Alternative Testosterone Formulations Beyond Injections and Topicals
Yes, there are two additional testosterone formulations available: oral testosterone undecanoate capsules and implantable testosterone pellets. 1
Oral Testosterone Undecanoate
Oral testosterone undecanoate (brand names include Jatenzo, Tlando) is an FDA-approved oral formulation that must be taken with food for proper absorption. 2
Dosing and Administration
- Starting dose is typically 200 mg twice daily with meals 2
- Dose range: 100 mg (morning only) to 400 mg twice daily based on testosterone levels 2
- Must be taken with food containing fat—absorption increases by 37% with 16% fat content, 87% with 33% fat, and 94% with 45% fat content compared to fasted conditions 2
- Dose adjustments are made on Days 28 and 56 based on testosterone levels drawn 3-5 hours after the morning dose 2
Key Characteristics
- Achieves average plasma testosterone concentrations of 393 ng/dL after 90 days of treatment 2
- Avoids first-pass hepatic metabolism through lymphatic absorption 3, 4
- Generates supraphysiological dihydrotestosterone (DHT) levels with a DHT:testosterone ratio of 0.36, which is higher than physiological 5
- Requires twice-daily dosing, which may reduce adherence 4
Important Safety Considerations
- FDA requires labeling warning about increased blood pressure and cardiovascular risk (myocardial infarction, stroke, cardiovascular death) 2
- Can cause polycythemia (increased hemoglobin/hematocrit) 2
- May worsen benign prostatic hyperplasia and increase prostate cancer risk 2
- Contraindicated in women, patients with breast or prostate cancer, and age-related hypogonadism 2
Implantable Testosterone Pellets
Testosterone pellets offer a long-term alternative requiring a minor surgical procedure for subcutaneous implantation, typically lasting 3-6 months. 1
Key Characteristics
- Provide sustained testosterone release over several months 1
- Require a minor surgical procedure for implantation under the skin 1
- Avoid daily administration and provide more stable levels than some other formulations 1
- Less commonly used due to the procedural requirement and potential for pellet extrusion 1
Comparison to Standard Formulations
Advantages of Oral Formulation
- Non-invasive route of administration 3, 4
- Avoids skin transfer risk seen with gels 1
- No injection discomfort 1
Disadvantages of Oral Formulation
- Requires strict adherence to twice-daily dosing with fatty meals 2
- Variable absorption depending on meal fat content 2
- Supraphysiological DHT levels may theoretically increase prostate-related risks 5
- More expensive than injectable testosterone 1
- Increased cardiovascular risk warnings 2
Advantages of Pellets
- Longest duration of action (3-6 months) 1
- No daily administration required 1
- Stable testosterone levels 1
Disadvantages of Pellets
- Requires minor surgical procedure 1
- Risk of pellet extrusion or infection 1
- Cannot easily adjust dose once implanted 1
- Less commonly available 1
Clinical Decision-Making
For most patients, transdermal preparations (gels, patches) remain the preferred first-line option due to stable testosterone levels and patient convenience, despite higher cost. 1
Oral testosterone undecanoate should be considered for patients who:
- Cannot tolerate injections or topical preparations 3, 4
- Are willing to adhere to twice-daily dosing with meals 2
- Do not have significant cardiovascular risk factors 2
- Understand the need for consistent meal fat content 2
Testosterone pellets should be considered for patients who:
- Have poor adherence to daily or weekly regimens 1
- Prefer the longest possible dosing interval 1
- Are willing to undergo minor surgical procedures 1
Monitoring Requirements
Regardless of formulation, testosterone levels should be measured 2-3 months after initiation or dose changes, then every 6-12 months once stable. 1, 6