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fulvestrant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
estrogen antagonists, including estrogen receptor down-regulators	1255	129453-61-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ZD9238 fulvestrant faslodex ICI 182,780	An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer. Molecular weight: 606.78 Formula: C32H47F5O3S CLOGP: 7.54 LIPINSKI: 2 HAC: 3 HDO: 2 TPSA: 57.53 ALOGS: -4.96 ROTB: 15 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ZD9238
fulvestrant
faslodex
ICI 182,780

An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.

Molecular weight: 606.78
Formula: C32H47F5O3S
CLOGP: 7.54
LIPINSKI: 2
HAC: 3
HDO: 2
TPSA: 57.53
ALOGS: -4.96
ROTB: 15

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
8.30	mg	P

ADMET properties:

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Property	Value	Reference
Vd (Volume of distribution)	4.15 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	16 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	11.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	0.10 %	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.00 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
April 25, 2002	FDA	ASTRAZENECA
March 10, 2004	EMA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Malignant neoplasm progression	4083.97	15.02	1860	60472	80261	63346429
Metastases to bone	2757.91	15.02	961	61371	20058	63406632
Neoplasm progression	2566.44	15.02	1057	61275	35371	63391319
Metastases to liver	2242.95	15.02	851	61481	22788	63403902
Neutropenia	1377.90	15.02	1233	61099	173772	63252918
White blood cell count decreased	872.56	15.02	865	61467	138239	63288451
Tumour marker increased	762.01	15.02	255	62077	4660	63422030
Metastases to lung	694.94	15.02	309	62023	12441	63414249
Osteonecrosis of jaw	550.56	15.02	373	61959	34750	63391940
Disease progression	522.97	15.02	623	61709	122135	63304555

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Xerosis	53.10	49.57	9	521	595	34955806

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Neoplasm progression	2136.84	15.34	898	48428	50784	79644278
Metastases to bone	1780.38	15.34	641	48685	23786	79671276
Malignant neoplasm progression	1776.11	15.34	1082	48244	134908	79560154
Metastases to liver	1317.99	15.34	536	48790	27778	79667284
Neutropenia	935.56	15.34	1014	48312	286696	79408366
White blood cell count decreased	919.66	15.34	829	48497	187459	79507603
Tumour marker increased	582.79	15.34	180	49146	4092	79690970
Fatigue	498.70	15.34	1476	47850	928251	78766811
Metastases to lung	479.13	15.34	231	49095	17932	79677130
Osteonecrosis of jaw	445.56	15.34	297	49029	42929	79652133

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L02BA03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Anti-estrogens
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:50792	estrogen receptor antagonists
CHEBI has role	CHEBI:50837	oestrogen antagonist
FDA EPC	N0000175582	Estrogen Receptor Antagonist
FDA MoA	N0000000145	Estrogen Receptor Antagonists
FDA MoA	N0000000168	Selective Estrogen Receptor Modulators
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D018931	Antineoplastic Agents, Hormonal
MeSH PA	D004965	Estrogen Antagonists

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.92	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
250MG/5ML (50MG/ML)	FULVESTRANT	FRESENIUS KABI USA	N210326	May 20, 2019	RX	SOLUTION	INTRAMUSCULAR	10188663	Feb. 14, 2034	TREATMENT OF HORMONE RECEPTOR POSITIVE ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN
250MG/5ML (50MG/ML)	FULVESTRANT	FRESENIUS KABI USA	N210326	May 20, 2019	RX	SOLUTION	INTRAMUSCULAR	9833459	Feb. 14, 2034	TREATMENT OF HORMONE RECEPTOR POSITIVE ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN
250MG/5ML (50MG/ML)	FULVESTRANT	FRESENIUS KABI USA	N210326	May 20, 2019	RX	SOLUTION	INTRAMUSCULAR	9271990	May 17, 2034	TREATMENT OF HORMONE RECEPTOR POSITIVE ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Estrogen receptor	Nuclear hormone receptor	P03372	ESR1_HUMAN	ANTAGONIST	Ki	9.62	WOMBAT-PK	CHEMBL
Estrogen receptor beta	Nuclear hormone receptor	Q92731	ESR2_HUMAN	ANTAGONIST	Ki	8.74	WOMBAT-PK	CHEMBL
Progesterone receptor	Nuclear hormone receptor	P06401	PRGR_HUMAN		IC50	9.68	CHEMBL
G-protein coupled estrogen receptor 1	GPCR	Q99527	GPER1_HUMAN		EC50	7	WOMBAT-PK
Bile acid receptor	Nuclear hormone receptor	Q96RI1	NR1H4_HUMAN		IC50	6.10	CHEMBL
Steroid hormone receptor ERR1	Nuclear hormone receptor	P11474	ERR1_HUMAN		IC50	8.70	CHEMBL
Bifunctional epoxide hydrolase 2	Enzyme	P34913	HYES_HUMAN		Ki	7.59	CHEMBL
Nuclear receptor subfamily 1 group I member 2	Nuclear hormone receptor	O75469	NR1I2_HUMAN		EC50	5.71	CHEMBL
NAD-dependent protein deacylase sirtuin-5, mitochondrial	Enzyme	Q9NXA8	SIR5_HUMAN		IC50	5.58	CHEMBL
Estrogen receptor	Transcription factor		ESR1_RAT		IC50	8.23	CHEMBL

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External reference:

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ID	Source
FVS	PDB_CHEM_ID
009642	NDDF
1015	IUPHAR_LIGAND_ID
104741	PUBCHEM_CID
16618	MMSL
203870	RXNORM
22X328QOC4	UNII
300687	MMSL
385519002	SNOMEDCT_US
4021350	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
FASLODEX	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0720	INJECTION	50 mg	INTRAMUSCULAR	NDA	25 sections
FASLODEX	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0720	INJECTION	50 mg	INTRAMUSCULAR	NDA	25 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9022	INJECTION	50 mg	INTRAMUSCULAR	ANDA	25 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9022	INJECTION	50 mg	INTRAMUSCULAR	ANDA	25 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0310-7720	INJECTION	50 mg	INTRAMUSCULAR	NDA authorized generic	25 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0310-7720	INJECTION	50 mg	INTRAMUSCULAR	NDA authorized generic	25 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0591-5019	INJECTION	250 mg	INTRAMUSCULAR	NDA	27 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0591-5019	INJECTION	250 mg	INTRAMUSCULAR	NDA	27 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0591-5019	INJECTION	250 mg	INTRAMUSCULAR	NDA	27 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0781-3079	INJECTION	50 mg	INTRAMUSCULAR	ANDA	27 sections

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