Pharmacokinetics And Relative Bioavailability Of Absorbed Testosterone After Administration Of A 1.62% Testosterone Gel To Different Application Sites In Men With Hypogonadism

Miller, Jodi; Britto, Margaret; Fitzpatrick, Sherahe; McWhirter, Cecilia; Testino, Samuel A; Brennan, John J.; ZumBrunnen, Troy L.

doi:10.4158/ep10192.or

Cited by 24 publications

(12 citation statements)

References 8 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A new formulation of testosterone gel (1.62%) was developed that delivers testosterone with a lower volume of gel than the current product. This allows the patient to reduce the total mass of gel applied from the current 5.0 g to 10.0 g per day to 1.25 g to 5.0 g per day [19,20].…”

Section: Introductionmentioning

confidence: 99%

Efficacy and Safety Study of 1.62% Testosterone Gel for the Treatment of Hypogonadal Men

Kaufman

Miller

Garwin

et al. 2011

The Journal of Sexual Medicine

Self Cite

View full text Add to dashboard Cite

Introduction Male hypogonadism is a significant and growing problem that can be successfully treated with testosterone replacement therapy. A new formulation of testosterone gel (1.62%) was developed with increased viscosity, reduced volume of application, and increased skin permeation compared with other currently available testosterone gels. Aim To evaluate the efficacy and safety of titrated doses of 1.62% testosterone gel after daily application to the skin of hypogonadal men for 182 days. Methods This was a multicenter, randomized, double-blind, placebo-controlled study in hypogonadal men (234 active; 40 placebo), 18 to 80 years of age with average serum total testosterone concentrations <300 ng/dL and prostate-specific antigen <2.5 ng/mL. Topical testosterone gel (1.62%), 1.25 g, 2.5 g, 3.75 g, and 5.0 g, or placebo gel was applied once daily to either upper arms/shoulders or abdomen. Dose adjustments were made on days 14, 28, and 42. Main Outcome Measures The percentage of subjects with serum total testosterone average concentrations (Cav) within the normal range of 300–1,000 ng/dL on study days 14, 56, 112, and 182. Results Following titration, significantly (P < 0.0001) more subjects receiving active treatment had testosterone Cav values (range 81.6% to 82.5%) within the eugonadal range compared with placebo (range 28.6% to 37.0%) on all study days. The 1.62% gel was safe and well tolerated. Conclusions In this study, treatment with 1.62% testosterone gel was safe and efficacious, resulting in an acceptable percentage of hypogonadal males achieving eugonadal serum testosterone levels.

show abstract

Section: Introductionmentioning

confidence: 99%

Efficacy and Safety Study of 1.62% Testosterone Gel for the Treatment of Hypogonadal Men

Kaufman

Miller

Garwin

et al. 2011

The Journal of Sexual Medicine

Self Cite

View full text Add to dashboard Cite

show abstract

“…One previous study has reported that the pharmacokinetics of scrotal application of testosterone gel was similar to that of a scrotal testosterone patch or a fivefold larger dose of non-scrotal testosterone gel, consistent with at least a fivefold higher transdermal bioavailability of testosterone (Kuhnert et al, 2005). Other studies assessing pharmacokinetics of testosterone application to non-scrotal skin have yielded variable time of peak concentration (Tmax) ranging from 6-16 h (Marbury et al, 2003;Miller et al, 2011;Olsson et al, 2014) but similar peak concentration (Cmax) as scrotal skin application (Rolf et al, 2002;Bouloux, 2005;Olsson et al, 2014). Although most studies revealed a marked delay in peak serum testosterone concentration, another study of 100 mg testosterone gel applied to non-scrotal skin in hypogonadal men reported rapid absorption kinetics and higher Cmax (≥13.4 ng/mL) (Wang et al, 2000).…”

Section: Discussionmentioning

confidence: 95%

Pharmacokinetics of testosterone cream applied to scrotal skin

et al. 2017

View full text Add to dashboard Cite

Scrotal skin is thin and has high steroid permeability, but the pharmacokinetics of testosterone via the scrotal skin route has not been studied in detail. The aim of this study was to define the pharmacokinetics of testosterone delivered via the scrotal skin route. The study was a single-center, three-phase cross-over pharmacokinetic study of three single doses (12.5, 25, 50 mg) of testosterone cream administered in random sequence on different days with at least 2 days between doses to healthy eugonadal volunteers with endogenous testosterone suppressed by administration of nandrolone decanoate. Serum testosterone, DHT and estradiol concentrations were measured by liquid chromatograpy, mass spectrometry in extracts of serum taken before and for 16 h after administration of each of the three doses of testosterone cream to the scrotal skin. Testosterone administration onto the scrotal skin produced a swift (peak 1.9-2.8 h), dose-dependent (p < 0.0001) increase in serum testosterone with the 25 mg dose maintaining physiological levels for 16 h. Serum DHT displayed a time- (p < 0.0001), but not dose-dependent, increase in concentration reaching a peak concentration of 1.2 ng/mL (4.1 nm) at 4.9 h which was delayed by 2 h after peak serum testosterone. There were no significant changes in serum estradiol over time after testosterone administration. We conclude that testosterone administration to scrotal skin is well tolerated and produces dose-dependent peak serum testosterone concentration with a much lower dose relative to the non-scrotal transdermal route.

show abstract

“…Good safety profiles and high rates of patient compliance have been reported with gel use [14,17]. Upon discontinuation, serum testosterone returns to hypogonadal levels within 2 to 3 days, which may be an advantage should termination of treatment be desired or necessary [18]. Others, however, may be unintentionally exposed to the gel through skin‐to‐skin contact, so users of testosterone gel need to be made aware of this possibility and potential implications [19,20].…”

Section: Discussionmentioning

confidence: 99%

One‐Year Efficacy and Safety Study of a 1.62% Testosterone Gel in Hypogonadal Men: Results of a 182‐Day Open‐Label Extension of a 6‐Month Double‐Blind Study

Kaufman

Miller

Fitzpatrick³

et al. 2012

The Journal of Sexual Medicine

Self Cite

View full text Add to dashboard Cite

Pharmacokinetics And Relative Bioavailability Of Absorbed Testosterone After Administration Of A 1.62% Testosterone Gel To Different Application Sites In Men With Hypogonadism

Cited by 24 publications

References 8 publications

Efficacy and Safety Study of 1.62% Testosterone Gel for the Treatment of Hypogonadal Men

Efficacy and Safety Study of 1.62% Testosterone Gel for the Treatment of Hypogonadal Men

Pharmacokinetics of testosterone cream applied to scrotal skin

One‐Year Efficacy and Safety Study of a 1.62% Testosterone Gel in Hypogonadal Men: Results of a 182‐Day Open‐Label Extension of a 6‐Month Double‐Blind Study

Contact Info

Product

Resources

About