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Chemical Name: Methyltestosterone
Drug Class: Oral Anabolic Steroid

Methyltestosterone represents the first successful attempt by scientists to produce an orally active version of testosterone. To do this, scientists simply methylated the testosterone molecule, to survive oral ingestion. As a result, by the  early 1950’s injectable testosterone (suspension), progesterone, and their new “Methyltestosterone”, comprised nearly 25% of Ciba’s total pharmaceutical turnover. (1). Unfortunately, this methylation caused an increase in liver enzymes in its users, indicating an increased level of activity by hepatic enzymes. To this day, surprisingly, Methyltestosterone still constitutes approximately a third of all testosterone prescriptions filled in the United States (2). Unfortunately, this is another area where scientists and doctors are well behind the performance enhancement curve, as most bodybuilders and athletes don’t bother with oral testosterone preparations unless they are looking for a very specific, short term results.

As it applies to athletes and bodybuilders, the structure of Methyltestosterone really limits its use to very precise applications. It’s 17-alpha-methyl alteration allows it to survive its first pass through the liver. Other than that, this alteration, as I mentioned in the previous paragraph, contributes to the hepatoxicity (liver toxicity). (3) Fortunately this compound actually doesn’t have adverse effects on cholesterol and, and has been shown to lower plasma viscosity. (4 ) However, since this is just an orally active testosterone, we can expect aromatization (conversion to estrogen) as well as virilization. In addition, as with any form type of Testosterone, it will convert to Dihydrotestosterone (DHT), which can contribute to both prostate enlargement and hair loss. Taking endogenous hormones will almost always affect your natural testosterone levels, and Methyltestosterone is no exception to this. Using Methyltestosterone will result in significant decreases in plasma levels of gonadotropins (LH and FSH), gonadal steroids, sex hormone binding globulin, free T3 and T4, as well as thyroid binding globulin (5). Typically, I recommend Arimidex (Anastrozole) at .5mgs/day to help lower estrogen levels or a similar ancillary compound.

I think that the effect you’ll typically get from Methyltestosterone is similar to what would be expected with something like Halotestin, as most athletes who use either of these drugs are typically looking for immediate increases in strength and aggression, with perhaps a rapid increase in the hardness of their physique. Methyltestosterone (and Halotestin for that matter) are both very good for achieving all of those effects. Unfortunately, due to possible liver complications, most athletes have found it prudent to limit their intake of Methyltestosterone to smaller doses (25-50mgs/day), and for limited time periods – up to six weeks at the end of a pre-contest cycle, or immediately before an athletic event or workout. This is the most common use for Methyltestosterone in a cycle. The user typically experiences a rapid increases in both strength and aggression when a (small) dose is taken prior to a workout or athletic event. It’s common to see 25mgs taken an hour before a work out or competition. Sometimes strongmen and powerlifters have found it beneficial to take a dose before each event or lift, during a competition.

Unfortunately, as a size or weight gain drug, Methyltestosterone is disappointing. There much are better orals than Methyltestosterone for size, but perhaps none as good at increasing aggression or strength- Halotestin comes to mind as a possible competitor in this category. If intake is limited to just pre-workout or competition, then it’s actually a pretty safe drug, and a decent buy.

Availability of this drug is high, but cost is a little on the high side as well. When you consider that it’s only going to be used for specific reasons and for short time periods, it’s usually a worthwhile buy.


1. Karl Huesler & Jaroslav Calvoda, Pharmaceuticals Division, Ciba-Geigy

2. Westaby, D., Ogle, S.J., Paradinas, F.J., et al Lancet, August 6:261, 1977

3. Lancet, August 6:261, 1977.

4. Clin Endocrinol (Oxf). 2002 Aug;57(2):209-14.

5. Psychoneuroendocrinology. 2003 Apr;28(3):317-31.

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