Efficacy and safety of the 2% formulation of testosterone topical solution applied to the axillae in androgen-deficient men

Clin Endocrinol (Oxf). 2011 Dec;75(6):836-43. doi: 10.1111/j.1365-2265.2011.04152.x.

Abstract

Objectives: Testosterone replacement therapy in hypogonadal men relieves symptoms and restores serum testosterone levels to the physiological range. In this study, we assessed the safety, pharmacokinetics, and efficacy of the 2% formulation of testosterone topical solution applied daily to the axillae.

Design and patients: An open-label trial was conducted in testosterone-deficient men who started on a daily dose of 60 mg of testosterone. Dose was adjusted on Days 45 and 90 when necessary to maintain serum testosterone levels within the physiological range (10·41-36·44 nmol/l) based on average serum testosterone levels on Days 15 and 60, respectively. Sexual function and mood changes were assessed by the Psychosexual Daily Questionnaire (PDQ) for the 7 days preceding visits at Days 1, 15, 60, and 120; and quality of life by SF-36 questionnaire on Days 1, 60, and 120. Safety parameters, laboratory tests, and adverse events were collected at each visit.

Results: Among the Completer Set (135 study completers and 3 patients who discontinued due to adverse events), 76·1% (Days 15/16), 84·8% (Days 60/61), and 84·1% (Days 120/121) had an average total testosterone level between 10·41-36·44 nmol/l. PDQ scores increased significantly from baseline to 120 days of treatment (p < 0·0001). Significant improvement was observed in the physical (p < 0·05) and mental (p < 0·0001) components of the SF-36 after 120 days of treatment. Adverse events reported in >2% of the 155 subjects who received ≥ 1 dose were application site irritation (7·1%), application site erythema (5·2%), headache (5·2%), increased hematocrit (3.9%), nasopharyngitis (3·9%), diarrhea (2·6%), and vomiting (2·6%).

Conclusions: These results indicate that once-daily application of the testosterone topical solution 2% to the axillae is a safe and effective treatment for androgen replacement in hypogonadal men.

Publication types

  • Clinical Trial
  • Multicenter Study

MeSH terms

  • Administration, Topical
  • Adult
  • Affect / drug effects
  • Aged
  • Androgens / deficiency*
  • Axilla
  • Chemistry, Pharmaceutical
  • Hormone Replacement Therapy / adverse effects
  • Hormone Replacement Therapy / methods
  • Humans
  • Hypogonadism / drug therapy*
  • Male
  • Middle Aged
  • Osmolar Concentration
  • Testosterone / administration & dosage*
  • Testosterone / adverse effects*
  • Treatment Outcome

Substances

  • Androgens
  • Testosterone