What are the oral testosterone replacement therapy (TRT) options?

From the Guidelines

Oral testosterone replacement therapy (TRT) options include testosterone undecanoate (Jatenzo, Andriol), which is the primary FDA-approved oral testosterone medication in the United States, with a typical dosage ranging from 158-396 mg taken twice daily with food 1.

Key Considerations

• Testosterone undecanoate is absorbed through the lymphatic system, bypassing first-pass liver metabolism when taken with fatty foods.
• Methyltestosterone (Android, Testred) is another option but is less commonly prescribed due to potential liver toxicity concerns.
• Oral testosterone is convenient but requires consistent dosing and food intake for stable hormone levels.
• Patients should have testosterone levels monitored regularly, typically 3-6 months after starting therapy and periodically thereafter.

Potential Side Effects and Contraindications

• Side effects may include acne, sleep apnea, polycythemia (increased red blood cell count), and potential cardiovascular risks.
• These medications are contraindicated in men with prostate or breast cancer, and caution is advised in those with liver disease, sleep apnea, or cardiovascular conditions.

Comparison with Other Formulations

• The FDA recently approved an oral formulation of testosterone undecanoate for use in the United States, but the evidence for efficacy or harms of oral testosterone was not evaluated in the review 1.
• No clinical trial directly compared an intramuscular versus a transdermal formulation of testosterone, and patient characteristics, testosterone levels, and outcome reporting varied in studies of intramuscular versus transdermal formulations 1.

Monitoring and Follow-up

• Regular monitoring of testosterone levels is essential to ensure stable hormone levels and minimize potential side effects.
• Patients should be closely monitored for signs of polycythemia, sleep apnea, and cardiovascular risks, and caution should be exercised in those with pre-existing conditions.

From the FDA Drug Label

Testosterone Undecanoate Capsules is a prescription medicine that contains testosterone. Testosterone Undecanoate Capsules are used to treat adult men who have low or no testosterone due to certain medical conditions

The oral testosterone replacement therapy (TRT) option is Testosterone Undecanoate Capsules.

• The available dosage strengths are:
  • 100 mg
  • 150 mg
  • 200 mg 2 2 2

From the Research

Oral Testosterone Replacement Therapy (TRT) Options

The available oral testosterone replacement therapy options include:

• Testosterone undecanoate, which is available in various formulations, including oral capsules 3, 4, 5, 6
• Methyltestosterone, however, it is associated with hepatic toxicity 3
• Other oral testosterone formulations, such as JATENZO and TLANDO, which have recently been approved by the US Food and Drug Administration 5, 6

Characteristics of Oral TRT Options

• Oral testosterone undecanoate has a short half-life, requiring multiple doses per day 3
• Testosterone undecanoate formulations, such as TLANDO, can restore testosterone levels to the normal range in the majority of hypogonadal males without requiring dose titration 5
• JATENZO and TLANDO use a self-emulsifying drug delivery system and lymphatic absorption, addressing some limitations of other dosing routes while providing a safe option without evidence of liver dysfunction 6

Comparison with Other TRT Options

• Oral TRT options are compared to other formulations, including transdermal gels, injectable testosterone, and transbuccal testosterone systems 7, 4
• The choice of TRT option depends on various factors, including safety, efficacy, cost-effectiveness, dosing flexibility, and side effects 7