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

Stem definitionDrug idCAS RN
antiestrogens or estrogen receptor modulators, clomifene and tamoxifen derivatives 4334 198481-32-2

Description:

MoleculeDescription

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: ONP

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

Drug dosage:

DoseUnitRoute
20 mg O

ADMET properties:

PropertyValueReference
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:

DateAgencyCompanyOrphan
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:

SourceCodeDescription
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 (View source of the data)

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 9.36 acidic
pKa2 11.25 acidic
pKa3 8.67 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Estrogen receptor Nuclear hormone receptor MODULATOR IC50 9.22 CHEMBL CHEMBL
Estrogen receptor beta Nuclear hormone receptor MODULATOR IC50 8.42 CHEMBL CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Duavee HUMAN PRESCRIPTION DRUG LABEL 2 0008-1123 TABLET, FILM COATED 20 mg ORAL NDA 32 sections
Duavee HUMAN PRESCRIPTION DRUG LABEL 2 63539-122 TABLET, FILM COATED 20 mg ORAL NDA 32 sections