CHF 4227

Identification

Name
CHF 4227
Accession Number
DB05882
Type
Small Molecule
Groups
Investigational
Description

CHF 4227 is a new selective estrogen receptor modulator (SERM). The compound has a high receptor affinity and has shown promising efficacy in the prevention of bone loss in animal models of osteoporosis. Additionally, the compound has shown no uterotrophic activity suggesting a potential therapeutic advantage over drugs normally used in postmenopausal therapy.

Synonyms
Not Available
Categories
UNII
Not Available
CAS number
Not Available
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

Investigated for use/treatment in osteoporosis.

Structured Indications
Not Available
Pharmacodynamics
Not Available
Mechanism of action

CHF 4227 binds with high affinity to the human estrogen receptor-alpha and beta. It compares favorably in efficacy and potency with raloxifene in preventing bone loss and in antagonizing EE2 stimulation of the uterus. This attribute along with the minimal uterine stimulation suggests a therapeutic advantage to CHF 4227 over EE2 or raloxifene for the treatment of postmenopausal women.

TargetActionsOrganism
UEstrogen receptor alphaNot AvailableHuman
UEstrogen receptor betaNot AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
Not Available

References

General References
  1. Galbiati E, Caruso PL, Amari G, Armani E, Ghirardi S, Delcanale M, Civelli M: Pharmacological actions of a novel, potent, tissue-selective benzopyran estrogen. J Pharmacol Exp Ther. 2002 Oct;303(1):196-203. [PubMed:12235251]
  2. Civelli M, Preti AP, Cenacchi V, Rondelli I, Guastalla D, Tarral A, Dostert P, Guillevic Y, Homery MC: Single and multiple ascending dose studies of a novel tissue-selective oestrogen receptor modulator, CHF 4227, in healthy postmenopausal women. Br J Clin Pharmacol. 2007 Sep;64(3):304-16. Epub 2007 Mar 16. [PubMed:17367495]
  3. Armamento-Villareal R, Sheikh S, Nawaz A, Napoli N, Mueller C, Halstead LR, Brodt MD, Silva MJ, Galbiati E, Caruso PL, Civelli M, Civitelli R: A new selective estrogen receptor modulator, CHF 4227.01, preserves bone mass and microarchitecture in ovariectomized rats. J Bone Miner Res. 2005 Dec;20(12):2178-88. Epub 2005 Aug 1. [PubMed:16294271]
External Links
PubChem Substance
347910291
Wikipedia
Selective_estrogen_receptor_modulator

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissu...
Gene Name
ESR1
Uniprot ID
P03372
Uniprot Name
Estrogen receptor
Molecular Weight
66215.45 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent m...
Gene Name
ESR2
Uniprot ID
Q92731
Uniprot Name
Estrogen receptor beta
Molecular Weight
59215.765 Da

Drug created on November 18, 2007 11:28 / Updated on November 06, 2017 06:45