Cloning, Expression, and Characterization of Rhesus Macaque Types 1 and 2 5alpha-Reductase: Evidence for Mechanism-Based Inhibition by Finasteride

September 1998 in “ The Journal of Steroid Biochemistry and Molecular Biology ”

Kenneth P. Ellsworth, B. Azzolina, George Cimis, Herbert G. Bull, Gerald F. Harris

5alpha-Reductase finasteride 5aR inhibitors isozymes mechanism-based inhibition Propecia

Studysummary This study concludes that rhesus macaques are a suitable model for testing the pharmacological properties of finasteride and other 5aR inhibitors, due to their biochemical similarity to humans.

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research Inhibition of Rat Alpha-Reductases by Finasteride: Evidence for Isozyme Differences in the Mechanism of Inhibition

98 citations , April 1997 in “The Journal of Steroid Biochemistry and Molecular Biology”

Finasteride effectively blocks rat enzymes, but with varying methods and strength.

research Effects of Finasteride, a Type 2 5-Alpha Reductase Inhibitor, on Fetal Development in the Rhesus Monkey (Macaca Mulatta)

67 citations , February 1997 in “Teratology”

This study demonstrated that high oral doses of finasteride caused external genital abnormalities in male rhesus monkey fetuses, but intravenous doses did not lead to abnormalities.

research Effect of MK-386, a Novel Inhibitor of Type 1 5 Alpha-Reductase, Alone and in Combination with Finasteride, on Serum Dihydrotestosterone Concentrations in Men

7 citations , August 1996 in “The Journal of Clinical Endocrinology and Metabolism”

Mechanism-Based Inhibition of Human Steroid 5α-Reductase by Finasteride: Enzyme-Catalyzed Formation of NADP-Dihydrofinasteride, a Potent Bisubstrate Analog Inhibitor

research Mechanism-Based Inhibition of Human Steroid 5α-Reductase by Finasteride: Enzyme-Catalyzed Formation of NADP-Dihydrofinasteride, a Potent Bisubstrate Analog Inhibitor

136 citations , March 1996 in “Journal of the American Chemical Society”

This study explains finasteride's high potency and specificity as a mechanism-based inhibitor for treating benign prostatic hyperplasia by detailing its interaction with human type 2 steroid 5α-reductase.

research 5α-Reductase Inhibitors/Finasteride: A Safe and Effective Treatment for Benign Prostatic Hyperplasia

24 citations , January 1996 in “The Prostate”

This study demonstrated that 12 months of 5 mg daily finasteride treatment reduced prostate volume, dihydrotestosterone, and prostate-specific antigen levels, while improving urinary flow rates and symptom scores in benign prostatic hyperplasia patients.

research Clinical and Hormonal Effects of the 5 Alpha-Reductase Inhibitor Finasteride in Idiopathic Hirsutism

17 citations , October 1994 in “The Journal of Clinical Endocrinology and Metabolism”

This study found that finasteride may effectively reduce hirsutism in women with idiopathic hirsutism, as evidenced by lower Ferriman-Gallwey scores and hormone levels, without significant adverse effects.

research The Effect of Finasteride, a 5 Alpha-Reductase Inhibitor, on Scalp Skin Testosterone and Dihydrotestosterone Concentrations in Patients With Male Pattern Baldness

61 citations , September 1994 in “The Journal of Clinical Endocrinology and Metabolism”

research LY191704: A Selective, Nonsteroidal Inhibitor of Human Steroid 5 Alpha-Reductase Type 1

53 citations , June 1993 in “Proceedings of the National Academy of Sciences of the United States of America”

This study identified LY191704 as a specific noncompetitive inhibitor of human 5 alpha-reductase type 1, which may be useful in treating endocrine disorders related to DHT overproduction.

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 Critical Developmental Periods for Effects on Male Rat Genitalia Induced by Finasteride, a 5α-Reductase Inhibitor

86 citations , March 1993 in “Toxicology and Applied Pharmacology”

Finasteride affects male rat genitalia development, causing abnormalities during specific pregnancy days.

research The Effect of Finasteride in Men with Benign Prostatic Hyperplasia

1040 citations , October 1992 in “The New England Journal of Medicine”

In this study, 5 mg of finasteride per day significantly improved urinary symptoms and reduced prostate volume in men with benign prostatic hyperplasia, but increased the risk of sexual dysfunction.

research Four-Amino Acid Segment in Steroid 5 Alpha-Reductase 1 Confers Sensitivity to Finasteride, a Competitive Inhibitor

83 citations , April 1992 in “Journal of Biological Chemistry”

Four-amino acid part makes enzyme sensitive to finasteride.

research External Genitalia Abnormalities in Male Rats Exposed In Utero to Finasteride, a 5α-Reductase Inhibitor

122 citations , July 1990 in “Teratology”

This study found that oral administration of finasteride to pregnant rats caused dosage-related developmental toxicities, including hypospadias and decreased anogenital distance in male offspring.

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.