Accession NumberDB05052
TypeSmall Molecule

MF101 is a novel estrogen receptor beta (ERβ) selective agonist and unlike currently available hormone therapies, does not activate the estrogen receptor alpha (ERα), known to be implicated in tumor formation. MF101 is an oral drug designed for the treatment of hot flashes and night sweats in peri-menopausal and menopausal women.

SynonymsNot Available
External IDs Not Available
Product Ingredients Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
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UNIINot Available
CAS numberNot Available
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InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
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Investigated for use/treatment in hormone replacement therapy: menopause and menopause.

Structured Indications Not Available
PharmacodynamicsNot Available
Mechanism of action

MF101 promoted ERbeta, but not ERalpha, activation of an estrogen response element (ERE) upstream of the luciferase reporter gene. MF101 also selectively regulates transcription of endogenous genes through ERbeta. The ERbeta-selectivity was not due to differential binding, since MF101 binds equally to ERalpha and ERbeta. Fluorescence resonance energy transfer and protease digestion studies showed that MF101 produces a different conformation in ERalpha from ERbeta, when compared with the conformations produced by estradiol. The specific conformational change induced by MF101 allows ERbeta to bind to an ERE and recruit coregulatory proteins that are required for gene activation. MF101 did not activate the ERalpha-regulated proliferative genes, c-myc and cyclin D1, or stimulate MCF-7 breast cancer cell proliferation or tumor formation in a mouse xenograft model.

TargetKindPharmacological actionActionsOrganismUniProt ID
Estrogen receptor betaProteinunknownNot AvailableHumanQ92731 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organismsNot Available
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Drug Interactions Not Available
Food InteractionsNot Available
Synthesis ReferenceNot Available
General References
  1. Cvoro A, Paruthiyil S, Jones JO, Tzagarakis-Foster C, Clegg NJ, Tatomer D, Medina RT, Tagliaferri M, Schaufele F, Scanlan TS, Diamond MI, Cohen I, Leitman DC: Selective activation of estrogen receptor-beta transcriptional pathways by an herbal extract. Endocrinology. 2007 Feb;148(2):538-47. Epub 2006 Nov 9. [PubMed:17095596 ]
External LinksNot Available
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Clinical Trials
Clinical Trials
1TerminatedTreatmentHealthy Volunteers1
1Unknown StatusTreatmentMenopausal Hot Flushes1
2CompletedTreatmentMenopausal Hot Flushes1
2CompletedTreatmentMenopausal Symptoms / Sleeping Quality1
3Unknown StatusTreatmentMenopausal Hot Flushes / Vasomotor Symptoms1
ManufacturersNot Available
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Dosage formsNot Available
PricesNot Available
PatentsNot Available
Experimental PropertiesNot Available
Predicted PropertiesNot Available
Predicted ADMET featuresNot Available
Mass Spec (NIST)Not Available
Spectrum TypeDescriptionSplash Key
ClassificationNot classified


Pharmacological action
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 manner (PubMed:20074560). Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by...
Gene Name:
Uniprot ID:
Molecular Weight:
59215.765 Da
Drug created on October 21, 2007 16:23 / Updated on August 17, 2016 12:24