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

Stem definitionDrug idCAS RN
antiestrogens or estrogen receptor modulators, clomifene and tamoxifen derivatives 4308 180916-16-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lasofoxifene
  • lasofoxifene tartrate
  • fablyn
  • CP-336156
  • CP-336,156
a SERM whose biological actions are largely mediated through binding to estrogen receptors, this binding results in the activation of some estrogenic pathways and a blockade of others, Lasofoxifene produces tissue and cell-specific effects in estrogen-responsive tissues
  • Molecular weight: 413.56
  • Formula: C28H31NO2
  • CLOGP: 6.71
  • LIPINSKI: 1
  • HAC: 3
  • HDO: 1
  • TPSA: 32.70
  • ALOGS: -6.02
  • ROTB: 6

Drug dosage:

DoseUnitRoute
0.50 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Feb. 24, 2009 EMA Dr. Friedrich Eberth Arzneimittel GmbH

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 G03XC03 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
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:50646 antiosteoporotic
CHEBI has role CHEBI:50792 estrogen receptor antagonists
CHEBI has role CHEBI:63951 estrogen receptor agonists
CHEBI has role CHEBI:77307 cardioprotective agents

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

DiseaseRelationSNOMED_IDDOID
Postmenopausal osteoporosis indication 102447009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.5 acidic
pKa2 8.9 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Estrogen receptor Nuclear hormone receptor AGONIST IC50 8.89 CHEMBL SCIENTIFIC LITERATURE
Estrogen receptor beta Nuclear hormone receptor AGONIST IC50 8.74 CHEMBL SCIENTIFIC LITERATURE
Estrogen receptor Transcription factor IC50 7.95 CHEMBL

External reference:

IDSource
D04672 KEGG_DRUG
190791-29-8 SECONDARY_CAS_RN
C0963839 UMLSCUI
CHEBI:135938 CHEBI
C3D PDB_CHEM_ID
CHEMBL328190 ChEMBL_ID
DB06202 DRUGBANK_ID
C111332 MESH_SUPPLEMENTAL_RECORD_UI
7542 IUPHAR_LIGAND_ID
7875 INN_ID
337G83N988 UNII
216416 PUBCHEM_CID

Pharmaceutical products:

None