How Oral Testosterone Now Has Changed from Its Initial Form of Methyltestosterone

Oral testosterone has changed significantly over the last few decades. Scientists have been working hard to uncover and perfect the most convenient and effective formulations of oral testosterone while simultaneously addressing toxicity concerns of methyltestosterone and introducing new forms of testosterone undecanoate (TU).

Striving to move medicine forward one step at a time and to make a difference in the lives of patients with hypogonadism (low testosterone), researchers have been busy developing improved testosterone therapies. 

This endeavor includes diversifying the route of administration and assessing testosterone absorption, toxicity, drug efficiency, patient experience, and level of convenience. 

Oral testosterone has come a long way, culminating in various forms readily available today. Patients now have a range of options when seeking testosterone treatment, which has steadily adapted to the actual needs of patients.

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History of Oral Testosterone

Testosterone therapy started as early as the 1930s when testosterone was isolated from bull testes for the first time in the Netherlands. At the same time, the first synthesized version of testosterone was produced, opening up new doors to treating patients with testosterone deficiency and paving the way for oral testosterone.

The first oral testosterone was developed in the form of 17α-methyltestosterone — a form of testosterone that is now obsolete. Due to its structure, long-term use of 17α-methyltestosterone was found to be toxic and lead to liver failure. As a result, its clinical use has been prohibited in Europe since the 1980s.

Since then, oral testosterone has steadily changed and garnered a lot of attention, particularly as it marks a highly convenient and painless testosterone therapy option. 

Continuous research ultimately led to the development of testosterone undecanoate, which has been approved by the Food and Drug Administration (FDA) and offers patients options for reliable testosterone replacement therapy (TRT).

The Birth of Testosterone Undecanoate (TU)

Testosterone undecanoate has been around for a good half a century, with its early beginnings dating back to the late 1970s. It’s considered orally and clinically effective, offering patients a safe oral alternative.

However, with 17α-methyltestosterone marking the first form of oral testosterone, other routes of administration dominated the industry for a long time. Testosterone was, therefore, compressed into pellets or administered as injections, while oral testosterone took a back seat for many years.

However, with progressing research and many factors in its favor, various forms of testosterone undecanoate are safely and effectively administered to patients all around the country today and its popularity is only rising.

Difference Between TU and Methyltestosterone

Testosterone does not necessarily equal testosterone and the same rings true for oral testosterone. Therefore, testosterone undecanoate and methyltestosterone are also vastly different, particularly when comparing TU to the toxic structure of 17α-methyltestosterone.

Methyltestosterone was synthesized with a methyl group in the 17α position and was made to be absorbed by the liver. Further research conducted on methyltestosterone, however, verified hepatotoxic properties — properties that have been proven to be toxic to the liver. Due to toxicity concerns, it is now considered an obsolete form of testosterone.

Learning from earlier forms of testosterone, testosterone undecanoate was then designed to bypass the liver and rely on absorption through the lymphatic system. Oral consumption leads to absorption by the gut via the lymph — a significant change from the former 17α-methyltestosterone.

Different Formulations of Testosterone Undecanoate

Several formulations of testosterone undecanoate have been introduced since the birth of TU in the 1970s. The first formulation of TU, Andriol, was found safe and effective, receiving the seal of approval for clinical use in many different countries. 

For full efficacy, however, you had to administer Andriol multiple times per day and keep up your intake of dietary fats. This led researchers, who were eager to find a testosterone therapy option that could enhance patient experiences, to carry on in their search for an effective, safe, and convenient alternative.

Other testosterone undecanoate formulations include Jatenzo, Tlando, and Kyzatrex — all of which have been approved by the FDA.

Advantages of Oral Testosterone Undecanoate

Testosterone undecanoate should be taken orally with food, usually twice a day. Unlike injections and other forms of testosterone, oral testosterone is a safe and painless way to maintain healthy testosterone levels.

Oral TU brings convenience to the table when compared to its non-oral counterparts, including forms like subcutaneous pellets, injections, nasal sprays, gels, and creams. Testosterone undecanoate is much easier to take, doesn’t create messes, and offers more accurate dosing and results.

In addition, some forms of oral testosterone undecanoate are available without health insurance as long as the patient has a current prescription; after all, testosterone is considered a “controlled substance” and therefore, requires a prescription by a qualified provider.

Other Routes of Administration

Testosterone replacement therapy has been available to patients with low T for a long time, however, other routes of administration are also used for the treatment of hypogonadism.

While injections, mainly in the form of testosterone cypionate and testosterone enanthate, are frequently administered to patients, many men seek a less painful alternative that can be administered more easily. 

This is especially important for patients who don’t have the time or bandwidth to return for regular administration visits and would like to self-administer their testosterone.

Other commonly used testosterone forms include gels and creams that offer limited efficacy, can be transferred over to other individuals upon touch, and can yield a wide range of results.

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Looking for Convenience? Oral Testosterone Might Be for You

Testosterone undecanoate is both effective and safe. But in addition to some of the more traditional forms of testosterone, it also offers a great deal of convenience: patients can take it regularly and with ease.

Reach out to your doctor and see if you’d be a good candidate for oral testosterone. It might help make your life a bit easier too.

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