Methyl-1-testosterone was first described in 1962. This compound was developed during some of the most active years of steroid research, a time when literally hundreds of different effective anabolic agents were being actively studied and pursued by drug companies. Although methyl-1-testosterone did see some favorable assays, displaying a high level of potency and an acceptable ratio of anabolic to androgenic effect, like most agents synthesized during this time period it never actually developed into a medicine. As is common in many areas of pharmaceutical research, a select number of agents were given the dollars for full studies and eventual release, and the rest were ignored. Methyl-1-testosteroe, for whatever reason, was simply not one of the select few drugs to reach pharmacy shelves, and it lay dormant in the medical books for approximately forty years.
Methyl-1-testosterone reemerged sharply in 2003, when it was introduced as an OTC (Over-The-Counter) "nutritional supplement" in the United States, due to the fact that it was unknown when the 1991 law controlling anabolic steroids was written, and therefore not included. The product was introduced to the market by Legal Gear, and was soon extremely popular due to its very high level of effectiveness. It was also soon the subject of many generic copies. Methyl-1-testosterone did not last long in the U.S., and laws were soon passed to include it as a controlled substance. The laws went into effect January 20, 2005, at which point the possession or distribution of this steroid started carrying the same Federal penalties as other anabolic steroids. This effectively ended the market for methyl-1-testosterone, and the agent is again unavailable to bodybuilders worldwide.
How is Methyl-1-testosterone Supplied
No prescription drug product containing methyl-1-testosterone currently exists. When it was sold as an OTC supplement, it was produced as an oral capsule and tablet in various strengths.
Structural Characteristics of Methyl-1-testosterone
Methyl-1-Testosterone is a derivative of dihydrotestosterone. It contains 1) the addition of a methyl group at carbon 17-alpha to protect the hormone during oral administration and 2) the introduction of a double bond between carbons 1 and 2, which helps to stabilize the 3-keto group and increase the steroid's anabolic properties.
Methyl-1-testosterone Side Effects (Estrogenic)
Although not studied, it is believed that the body does not appreciably aromatize methyl-1-testosterone. It is of note, however, that this steroid likely has inherent progestational activity. The side effects associated with progesterone are similar to those of estrogen, including negative feedback inhibition of testosterone production and enhanced rate of fat storage. Progestins also augment the stimulatory effect of estrogens on mammary tissue growth. There appears to be a strong synergy between these two hormones here, such that gynecomastia might even occur with the help of progestins, without excessive estrogen levels. The use of an anti-estrogen, which inhibits the estrogenic component of this disorder, is often sufficient to mitigate gynecomastia caused by progestational anabolic/androgenic steroids.
Methyl-1-testosterone Side Effects (Androgenic)
Although classified as an anabolic steroid, androgenic side effects are still possible with this substance. This may include bouts of oily skin, acne, and body/facial hair growth. Anabolic/androgenic steroids may also aggravate male pattern hair loss. Women are warned of the potential virilizing effects of anabolic/androgenic steroids. These may include a deepening of the voice, menstrual irregularities, changes in skin texture, facial hair growth, and clitoral enlargement. Its low relative androgenicity could theoretically make this preparation acceptable to women, although (in practice) not its very high potency. Although methyl-1-testosterone is primarily anabolic in nature, strong androgenic side effects are possible with higher doses, and should be carefully considered. Note that the 5-alpha reductase enzyme does not metabolize methyl-1-testosterone, so its relative androgenicity is not affected by finasteride or dutasteride.
Methyl-1-testosterone Side Effects (Hepatotoxicity)
Methyl-1-testosterone is a cl 7-alpha alkylated compound. This alteration protects the drug from deactivation by the liver, allowing a very high percentage of the drug entry into the bloodstream following oral administration. Cl 7-alpha alkylated anabolic/androgenic steroids can be hepatotoxic. Prolonged or high exposure may result in liver damage. In rare instances life-threatening dysfunction may develop. It is advisable to visit a physician periodically during each cycle to monitor liver function and overall health. Intake of cl 7-alpha alkylated steroids is commonly limited to 6-8 weeks, in an effort to avoid escalating liver strain.
Methyl-1-testosterone Side Effects (Cardiovascular)
Anabolic/androgenic steroids can have deleterious effects on serum cholesterol. This includes a tendency to reduce HDL (good) cholesterol values and increase LDL (bad) cholesterol values, which may shift the HDL to LDL balance in a direction that favors greater risk of arteriosclerosis. The relative impact of an anabolic/androgenic steroid on serum lipids is dependant on the dose, route of administration (oral vs. injectable), type of steroid (aromatizable or non-aromatizable), and level of resistance to hepatic metabolism. Although not extensively studied in humans, the oral route, high relative potency, and poorly or non-aromatizable nature of methyl-1-testosterone suggest that this agent is extremely prone to negatively altering lipid values and increasing atherogenic risk. Anabolic/androgenic steroids may also adversely affect blood pressure and triglycerides, reduce endothelial relaxation, and support left ventricular hypertrophy, all potentially increasing the risk of cardiovascular disease and myocardial infarction.
To help reduce cardiovascular strain it is advised to maintain an active cardiovascular exercise program and minimize the intake of saturated fats, cholesterol, and simple carbohydrates at all times during active AAS administration. Supplementing with fish oils (4 grams per day) and a natural cholesterol/antioxidant formula such as Lipid Stabil or a product with comparable ingredients is also recommended.
Methyl-1-testosterone Side Effects (Testosterone Suppression)
All anabolic/androgenic steroids when taken in doses sufficient to promote muscle gain are expected to suppress endogenous testosterone production. Without the intervention of testosterone-stimulating substances, testosterone levels should return to normal within 1-4 months of drug secession. Note that prolonged hypogonadotrophic hypogonadism can develop secondary to steroid abuse, necessitating medical intervention.
Methyl-1-testosterone Administration (General)
Prescribing guidelines generally advise that oral steroids can be taken with or without meals. The difference in bioavailability is generally not regarded as substantial. However, a 2016 study on newborn infants did find the absorption of oxandrolone to be significantly improved when dissolved directly in fat (MCT oil). If the diet includes considerable fat content, taking this oral steroid with meals might be more advantageous.
Methyl-1-testosterone Administration (Men)
Methyl-1-Testosterone was never approved for use in humans. Prescribing guidelines are unavailable. For physique- or performance-enhancing purposes, a typical effective oral daily dose will be in the range of 5-10 mg, taken for no longer than 4-6 weeks. A dose of 20 mg is sometimes used, although this increases the likelihood for side effects. Many users feel they are better served by not exceeding a 10 mg daily dose, and instead stack it with an injectable like testosterone cypionate (200-400 mg per week) when a stronger effect is needed. This may reduce liver toxicity compared to a higher dose of MIT, and also provide a more balanced cycle in terms of anabolic vs. androgenic effect. A common complaint when MIT is taken alone is lethargy, which may be due, in part, to its low androgenic or estrogenic component. Stacking it with an aromatizable androgen like testosterone will usually alleviate this problem. Note that while a small percentage of users exceed 20 mg per day, it should be remembered that even this is a serious dose for a potent steroid like this, and is not to be taken lightly, either for its effectiveness or toxicity. Like Anadrol/ methyl-1-testosterone is not necessarily a friendly steroid, but it is definitely an effective one.
Methyl-1-testosterone Administration (Women)
Methyl-1-Testosterone was never approved for use in humans. Prescribing guidelines are unavailable. This agent is not recommended for women for physique- or performance-enhancing purposes due to its high potency and tendency to produce virilizing side effects.
Methyl-1-Testosterone is not produced as a prescription drug. It is presently available only as an underground steroid product.
Newbies Research Guide reference
Methyltestosterone is one of the oldest available oral steroids. It is produced by many various manufacturers and sold in a number of countries including the U.S.. It is quite androgenic, with minimal anabolic effects. For athletic purposes, methyltest is generally only used to stimulate aggression among power lifters and those looking to boost up their workouts. Many methyltest tabs are sublingual (to be placed under the tongue) for faster absorption. These tabs can generally be identified by a notable citrus flavor to them. A couple tabs placed under the tongue before a visit to the gym may make for an aggressive workout. Aside from this, methyltest offers little except androgenic side effects. It is quite toxic, elevating liver enzymes and causing acne, gynocomastia, aggression and water retention quite easily. Were one to tolerate these side-effects, methyltest will offer little more than some slight strength gains. One looking for quality muscle mass from a steroid cycle should be looking elsewhere. Counterfeit steroids sometimes contain only methyltest in an effort to deceive the buyer. This is due to the fact that it is very cheap in bulk and obviously may fool an inexperienced user.
Wlliam Llewellyn (2017) - Anabolics
Newbies Research Guide