fulvestrant Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
1255 129453-61-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ZD9238
  • fulvestrant
  • faslodex
  • ICI 182,780
  • Molecular weight: 606.78
  • Formula: C32H47F5O3S
  • CLOGP: 7.35
  • LIPINSKI: 2
  • HAC: 3
  • HDO: 2
  • TPSA: 57.53
  • ALOGS: -4.96
  • ROTB: 15

Drug dosage:

DoseUnitRoute
8.30 mg P

Approvals:

DateAgencyCompanyOrphan
March 10, 2004 EMA
April 25, 2002 FDA ASTRAZENECA

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Malignant neoplasm progression 848.90 32.26 220 2088 17573 3365978
Disease progression 482.80 32.26 163 2145 32096 3351455
Breast cancer metastatic 412.74 32.26 81 2227 1752 3381799
Metastases to bone 410.82 32.26 88 2220 2973 3380578
Metastases to liver 371.26 32.26 85 2223 3911 3379640
Pseudocirrhosis 301.44 32.26 40 2268 38 3383513
Neoplasm progression 297.81 32.26 75 2233 5169 3378382
Fatigue 266.68 32.26 153 2155 107087 3276464
Breast cancer 211.86 32.26 63 2245 8054 3375497
Nausea 195.68 32.26 135 2173 129510 3254041
Dyspnoea 173.63 32.26 115 2193 102819 3280732
Neutropenia 164.88 32.26 76 2232 33310 3350241
Cough 152.06 32.26 76 2232 39782 3343769
Asthenia 136.79 32.26 84 2224 65581 3317970
Tumour marker increased 129.04 32.26 25 2283 498 3383053
Portal hypertension 123.07 32.26 27 2281 1008 3382543
White blood cell count decreased 114.32 32.26 54 2254 24893 3358658
Injection site pain 110.11 32.26 61 2247 39187 3344364
Pulmonary embolism 105.63 32.26 53 2255 27835 3355716
Diarrhoea 93.37 32.26 80 2228 104268 3279283
Product use issue 93.31 32.26 41 2267 15960 3367591
Pleural effusion 90.12 32.26 42 2266 18737 3364814
Metastases to lung 85.89 32.26 24 2284 2440 3381111
Off label use 84.91 32.26 58 2250 53919 3329632
Hot flush 84.85 32.26 31 2277 7470 3376081
Metastases to lymph nodes 84.51 32.26 21 2287 1354 3382197
Alopecia 83.54 32.26 40 2268 18946 3364605
Arthralgia 80.90 32.26 59 2249 60802 3322749
Breast cancer female 79.00 32.26 20 2288 1391 3382160
Back pain 77.27 32.26 48 2260 37957 3345594
Hepatic failure 67.62 32.26 29 2279 10623 3372928
Decreased appetite 66.15 32.26 45 2263 41445 3342106
Vomiting 64.79 32.26 61 2247 89470 3294081
Bone pain 63.36 32.26 27 2281 9734 3373817
Oestradiol increased 61.70 32.26 10 2298 66 3383485
Breast cancer recurrent 61.21 32.26 14 2294 631 3382920
Dizziness 60.89 32.26 55 2253 76457 3307094
Constipation 60.27 32.26 38 2270 30774 3352777
Metastases to central nervous system 60.14 32.26 19 2289 2944 3380607
Aspartate aminotransferase increased 59.56 32.26 33 2275 21080 3362471
Hypoaesthesia 57.05 32.26 34 2274 24905 3358646
Alanine aminotransferase increased 53.47 32.26 32 2276 23608 3359943
Pain 52.16 32.26 49 2259 71508 3312043
Blood bilirubin increased 51.89 32.26 24 2284 10485 3373066
Metastases to skin 50.81 32.26 10 2298 216 3383335
Pain in extremity 50.57 32.26 41 2267 49171 3334380
Neuropathy peripheral 49.40 32.26 27 2281 16780 3366771
Metastasis 48.62 32.26 14 2294 1583 3381968
RET gene mutation 47.45 32.26 6 2302 2 3383549
Thrombocytopenia 46.30 32.26 34 2274 35234 3348317
Stomatitis 46.16 32.26 23 2285 11829 3371722
Throat irritation 45.80 32.26 18 2290 5276 3378275
Death 45.78 32.26 66 2242 152258 3231293
Rash 45.02 32.26 45 2263 70776 3312775
Ascites 45.00 32.26 21 2287 9356 3374195
Platelet count decreased 44.21 32.26 30 2278 27438 3356113
Dehydration 43.18 32.26 32 2276 33617 3349934
Anaemia 43.03 32.26 39 2269 54294 3329257
Lymphoedema 42.96 32.26 12 2296 1215 3382336
Osteonecrosis of jaw 42.75 32.26 21 2287 10475 3373076
Dysgeusia 41.06 32.26 21 2287 11403 3372148
Paraesthesia 39.43 32.26 28 2280 27520 3356031
Invasive ductal breast carcinoma 39.42 32.26 10 2298 700 3382851
Neuralgia 38.88 32.26 14 2294 3225 3380326
Injection site extravasation 37.99 32.26 13 2295 2580 3380971
Injection site necrosis 36.42 32.26 9 2299 566 3382985
Tongue neoplasm malignant stage unspecified 36.30 32.26 8 2300 304 3383247
Ejection fraction decreased 35.51 32.26 14 2294 4133 3379418
Drug intolerance 34.78 32.26 19 2289 11779 3371772
Injection site haematoma 33.81 32.26 12 2296 2651 3380900
Pyrexia 33.27 32.26 41 2267 81074 3302477
Hypertension 33.18 32.26 29 2279 38437 3345114
Peripheral motor neuropathy 32.88 32.26 8 2300 471 3383080
Hypersensitivity 32.37 32.26 25 2283 27875 3355676
Hepatic lesion 32.36 32.26 9 2299 897 3382654

Pharmacologic Action:

SourceCodeDescription
ATC L02BA03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONE ANTAGONISTS AND RELATED AGENTS
Anti-estrogens
FDA MoA N0000000168 Selective Estrogen Receptor Modulators
MeSH PA D000970 Antineoplastic Agents
MeSH PA D018931 Antineoplastic Agents, Hormonal
MeSH PA D004965 Estrogen Antagonists
MeSH PA D065171 Estrogen Receptor Antagonists
MeSH PA D006727 Hormone Antagonists
MeSH PA D006730 Hormones, Hormone Substitutes, and Hormone Antagonists
CHEBI has role CHEBI:50792 estrogen receptor antagonist
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:50837 estrogen antagonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Metastatic Breast Cancer Progression Post-Antiestrogen Therapy indication
Blood coagulation disorder contraindication 64779008 DOID:1247
Disease of liver contraindication 235856003 DOID:409
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Breastfeeding (mother) contraindication 413712001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.92 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 6774122 Jan. 9, 2021 TREATMENT OF HORMONE RECEPTOR POSITIVE HER2-NEGATIVE ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN NOT PREVIOUSLY TREATED WITH ENDOCRINE THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 6774122 Jan. 9, 2021 TREATMENT OF HORMONE RECEPTOR POSITIVE METASTATIC BREAST CANCER IN POSTMENOPAUSAL WOMEN WITH DISEASE PROGRESSION FOLLOWING ANTIESTROGEN THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 6774122 Jan. 9, 2021 TREATMENT OF HR-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER IN COMBINATION WITH PALBOCOCLIB IN WOMEN WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 6774122 Jan. 9, 2021 TREATMENT OF HR-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER-2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER IN COMBINATION WITH PALBOCOCLIB OR ABEMACICLIB IN WOMEN WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 7456160 Jan. 9, 2021 TREATMENT OF HORMONE RECEPTOR POSITIVE HER2-NEGATIVE ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN NOT PREVIOUSLY TREATED WITH ENDOCRINE THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 7456160 Jan. 9, 2021 TREATMENT OF HORMONE RECEPTOR POSITIVE METASTATIC BREAST CANCER IN POSTMENOPAUSAL WOMEN WITH DISEASE PROGRESSION FOLLOWING ANTIESTROGEN THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 7456160 Jan. 9, 2021 TREATMENT OF HR-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER IN COMBINATION WITH PALBOCOCLIB IN WOMEN WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 7456160 Jan. 9, 2021 TREATMENT OF HR-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER-2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER IN COMBINATION WITH PALBOCOCLIB OR ABEMACICLIB IN WOMEN WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 8329680 Jan. 9, 2021 TREATMENT OF HORMONE RECEPTOR POSITIVE HER2-NEGATIVE ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN NOT PREVIOUSLY TREATED WITH ENDOCRINE THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 8329680 Jan. 9, 2021 TREATMENT OF HORMONE RECEPTOR POSITIVE METASTATIC BREAST CANCER IN POSTMENOPAUSAL WOMEN WITH DISEASE PROGRESSION FOLLOWING ANTIESTROGEN THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 8329680 Jan. 9, 2021 TREATMENT OF HR-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER IN COMBINATION WITH PALBOCOCLIB IN WOMEN WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 8329680 Jan. 9, 2021 TREATMENT OF HR-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER-2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER IN COMBINATION WITH PALBOCOCLIB OR ABEMACICLIB IN WOMEN WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 8466139 Jan. 9, 2021 TREATMENT OF HORMONE RECEPTOR POSITIVE HER2-NEGATIVE ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN NOT PREVIOUSLY TREATED WITH ENDOCRINE THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 8466139 Jan. 9, 2021 TREATMENT OF HORMONE RECEPTOR POSITIVE METASTATIC BREAST CANCER IN POSTMENOPAUSAL WOMEN WITH DISEASE PROGRESSION FOLLOWING ANTIESTROGEN THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 8466139 Jan. 9, 2021 TREATMENT OF HR-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER IN COMBINATION WITH PALBOCOCLIB IN WOMEN WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR 8466139 Jan. 9, 2021 TREATMENT OF HR-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER-2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER IN COMBINATION WITH PALBOCOCLIB OR ABEMACICLIB IN WOMEN WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR Feb. 19, 2019 TREATMENT OF HORMONE RECEPTOR (HR)-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER IN COMBINATION THERAPY WITH PALBOCICLIB AND FULVESTRANT IN WOMEN WITH DISEASE PROGRESSION FOLLOWING ENDOCRINE THERAPY.
50MG/ML FASLODEX ASTRAZENECA N021344 April 25, 2002 RX INJECTABLE INTRAMUSCULAR Aug. 25, 2020 MONOTHERAPY FOR THE TREATMENT OF HORMONE RECEPTOR (HR) POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE, ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN NOT PREVIOUSLY TREATED WITH ENDOCRINE THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Estrogen receptor beta Nuclear hormone receptor ANTAGONIST Ki 8.74 WOMBAT-PK CHEMBL
Estrogen receptor Nuclear hormone receptor ANTAGONIST Ki 9.62 WOMBAT-PK CHEMBL
G-protein coupled estrogen receptor 1 GPCR EC50 7 WOMBAT-PK
Nuclear receptor subfamily 1 group I member 2 Nuclear hormone receptor EC50 5.71 CHEMBL
Bile acid receptor Nuclear hormone receptor IC50 6.10 CHEMBL
Bifunctional epoxide hydrolase 2 Enzyme Ki 7.59 CHEMBL
Steroid hormone receptor ERR1 Nuclear hormone receptor IC50 8.70 CHEMBL
Progesterone receptor Nuclear hormone receptor IC50 9.68 CHEMBL
Estrogen receptor Transcription factor IC50 8.23 CHEMBL

External reference:

IDSource
1015 IUPHAR_LIGAND_ID
4021350 VUID
N0000148770 NUI
C0935916 UMLSCUI
D01161 KEGG_DRUG
22X328QOC4 UNII
7712 INN_ID
DB00947 DRUGBANK_ID
d04799 MMSL
16618 MMSL
282357 RXNORM
385519002 SNOMEDCT_US
404845006 SNOMEDCT_US
4021350 VANDF
N0000010122 NDFRT
N0000148770 NDFRT
009642 NDDF
CHEMBL1358 ChEMBL_ID
C070081 MESH_SUPPLEMENTAL_RECORD_UI
104741 PUBCHEM_CID
CHEBI:31638 CHEBI
FVS PDB_CHEM_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
FASLODEX HUMAN PRESCRIPTION DRUG LABEL 1 0310-0720 INJECTION 50 mg INTRAMUSCULAR NDA 18 sections