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The paper, entitled "Liquiritigenin is a plant-derived highly selectiveestrogen receptor beta agonist" provides details of the selectivetranscriptional activation of liquiritigenin to the estrogen receptor beta,highlights the advantages of an estrogen receptor beta targeted drug anddiscusses the isolation and structural identification of the pure chemicalcompound from Bionovo's MF101.
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In brief, the currently available estrogen therapies used to treatmenopausal symptoms are non-selective to both of the two known estrogenreceptors, alpha and beta. Because of this non-selectivity, all estrogensmarketed to treat menopausal symptoms have the potential to cause elevatedrisks for breast and uterine cancers due to the proliferative effects onbreast and uterine tissues mediated through the estrogen receptor alpha.Selective activation of the estrogen receptor beta, however, does not lead toproliferation of MCF-7 breast cancer cell lines or an increase for uterinecancer in mouse xenograph models. Bionovo is taking advantage of thedifferential effects caused by the two estrogen receptors on cancer formationby developing selective estrogen receptor beta drugs. The mechanism of actionof MF101 as a selective estrogen receptor beta therapy may provide a safer,long-term alternative to treat menopausal symptoms.
"Our study findings show a pure chemical compound from MF101 that isselective to the estrogen receptor beta which could lead to multiple noveltherapies for the treatment of common conditions such as menopausal hotflashes, vaginal dryness and osteoporosis," said Dale Leitman, M.D., Ph.D.,Center for Reproductive Sciences, University of California, San Francisco,principal investigator of the study and member of Bionovo's ScientificAdvisory Board. "Unlike any of the drugs we currently prescribe to women,MF101 and liquiritigenin are highly selective to the estrogen receptor beta,and from a mechanistic standpoint, they could be safer drugs to treat manysymptoms of menopause."
"We are very pleased to have advanced our ability to characterize MF101 byisolating this chemical compound and this new discovery will significantlystrengthen our intellectual property position for our lead compound," addedIsaac Cohen, chairman and CEO of Bionovo. "Given the increasing population ofwomen entering menopause, and the lack of safe and effective treatments forthese women, we are excited to be on the forefront of developing moreselective and safer alternative drugs for this enormous indication."
About MF101
MF101 is an oral drug designed for the treatment of hot flashes and nightsweats in peri-menopausal and menopausal women. MF101 is a novel estrogenreceptor beta selective agonist and unlike currently available hormonetherapies, does not activate the estrogen receptor alpha, known to beimplicated in tumor formation. Two hundred and seventeen women were enrolledinto a double-blind, placebo-controlled, randomized Phase 2 clinical trialunder the directorship of Dr. Deborah Grady in early 2007. Trial resultsshowed that MF101 10 grams/day was statistically superior to placebo atreducing hot flashes and was extremely well tolerated with no serious sideeffects.
Bionovo, Inc.
Bionovo is a pharmaceutical company focused on the discovery anddevelopment of safe and effective treatments for wome
