Disease relevance of Epristeride

• We determined the effects of epristeride, a 5 alpha-reductase inhibitor, on the density of TXA2 receptors in rat aortic smooth muscle cells and human erythroleukemia cells, a megakaryocyte-like cell, in vitro, and in rat platelets and aortic membranes in vivo [1].
• The mechanism of epristeride against benign prostatic hyperplasia [2].
• Reversible long-term toxicity of epristeride in beagle dogs [3].

High impact information on Epristeride

• This study evaluates the effects of the 5 alpha R inhibitor, epristeride, on cultured stromal and epithelial cells from benign, hyperplastic adult prostates [4].
• Treatment of male rats with epristeride for 2 weeks significantly (P < .01) decreased TXA2 receptor density in aortic membranes (41 +/- 3 for vehicle, n = 10; 27 +/- 3 fmol/mg protein for epristeride, n = 11) but did not significantly change TXA2 receptor density in platelets [1].
• Therefore, the mechanism of epristeride in the treatment of benign prostatic hyperplasia might be apoptosis stimulated by decreasing dihydrotestosterone level [2].
• The cells treated with epristeride showed a reduction in cell size, an increase in the cytoplasm/nuclear ratio, which is indicative of the condensation of nuclear chromatin, a significant decrease in optical density at 580 nm (OD580 nm), and an oligonucleosomal ladder and a subdiploid peak of DNA characteristic of apoptosis [2].
• The results of inhibition studies with over 30 known SR inhibitors, including epristeride, 4MA, and finasteride, indicate that the monkey SR isoenzymes are functionally more similar to the human than the rat homologues [5].

Biological context of Epristeride

• Pharmacokinetics and absolute bioavailability of epristeride in healthy male subjects [6].
• The objective of the current investigation was to describe the pharmacokinetics and absolute oral bioavailability of epristeride [6].

Anatomical context of Epristeride

• Inhibition of cultured rat prostatic epithelial cell growth by epristeride in vitro [7].
• Semen samples were divided into 4 groups and treated with vehicle and epristeride [8].

Associations of Epristeride with other chemical compounds

• Comparative study of human steroid 5alpha-reductase isoforms in prostate and female breast skin tissues: sensitivity to inhibition by finasteride and epristeride [9].

Gene context of Epristeride

• These results suggest that this 3-androstene-3-carboxylic acid is a specific and selective inhibitor of the human type 2 SR, and that epristeride is an attractive compound for further investigation as a safe and effective therapeutic agent in the potential treatment of disease states associated with DHT-induced tissue growth [10].
• In addition, using samples of the individually expressed two known forms of human SRs, epristeride has been shown to be a selective inhibitor of the recombinant human SR type 2, the predominant activity found in the prostate of man [10].
• RESULTS: Epristeride attenuated growth of epithelial cells induced by exogenous EGF, IGF-I [7].
• Finasteride and Epristeride are also inhibitors of skin 5alpha-reductase, which possesses a comparable Ki for Finasteride to that of the low Km prostatic enzyme, but Epristeride was a less potent inhibitor of the skin enzyme relative to the prostate isoform [9].
• Effect of epristeride on expression of TGF-beta receptor in rat prostatic epithelial cells in vitro [11].

Analytical, diagnostic and therapeutic context of Epristeride

• Effects of a new 5 alpha reductase inhibitor (epristeride) on human prostate cell cultures [4].
• However, little is known about the histopathology of the prostate after treatment with epristeride [2].
• The activity of ACP was decreased by both castration and epristeride treatment [12].
• METHODS: RT-PCR and Western blot were used to quantitatively detect the mRNA and protein expressions of TbetaR II in rat prostatic epithelial cells treated or untreated with epristeride [11].
• Blood samples were obtained over 72h for the determination of epristeride plasma concentrations using a sensitive high-performance liquid chromatography assay [6].

References