Sex Med. 2015 Sep 17;3(4):269-79. doi: 10.1002/sm2.80. eCollection 2015 Dec.
Pharmacokinetic Profile of Subcutaneous Testosterone Enanthate Delivered via a Novel, Prefilled Single-Use Autoinjector: A Phase II Study.
Sexual medicine
Jed Kaminetsky, Jonathan S Jaffe, Ronald S Swerdloff
Affiliations
Affiliations
- Manhattan Medical Research University Urology New York NY USA.
- Antares Pharma, Inc. Ewing NJ USA.
- Endocrinology Los Angeles Biomedical Research Institute Harbor-University of California Medical Center Torrance CA USA.
PMID: 26797061
PMCID: PMC4721027 DOI: 10.1002/sm2.80
Abstract
INTRODUCTION: Hypogonadism is one of the most common male endocrine problems. Although many treatments are currently available, unmet need exists for new testosterone (T) replacement therapies that are simple to administer and use, are safe, and mimic physiologic T levels.
AIM: The study aim was to determine the pharmacokinetics (PK), safety, and tolerability of T enanthate (TE) administered via a novel single-use autoinjector system, which was designed to eject high-viscosity solutions from a prefilled syringe fitted with a five-eighths-inch 27-gauge needle.
METHODS: Thirty-nine men with hypogonadism entered this dose-finding, open-label, parallel-group study. Patients were washed out of their topical T regimens and randomized to receive 50 or 100 mg of subcutaneous (SC) TE weekly. The reference group were patients with hypogonadism who were maintained on standard 200-mg intramuscular (IM) TE.
MAIN OUTCOME MEASURE: The primary outcome measure was the PK profile of SC TE, analyzed in reference to T levels used by the Food and Drug Administration to approve T products. Secondary outcome measures were safety and tolerability assessments.
RESULTS: Both doses of SC TE achieved normal average concentrations of serum T within a 168-h dosing interval after injection. Concentration ranges were similar at all time points following 50-mg SC TE injections and following the third injection in the 100-mg arm. Mean steady-state T concentration at week 6 was 422.4 and 895.5 ng/dL for the 50- and 100-mg SC TE arms, respectively. SC TE demonstrated PK dose proportionality. SC TE restored normal serum T with low variation relative to 200-mg IM without clinically significant adverse events.
CONCLUSIONS: Administration of TE via this novel injection system restored T levels to normal range in men with hypogonadism. SC TE dosed weekly demonstrated steady, dose-proportional measures of exposure and was well-tolerated. Kaminetsky J, Jaffe JS, Swerdloff RS. Pharmacokinetic profile of subcutaneous testosterone enanthate delivered via a novel, prefilled single-use autoinjector: A phase II study. Sex Med 2015;3:263-273.
Keywords: Autoinjector; Clinical Trial; Hypogonadism; Male; Phase II; Subcutaneous Injection; Testosterone; Viscosity
References
- Diabetes Care. 2011 Apr;34(4):828-37 - PubMed
- Ther Clin Risk Manag. 2008 Feb;4(1):269-86 - PubMed
- Endocr Pract. 2002 Nov-Dec;8(6):440-56 - PubMed
- Ann Pharmacother. 2014 Jul 2;48(9):1138-1144 - PubMed
- J Androl. 2012 Mar-Apr;33(2):190-201 - PubMed
- Hum Reprod. 2009 Feb;24(2):425-8 - PubMed
- JAMA Intern Med. 2013 Aug 12;173(15):1465-6 - PubMed
- PLoS One. 2014 Jan 29;9(1):e85805 - PubMed
- J Clin Endocrinol Metab. 2007 Nov;92(11):4241-7 - PubMed
- Saudi Med J. 2006 Dec;27(12):1843-6 - PubMed
- Expert Opin Drug Deliv. 2008 Apr;5(4):471-81 - PubMed
- Aging Male. 2008 Dec;11(4):171-8 - PubMed
- J Clin Endocrinol Metab. 2004 Dec;89(12):5920-6 - PubMed
- Clin Interv Aging. 2007;2(4):577-90 - PubMed
- J Androl. 2010 Sep-Oct;31(5):457-65 - PubMed
- Eur J Endocrinol. 1995 Apr;132(4):514-9 - PubMed
- J Sex Med. 2014 Feb;11(2):553-62 - PubMed
- Asian J Androl. 2010 Mar;12(2):227-33 - PubMed
- JAMA. 2013 Nov 6;310(17):1829-36 - PubMed
- J Clin Endocrinol Metab. 1999 Oct;84(10):3469-78 - PubMed
- Heart. 2010 Nov;96(22):1821-5 - PubMed
- J Clin Rheumatol. 2014 Aug;20(5):256-60 - PubMed
- J Clin Endocrinol Metab. 2010 Jun;95(6):2536-59 - PubMed
- Hum Reprod. 1995 Apr;10(4):862-5 - PubMed
- Int J Endocrinol. 2012;2012:625434 - PubMed
- Int J Clin Pract. 2014 Oct;68(10):1257-63 - PubMed
- J Sex Med. 2013 Sep;10(9):2326-33 - PubMed
- J Diabetes Sci Technol. 2007 Sep;1(5):725-9 - PubMed
- LGBT Health. 2014 Sep;1(3):165-7 - PubMed
- J Androl. 2001 Nov-Dec;22(6):1053-60 - PubMed
- Clin Endocrinol (Oxf). 1999 Jan;50(1):57-62 - PubMed
- Arch Intern Med. 2006 Aug 14-28;166(15):1660-5 - PubMed
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