Identification

Generic Name
CHF 4227
DrugBank Accession Number
DB05882
Background

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.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in osteoporosis.

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Contraindications & Blackbox Warnings
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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 AvailableHumans
UEstrogen receptor betaNot AvailableHumans
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

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
Not Available
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
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. [Article]
  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. [Article]
  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. [Article]
PubChem Substance
347910291
Wikipedia
Selective_estrogen_receptor_modulator

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

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

Targets

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Kind
Protein
Organism
Humans
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
Humans
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 at November 18, 2007 18:28 / Updated at June 12, 2020 16:52