lasofoxifene 🐶 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	4308	180916-16-9

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.50	mg	O

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
Postmenopausal osteoporosis	indication	102447009

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Estrogen receptor	Nuclear hormone receptor	P03372	ESR1_HUMAN	AGONIST	IC50	8.89	CHEMBL	SCIENTIFIC LITERATURE
Estrogen receptor beta	Nuclear hormone receptor	Q92731	ESR2_HUMAN	AGONIST	IC50	8.74	CHEMBL	SCIENTIFIC LITERATURE
Estrogen receptor	Transcription factor		ESR1_RAT ESR2_RAT		IC50	7.95	CHEMBL

External reference:

ID	Source
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