title: The efficacy, bioavailability and safety of a novel hydroalcoholic testosterone gel 2% in hypogonadal men: results from phase II open-label studies.
abstract: Pharmacokinetics, pharmacodynamics and safety of a novel hydroalcoholic testosterone gel 2% (TG) were evaluated in phase II sequential dose escalation studies using 3 application sites (thigh, abdomen and shoulder/upper arm) and 2 application methods. Hypogonadal men (n = 40), 18-75 years, with serum testosterone <300 ng dl(-1) were included in both studies. Study 1 evaluated hand-applied multiple doses of TG 1.25, 2.50 and 3.75 ml (23, 46 and 70 mg of testosterone, respectively), once daily for 10 days to shoulder/upper arm. Study 2 evaluated applicator-applied (TG 1.25, 2.50 and 3.75 ml) versus hand-applied (TG 2.5 ml) doses, once daily for 7 days to shoulder/upper arm. Primary endpoint for both studies was responder rate (Cave testosterone levels between 298 and 1050 ng dl(-1) ). In Study 1 following multiple applications, >70% participants in each group were responders. Dose-dependent increase was observed in PK values for total testosterone, free testosterone and DHT. In Study 2, responder rate was dose proportional: 16.7%, 50.0% and 77.8% responders in TG 1.25, 2.50 and 3.75 ml groups respectively. The bioavailability was highest for the shoulder application. There was a significant improvement in almost all the domains of sexual functioning. Applicator-application was preferred over hand-application by majority of the participants. TG was found to be safe and well tolerated in hypogonadal men.
authors.affiliation: AccuMed Research, Garden City, NY, USA.
authors.forename: M
authors.initials: M
authors.lastname: Efros
authors.affiliation: Ferring Galenisches Labor AG, Allschwil, Switzerland.
authors.forename: D
authors.initials: D
authors.lastname: Carrara
authors.affiliation: International Pharma Science Center, Ferring Pharmaceuticals, Copenhagen, Denmark.
authors.forename: A
authors.initials: A
authors.lastname: Neijber
mesh_terms: D000293:Adolescent; D000328:Adult; D000368:Aged; D001682:Biological Availability; D013196:Dihydrotestosterone / Q000097:blood; D005782:Gels / Q000009:adverse effects / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D006801:Humans; D007006:Hypogonadism / Q000188:drug therapy*; D008297:Male; D008875:Middle Aged; D013739:Testosterone / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D016896:Treatment Outcome; D055815:Young Adult
chemical_list: D005782:Gels; D013196:Dihydrotestosterone; D013739:Testosterone
keywords: Efficacy; hydroalcoholic testosterone gel 2%; male hypogonadism; pharmacokinetics; pump applicator