Technical Information

  • CAS no.: 737789-87-6

  • Type: API

  • Usage: Adult advanced prostate cancer

  • Technical description
    Relugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist used in the treatment of several hormone-responsive conditions. Relugolix has also been studied in the symptomatic treatment of endometriosis. Relugolix is the first (and currently only) orally-administered GnRH receptor antagonist approved for the treatment of prostate cancer – similar therapies such as [degarelix] require subcutaneous administration – and therefore provides a less burdensome therapeutic option for patients who might otherwise require clinic visits for administration by healthcare professionals. In addition to its relative ease-of-use, relugolix was shown to be superior in the depression of testosterone levels when compared to [leuprolide], another androgen deprivation therapy used in the treatment of prostate cancer.

  • IUPAC name: 2-(2-oxo-1-phenyl-5-pyridin-2-yl-3-pyridinyl)benzonitrile 1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea.

  • Molecular formula: C29H27F2N7O5S

  • Molecular Weight: 623.6 g/mol

  • Class: Gonadotropin-releasing hormone (GnRH) receptor antagonist.

  • Synonyms: AK-385, RVT-601.

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