Methyltestosterone is an anabolic steroid hormone used to treat men with a testosterone deficiency. It is also used in women to treat breast cancer, breast pain, swelling due to pregnancy, and with the addition of estrogen it can treat symptoms of menopause. The effects of testosterone in humans and other vertebrates occur by way of two main mechanisms: by activation of the androgen receptor (directly or as DHT), and by conversion to estradiol and activation of certain estrogen receptors. Free testosterone (T) is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor, or can be reduced to 5α-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5α-reductase. DHT binds to the same androgen receptor even more strongly than T, so that its androgenic potency is about 2.5 times that of T. The T-receptor or DHT-receptor complex undergoes a structural change that allows it to move into the cell nucleus and bind directly to specific nucleotide sequences of the chromosomal DNA. The areas of binding are called hormone response elements (HREs), and influence transcriptional activity of certain genes, producing the androgen effects. Methyltestosterone is marketed under the brand names Android, Androral, Metandren, Oraviron, Testred, Virilon.

Methyl-1-testosterone(M1T)(17alpha-hydroxy-17-methyl- 5-androst-1-en-3-one) is a new designer steroid that is most likely produced to circumvent the legal restrictions. It is advertised to be highly anabolic and moderately androgenic and not convertible to estrogens. However, in scientific literature, it was reported to show anabolic properties of 25% and androgenic properties of 50% compared with testosterone propionate after im injection in castrated rats. In February 2006, Health Canada (Federal Department) warned consumers not to use M1T-containing products because of potentially serious health risks such as liver disorders and hardening of the arteries. Since 2006, M1T is explicitly listed on the World Anti-Doping Agency list of prohibited substances, and therefore, its use by athletes is prohibited.