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

Stem definition	Drug id	CAS RN
antiestrogens or estrogen receptor modulators, clomifene and tamoxifen derivatives	4334	198481-32-2

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

TSE424
TSE-424
bazedoxifene acetate
bazedoxifene
conbriza

an estrogen agonist/antagonist that acts as an agonist in some estrogen-sensitive tissues and an antagonist in others

Molecular weight: 470.61
Formula: C30H34N2O3
CLOGP: 7.15
LIPINSKI: 1
HAC: 5
HDO: 2
TPSA: 57.86
ALOGS: -5.92
ROTB: 7

Status: OFP

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

Drug dosage:

Dose	Unit	Route
20	mg	O

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	15.40 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	6.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	30 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Oct. 3, 2013	FDA	WYETH PHARMS PFIZER

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	G03CC07	GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM ESTROGENS Estrogens, combinations with other drugs
ATC	G03XC02	GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM OTHER SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM Selective estrogen receptor modulators
FDA MoA	N0000000168	Selective Estrogen Receptor Modulators
MeSH PA	D050071	Bone Density Conservation Agents
MeSH PA	D020847	Estrogen Receptor Modulators
MeSH PA	D006727	Hormone Antagonists
MeSH PA	D020845	Selective Estrogen Receptor Modulators
FDA EPC	N0000175826	Estrogen Agonist/Antagonist

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

Disease	Relation	SNOMED_ID	DOID
Postmenopausal osteoporosis	indication	102447009
Menopausal flushing	indication	198436008

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.36	acidic
pKa2	11.25	acidic
pKa3	8.67	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 20MG BASE;0.45MG	DUAVEE	WYETH PHARMS	N022247	Oct. 3, 2013	RX	TABLET	ORAL	6479535	May 6, 2024	PREVENTION OF POSTMENOPAUSAL OSTEOPOROSIS
EQ 20MG BASE;0.45MG	DUAVEE	WYETH PHARMS	N022247	Oct. 3, 2013	RX	TABLET	ORAL	6479535	May 6, 2024	TREATMENT OF MODERATE TO SEVERE VASOMOTOR SYMPTOMS ASSOCIATED WITH MENOPAUSE
EQ 20MG BASE;0.45MG	DUAVEE	WYETH PHARMS	N022247	Oct. 3, 2013	RX	TABLET	ORAL	7683051	March 10, 2027	PREVENTION OF POSTMENOPAUSAL OSTEOPOROSIS
EQ 20MG BASE;0.45MG	DUAVEE	WYETH PHARMS	N022247	Oct. 3, 2013	RX	TABLET	ORAL	7683051	March 10, 2027	TREATMENT OF MODERATE TO SEVERE VASOMOTOR SYMPTOMS ASSOCIATED WITH MENOPAUSE

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Estrogen receptor	Nuclear hormone receptor	P03372	ESR1_HUMAN	MODULATOR	IC50	9.22		CHEMBL	CHEMBL
Estrogen receptor beta	Nuclear hormone receptor	Q92731	ESR2_HUMAN	MODULATOR	IC50	8.42		CHEMBL	CHEMBL

External reference:

ID	Source
D03062	KEGG_DRUG
198481-33-3	SECONDARY_CAS_RN
4033041	VANDF
C2346970	UMLSCUI
CHEBI:135947	CHEBI
29S	PDB_CHEM_ID
CHEMBL46740	ChEMBL_ID
CHEMBL2106615	ChEMBL_ID
DB06401	DRUGBANK_ID
C447119	MESH_SUPPLEMENTAL_RECORD_UI
7355	IUPHAR_LIGAND_ID
8168	INN_ID
Q16TT9C5BK	UNII
154257	PUBCHEM_CID
1441386	RXNORM
27928	MMSL
d07783	MMSL
015232	NDDF
015233	NDDF
440186005	SNOMEDCT_US
702401005	SNOMEDCT_US
895426008	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Duavee	HUMAN PRESCRIPTION DRUG LABEL	2	0008-1123	TABLET, FILM COATED	20 mg	ORAL	NDA	34 sections
Duavee	HUMAN PRESCRIPTION DRUG LABEL	2	0008-1123	TABLET, FILM COATED	20 mg	ORAL	NDA	34 sections
Duavee	HUMAN PRESCRIPTION DRUG LABEL	2	0008-1123	TABLET, FILM COATED	20 mg	ORAL	NDA	34 sections
Duavee	HUMAN PRESCRIPTION DRUG LABEL	2	63539-122	TABLET, FILM COATED	20 mg	ORAL	NDA	34 sections
Duavee	HUMAN PRESCRIPTION DRUG LABEL	2	63539-122	TABLET, FILM COATED	20 mg	ORAL	NDA	34 sections