Abstract:
:2-Methoxyestradiol (2MeO-E2) is an endogenous metabolite of estrogen which was initially considered to be inactive. During the last few decades it has been shown that 2MeO-E2 is a promising anticancer drug. In vitro experiments have demonstrated that it has several anticancer activities, and potential to alleviate hypertension, glomerulosclerosis, hypercholesterolemia, and other disorders. However, due to its low solubility and extensive glucuronidation, to achieve effective concentrations large doses of 2MeO-E2 would be required. Clinical studies reflected very high inter- and intrapatient variability and oral bioavailability of 1 to 2%. Thus, this review paper highlights the origin of this compound, its therapeutic promises, and possible mechanisms of action. It also discusses the pharmacokinetic properties of 2MeO-E2 as well as current developments to overcome low drug solubility and its extensive first pass metabolism.
journal_name
Mol Pharmjournal_title
Molecular pharmaceuticsauthors
Verenich S,Gerk PMdoi
10.1021/mp100190fsubject
Has Abstractpub_date
2010-12-06 00:00:00pages
2030-9issue
6eissn
1543-8384issn
1543-8392journal_volume
7pub_type
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