Chemical: Drug
fulvestrant

PharmGKB contains no prescribing info for this . Contact us to report known genotype-based dosing guidelines, or if you are interested in developing guidelines.


Annotated Labels

  1. Annotation of FDA Label for fulvestrant and ESR1,PGR
  2. Annotation of EMA Label for fulvestrant and ESR1,ESR2,MKI67
  3. Annotation of PMDA Label for fulvestrant and ESR1,ESR2


last updated 10/25/2013

2. Annotation of EMA Label for fulvestrant and ESR1,ESR2,MKI67

Testing required

Summary

The EMA European Public Assessment Report (EPAR) contains biomarker information regarding the indication of Fulvestrant (Faslodex) in postmenopausal women with estrogen receptor positive breast cancer due to its mechanism of action.

There's more of this label. Read more.


3. Annotation of PMDA Label for fulvestrant and ESR1,ESR2

Testing required

Summary

The PMDA package insert for fulvestrant states that it is indicated for postmenopausal women with hormone-receptor positive breast cancer, and that fulvestrant should not be used in women negative for hormone receptor.

There's more of this label. Read more.


PharmGKB contains no Clinical Variants that meet the highest level of criteria.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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Overview

Generic Names
  • ICI 182,780
  • fulvestrant
Trade Names
  • Faslodex
Brand Mixture Names

PharmGKB Accession Id

PA164747170

Type(s):

Drug

Other Vocabularies

Chemical Properties

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

Source: PubChem

InChI String

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

Source: PubChem

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

EvidenceGene
No Dosing Guideline available DL No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
CYP3A4
No Dosing Guideline available DL No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
ESR1
No Dosing Guideline available DL No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
ESR2
No Dosing Guideline available DL No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
MKI67
No Dosing Guideline available DL No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
PGR

Drug Targets

Gene Description
ESR1 (source: Drug Bank )

Curated Information ?

EvidenceDrug
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
anastrozole

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to fulvestrant: 7

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Fulvestrant decreases anastrozole drug concentrations when taken concurrently by patients with metastatic breast cancer treated on SWOG study S0226. British journal of clinical pharmacology. 2016. Hertz Daniel L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Activating ESR1 mutations in hormone-resistant metastatic breast cancer. Nature genetics. 2013. Robinson Dan R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
ESR1 ligand-binding domain mutations in hormone-resistant breast cancer. Nature genetics. 2013. Toy Weiyi, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Challenges in pharmacogenetics. European journal of clinical pharmacology. 2013. Cascorbi Ingolf, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Adenosine A1 receptor, a target and regulator of estrogen receptoralpha action, mediates the proliferative effects of estradiol in breast cancer. Oncogene. 2010. Lin Z, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Family 1 uridine-5'-diphosphate glucuronosyltransferases (UGT1A): from Gilbert's syndrome to genetic organization and variability. Archives of toxicology. 2008. Strassburg Christian P, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
An intron 1 enhancer element mediates oestrogen-induced suppression of ERBB2 expression. Oncogene. 1997. Bates N P, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0310-0720-50
DrugBank:
DB00947
ChEBI:
31638
KEGG Drug:
D01161
PubChem Compound:
104741
IUPHAR Ligand:
1015
Drugs Product Database (DPD):
2248624
BindingDB:
50169743
Therapeutic Targets Database:
DAP000319
FDA Drug Label at DailyMed:
83d7a440-e904-4e36-afb5-cb02b1c919f7

Clinical Trials

These are trials that mention fulvestrant and are related to either pharmacogenetics or pharmacogenomics.

No trials loaded.

NURSA Datasets

provided by nursa.org

No NURSA datasets available.

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Sources for PharmGKB drug information: DrugBank, PubChem.