MK-0773 is a selective androgen receptor modulator (SARM) developed by Merck and GTx for the treatment of sarcopenia, a condition characterized by the loss of muscle mass and strength in older adults. This orally active compound is a 4-azasteroid and a potent agonist of the androgen receptor (AR). MK-0773 exhibits tissue-selective androgenic effects, significantly increasing lean body mass with anabolic effects comparable to approximately 80% of those induced by dihydrotestosterone (DHT). However, it demonstrates minimal impact on reproductive tissues such as the uterus, sebaceous glands, and prostate, indicating a reduced propensity for virilization.
In clinical studies, MK-0773 has shown promising results in elderly women with sarcopenia, leading to a significant increase in lean body mass and muscle strength compared to placebo, although the latter did not reach statistical significance. The drug also demonstrated a favorable safety profile, with no evidence of androgenization. However, some participants experienced elevated liver enzymes, which resolved after discontinuing the treatment.
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| Other Names | PF-05314882, MK 0773, CHEMBL3221237 |
|---|---|
| IUPAC Name | (1S, 3aS, 3bS, 5aR, 9aS, 9bS, 11aS)-8-fluoro-N-(1H-imidazo[4, 5-b]pyridin-2-ylmethyl)-6, 9a, 11a-trimethyl-7-oxo-2, 3, 3a, 3b, 4, 5, 5a, 9b, 10, 11-decahydro-1H-indeno[5, 4-f]quinoline-1-carboxamide |
| CAS | 606101-58-0 |
| Molecular Weight | 479.6 |
| Molecular Formula | C27H34FN5O2 |
| SMILES | C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2C(=O)NCC4=NC5=C(N4)C=CC=N5)CC[C@@H]6[C@@]3(C=C(C(=O)N6C)F)C |