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

Stem definition	Drug id	CAS RN
aromatase inhibitors	1122	107868-30-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: aromasine FCE 24304 exemestane aromasin	a hormonal antineoplastic agent Molecular weight: 296.41 Formula: C20H24O2 CLOGP: 3.28 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 34.14 ALOGS: -4.64 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

aromasine
FCE 24304
exemestane
aromasin

a hormonal antineoplastic agent

Molecular weight: 296.41
Formula: C20H24O2
CLOGP: 3.28
LIPINSKI: 0
HAC: 2
HDO: 0
TPSA: 34.14
ALOGS: -4.64
ROTB: 0

Status: OFP

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

Drug dosage:

Dose	Unit	Route
25	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	42 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.35 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	1 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Oct. 21, 1999	FDA	PHARMACIA AND UPJOHN

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	1894.25	13.71	1025	48305	81096	63358596
Metastases to bone	1354.28	13.71	536	48794	20483	63419209
Metastases to liver	1084.03	13.71	473	48857	23166	63416526
Neoplasm progression	914.84	13.71	482	48848	35946	63403746
Osteonecrosis of jaw	675.88	13.71	390	48940	34733	63404959
Disease progression	552.10	13.71	573	48757	122185	63317507
Metastases to lung	450.83	13.71	213	49117	12537	63427155
Breast cancer metastatic	389.12	13.71	189	49141	11829	63427863
Metastases to lymph nodes	376.12	13.71	164	49166	7994	63431698
Tumour marker increased	371.85	13.71	141	49189	4774	63434918

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FDA Adverse Event Reporting System (Male)

None

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	1060.73	14.42	403	35566	24024	79684395
Malignant neoplasm progression	900.99	14.42	629	35340	135361	79573058
Neoplasm progression	731.07	14.42	389	35580	51293	79657126
Metastases to liver	679.95	14.42	306	35663	28008	79680411
Osteonecrosis of jaw	478.51	14.42	277	35692	42949	79665470
Disease progression	372.98	14.42	437	35532	183925	79524494
Metastases to lung	345.01	14.42	167	35802	17996	79690423
Breast cancer metastatic	334.14	14.42	131	35838	8471	79699948
Metastases to lymph nodes	300.16	14.42	128	35841	10269	79698150
Stomatitis	288.54	14.42	343	35626	146414	79562005

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L02BG06	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Aromatase inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:50790	aromatase inhibitors
CHEBI has role	CHEBI:78298	environmental contaminants
FDA EPC	N0000175563	Aromatase Inhibitor
FDA MoA	N0000175080	Aromatase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D047072	Aromatase Inhibitors
MeSH PA	D004791	Enzyme Inhibitors

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

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Disease	Relation	SNOMED_ID
Hormone receptor positive malignant neoplasm of breast	indication	417181009
Advanced Breast Cancer Progression Post-Antiestrogen Therapy	indication
Prevention of Breast Carcinoma	off-label use
Pregnancy, function	contraindication	289908002
Osteopenia	contraindication	312894000

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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	5.69		WOMBAT-PK	CHEMBL
Androgen receptor	Nuclear hormone receptor	P10275	ANDR_HUMAN					WOMBAT-PK

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External reference:

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ID	Source
EXM	PDB_CHEM_ID
007997	NDDF
116115004	SNOMEDCT_US
180650	MMSL
258494	RXNORM
31449	MMSL
387017005	SNOMEDCT_US
4021191	VUID
4021191	VANDF
60198	PUBCHEM_CID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Aromasin	HUMAN PRESCRIPTION DRUG LABEL	1	0009-7663	TABLET	25 mg	ORAL	NDA	27 sections
Aromasin	HUMAN PRESCRIPTION DRUG LABEL	1	0009-7663	TABLET	25 mg	ORAL	NDA	27 sections
Aromasin	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5261	TABLET	25 mg	ORAL	NDA	13 sections
Exemestane	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0080	TABLET, FILM COATED	25 mg	ORAL	ANDA	27 sections
Exemestane	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0080	TABLET, FILM COATED	25 mg	ORAL	ANDA	27 sections
Exemestane	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5001	TABLET, FILM COATED	25 mg	ORAL	ANDA	27 sections
Exemestane	HUMAN PRESCRIPTION DRUG LABEL	1	0832-0595	TABLET	25 mg	ORAL	ANDA	27 sections
Exemestane	HUMAN PRESCRIPTION DRUG LABEL	1	0832-0595	TABLET	25 mg	ORAL	ANDA	27 sections
Exemestane	HUMAN PRESCRIPTION DRUG LABEL	1	0832-0595	TABLET	25 mg	ORAL	ANDA	27 sections
Exemestane	HUMAN PRESCRIPTION DRUG LABEL	1	44278-025	TABLET	25 mg	ORAL	ANDA	26 sections

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