Effects of a novel finasteride 0.25% topical solution on scalp and serum dihydrotestosterone in healthy men with androgenetic alopecia

Int J Clin Pharmacol Ther. 2016 Jan;54(1):19-27. doi: 10.5414/CP202467.

Abstract

Objective: The effects on scalp and serum dihydrotestosterone (DHT) of different doses of a novel topical solution of 0.25% finasteride (P-3074), a type 2 5α-reductase, were investigated in men with androgenetic alopecia.

Methods: Two randomized, parallel-group studies were conducted. Study I: 18 men received 1 mL (2.275 mg) P-3074, applied to the scalp once a day (o.d.) or twice a day (b.i.d), or 1 mg oral tablet o.d. for 1 week. Study II: 32 men received P-3074 at the dose of 100 (0.2275 mg), 200 (0.455 mg), 300 (0.6285 mg), or 400 (0.91 mg) μL or the vehicle o.d. for 1 week. Scalp and serum DHT and serum testosterone were evaluated at baseline and treatment end.

Results: Change from baseline in scalp DHT was -70% for P-3074 o.d. and approx. -50% for P-3074 b.i.d. and the tablet. Serum DHT decreased by 60 - 70%. The doses of 100 and 200 μL P-3074 resulted in a -47/-52% scalp DHT reduction, similar to the 300 and 400 μL doses (i.e., -37/-54%). A -5.6% inhibition was observed for the vehicle. Serum DHT was reduced by only -24/-26% with 100 and 200 μL P-3074 and by -44/-48% with 300 and 400 μL P-3074. No relevant changes occurred for serum testosterone.

Conclusions: The novel finasteride 0.25% solution applied o.d. at the doses of 100 and 200 μL results in an appropriate inhibition of scalp DHT potentially minimizing the untoward sexual side-effects linked to a systemic DHT reduction.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • 5-alpha Reductase Inhibitors / administration & dosage*
  • Administration, Topical
  • Adolescent
  • Adult
  • Aged
  • Alopecia / drug therapy*
  • Alopecia / metabolism
  • Dihydrotestosterone / analysis*
  • Dihydrotestosterone / blood
  • Finasteride / administration & dosage*
  • Finasteride / adverse effects
  • Humans
  • Male
  • Middle Aged
  • Scalp / chemistry*

Substances

  • 5-alpha Reductase Inhibitors
  • Dihydrotestosterone
  • Finasteride