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Epristeride SmithKline Beecham.
Hedge SS. Hedge SS. IDrugs. 1998 May;1(1):152-7. IDrugs. 1998. PMID: 18465521
Epristeride is a transition-state, noncompetitive steroid 5-alpha-reductase inhibitor under development by SmithKline Beecham for the treatment of benign prostatic hyperplasia and acne. ...Recordati has co-marketing rights for epristeride [162547], [162519]. Analyst
Epristeride is a transition-state, noncompetitive steroid 5-alpha-reductase inhibitor under development by SmithKline Beecham for the
Epristeride is a selective and specific uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2.
Levy MA, Brandt M, Sheedy KM, Dinh JT, Holt DA, Garrison LM, Bergsma DJ, Metcalf BW. Levy MA, et al. J Steroid Biochem Mol Biol. 1994 Feb;48(2-3):197-206. doi: 10.1016/0960-0760(94)90145-7. J Steroid Biochem Mol Biol. 1994. PMID: 8142295
The affinity of epristeride for each of these 12 potential targets was found to be at least 1000-fold weaker than that for SR, the intended target. ...Nonetheless, the mechanisms of SR inhibition for both isoenzymes involve formation of a ternary complex with epristerid
The affinity of epristeride for each of these 12 potential targets was found to be at least 1000-fold weaker than that for SR, the in …
In vitro effects of epristeride on sperm in rats, dogs and man.
Wu JH, Sun ZY, Cao L. Wu JH, et al. Arch Androl. 2006 May-Jun;52(3):191-5. doi: 10.1080/01485010500379830. Arch Androl. 2006. PMID: 16574601
The study was conducted to evaluate in vitro effects of epristeride on sperm in rats, beagle dogs and man. Semen samples were divided into 4 groups and treated with vehicle and epristeride. ...Therefore, epristeride had a toxic effect on sperm, and the effect …
The study was conducted to evaluate in vitro effects of epristeride on sperm in rats, beagle dogs and man. Semen samples were divided …
Discovery of a novel hybrid from finasteride and epristeride as 5alpha-reductase inhibitor.
Yao Z, Xu Y, Zhang M, Jiang S, Nicklaus MC, Liao C. Yao Z, et al. Bioorg Med Chem Lett. 2011 Jan 1;21(1):475-8. doi: 10.1016/j.bmcl.2010.10.112. Epub 2010 Oct 28. Bioorg Med Chem Lett. 2011. PMID: 21094046 Free PMC article.
Finasteride and epristeride both inhibit 5alpha-reductase with high potency via competitive and non-competitive mechanism, respectively. A new hybrid of finasteride and epristeride was designed as a new 5alpha-reductase inhibitor based on combination principles in m …
Finasteride and epristeride both inhibit 5alpha-reductase with high potency via competitive and non-competitive mechanism, respective …
Reversible long-term toxicity of epristeride in beagle dogs.
Sun ZY, Feng J, Qi XD, Wu HY, Zheng WJ, Tu ZH. Sun ZY, et al. Toxicol Appl Pharmacol. 1999 Jan 15;154(2):145-52. doi: 10.1006/taap.1998.8579. Toxicol Appl Pharmacol. 1999. PMID: 9925798
Groups A and B were placebo-treated for 180 and 240 days, Groups C and D were treated with 10 and 100 mg/kg epristeride for 180 days, and Groups E and F were treated with 10 and 100 mg/kg epristeride for 180 days and then were placebo-treated for 60 days (total 240 …
Groups A and B were placebo-treated for 180 and 240 days, Groups C and D were treated with 10 and 100 mg/kg epristeride for 180 days, …
The mechanism of epristeride against benign prostatic hyperplasia.
Sun ZY, Wu HY, Wang MY, Tu ZH. Sun ZY, et al. Eur J Pharmacol. 1999 Apr 29;371(2-3):227-33. doi: 10.1016/s0014-2999(99)00109-0. Eur J Pharmacol. 1999. PMID: 10357260
Epristeride, a 5alpha-reductase inhibitor, decreases prostate size and improves symptoms in men with benign prostatic hyperplasia. However, little is known about the histopathology of the prostate after treatment with epristeride. To study the relationship between a
Epristeride, a 5alpha-reductase inhibitor, decreases prostate size and improves symptoms in men with benign prostatic hyperplasia. Ho
Effects of a new 5 alpha reductase inhibitor (epristeride) on human prostate cell cultures.
Robinson EJ, Collins AT, Robson CN, Neal DE. Robinson EJ, et al. Prostate. 1997 Sep 1;32(4):259-65. doi: 10.1002/(sici)1097-0045(19970901)32:4<259::aid-pros5>3.0.co;2-e. Prostate. 1997. PMID: 9288184

RESULTS: Stromal cell proliferation in response to testosterone was dose-dependently inhibited by epristeride (1 x 10(-9) -3 x 10(-7) M, P < 0.05). However, epristeride had no effect on DHT-induced growth or the growth of androgen-unresponsive stroma. ...Transfor

RESULTS: Stromal cell proliferation in response to testosterone was dose-dependently inhibited by epristeride (1 x 10(-9) -3 x 10(-7) …
Normal-phase high-performance liquid chromatographic determination of epristeride, a prostatic steroid 5 alpha-reductase enzyme inhibitor, in human plasma.
Boppana VK, Miller-Stein C, Rhodes GR. Boppana VK, et al. J Chromatogr. 1993 Feb 12;631(1-2):251-4. doi: 10.1016/0021-9673(93)80529-h. J Chromatogr. 1993. PMID: 8450017
Epristeride is currently in development for the treatment of benign prostatic hyperplasia. ...The absolute recovery of epristeride from plasma was 90.2 +/- 2.96. The limit of quantification for epristeride was 2.5 ng/ml. ...
Epristeride is currently in development for the treatment of benign prostatic hyperplasia. ...The absolute recovery of epristeride
Effect of epristeride on the expression of IGF-1 and TGF-beta receptors in androgen-induced castrated rat prostate.
Wu SF, Sun HZ, Qi XD, Tu ZH. Wu SF, et al. Exp Biol Med (Maywood). 2001 Nov;226(10):954-60. doi: 10.1177/153537020122601012. Exp Biol Med (Maywood). 2001. PMID: 11682703
This study was designed to assess the effects of epristeride on expression of these two factors at mRNA and protein levels in castrated rats maintained with exogenous testosterone. Epristeride treatment caused significant reduction in ventral prostate weight in a do …
This study was designed to assess the effects of epristeride on expression of these two factors at mRNA and protein levels in castrat …
Pharmacokinetics and absolute bioavailability of epristeride in healthy male subjects.
Benincosa LJ, Audet PR, Lundberg D, Zariffa N, Jorkasky DK. Benincosa LJ, et al. Biopharm Drug Dispos. 1996 Apr;17(3):249-58. doi: 10.1002/(SICI)1099-081X(199604)17:3<249::AID-BDD952>3.0.CO;2-E. Biopharm Drug Dispos. 1996. PMID: 8983399 Clinical Trial.
Blood samples were obtained over 72h for the determination of epristeride plasma concentrations using a sensitive high-performance liquid chromatography assay. ...The % AUC associated with the lambda 2 exponential phase was approximately 68%. This long half-life allows for …
Blood samples were obtained over 72h for the determination of epristeride plasma concentrations using a sensitive high-performance li …
42 results