Methyltestosterone is a synthetic anabolic steroid used for the replacement therapy in conditions associated with testosterone deficiencies in males, such as hypogonadism, and treatment of advancing inoperable metastatic breast cancer in females. Also, has antineoplastic properties and so has been used secondarily in women with advanced breast cancer.
- Mechanism
- Curator reviewed
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.
- Primary indication
- Methyltestosterone is an anabolic steroid hormone used to treat men with a testosterone deficiency.Curator reviewed · 5 structured indications
- Formula / weight
- C20H30O2 · 302.451 g/mol (avg)
- First approval
- Canada, 1997 · United States, 1973
- Also known as
- 17-methyltestosterone · Virilon
- Code names
- L 589.372 · NSC-139965 · RU 24400
- Brand names
Resolves to
GCKMFJBGXUYNAG-HLXURNFRSA-NSMILES[H][C@@]12CC[C@](C)(O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12CWhat you can answer from here — as of September 23, 2026
Which drugs share a target with Methyltestosterone, and which of those have an active Phase 3 trial?
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