Disclosed are a phthalazinone compound, and a preparation method therefor and the medical use thereof. In particular, disclosed are a compound as represented by formula (I), and a pharmacodynamically acceptable salt, and the use of the compound as an androgen receptor (AR) for degradation.

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We disclose a pharmaceutical composition adapted for oral delivery comprising native testosterone; a treatment regimen comprising administration of the composition(s); and methods and uses for the treatment of hormone related conditions such as hypogonadism in human male, female and transgender subjects.

We disclose a pharmaceutical composition adapted for oral delivery comprising native testosterone; a treatment regimen comprising administration of the composition(s); and methods and uses for the treatment of hormone related conditions such as hypogonadism in human male, female and transgender subjects.

Microemulsions are described where hydrophobic liquid droplets are distributed in a continuous hydrophilic liquid phase. The described microemulsions may be thought of as modified oil-in-water (MOIW) microemulsions, where both the “oil” and “water” phases of the microemulsion are modified. The oil phase droplets of the MOIW microemulsion are modified with alcohol and can solubilize alcohol-soluble species, including nonderivatized hormones. The polar continuous “water” phase of the MOIW microemulsion is modified with a sugar or sugar alcohol.

Microemulsions are described where hydrophobic liquid droplets are distributed in a continuous hydrophilic liquid phase. The described microemulsions may be thought of as modified oil-in-water (MOIW) microemulsions, where both the “oil” and “water” phases of the microemulsion are modified. The oil phase droplets of the MOIW microemulsion are modified with alcohol and can solubilize alcohol-soluble species, including nonderivatized hormones. The polar continuous “water” phase of the MOIW microemulsion is modified with a sugar or sugar alcohol.

Disclosed are effective fixed dose oral testosterone undecanoate compositions for use in regimens without dose titration and methods for treatment of patients in need of testosterone replacement therapy. Also disclosed are criteria for continuation and discontinuation of such regimens, based on single serum T concentration levels measured at a steady state at predetermined times after initiation of said regimen and at a predetermined number of hours after administration of a morning dose of the regimen.

Disclosed are effective fixed dose oral testosterone undecanoate compositions for use in regimens without dose titration and methods for treatment of patients in need of testosterone replacement therapy. Also disclosed are criteria for continuation and discontinuation of such regimens, based on single serum T concentration levels measured at a steady state at predetermined times after initiation of said regimen and at a predetermined number of hours after administration of a morning dose of the regimen.

A pharmaceutical formulation of testosterone undecanoate is provided. Methods of treating a testosterone deficiency or its symptoms with the inventive formulations are also provided.

The present invention provides a compound or a pharmaceutically acceptable salt, isomer, prodrug, polymorph or solvate thereof, and a preparation method therefor and use thereof. The compound provided in the present invention has comparable or superior activity to Elagolix as a GnRHR antagonist in calcium flux assays and have better pharmacokinetic properties.

The present invention provides a compound or a pharmaceutically acceptable salt, isomer, prodrug, polymorph or solvate thereof, and a preparation method therefor and use thereof. The compound provided in the present invention has comparable or superior activity to Elagolix as a GnRHR antagonist in calcium flux assays and have better pharmacokinetic properties.