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 3 3Abbreviations: r5AR1, rat 5α-reductase 1; r5AR2, rat 5α-reductase 2; and DHT, dihydrotestosterone.
October 2001
in “Biochemical Pharmacology”
TLDR GI198745 is more potent and longer-lasting than finasteride, potentially better for treating hair loss.
The study compared the effectiveness of two drugs, GI198745 and finasteride, in inhibiting rat type 1 and 2 steroid 5α-reductases. GI198745 was found to be more potent and longer-lasting in inhibiting both enzymes, making it a potentially better treatment option for hair loss and other androgen-related disorders. The study also identified time-dependent inhibition as a factor affecting the progress curves and suggested that the drugs' different in vivo activities may be due to their pharmacokinetic parameters and mechanisms of inhibition.
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Cited in this study
research Inhibition of rat α-reductases by finasteride: Evidence for isozyme differences in the mechanism of inhibition
Finasteride effectively blocks rat enzymes, but with varying methods and strength.
research Mechanism-Based Inhibition of Human Steroid 5α-Reductase by Finasteride: Enzyme-Catalyzed Formation of NADP−Dihydrofinasteride, a Potent Bisubstrate Analog Inhibitor
Finasteride effectively blocks enzyme causing male pattern baldness.
research Finasteride: A slow-binding 5.alpha.-reductase inhibitor
Finasteride slowly binds to 5-alpha-reductase, affecting enzyme stability and inhibitor potency.
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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 3 3Abbreviations: r5AR1, rat 5α-reductase 1; r5AR2, rat 5α-reductase 2; and DHT, dihydrotestosterone.
GI198745 is more potent and longer-lasting than finasteride, potentially better for treating hair loss.
research Mechanism-Based Inhibition of Human Steroid 5α-Reductase by Finasteride: Enzyme-Catalyzed Formation of NADP−Dihydrofinasteride, a Potent Bisubstrate Analog Inhibitor
Finasteride effectively blocks enzyme causing male pattern baldness.