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

Stem definition	Drug id	CAS RN
aromatase inhibitors, imidazole-triazole derivatives	210	120511-73-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: anastrozole anastrazole anastrol arimidex	A nitrile and triazole derivative that acts as a selective nonsteroidal aromatase inhibitor. It is used in the treatment of ESTROGEN NUCLEAR RECEPTOR-positive breast cancer in postmenopausal women. Molecular weight: 293.37 Formula: C17H19N5 CLOGP: 1.75 LIPINSKI: 0 HAC: 5 HDO: 0 TPSA: 78.29 ALOGS: -3.65 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

anastrozole
anastrazole
anastrol
arimidex

A nitrile and triazole derivative that acts as a selective nonsteroidal aromatase inhibitor. It is used in the treatment of ESTROGEN NUCLEAR RECEPTOR-positive breast cancer in postmenopausal women.

Molecular weight: 293.37
Formula: C17H19N5
CLOGP: 1.75
LIPINSKI: 0
HAC: 5
HDO: 0
TPSA: 78.29
ALOGS: -3.65
ROTB: 4

Status: OFP

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

Drug dosage:

Dose	Unit	Route
1	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	80 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	10 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.50 mg/mL	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.06 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Dec. 27, 1995	FDA	ASTRAZENECA

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
Metastases to bone	1105.59	11.70	468	50535	20551	63417468
Malignant neoplasm progression	829.12	11.70	616	50387	81505	63356514
Metastases to liver	615.04	11.70	324	50679	23315	63414704
Metastases to lung	483.94	11.70	226	50777	12524	63425495
Osteonecrosis	352.83	11.70	229	50774	24301	63413718
Hot flush	348.11	11.70	305	50698	50854	63387165
Breast cancer recurrent	290.63	11.70	115	50888	4226	63433793
Breast cancer metastatic	282.37	11.70	154	50849	11864	63426155
Disease progression	275.22	11.70	411	50592	122347	63315672
Bone pain	257.63	11.70	266	50737	54375	63383644

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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
Growth retardation	86.52	25.60	20	1839	1828	34953244
Mesenteric vein thrombosis	78.04	25.60	16	1843	833	34954239
Performance enhancing product use	68.04	25.60	10	1849	67	34955005
Secondary hypogonadism	48.00	25.60	9	1850	293	34954779
Haematocrit increased	44.20	25.60	12	1847	2101	34952971
Metastases to bone	39.55	25.60	17	1842	11953	34943119
Spondylolisthesis	39.52	25.60	9	1850	768	34954304
Glucose tolerance decreased	37.60	25.60	6	1853	73	34954999
Breast cancer recurrent	36.37	25.60	5	1854	19	34955053
Autoimmune thyroiditis	35.82	25.60	9	1850	1165	34953907

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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
Metastases to bone	740.63	11.71	324	40968	24103	79678993
Malignant neoplasm progression	421.83	11.71	431	40861	135559	79567537
Metastases to liver	404.65	11.71	225	41067	28089	79675007
Metastases to lung	349.29	11.71	176	41116	17987	79685109
Hot flush	327.01	11.71	252	41040	54625	79648471
Breast cancer recurrent	273.61	11.71	89	41203	2888	79700208
Breast cancer metastatic	260.23	11.71	114	41178	8488	79694608
Breast cancer	236.65	11.71	171	41121	33610	79669486
Osteonecrosis	216.89	11.71	157	41135	30938	79672158
Bone pain	216.37	11.71	200	41092	55542	79647554

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L02BG03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Aromatase inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:50790	aromatase inhibitors
FDA EPC	N0000175563	Aromatase Inhibitor
FDA MoA	N0000175080	Aromatase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D018931	Antineoplastic Agents, Hormonal
MeSH PA	D047072	Aromatase Inhibitors
MeSH PA	D004791	Enzyme Inhibitors
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
Hormone receptor positive malignant neoplasm of breast	indication	417181009
Malignant tumor of ovary	off-label use	363443007	DOID:2394
Hypercholesterolemia	contraindication	13644009
Pregnancy, function	contraindication	289908002
Osteopenia	contraindication	312894000
Breastfeeding (mother)	contraindication	413712001
Myocardial ischemia	contraindication	414795007	DOID:3393

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🐶 Veterinary Drug Use

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🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.56	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Aromatase	Enzyme	P11511	CP19A_HUMAN	INHIBITOR	IC50	6.22		WOMBAT-PK	CHEMBL

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External reference:

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ID	Source
005094	NDDF
108774000	SNOMEDCT_US
173198	MMSL
2187	PUBCHEM_CID
262485	RXNORM
2Z07MYW1AZ	UNII
386910003	SNOMEDCT_US
4020948	VUID
4020948	VANDF
4200	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Anastrozole	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7536	TABLET, FILM COATED	1 mg	ORAL	ANDA	28 sections
Anastrozole	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7536	TABLET, FILM COATED	1 mg	ORAL	ANDA	28 sections
Anastrozole	HUMAN PRESCRIPTION DRUG LABEL	1	0781-5356	TABLET, FILM COATED	1 mg	ORAL	ANDA	29 sections
Anastrozole	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6195	TABLET	1 mg	ORAL	ANDA	26 sections
Anastrozole	Human Prescription Drug Label	1	16571-421	TABLET	1 mg	ORAL	ANDA	29 sections
Anastrozole	HUMAN PRESCRIPTION DRUG LABEL	1	16729-035	TABLET	1 mg	ORAL	ANDA	26 sections
Anastrozole	HUMAN PRESCRIPTION DRUG LABEL	1	21695-990	TABLET	1 mg	ORAL	ANDA	27 sections
Anastrozole	HUMAN PRESCRIPTION DRUG LABEL	1	23155-857	TABLET	1 mg	ORAL	ANDA	28 sections
Anastrozole	HUMAN PRESCRIPTION DRUG LABEL	1	42254-161	TABLET	1 mg	ORAL	ANDA	28 sections
ANASTROZOLE	HUMAN PRESCRIPTION DRUG LABEL	1	42291-016	TABLET	1 mg	ORAL	ANDA	32 sections

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