Finasteride: The First 5α‐Reductase Inhibitor

@article{Sudduth1993FinasterideTF, title={Finasteride: The First 5$\alpha$‐Reductase Inhibitor}, author={S L Sudduth and Michael J. Koronkowski}, journal={Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy}, year={1993}, volume={13}, url={https://api.semanticscholar.org/CorpusID:71103672} }
Its efficacy in regression of prostate gland enlargement is rapid and predictable, although correlation with subsequent improvement in urinary flow and symptoms is highly variable, and finasteride may hold promise for other DHT‐mediated disorders such as acne, facial hirsutism, frontal lobe alopecia, and prostate cancer, but its use in these conditions remains investigational.
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A new look at the 5alpha-reductase inhibitor finasteride.

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Finasteride-Its Impact on Sexual Function and Prostate Cancer

The sexual adverse effects associated with finasteride should be viewed in relation to normal prevalence and natural history of erectile dysfunction in the population, age of the patient, other confounding factors and also nocebo effect.

Pharmacodynamic Modeling of Finasteride, a 5α‐Reductase Inhibitor

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Comparison of cyproterone acetate plus ethinyl estradiol and finasteride in the treatment of hirsutism

CPA+E appears to be more effective than 5α-reductase inhibitor finasteride in long-term treatment of hirsute women, and Diane® is also a cost-effective drug.

Pharmacokinetics and pharmacodynamics of TF-505, a novel nonsteroidal 5alpha-reductase inhibitor, in normal subjects treated with single or multiple doses.

TF-505 was well tolerated in healthy male volunteers and the predicted effect curves matched the observed data when the indirect response model was applied to the time course of the suppressant effect of TF-505 on plasma DHT concentrations after both the single and multiple studies.

Evaluation of the therapeutic effects of AGA drugs by measuring finasteride, dutasteride, and dihydrotestosterone in hair.

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64 References

The clinical development of a 5α-reductase inhibitor, finasteride

Hormonal effects of an orally active 4‐azasteroid inhibitor of 5α‐reductase in humans

It is concluded that MK‐906 is a highly effective 5α‐reductase inhibitor in vivo, and both hepatic and extrasplanchnic 5α-reductases are inhibited.

Effects of finasteride (MK-906), a 5 alpha-reductase inhibitor, on circulating androgens in male volunteers.

Finasteride is well tolerated by normal volunteers and results in significant suppression of serum DHT at all doses tested, and the T/DHT ratio increased with all doses and returned to baseline when drug was discontinued.

Hormonal effects, tolerability, and preliminary kinetics in men of MK-906, a 5α-reductase inhibitor

Effect of MK-906, a specific 5 alpha-reductase inhibitor, on serum androgens and androgen conjugates in normal men.

While all three steroids appeared to be good markers of systemic 5 alpha-reductase inhibition, further research will be needed to determine which steroid best reflects tissue DHT levels in patients receiving these inhibitors.

One‐Year Experience in the Treatment of Benign Prostatic Hyperplasia with Finasteride

It is concluded that finasteride has the potential to be an effective chronic therapy for benign prostatic hyperplasia and can reduce prostate size and improve maximum urinary flow with no loss of efficacy after 1 year of treatment.

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

The conversion of testosterone to 5a-dihydrotestosterone by prostate particulates from rats, dogs, and humans was investigated, and significant species differences were found with their pH profiles,…

Inhibitors of steroid 5 alpha-reductase in benign prostatic hyperplasia, male pattern baldness and acne.

Effect of castration, DES, flutamide, and the 5α‐reductase inhibitor, MK‐906, on the growth of the dunning rat prostatic carcinoma, R‐3327

The failure of MK‐906 to influence tumor growth in the TP‐treated castrates strongly suggests that the R‐3327 tumor can respond to testosterone directly, and is unlikely to be affected by a pure 5α‐reductase inhibitor such as MK‐ 906.

Disposition and pharmacokinetics of [14C]finasteride after oral administration in humans.

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