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

    October 2001 in “ Biochemical Pharmacology
    J. Darren Stuart, Frank X. Lee, Deborah Simpson Noel, Sue H. Kadwell, Laurie K. Overton, Christine Hoffman, Thomas A. Kost, Timothy K. Tippin, Russell L. Yeager, Kenneth Batchelor, H. Neal Bramson
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    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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