Finally! A safe, effective oral testosterone pill: Jatenzo!

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At our hormone replacement clinics, we are dedicated to staying up-to-date on all new developments and breakthroughs concerning Testosterone Replacement Therapy (TRT). We monitor all aspects of testosterone regimens, including delivery methods.

Until recently the most common methods of testosterone therapy were: Intramuscular testosterone injections; testosterone patches; and testosterone gels. Each one of these methods has advantages and disadvantages. Here is a brief review of these approaches:

Testosterone injections. Testosterone injections are painless and result in increased amounts of both free testosterone and total testosterone. The downside of injections is that they are somewhat inconvenient, and some people have a fear of needles.
Testosterone patches. Testosterone patches are easy to apply. The downside of using this method of testosterone replacement is that this method is transdermal, which means the testosterone must penetrate the skin to enter the bloodstream. This may result in less testosterone surviving the journey through skin, muscle, fat, and blood vessels before it can get to work. Another disadvantage of testosterone patches is they may be hazardous to women and children who accidentally come in contact with them. Testosterone patches may also cause skin irritation.
Testosterone gels. Testosterone gels have the same advantages (easy to apply) and disadvantages (inefficient delivery of the hormone, skin irritation, and risk to women and children) of testosterone patches.

All three of the above-mention delivery systems work, but they also come with the problems mentioned.

However, there is a new kid on the block: Jatenzo

For the first time, TRT is available safely, via an oral, soft gel capsule called Jatenzo. Jatenzo is the only FDA-approved oral TRT delivery method.

This is an exciting new development for a few reasons. First, a safe and effective form of oral testosterone has not until now been available. This was a result of liver toxicity side effects from testosterone in a pill form.

The problem with earlier testosterone pills is that despite being absorbed by the digestive system, the testosterone was metabolized by the liver, which caused adverse side effects. As a result, oral testosterone was rarely prescribed in the United States.

To bypass the liver, Jatenzo was created by alkalizing the testosterone at the carbon-17 position, and fatty-acid esterification of testosterone to alter it to a testosterone ester. This alteration enabled the testosterone to be processed via the lymphatic system and thus bypass the liver, and all of the severe side effects of previous oral testosterone.

A second benefit of undergoing TRT in pill form is convenience. No more measuring the liquid into the syringe, and applying the gel or patch. These methods are effective, but they have the drawbacks mentioned above.

A third benefit is minimal side effects. Earlier oral versions of TRT wreaked havoc on the digestive system (i.e. diarrhea, nausea, burping), and damaged the liver. With Jatenzo side effects, while they do occur, are rare and nowhere nearly as severe as earlier oral testosterone pills.

An Expert Weighs in on Jatenzo

At the 2021 Sexual Medicine Society of North America Fall Scientific Meeting, encouraging conclusions on the effectiveness and safety of Jatenzo were presented. Dr. Ronald Swerdloff, MD, a lead researcher of the study, discussed why Jatenzo has overcome the problems encountered by earlier types of oral testosterone. Dr. Swerdloff is a professor of medicine and senior investigator at The Lundquist Institute, Harbor-UCLA Medical Center, and David Geffen School of Medicine, University of California, Los Angeles.

“Male hypogonadism is a condition that occurs in a significant number of our population and there are a number of testosterone formulations and routes of administration that are used to treat this condition. Routes of administration available to physicians include injections, transdermal preparations, transbuccal administration, long-acting injectables, intranasal and oral medications. Until the last couple of years, we did not have an oral preparation that we could use effectively and safely.

“In 2019, the FDA reapproved a new oral formulation of testosterone undecanoate (Jatenzo), which is taken twice a day as capsules and absorbed through the intestine. The difference between this compound and other compounds that were orally administered is that this new formulation is absorbed through the lymphatic system, rather than going directly to the liver.

“The reason why that was important is that previously, the oral preparations that were available either were very short-acting or had liver toxicity. We demonstrated the efficacy of Jatenzo, showing that this preparation would result in blood levels of testosterone that were quite normal even when ingesting a normal diet. We have now presented two-year safety data demonstrating longer-term safety of the preparation.

“This study had previously shown that you could increase the testosterone level from clearly low levels into the normal reference range. We were quite sure about the efficacy, but we also wanted to demonstrate, over a 2-year period of time, that the safety criteria were met. The best part about this study is that we clearly showed that there was no significant liver toxicity. We also looked at other types of changes that might be important.

“There were very small increases in blood pressure (between 5 to 7 mm of mercury) that have been seen with other testosterone formulations. In addition to that, there was a small increase in the hemoglobin and hematocrit.

“Five of about 86 individuals had levels that were high enough that we thought the dose should be reduced in those individuals by the practicing physician. That's also a class effect. The stimulation of red blood cell production can be a benefit for people who are anemic since the low levels of hemoglobin will be increased into the normal range.

“We didn't see any clinically significant changes on the prostate gland, which is very important for the urologists who see people who have prostate cancer or prostate enlargement. Thus, at least for the 2-year period of time, prostate disorders didn't seem to be a problem either in terms of symptom score or any significant increase in the incidence of prostate cancer.

“We add that the study was not powered to detect a small increase in prostate cancer but ongoing studies with a testosterone gel are looking at a much larger population of men with hypogonadism to confirm testosterone prostate safety over a 5-year treatment interval. In the present study, there was nothing that was surprising.

“I think that the real positive thing about this is that we now have an oral drug when taken twice a day gives another option to patients who are being managed by urologists, internists, and endocrinologists. There is a lot of comfort in that for the patients as well as the prescribers.

“I think the significance...(of the study) is that we have an oral agent, which many patients prefer, and that this oral agent is effective in raising the low testosterone levels into the normal range. Most importantly, for the safety study, it looks like the medication has no concerning adverse effects, although we recommend physicians monitor hemoglobin and hematocrit levels to detect erythrocytosis.

“If present, you can adjust the dose, which can be done with this oral preparation because there are different dosages available. In this study, the individuals may have had their dose increased or decreased by 50%, but most of the individuals ended up with the basic starting dose.

“The take-home message is quite clear, and it is that you have another medication which you can use to treat patients with hypogonadism, and the medication is not only effective, but it seems to be quite safe. You need to talk to your patients and ask them what route of administration they would prefer.

“Some people like injections, some people like administration on the skin, and some people would prefer pills. I might say that one of the benefits of a pill over the skin medication is that the transdermal medication could be transferred to a female partner or a child by contact with the skin, which may an issue of concern because of the FDA required a boxed warning for transdermal testosterone medications.

“The good news is that the pharmacokinetics of this oral testosterone undecanoate is such that the levels if taken twice a day, remain in the normal range. Thus, you don't have as many ups and downs seen previously in other formulations of the same drug. This is a real improvement in that regard.”

Who should not take Jatenzo

If you have any of the following conditions, Jatenzo might not be safe:

Prostate cancer
High blood pressure
Liver or kidney disease
Male breast cancer
Depression
Suicidal thoughts
Sleep apnea
Pregnancy
Under the age of 18

Possible side effects of Jatenzo

If you experience any of the following side effects from Jatenzo, contact us at once:

Any changes in mood
Signs of liver problems (yellow eyes, dark urine, incessant itching)
Any swelling in your legs, ankles, or feet
Breathing difficulties while sleeping
Coughing up blood
Signs of an enlarged prostate (loss of bladder control, reduced urine stream, elevated need to urinate)

Before we prescribe Jatenzo we will ask you to complete a detailed medical questionnaire, find out what other drugs you are taking, and complete a blood test analysis to ensure that Jatenzo is right for you. We will also provide you with precise, detailed instructions on when to take the medicine, how to take Jatenzo (with food), the exact dosage, storage instructions, and more reminders of side effects.

Your safety is paramount, and we do not compromise on that issue whatsoever. We will also continually monitor your treatment, both for safety and effectiveness. We may alter the dose as needed.

To sum it up, until the recent appearance and FDA approval of Jatenzo, oral testosterone pills have been nearly impossible to find, with good reasons: liver toxicity, and poor absorption. But thanks to Jatenzo, those problems have been overcome.

For the first time, there is an efficient and safe oral testosterone pill that can be legally prescribed in the United States.

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