Current and emerging testosterone therapies for male hypogonadism

Figures & data

Figure 1 History of testosterone therapy.

Notes: ^aNot approved for use in the US; ^bno longer approved for use in the US. Adapted from Nieschlag E, Behre HM, Bouchard P, et al. Testosterone replacement therapy: current trends and future directions. Human Reproduction Update. 2004;10(5):409–419, by permission of Oxford University Press¹⁹ and Pfeil E, Dobs AS. Current and future testosterone delivery systems for treatment of the hypogonadal male. Expert Opinion on Drug Delivery. 2008;5(4):471–481, copyright © 2008, Informa Healthcare. Reproduced with permission of Informa Healthcare.²⁸
Abbreviation: SC, subcutaneous.

Figure 2 Clinically significant effects of testosterone replacement.

Note: Adapted from Pfeil E, Dobs AS. Current and future testosterone delivery systems for treatment of the hypogonadal male. Expert Opinion on Drug Delivery. 2008;5(4):471–481, copyright © 2008, Informa Healthcare. Reproduced with permission of Informa Healthcare²⁸ and Edelstein D, Sivanandy M, Shahani S, Basaria S. The latest options and future agents for treating male hypogonadism. Expert Opinion on Pharmacotherapy. 2007;8(17):2991–3008, copyright © 2007, Informa Healthcare. Reproduced with permission of Informa Healthcare.⁴ Image © iStock.com/alexandragl1.
Abbreviations: ↑, increased; ↓, decreased; HDL, high-density lipoprotein; PSA, prostate-specific antigen.

Table 1 Testosterone therapies by formulation/route

Formulation/route	Dosing ranges	Dosing frequency
Testosterone implants^Citation30	150–450 mg	Every 3–6 months
Intramuscular injections
Testosterone esters^Citation89	50–400 mg	Every 2–4 weeks
Testosterone undecanoate^Citation34,Citation35	750 mg, and then 750 mg 4 weeks later, and then 750 mg every 10 weeks thereafter; 1,000 mg every 10–14 weeks	Every 10–14 weeks
Oral^Citation36 (not United States Food and Drug	120–160 mg daily, in two divided doses, for the first 2–3 weeks. Then, 40–120 mg daily	Once to twice a day
Administration-approved)
Transdermal
Testosterone patch^Citation37	2–6 mg	Once daily
Testosterone gel^Citation39,Citation90,Citation91	50–100 mg (1% gel) 20.25–81 mg (1.62% gel) 10–70 mg (2% gel)	Once daily
Testosterone solution^Citation42	60–120 mg	Once daily
Transbuccal^Citation44	30 mg	Two times a day
Intranasal testosterone^Citation48	11 mg	Three times a day

Table 2 Emerging testosterone therapies

Formulation/route	Dosing ranges	Dosing frequency
Phase III
Subcutaneous self-administered testosterone^Citation50	50–100 mg	Once weekly
Oral testosterone undecanoate^Citation53,Citation55	100–300 mg	Twice daily
Testosterone gel^Citation58	50 mg	Once daily
Phase II
Unmodified oral testosterone^Citation61	120–240 mg	Twice daily
Spray-on testosterone^Citation64	10–70 mg	Once daily

Table 3 Potential cardiovascular risks and benefits of testosterone

Potential cardiovascular risks  ↑ hematocrit^Citation92  ↓ (limited) HDL cholesterol^Citation92  ↑ risk of MI^Citation69  ↑ all-cause mortality^Citation68  ↑ risk of ischemic stroke^Citation68 Potential cardiovascular benefits  ↓ systolic and diastolic blood pressure^Citation85  ↓ blood glucose^Citation85  ↓ hemoglobin A1c^Citation85  ↓ LDL cholesterol^Citation85  ↑ HDL cholesterol^Citation85  ↓ triglycerides^Citation85  ↓ serum total cholesterol^Citation85,Citation93  ↑ hemoglobin^Citation92  ↑ body composition^Citation27  ↓ body fat^Citation27 Protective against MI^Citation86   ↑ exercise performance^Citation94   ↑ ischemic threshold^Citation94   ↓ risk of MIand exercise-induced MI^Citation95,Citation96  Possible reduction in risk of atherosclerosis^Citation97

Abbreviations: ↑, increased; ↓, decreased; HDL, high-density lipoprotein; MI, myocardial infarction; LDL, low-density lipoprotein.

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