Drostanolone propionate

The principal clinical indication of drostanolone propionate in the United States as well as international markets was the treatment of advanced inoperable breast cancer in women.^[1]

Hormonal treatment is part of the complex therapy for some kind of tumors, particularly the ones associated with hormone-active tissues like breast or prostate cancer. Some types of breast cancer cells, expressing estrogen receptors (called ER+ cancers), use estrogen for their growth and dissemination. That is why drugs that block estrogen receptors or decrease their expression on the cell membrane, antiestrogens, could limit the tumor spread and size. Drostanolone propionate has been FDA approved^[7] as an antiestrogenic drug for the treatment of breast cancer. By the time of its release, there were not many alternatives for patients with breast cancer and drostanolone propionate was a revolution for these patients. As it has lower androgenic rate compared to testosterone, the risk of virilization is much lighter. Due to this fact, women, who usually do not respond well to any AAS, were having much greater chance to survive cancer. Drostanolone propionate can also be used for breast tumors that do not respond well to other treatments or also as palliative care for advanced incurable tumors. The effects of the product depend of course on the dose and period of administration. The risk of virilization becomes greater with high doses and continuous administration period.

Drostanolone propionate is or has been used for physique- and performance-enhancing purposesbycompetitive athletes, bodybuilders, and powerlifters.^[1]

Drostanolone propionate produces considerably less virilization in women compared to equal doses of testosterone propionate.^[1] However, since the given dosage for breast cancer was relatively high (200 mg/twice a week),^[8] mild virilization including oily skin, acne, voice deepening, hirsutism, and clitoral enlargement could still occur, and marked virilization could manifest with long-term therapy.^[1] The drug has no estrogenic activity and hence has no propensity for causing gynecomastia (in males) or fluid retention.^[1] Drostanolone propionate is not known to pose a risk of hepatotoxicity.^[9][1]

Drostanolone propionate is a prodrugofdrostanolone.^[1] Like other AAS, drostanolone is an agonist of the androgen receptor (AR).^[1] It is not a substrate for 5α-reductase and is a poor substrate for 3α-hydroxysteroid dehydrogenase (3α-HSD), and therefore shows a high ratio of anabolictoandrogenic activity.^[1] As a DHT derivative, drostanolone is not a substrate for aromatase and hence cannot be aromatized into estrogenic metabolites.^[1] While no data are available on the progestogenic activity of drostanolone, it is thought to have low or no such activity similarly to other DHT derivatives.^[1] Since the drug is not 17α-alkylated, it is not known to cause hepatotoxicity.^[1]

Drostanolone propionate, via its active form drostanolone, interacts with the AR and activates a cascade of genetic changes, including increased protein synthesis (anabolism) and decreased amino acid degradation (catabolism). It also induces a reduction or inhibition of prolactinorestrogen receptors in the breasts, which is linked to its antitumor effects.^[10]

Drostanolone propionate is not active via the oral route and must be administered via intramuscular injection.^[1] The elimination half-life of the drug via this route is approximately 2 days.^[1] It has a much longer elimination half-life via intramuscular injection than drostanolone.^[1] Drostanolone propionate is metabolized into drostanolone, which is the active form.^[1]

Drostanolone propionate, or drostanolone 17β-propionate, is a synthetic androstane steroid and a derivative of DHT.^[11][12][1] It is the C17β propionate (propanoate) esterofdrostanolone, which itself is 2α-methyl-4,5α-dihydrotestosterone (2α-methyl-DHT) or 2α-methyl-5α-androstan-17β-ol-3-one.^[11][12][1]

Drostanolone and drostanolone propionate were first described in 1959.^[1][4] The related AAS oxymetholone and methasterone (methyldrostanolone) were first described in the same paper as well.^[1] Drostanolone propionate was introduced for medical use in the United States in 1961 and in Europe shortly thereafter.^[5]

Drostanolone propionate is the generic name of the drug and its BANMTooltip British Approved Name, while dromostanolone propionate is the USANTooltip United States Adopted Name and USPTooltip United States Pharmacopeia; there is no INNTooltip International Nonproprietary Name for this form.^[11][12][13] The generic name of the unesterified form of the drug is drostanoloneordromostanolone and the former is its INNTooltip International Nonproprietary Name, BANTooltip British Approved Name, and DCFTooltip Dénomination Commune Française while there is no USANTooltip United States Adopted Name.^{[11][12][13][2]}

Drostanolone propionate was marketed under a variety of brand names including Drolban, Masterid, Masteril, Masteron, Masterone, Mastisol, Metormon, Permastril, and Prometholone.^[11][12][1]

Drostanolone propionate appears to no longer be marketed.^[1][2] It was previously available in the United States, Europe, and Japan.^[12][1] In Europe, it was specifically marketed in the United Kingdom, Germany, Belgium, France, Spain, Portugal, Italy, and Bulgaria.^[12][1]

Drostanolone propionate, along with other AAS, is a schedule III controlled substance in the United States under the Controlled Substances Act.^[6]

• Masteron Propionate Genetix Pharma