Recent Advances in Drug Design and Drug Discovery for Androgen-Dependent Diseases

February 2016 in “ Current Medicinal Chemistry ”

Marisa Cabeza, Araceli Sánchez-Márquez, Mariana Garrido, Aylin Viviana Silva Ortiz, Eugene Bratoeff

From the encyclopedia

Frontline, gold standard treatment for combatting androgenic alopecia

Heavy duty finasteride that comes with higher risks

Studysummary This review discusses various targets for treating prostate cancer and benign prostatic hyperplasia and reports on recent studies of new compounds and 5α-reductase inhibitors, but provides no new experimental results.

Automatically generated from the study's abstract, not written by a person, and not a review of the full paper. Not medical advice or a treatment recommendation. Read the original study, and consult a qualified healthcare professional before changing treatment. Full disclaimer

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research New Ester Derivatives of Dehydroepiandrosterone as 5α-Reductase Inhibitors

14 citations , June 2011 in “Steroids”

This study found that several dehydroepiandrosterone ester derivatives effectively reduced prostate and seminal vesicle weight in gonadectomized hamsters treated with testosterone, demonstrating potential antiandrogen effects comparable to Finasteride.

research Novel C-6 Substituted and Unsubstituted Pregnane Derivatives as 5α-Reductase Inhibitors and Their Effect on Hamster Flank Organs Diameter Size

15 citations , May 2009 in “Steroids”

This study found that progesterone derivatives with chlorine or bromine substituents were effective in inhibiting 5α-reductase activity in human prostate and exhibited antiandrogenic effects in hamster flank organs.

research In Vivo and In Vitro Effect of Novel 4,16-Pregnadiene-6,20-Dione Derivatives as 5α-Reductase Inhibitors

27 citations , July 2008 in “The Journal of Steroid Biochemistry and Molecular Biology”

The new compounds may be more effective and cheaper than current treatments for conditions like baldness.

research Biological Activity of Novel Progesterone Derivatives Having Bulky Ester Side Chains at C-3

15 citations , April 2008 in “Steroids”

This study found that pregnane derivatives with higher lipophilicity, like compound 9d, had stronger androgen receptor binding and greater antiandrogenic effects in rats, correlating relative binding affinity with log P values.

research Androgen Biosynthetic Pathways in the Human Prostate

160 citations , April 2008 in “Baillière's best practice and research in clinical endocrinology and metabolism/Baillière's best practice & research. Clinical endocrinology & metabolism”

This review outlines the complexities of understanding DHT biosynthesis and metabolism in the human prostate and reports no new findings, emphasizing the need for further research into the pathways involved.

research Recent Advances in the Chemistry and Pharmacological Activity of New Steroidal Antiandrogens and 5α-Reductase Inhibitors

20 citations , March 2005 in “Current Medicinal Chemistry”

This study reports that newly synthesized steroidal trienones exhibit higher 5α-reductase inhibitory activity than dienones in various biological models, suggesting potential use in treating androgen-dependent diseases.

research New 5α-Reductase Inhibitors: In Vitro and In Vivo Effects

45 citations , February 2005 in “Steroids”

This study reported that certain newly synthesized steroidal derivatives showed stronger inhibitory activity against the 5α-reductase enzyme than finasteride in hamsters, suggesting their potential as enzyme inhibitors.

research Marked Suppression of Dihydrotestosterone in Men with Benign Prostatic Hyperplasia by Dutasteride, a Dual 5α-Reductase Inhibitor

408 citations , May 2004 in “The Journal of clinical endocrinology and metabolism/Journal of clinical endocrinology & metabolism”

This study found that dutasteride more effectively reduced serum dihydrotestosterone levels than finasteride in patients with benign prostatic hyperplasia.

Pharmacokinetic Parameters and Mechanisms of Inhibition of Rat Type 1 and 2 Steroid 5α-Reductases: Determinants for Different In Vivo Activities of GI198745 and Finasteride in the Rat

research Pharmacokinetic Parameters and Mechanisms of Inhibition of Rat Type 1 and 2 Steroid 5α-Reductases: Determinants for Different In Vivo Activities of GI198745 and Finasteride in the Rat

22 citations , October 2001 in “Biochemical Pharmacology”

This study found that GI198745 acts as a time-dependent inhibitor of rat 5α-reductase type 2 but a rapid-equilibrium inhibitor of type 1, potentially making it more effective than finasteride in preventing rat prostate growth.

Synthesis and In Vitro Study of 17β-[N-Ureylene-N,N′-Disubstituted]-4-Methyl-4-Aza-5α-Androstan-3-Ones as Selective Inhibitors of Type I 5α-Reductase

research Synthesis and In Vitro Study of 17β-[N-Ureylene-N,N′-Disubstituted]-4-Methyl-4-Aza-5α-Androstan-3-Ones as Selective Inhibitors of Type I 5α-Reductase

5 citations , February 1997 in “Bioorganic & Medicinal Chemistry”

This study found that among 17 beta-(N-ureylene-N,N'-disubstituted)-4-azasteroids, those with an N'-phenyl moiety were the most effective inhibitors of human type I 5 alpha-reductase.

research Finasteride: A Slow-Binding 5-Alpha-Reductase Inhibitor

70 citations , June 1993 in “Biochemistry”

This study found that the binding of finasteride to the enzyme 5a-reductase occurs at a slower rate than previously assumed, complicating the estimation of its real inhibitory constant.

research Species Differences in Prostatic Steroid 5α-Reductases of Rat, Dog, and Human

193 citations , August 1985 in “Endocrinology”

This study found significant species differences in the enzyme activity and inhibitor affinities of prostatic 5α-reductases from rats, dogs, and humans, with variable potencies for different 3-oxo-4-azasteroid inhibitors across species.