2004 Mar;90 Suppl 1:S7-10. doi: 10.1038/sj.bjc.6601630. [PubMed:15094758]
  2. Rocca A, Maltoni R, Bravaccini S, Donati C, Andreis D: Clinical utility of fulvestrant in the treatment of breast cancer: a report on the emerging clinical evidence. Cancer Manag Res. 2018 Aug 30;10:3083-3099. doi: 10.2147/CMAR.S137772. eCollection 2018. [PubMed:30214302]
  3. Fluvestrant FDA label [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A1
Uniprot ID
P22309
Uniprot Name
UDP-glucuronosyltransferase 1-1
Molecular Weight
59590.91 Da
References
  1. Dancygier H. (2010). Clinical Hepatology. Springer-Verlag. [ISBN:978-3-642-04509-7]

Drug created on June 13, 2005 07:24 / Updated on November 16, 2019 10:30