Are oral testosterone pills effective?

October 8, 2025 •

4 min read

Hypogonadism, or low testosterone, affects an estimated 4 to 5 million men in the United States, yet only about 5% receive treatment [1.8.5]. The question for many is: are oral testosterone pills effective and safe for managing this condition?

Quick Summary

Modern oral testosterone pills are a convenient and effective option for treating low testosterone, comparable to injections [1.2.2]. Newer formulations have overcome past liver safety concerns and offer stable hormone levels [1.3.2, 1.2.2].

Key Points

Modern Pills Are Liver-Safe: Unlike older versions, new FDA-approved oral testosterone (testosterone undecanoate) is absorbed via the lymphatic system, bypassing the liver and avoiding toxicity [1.3.2].
High Efficacy: Clinical studies show oral pills like Jatenzo and Kyzatrex are highly effective, normalizing testosterone levels in 87% to 96% of men with hypogonadism [1.2.2].
Comparable to Injections: Research suggests oral testosterone is as effective as injections for improving mood, body composition, and sexual function [1.2.2].
Stable Hormone Levels: Twice-daily dosing mimics the body’s natural rhythm, avoiding the "peaks and troughs" associated with testosterone injections [1.2.2].
No Transference Risk: Oral pills eliminate the risk of accidentally transferring the hormone to women or children, a major concern with topical gels [1.6.5].
Blood Pressure Risk: The main safety concern is a potential increase in blood pressure, which can elevate cardiovascular risk and requires monitoring [1.4.5, 1.9.2].
Prescription Required: All effective and safe oral testosterone medications are available by prescription only after a diagnosis of hypogonadism [1.3.1].

The Evolution of Oral Testosterone Therapy

For decades, testosterone replacement therapy (TRT) was dominated by injections, gels, and patches. Early oral testosterone options, specifically methyltestosterone, fell out of favor due to a significant risk of liver toxicity [1.5.1, 1.5.3]. This was because the medication was processed through the liver, leading to potential damage with long-term use [1.3.1].

However, a new generation of oral testosterone has emerged, making pills a viable and safe option for many patients [1.6.1]. Modern FDA-approved medications use testosterone undecanoate. This formulation has a unique delivery system that bypasses the liver, instead being absorbed through the intestinal lymphatic system [1.3.1, 1.3.2]. This crucial difference eliminates the risk of hepatotoxicity associated with older pills [1.2.5].

Current FDA-Approved Oral Testosterone Pills

Several oral testosterone undecanoate capsules are now available by prescription in the United States:

Jatenzo®: Approved in 2019, Jatenzo was a significant step forward. In clinical trials, it restored testosterone to normal levels in 87% of men within a few months [1.2.2, 1.3.6].
Tlando®: This fixed-dose option (225 mg) was approved in 2022. A study showed it brought 80% of participants to a normal testosterone range within 24 days [1.2.2, 1.2.5, 1.3.6].
Kyzatrex™: Also approved in 2022, Kyzatrex has demonstrated up to 96% effectiveness in boosting testosterone levels to the normal range [1.2.2, 1.7.2, 1.7.3].

These medications are typically taken twice daily with food to ensure proper absorption and maintain stable hormone levels throughout the day, mimicking the body's natural rhythm [1.2.2, 1.3.2].

Effectiveness Compared to Other TRT Methods

Research indicates that modern oral testosterone pills are just as effective as testosterone injections at increasing hormone levels and improving symptoms of hypogonadism, such as low energy, mood changes, and reduced sexual function [1.2.2]. The primary difference lies in the delivery method and hormone level stability.

Oral Pills vs. Injections

Injections deliver a large dose of testosterone that gradually tapers off over one to two weeks [1.2.2, 1.3.4]. This can lead to a "peak and trough" effect, causing fluctuations in mood and energy levels, especially just before the next shot is due [1.2.2, 1.3.4]. Oral pills, taken twice daily, provide a steadier stream of hormones, which helps keep mood and energy more stable [1.2.2]. While injections have a lower risk of missed doses, oral pills are non-invasive and avoid needle phobia [1.2.2, 1.3.4].

Oral Pills vs. Gels

Topical gels are applied daily but come with their own set of challenges. Absorption can be inconsistent and is affected by factors like skin dryness or sweating [1.6.4]. The biggest concern with gels is the risk of transference to others, such as women and children, through skin-to-skin contact, which can cause serious health issues [1.6.4, 1.6.5]. Oral pills completely eliminate this risk of transference [1.3.4].

Comparison of TRT Methods


Method	Pros	Cons	Administration Frequency
Oral Pills (Undecanoate)	- Convenient, non-invasive [1.2.2] - Stable hormone levels [1.2.2] - No risk of transference [1.3.4] - Bypasses the liver [1.3.2]	- Must be taken twice daily with food [1.2.2] - Higher cost, few generics [1.2.2] - Can increase blood pressure [1.9.2]	Twice Daily [1.2.2]
Injections	- Less frequent dosing [1.3.4] - Lower cost (generics available) [1.3.4] - Rapid absorption [1.6.3]	- "Peak and trough" effect [1.3.4] - Needle phobia, injection site pain [1.3.4] - Higher risk of polycythemia (high red blood cell count) [1.6.6]	Weekly to Every 10-12 Weeks [1.3.4]
Topical Gels	- Easy to use [1.3.4] - Daily application provides consistency	- Risk of transference to others [1.6.4] - Skin irritation [1.6.4] - Variable absorption [1.6.4] - Must wait before showering/swimming [1.6.4]	Daily [1.3.4]

Potential Side Effects and Safety Considerations

While modern oral testosterone is considered safe for the liver, like all forms of TRT, it carries potential side effects [1.6.1]. The most significant warning associated with testosterone undecanoate is an increase in blood pressure, which can elevate the risk of heart attack or stroke [1.4.5, 1.9.2]. Regular blood pressure monitoring is essential for anyone on this therapy [1.4.5].

Other common side effects can include [1.4.3, 1.9.5]:

Headache
An increase in red blood cell count (polycythemia)
Nausea
Diarrhea
A decrease in HDL ("good") cholesterol

Long-term use of any testosterone therapy may also limit sperm production, cause testicular shrinkage, and potentially worsen sleep apnea or benign prostatic hyperplasia (BPH) [1.9.3]. It is crucial to have a thorough medical evaluation and ongoing monitoring by a healthcare provider before and during treatment [1.3.1].

Conclusion

So, are oral testosterone pills effective? The answer is a definitive yes. The new generation of testosterone undecanoate capsules—like Jatenzo, Kyzatrex, and Tlando—are a highly effective, safe, and convenient treatment for men diagnosed with hypogonadism [1.2.1, 1.2.2]. They offer comparable efficacy to injections and gels while avoiding the liver toxicity of older oral forms, the hormonal fluctuations of injections, and the transference risk of gels [1.3.2, 1.6.5]. However, due to the risk of increased blood pressure and other potential side effects, treatment must be managed under the strict supervision of a qualified healthcare provider to ensure the benefits outweigh the risks [1.4.5].

For more information from an authoritative source, you can visit the Endocrine Society's page on testosterone therapy.

Frequently Asked Questions

Older oral testosterone pills (methyltestosterone) were known to cause liver damage. However, modern FDA-approved oral testosterone, which uses testosterone undecanoate (e.g., Jatenzo, Kyzatrex), bypasses the liver and is not associated with liver toxicity [1.3.2, 1.6.1].

Studies show that modern oral testosterone pills are as effective as injections at raising testosterone levels and improving symptoms like mood, energy, and sexual function. Oral pills provide more stable hormone levels, while injections are administered less frequently [1.2.2].

The most common FDA-approved brands for oral testosterone undecanoate in the U.S. are Jatenzo, Kyzatrex, and Tlando [1.3.1, 1.3.6].

Improvements in energy and mood may be noticed within a few weeks of starting treatment [1.2.3]. More significant changes, like increased muscle mass or improvements in erectile dysfunction, can take three to six months [1.2.2].

A primary warning for modern oral testosterone undecanoate is that it can cause an increase in blood pressure, which may raise the risk of major cardiovascular events like heart attack and stroke. Regular monitoring by a doctor is essential [1.4.5, 1.9.2].

Yes, it is recommended to take oral testosterone capsules with food. This aids in the proper absorption of the medication through the lymphatic system [1.2.2, 1.3.2].

No, effective and FDA-approved oral testosterone medications are only available with a prescription from a licensed healthcare provider after being diagnosed with a condition like hypogonadism. Over-the-counter products claiming to boost testosterone are not the same and could be harmful [1.3.1].