Oral free/base (unesterified) testosterone is more effective and safer than synthetic AAS

A number of my blog readers contacted me over the last 2 weeks and urged me to write this post in response to the recent FDA approval of the first oral testosterone (T) product in the USA. The approved product will contain the testosterone ester undecanoate in the form of tablets.

https://www.fda.gov/news-events/press-announcements/fda-approves-new-oral-testosterone-capsule-treatment-men-certain-forms-hypogonadism

Well here is my take on this recent FDA decision. Most males will end up getting examined by an endocrinologist (endo) at least once in their lifespan, usually in regards to prostate health or declining virility due to aging (or iatrogenic reasons). If the patient is lucky enough to be considered worthy of conversing with by the medical authority in the room, the patient will often hear lengthy lectures on TRT and how oral T (and other AAS) is ineffective. As such, most endos will demand that their patients submit to injection hormonal therapy, which often results in elevated estrogen, gyno, blood count abnormalities, etc. This attitude from the vast majority of endos is not a coincidence – i.e. it stems directly from official FDA dogma/policy formulated decades ago and still in use today. It is beyond baffling to me why FDA and the medical profession would accept that steroids like pregnenolone, DHEA, progesterone, etc are highly bioavailable when administered orally yet somehow steroids like T, DHT, and various other synthetic derivatives are not. The only conclusion I can draw is that FDA purposefully tries to poison the field and steer the public away from oral route, which is easy and accessible for most people. In contrast, when it comes to injections most people depend on doctors to both prescribe and administer them.

Well, hopefully my readers who are more open minded will show the studies below to their doctors and demand an answer as to why this travesty continues. As the studies towards the end of the post demonstrate, not only is free/base T orally bioavailable, but even massive doses (400mg daily) have no negative side effects on the liver and in fact accelerates the activity of several liver detox enzymes. The latter effect is highly sought-after by Big Pharma and many drugs are currently being developed/tested with the hope that such a liver-metabolism-enhancing compound will be brought to market as it has tremendous potential for treating everything from obesity, to gyno, to side effects of toxic chemotherapy. Thus, as one of the studies below directly stated, artificial/synthetic T derivatives such as 17a-methylated varieties, 19-nortestosterone derivatives (and in general any other AAS with bizarre modifications to make them less metabolizable and longer acting) have no advantages over free/base T neither due to cost nor effectiveness. In fact, unlike the readily observed liver-toxicity (including liver cancer) from various synthetic AAS, using free/base T may actually cure 60%+ of even advanced cases of liver failure (cirrhosis), as confirmed by extensive human studies several decades ago.

https://www.ncbi.nlm.nih.gov/pubmed/14139786

https://www.ncbi.nlm.nih.gov/pubmed/4577116

https://www.ncbi.nlm.nih.gov/pubmed/14109120

https://www.tandfonline.com/doi/abs/10.1080/00325481.1964.11694984

So, what does that have to do with FDA’s recent T undecanoate approval? Well, according to one of the studies below, that specific T ester only works if it is dissolved in oil AND administered with a large meal containing significant amounts of fat. On the other hand, oral free/base T was absorbed without using any carriers or fatty meals. In addition, androgen esters often have unpredictable effects and in some cases may be even carcinogenic, while the free/base steroid is highly protective. It just so happens that the formulation FDA approved does NOT contain any oils as carrier/solvent and does not carry a recommendation to consume with a significant amount of fat. So, at best the formulation will be ineffective and at worst it may be carcinogenic.

https://www.ncbi.nlm.nih.gov/pubmed/9687988

“…”…CONCLUSIONS. Slow-release implants of DHT administered to L-W rats at age 12 months reduced by 50% the development of spontaneous P-SV tumors by age 24 months…In 1987, we reported that testosterone propionate (TP) promoted, but that dihydrotestosterone (DHT) did not promote, the development of cancers in the accessory sex glands [prostate and seminal vesicles (P-SV)] of Lobund-Wistar (L-W) rats [1]…The inhibitory effect of DHT on induced P-SV tumors was confirmed in Fischer [2] and in L-W rats [3].”
“…The inhibitory effects of DHT reported by us [1,5], contrasting with the reported trophic effect of DHT (6–8), was clarified: DHT (5a-Androstan-17b-ol-3-one) inhibited the development of induced P-SV tumors, but DHT propionate promoted tumor development [3].

I highly doubt the FDA considered any of these issues before approving a suboptimal, patented, potentially toxic, oral T formulation that also costs orders of magnitude more compared to free/base T that can be obtained with a prescription from any compounding pharmacy. But hey, what do I know! I don’t have a medical degree and apparently one is needed for a person to be allowed to form their own opinion based on published scientific evidence spanning several decades. Your doctor knows best. /s

https://www.ncbi.nlm.nih.gov/pubmed/580151

https://www.ncbi.nlm.nih.gov/pubmed/520403
“…Twenty-six male volunteers received a single oral dose of testosterone as free crystals or as the undecanoate ester. The latter was given either in crystalline form or in arachis oil. All preparations were tested three times in the same individual, whilst fasting on 2 days and on one day together with a breakfast rich in fat. Serum testosterone concentration was measured at intervals for up to 6–24 h after the dose. A significant and reproducible rise in serum testosterone level was found after ingestion of free testosterone. Testosterone esterified with undecylenic acid was only effective when administered in arachis oil. The meal increased the bioavailability of the ester, but had hardly any effect on that of the free hormone. It is concluded that bioavailability of oral testosterone can be improved by pharmaceutical means to an extent sufficient to produce adequate blood levels in substitution therapy.”

https://www.thelancet.com/journals/lancet/article/PIIS0140-6736(74)90216-5/fulltext
“…200 mg. of free testosterone (2-5 µ particles compressed into conventional tablets) produced normal male serum-testosterone levels for 5-7 hours in four subjects without testicular function. Serum-testosterone levels were still at least five times higher than initial values 6-8 hours after tablet ingestion. The clinical effectiveness of oral free testosterone 100 mg. 4 times a day was established in a double-blind trial in five eunuchs. It is concluded that artificial testosterone derivatives have no advantages, either in effect or cost, over oral androgen therapy. Adequate oral doses of natural free testosterone are fully effective in replacing hormonal testicular function.”

https://www.thelancet.com/journals/lancet/article/PIIS0140-6736(78)90402-6/fulltext

“…17α-methyltestosterone impairs liver function and may even lead to hepatoma,’ and presumably, 17α-alkylated androgens or anabolic steroids will have to be abandoned. In 1974 we showed that free testosterone in tablet form at a dose of 400 mg/day is an effective form of androgen therapy.[2] We have now followed up ten men with no testicular function (castrates and eunuchs) who have been on continuous oral testosterone treatment for up to 7.5 years; liver function has remained normal.”

https://www.ncbi.nlm.nih.gov/pubmed/947655

“…Six normal male volunteers ingested a dose of 400 mg free testosterone daily as tablets over 21 days. By the end of treatment intravenous antipyrine half-life had decreased significantly from 8.0 +/- 2.7 to 5.7 +/- 2.6 hr. The subjects eliminated testosterone from serum more rapidly on the twenty-first day of testosterone ingestion than on the first day. Serum albumin, bilirubin, prothrombin, alanine-amino-transferase, and alkaline phosphatases were unchanged during the experiment. It is concluded that oral testosterone treatment induces the hepatic drug-metabolizing system including that of testosterone.”

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