Bolasterone was first described in 1959. It was closely evaluated for anabolic and androgenic effect approximately 3 years later. The drug was developed by Upjohn, and sold in the U.S. during the 1960’s under the Myagen brand name. It was mainly indicated for the treatment of advanced breast cancer in women, although the agent was also investigated for its stimulatory effect on blood cells and its general anabolic (lean-tissue sparing) activity. Bolasterone was ultimately a short-lived drug, disappearing from the U.S. market shortly after its release. By the 1980’s, bolasterone had been out of commerce for so long that it was all but forgotten among athletes. Although bolasterone is no longer produced, the drug remains listed in the U.S. Pharmacopeias, suggesting it would not be impossible to see this agent for sale (legally) in the U.S. again, perhaps under order by a private compounding pharmacy. The reemergence of an actual commercial bolasterone compound, however, remains very unlikely.
How is Bolasterone Supplied
Bolasterone is no longer available as a prescription drug product.
Structural Characteristics of Bolasterone
Bolasterone is a modified form of testosterone. It differs by: 1) the addition of a methyl group at carbon 17-alpha, which helps protect the hormone during oral administration, and 2) the introduction of a methyl group at carbon 7 (alpha), which inhibits 5-alpha reduction and shifts the anabolic to androgenic ratio in favor of the former. 7,17-dimethylated steroids also tend to be very resistant to metabolism and serum-binding proteins, greatly enhancing their relative biological activity.
Bolasterone Side Effects (Estrogenic)
Bolasterone is aromatized by the body, and is considered a highly estrogenic steroid due to its conversion to 7,17- dimethylestradiol (an estrogen with high biological activity). Gynecomastia may be a concern during treatment, especially when higher than normal therapeutic doses are used. At the same time water retention can become a problem, causing a notable loss of muscle definition as both subcutaneous water retention and fat levels build. To avoid strong estrogenic side effects, it may be necessary to use an anti-estrogen such as Nolvadex. One may alternately use an aromatase inhibitor like Arimidex (anastrozole), which is a more effective remedy for estrogen control. Aromatase inhibitors, however, can be quite expensive in comparison to standard estrogen maintenance therapies, and may also have negative effects on blood lipids.
Bolasterone Side Effects (Androgenic)
Although bolasterone is classified as an anabolic steroid, androgenic side effects are still possible with this substance. These may include bouts of oily skin, acne, and body/facial hair growth. Higher doses are more likely to cause such side effects. Anabolic/androgenic steroids may also aggravate male pattern hair loss. Women are additionally 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. Bolasterone is unaffected by the 5-alpha reductase enzyme, so its relative androgenicity is not affected by the concurrent use of finasteride or dutasteride. Note that studies administering 1mg and 2mg of bolasterone per day have shown no outward androgenic side effects in children and hypogonadotrophic males, as would be characterized by public hair growth, genital changes, voice changes, and acne. Higher doses remain likely to induce androgenic effects. Bolasterone is considered to have a comparable ratio of anabolic to androgenic effect as oxymetholone and methandrostenolone.
Bolasterone Side Effects (Hepatotoxicity)
Bolasterone is a c17-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. C17-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 c17-alpha alkylated steroids is commonly limited to 6-8 weeks, in an effort to avoid escalating liver strain. Studies administering 1mg and 2mg of bolasterone daily for 6 weeks to 27 patients have demonstrated a trend toward increases in serum alkaline phosphatase (a marker of liver stress), although no significant untoward effects on the liver were documented.
Bolasterone 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. Bolasterone has a strong effect on the hepatic management of cholesterol due to its structural resistance to liver breakdown and route of administration. 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. Studies administering 1mg and 2mg of bolasterone daily for 6 weeks to 27 patients have demonstrated a trend toward increased serum cholesterol. Although no HDL and LDL breakdown was provided, it can be assumed based on the structure and route of administration that bolasterone significantly shifted the ratio of these two fractions of cholesterol further apart, measurably increasing atherogenic risk.
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.
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.
Bolasterone Administration (General)
Studies have shown that taking an oral anabolic steroid with food may decrease its bioavailability. This is caused by the fat-soluble nature of steroid hormones, which can allow some of the drug to dissolve with undigested dietary fat, reducing its absorption from the gastrointestinal tract. For maximum utilization, this steroid should be taken on an empty stomach.
Bolasterone Administration (Men)
Clinical studies have demonstrated that significant nitrogen retention and weight gain can be induced with a daily dosage of 1-2mg per day. In the athletic arena, doses of 2-5 mg daily seem to be most reasonable, taken in cycles lasting no more than 6-8 weeks in length to minimize hepatotoxicity. This level is sufficient for strong increases in muscle size and strength, although such gains will likely be accompanied by significant water retention.
Bolasterone Administration (Women)
Bolasterone was not widely used with women in clinical medicine. When applied, it was most often used as a secondary medication during inoperable breast cancer, when other therapies have failed to produce a desirable effect. The dosage used for this application would be as high as 10 mg per day, a level that has caused significant virilization among patients. Bolasterone is generally not recommended for women for physique- or performanceenhancing purposes due to its very strong nature and tendency to produce virilizing side effects.
Bolasterone is no longer produced as a prescription drug, although a handful of underground laboratories have taken to selling this material.
Newbies Research Guide reference
This was originally a popular oral steroid being used in Europe. It had functions similar to dianabol, but it has long since been discontinued. Several years ago bolasterone became the first big name counterfeit steroid to be internationally marked. Belonging to a group of steroids titled the DDR compounds, inferring they came from East Germany, this steroid was billed as the best drug ever made. It became very popular partially because several respected steroid experts were in on the production of it, and gave it rave reviews in their publications. Thousands of 30 cc vials of this injectable steroid were sold at a price of over 200 dollars a piece. It was said to contain ten milligram of the drug per cc, but it actually contained a low dosage of several domestic steroids mixed together. In the spring of 1986 the makers of this drug were busted. There are still at least three other counterfeiters using the bolasterone name: UCLA bolasterone, available in a 10 cc vial; new bolasterone, available in a 10 cc vial, and bolasterone depot available in a 50 cc vial. All of these items are the worst kind of counterfeit steroids made. They are worthless and dangerous. Many athletes are still taking these drugs. It is obvious that any item carrying a bolasterone or GDR label should be avoided.
Wlliam Llewellyn (2011) - Anabolics
Newbies Research Guide